Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS.
Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA.
An antiandrogen with about the same potency as cyproterone in rodent and canine species.
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Compounds which inhibit or antagonize the biosynthesis or actions of androgens.
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
The surgical removal of one or both testicles.
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
Tumors or cancer of the PROSTATE.
Organic compounds containing the -CN radical. The concept is distinguished from CYANIDES, which denotes inorganic salts of HYDROGEN CYANIDE.
A synthetic non-aromatizable androgen and anabolic steroid. It binds strongly to the androgen receptor and has therefore also been used as an affinity label for this receptor in the prostate and in prostatic tumors.
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids.
Steroidal compounds related to TESTOSTERONE, the major mammalian male sex hormone. Testosterone congeners include important testosterone precursors in the biosynthetic pathways, metabolites, derivatives, and synthetic steroids with androgenic activities.
A ligand that binds to but fails to activate the INTERLEUKIN 1 RECEPTOR. It plays an inhibitory role in the regulation of INFLAMMATION and FEVER. Several isoforms of the protein exist due to multiple ALTERNATIVE SPLICING of its mRNA.
A disorder of sexual development transmitted as an X-linked recessive trait. These patients have a karyotype of 46,XY with end-organ resistance to androgen due to mutations in the androgen receptor (RECEPTORS, ANDROGEN) gene. Severity of the defect in receptor quantity or quality correlates with their phenotypes. In these genetic males, the phenotypic spectrum ranges from those with normal female external genitalia, through those with genital ambiguity as in Reifenstein Syndrome, to that of a normal male with INFERTILITY.
Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS.
A gland in males that surrounds the neck of the URINARY BLADDER and the URETHRA. It secretes a substance that liquefies coagulated semen. It is situated in the pelvic cavity behind the lower part of the PUBIC SYMPHYSIS, above the deep layer of the triangular ligament, and rests upon the RECTUM.
A strain of albino rat used widely for experimental purposes because of its calmness and ease of handling. It was developed by the Sprague-Dawley Animal Company.
The relationship between the dose of an administered drug and the response of the organism to the drug.
Compounds that bind to and block the stimulation of PURINERGIC P1 RECEPTORS.
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
A family of hexahydropyridines.
Drugs that bind to but do not activate SEROTONIN 5-HT3 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT3 RECEPTOR AGONISTS.
Certain tumors that 1, arise in organs that are normally dependent on specific hormones and 2, are stimulated or caused to regress by manipulation of the endocrine environment.
Chemical substances which inhibit the function of the endocrine glands, the biosynthesis of their secreted hormones, or the action of hormones upon their specific sites.
Drugs that bind to but do not activate excitatory amino acid receptors, thereby blocking the actions of agonists.
C18 steroid with androgenic and anabolic properties. It is generally prepared from alkyl ethers of ESTRADIOL to resemble TESTOSTERONE but less one carbon at the 19 position.
Agents that antagonize ANGIOTENSIN RECEPTORS. Many drugs in this class specifically target the ANGIOTENSIN TYPE 1 RECEPTOR.
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
A cell line derived from cultured tumor cells.
Drugs that bind to but do not activate SEROTONIN 5-HT2 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN 5-HT2 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more specific 5-HT2 receptor subtypes.
Compounds that selectively bind to and block the activation of ADENOSINE A2 RECEPTORS.
Compounds that bind to and block the stimulation of ADENOSINE A1 RECEPTORS.
A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.
Compounds that bind to and block the stimulation of PURINERGIC P2 RECEPTORS.
Agents inhibiting the effect of narcotics on the central nervous system.
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
An enzyme that catalyzes the reduction of TESTOSTERONE to 5-ALPHA DIHYDROTESTOSTERONE.
RNA sequences that serve as templates for protein synthesis. Bacterial mRNAs are generally primary transcripts in that they do not require post-transcriptional processing. Eukaryotic mRNA is synthesized in the nucleus and must be exported to the cytoplasm for translation. Most eukaryotic mRNAs have a sequence of polyadenylic acid at the 3' end, referred to as the poly(A) tail. The function of this tail is not known for certain, but it may play a role in the export of mature mRNA from the nucleus as well as in helping stabilize some mRNA molecules by retarding their degradation in the cytoplasm.
Microsatellite repeats consisting of three nucleotides dispersed in the euchromatic arms of chromosomes.
Retrograde flow of gastric juice (GASTRIC ACID) and/or duodenal contents (BILE ACIDS; PANCREATIC JUICE) into the distal ESOPHAGUS, commonly due to incompetence of the LOWER ESOPHAGEAL SPHINCTER.
The intracellular transfer of information (biological activation/inhibition) through a signal pathway. In each signal transduction system, an activation/inhibition signal from a biologically active molecule (hormone, neurotransmitter) is mediated via the coupling of a receptor/enzyme to a second messenger system or to an ion channel. Signal transduction plays an important role in activating cellular functions, cell differentiation, and cell proliferation. Examples of signal transduction systems are the GAMMA-AMINOBUTYRIC ACID-postsynaptic receptor-calcium ion channel system, the receptor-mediated T-cell activation pathway, and the receptor-mediated activation of phospholipases. Those coupled to membrane depolarization or intracellular release of calcium include the receptor-mediated activation of cytotoxic functions in granulocytes and the synaptic potentiation of protein kinase activation. Some signal transduction pathways may be part of larger signal transduction pathways; for example, protein kinase activation is part of the platelet activation signal pathway.
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
Development of female secondary SEX CHARACTERISTICS in the MALE. It is due to the effects of estrogenic metabolites of precursors from endogenous or exogenous sources, such as ADRENAL GLANDS or therapeutic drugs.
An agent with anti-androgen and progestational properties. It shows competitive binding with dihydrotestosterone at androgen receptor sites.
Drugs that bind to but do not activate GABA-A RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-A RECEPTOR AGONISTS.
Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.
Drugs that bind to but do not activate histamine receptors, thereby blocking the actions of histamine or histamine agonists. Classical antihistaminics block the histamine H1 receptors only.
Drugs that bind to but do not activate serotonin receptors, thereby blocking the actions of serotonin or SEROTONIN RECEPTOR AGONISTS.
Thiohydantoin benzene derivative.
Proteins that enhance gene expression when associated with ligand bound activated NUCLEAR RECEPTORS. The coactivators may act through an enzymatic process that affects the rate of transcription or the structure of chromatin. Alternatively nuclear receptor coactivators can function as adaptor proteins that bring nuclear receptors into close proximity with transcriptional complexes.
Drugs that bind to but do not activate GABA RECEPTORS, thereby blocking the actions of endogenous GAMMA-AMINOBUTYRIC ACID and GABA RECEPTOR AGONISTS.
A glycoprotein that is a kallikrein-like serine proteinase and an esterase, produced by epithelial cells of both normal and malignant prostate tissue. It is an important marker for the diagnosis of prostate cancer.
A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed)
Glycoproteins which contain sialic acid as one of their carbohydrates. They are often found on or in the cell or tissue membranes and participate in a variety of biological activities.
A class of drugs designed to prevent leukotriene synthesis or activity by blocking binding at the receptor level.
Proteins found usually in the cytoplasm or nucleus that specifically bind steroid hormones and trigger changes influencing the behavior of cells. The steroid receptor-steroid hormone complex regulates the transcription of specific genes.
A transcription factor that partners with ligand bound GLUCOCORTICOID RECEPTORS and ESTROGEN RECEPTORS to stimulate GENETIC TRANSCRIPTION. It plays an important role in FERTILITY as well as in METABOLISM of LIPIDS.
A genus of CRUSTACEA of the order ANOSTRACA, found in briny pools and lakes and often cultured for fish food. It has 168 chromosomes and differs from most crustaceans in that its blood contains hemoglobin.
Unsaturated derivatives of the ESTRANES with methyl groups at carbon-13, with no carbon at carbon-10, and with no more than one carbon at carbon-17. They must contain one or more double bonds.
Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action.
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
Drugs that bind to but do not activate SEROTONIN 5-HT1 RECEPTORS, thereby blocking the actions of SEROTONIN 5-HT1 RECEPTOR AGONISTS. Included under this heading are antagonists for one or more of the specific 5-HT1 receptor subtypes.
The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in neoplastic tissue.
A potent noncompetitive antagonist of the NMDA receptor (RECEPTORS, N-METHYL-D-ASPARTATE) used mainly as a research tool. The drug has been considered for the wide variety of neurodegenerative conditions or disorders in which NMDA receptors may play an important role. Its use has been primarily limited to animal and tissue experiments because of its psychotropic effects.
The male gonad containing two functional parts: the SEMINIFEROUS TUBULES for the production and transport of male germ cells (SPERMATOGENESIS) and the interstitial compartment containing LEYDIG CELLS that produce ANDROGENS.
Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others.
Histochemical localization of immunoreactive substances using labeled antibodies as reagents.
Disorders characterized by an abnormal reduction in muscle volume due to a decrease in the size or number of muscle fibers. Atrophy may result from diseases intrinsic to muscle tissue (e.g., MUSCULAR DYSTROPHY) or secondary to PERIPHERAL NERVOUS SYSTEM DISEASES that impair innervation to muscle tissue (e.g., MUSCULAR ATROPHY, SPINAL).
Cell surface receptors that are specific for INTERLEUKIN-1. Included under this heading are signaling receptors, non-signaling receptors and accessory proteins required for receptor signaling. Signaling from interleukin-1 receptors occurs via interaction with SIGNAL TRANSDUCING ADAPTOR PROTEINS such as MYELOID DIFFERENTIATION FACTOR 88.
A variation of the PCR technique in which cDNA is made from RNA via reverse transcription. The resultant cDNA is then amplified using standard PCR protocols.
Surgical removal or artificial destruction of gonads.
Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).
Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.
All of the processes involved in increasing CELL NUMBER including CELL DIVISION.
Compounds with BENZENE fused to AZEPINES.
The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.
Benzopyrroles with the nitrogen at the number one carbon adjacent to the benzyl portion, in contrast to ISOINDOLES which have the nitrogen away from the six-membered ring.
Unsaturated androstanes which are substituted with one or more hydroxyl groups in any position in the ring system.
The unspecified form of the steroid, normally a major metabolite of TESTOSTERONE with androgenic activity. It has been implicated as a regulator of gonadotropin secretion.
CELL LINES derived from the CV-1 cell line by transformation with a replication origin defective mutant of SV40 VIRUS, which codes for wild type large T antigen (ANTIGENS, POLYOMAVIRUS TRANSFORMING). They are used for transfection and cloning. (The CV-1 cell line was derived from the kidney of an adult male African green monkey (CERCOPITHECUS AETHIOPS).)
The uptake of naked or purified DNA by CELLS, usually meaning the process as it occurs in eukaryotic cells. It is analogous to bacterial transformation (TRANSFORMATION, BACTERIAL) and both are routinely employed in GENE TRANSFER TECHNIQUES.
Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important.
A group of compounds that contain the structure SO2NH2.
Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses.
The action of a drug that may affect the activity, metabolism, or toxicity of another drug.
Tumors or cancer of the PROSTATE which can grow in the presence of low or residual amount of androgen hormones such as TESTOSTERONE.
Elements of limited time intervals, contributing to particular results or situations.
Purine bases found in body tissues and fluids and in some plants.
A plant genus of the family RUTACEAE. Members contain ponfolin, a coumarin (COUMARINS).
Compounds with a six membered aromatic ring containing NITROGEN. The saturated version is PIPERIDINES.
Cells grown in vitro from neoplastic tissue. If they can be established as a TUMOR CELL LINE, they can be propagated in cell culture indefinitely.
Established cell cultures that have the potential to propagate indefinitely.
Endogenous compounds and drugs that bind to and activate SEROTONIN RECEPTORS. Many serotonin receptor agonists are used as ANTIDEPRESSANTS; ANXIOLYTICS; and in the treatment of MIGRAINE DISORDERS.
Drugs that selectively bind to but do not activate HISTAMINE H3 RECEPTORS. They have been used to correct SLEEP WAKE DISORDERS and MEMORY DISORDERS.
An X-linked recessive form of spinal muscular atrophy. It is due to a mutation of the gene encoding the ANDROGEN RECEPTOR.
A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research.
Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.
Naturally occurring or experimentally induced animal diseases with pathological processes sufficiently similar to those of human diseases. They are used as study models for human diseases.
Descriptions of specific amino acid, carbohydrate, or nucleotide sequences which have appeared in the published literature and/or are deposited in and maintained by databanks such as GENBANK, European Molecular Biology Laboratory (EMBL), National Biomedical Research Foundation (NBRF), or other sequence repositories.
Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
An oxidoreductase that catalyzes the conversion of 3-oxo-delta4 steroids into their corresponding 5alpha form. It plays an important role in the conversion of TESTOSTERONE into DIHYDROTESTOSTERONE and PROGESTERONE into DIHYDROPROGESTERONE.
Peptides whose amino and carboxy ends are linked together with a peptide bond forming a circular chain. Some of them are ANTI-INFECTIVE AGENTS. Some of them are biosynthesized non-ribosomally (PEPTIDE BIOSYNTHESIS, NON-RIBOSOMAL).
Carrier proteins produced in the Sertoli cells of the testis, secreted into the seminiferous tubules, and transported via the efferent ducts to the epididymis. They participate in the transport of androgens. Androgen-binding protein has the same amino acid sequence as SEX HORMONE-BINDING GLOBULIN. They differ by their sites of synthesis and post-translational oligosaccharide modifications.
The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.
Increase in constituent cells in the PROSTATE, leading to enlargement of the organ (hypertrophy) and adverse impact on the lower urinary tract function. This can be caused by increased rate of cell proliferation, reduced rate of cell death, or both.
The observable response an animal makes to any situation.
A delta-4 C19 steroid that is produced not only in the TESTIS, but also in the OVARY and the ADRENAL CORTEX. Depending on the tissue type, androstenedione can serve as a precursor to TESTOSTERONE as well as ESTRONE and ESTRADIOL.
One of the ESTROGEN RECEPTORS that has greater affinity for ISOFLAVONES than ESTROGEN RECEPTOR ALPHA does. There is great sequence homology with ER alpha in the DNA-binding domain but not in the ligand binding and hinge domains.
An antagonist of ANGIOTENSIN TYPE 1 RECEPTOR with antihypertensive activity due to the reduced pressor effect of ANGIOTENSIN II.
Drugs that bind to but do not activate GABA-B RECEPTORS thereby blocking the actions of endogenous or exogenous GABA-B RECEPTOR AGONISTS.
Identification of proteins or peptides that have been electrophoretically separated by blot transferring from the electrophoresis gel to strips of nitrocellulose paper, followed by labeling with antibody probes.
Drugs that inhibit 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE. They are commonly used to reduce the production of DIHYDROTESTOSTERONE.
Within a eukaryotic cell, a membrane-limited body which contains chromosomes and one or more nucleoli (CELL NUCLEOLUS). The nuclear membrane consists of a double unit-type membrane which is perforated by a number of pores; the outermost membrane is continuous with the ENDOPLASMIC RETICULUM. A cell may contain more than one nucleus. (From Singleton & Sainsbury, Dictionary of Microbiology and Molecular Biology, 2d ed)
Cell surface receptors that bind BRADYKININ and related KININS with high affinity and trigger intracellular changes which influence the behavior of cells. The identified receptor types (B-1 and B-2, or BK-1 and BK-2) recognize endogenous KALLIDIN; t-kinins; and certain bradykinin fragments as well as bradykinin itself.
A histamine congener, it competitively inhibits HISTAMINE binding to HISTAMINE H2 RECEPTORS. Cimetidine has a range of pharmacological actions. It inhibits GASTRIC ACID secretion, as well as PEPSIN and GASTRIN output.
An eleven-amino acid neurotransmitter that appears in both the central and peripheral nervous systems. It is involved in transmission of PAIN, causes rapid contractions of the gastrointestinal smooth muscle, and modulates inflammatory and immune responses.
Conditions in which a bifurcation or trifurcation of the molar tooth root becomes denuded as a result of periodontal disease. It may be followed by tooth mobility, temperature sensitivity, pain, and alveolar bone resorption.
A 21-amino acid peptide produced in a variety of tissues including endothelial and vascular smooth-muscle cells, neurons and astrocytes in the central nervous system, and endometrial cells. It acts as a modulator of vasomotor tone, cell proliferation, and hormone production. (N Eng J Med 1995;333(6):356-63)
Compounds that selectively bind to and block the activation of ADENOSINE A3 RECEPTORS.
A class of cell surface receptors for TACHYKININS with a preference for SUBSTANCE P. Neurokinin-1 (NK-1) receptors have been cloned and are members of the G protein coupled receptor superfamily. They are found on many cell types including central and peripheral neurons, smooth muscle cells, acinar cells, endothelial cells, fibroblasts, and immune cells.
Seven membered heterocyclic rings containing a NITROGEN atom.
The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM.
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
A biochemical messenger and regulator, synthesized from the essential amino acid L-TRYPTOPHAN. In humans it is found primarily in the central nervous system, gastrointestinal tract, and blood platelets. Serotonin mediates several important physiological functions including neurotransmission, gastrointestinal motility, hemostasis, and cardiovascular integrity. Multiple receptor families (RECEPTORS, SEROTONIN) explain the broad physiological actions and distribution of this biochemical mediator.
Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control (induction or repression) of gene action at the level of transcription or translation.
Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.
A derivative of benzodiazepine that acts on the cholecystokinin A (CCKA) receptor to antagonize CCK-8's (SINCALIDE) physiological and behavioral effects, such as pancreatic stimulation and inhibition of feeding.
Cell surface proteins that bind cholecystokinin (CCK) with high affinity and trigger intracellular changes influencing the behavior of cells. Cholecystokinin receptors are activated by GASTRIN as well as by CCK-4; CCK-8; and CCK-33. Activation of these receptors evokes secretion of AMYLASE by pancreatic acinar cells, acid and PEPSIN by stomach mucosal cells, and contraction of the PYLORUS and GALLBLADDER. The role of the widespread CCK receptors in the central nervous system is not well understood.
Supporting cells projecting inward from the basement membrane of SEMINIFEROUS TUBULES. They surround and nourish the developing male germ cells and secrete ANDROGEN-BINDING PROTEIN and hormones such as ANTI-MULLERIAN HORMONE. The tight junctions of Sertoli cells with the SPERMATOGONIA and SPERMATOCYTES provide a BLOOD-TESTIS BARRIER.
Specific molecular sites or proteins on or in cells to which VASOPRESSINS bind or interact in order to modify the function of the cells. Two types of vasopressin receptor exist, the V1 receptor in the vascular smooth muscle and the V2 receptor in the kidneys. The V1 receptor can be subdivided into V1a and V1b (formerly V3) receptors.
A microsomal cytochrome P450 enzyme that catalyzes the 17-alpha-hydroxylation of progesterone or pregnenolone and subsequent cleavage of the residual two carbons at C17 in the presence of molecular oxygen and NADPH-FERRIHEMOPROTEIN REDUCTASE. This enzyme, encoded by CYP17 gene, generates precursors for glucocorticoid, androgen, and estrogen synthesis. Defects in CYP17 gene cause congenital adrenal hyperplasia (ADRENAL HYPERPLASIA, CONGENITAL) and abnormal sexual differentiation.
One of the ESTROGEN RECEPTORS that has marked affinity for ESTRADIOL. Its expression and function differs from, and in some ways opposes, ESTROGEN RECEPTOR BETA.
Drugs that bind to but do not activate SEROTONIN 5-HT4 RECEPTORS, thereby blocking the actions of SEROTONIN or SEROTONIN RECEPTOR AGONISTS.
The D-enantiomer is a potent and specific antagonist of NMDA glutamate receptors (RECEPTORS, N-METHYL-D-ASPARTATE). The L form is inactive at NMDA receptors but may affect the AP4 (2-amino-4-phosphonobutyrate; APB) excitatory amino acid receptors.
An anthracene derivative that disrupts MITOCHONDRIA function and structure and is used for the treatment of DERMATOSES, especially PSORIASIS. It may cause FOLLICULITIS.
A group of polycyclic compounds closely related biochemically to TERPENES. They include cholesterol, numerous hormones, precursors of certain vitamins, bile acids, alcohols (STEROLS), and certain natural drugs and poisons. Steroids have a common nucleus, a fused, reduced 17-carbon atom ring system, cyclopentanoperhydrophenanthrene. Most steroids also have two methyl groups and an aliphatic side-chain attached to the nucleus. (From Hawley's Condensed Chemical Dictionary, 11th ed)
Common name for small PASSERIFORMES in the family Fringillidae. They have a short stout bill (BEAK) adapted for crushing SEEDS. Some species of Old World finches are called CANARIES.
The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.
Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
A subclass of cannabinoid receptor found primarily on central and peripheral NEURONS where it may play a role modulating NEUROTRANSMITTER release.
A saclike, glandular diverticulum on each ductus deferens in male vertebrates. It is united with the excretory duct and serves for temporary storage of semen. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)
An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.
A birth defect due to malformation of the URETHRA in which the urethral opening is below its normal location. In the male, the malformed urethra generally opens on the ventral surface of the PENIS or on the PERINEUM. In the female, the malformed urethral opening is in the VAGINA.
Cell surface proteins that bind THROMBOXANES with high affinity and trigger intracellular changes influencing the behavior of cells. Some thromboxane receptors act via the inositol phosphate and diacylglycerol second messenger systems.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.
The parts of a macromolecule that directly participate in its specific combination with another molecule.
Those characteristics that distinguish one SEX from the other. The primary sex characteristics are the OVARIES and TESTES and their related hormones. Secondary sex characteristics are those which are masculine or feminine but not directly related to reproduction.
A competitive histamine H2-receptor antagonist. Its main pharmacodynamic effect is the inhibition of gastric secretion.
A subfamily of G-PROTEIN-COUPLED RECEPTORS that bind the neurotransmitter DOPAMINE and modulate its effects. D2-class receptor genes contain INTRONS, and the receptors inhibit ADENYLYL CYCLASES.
A group of cytochromes with covalent thioether linkages between either or both of the vinyl side chains of protoheme and the protein. (Enzyme Nomenclature, 1992, p539)
Cytoplasmic proteins that specifically bind glucocorticoids and mediate their cellular effects. The glucocorticoid receptor-glucocorticoid complex acts in the nucleus to induce transcription of DNA. Glucocorticoids were named for their actions on blood glucose concentration, but they have equally important effects on protein and fat metabolism. Cortisol is the most important example.
A nonapeptide messenger that is enzymatically produced from KALLIDIN in the blood where it is a potent but short-lived agent of arteriolar dilation and increased capillary permeability. Bradykinin is also released from MAST CELLS during asthma attacks, from gut walls as a gastrointestinal vasodilator, from damaged tissues as a pain signal, and may be a neurotransmitter.
A class of cell surface receptors for tachykinins that prefers neurokinin A; (NKA, substance K, neurokinin alpha, neuromedin L), neuropeptide K; (NPK); or neuropeptide gamma over other tachykinins. Neurokinin-2 (NK-2) receptors have been cloned and are similar to other G-protein coupled receptors.
Compounds which inhibit or antagonize the action or biosynthesis of estrogenic compounds.
Compounds that inhibit or block the activity of CANNABINOID RECEPTORS.
Compounds or agents that combine with an enzyme in such a manner as to prevent the normal substrate-enzyme combination and the catalytic reaction.
The process in developing sex- or gender-specific tissue, organ, or function after SEX DETERMINATION PROCESSES have set the sex of the GONADS. Major areas of sex differentiation occur in the reproductive tract (GENITALIA) and the brain.
Agents that are administered in association with anesthetics to increase effectiveness, improve delivery, or decrease required dosage.
Injections into the cerebral ventricles.
A specific opiate antagonist that has no agonist activity. It is a competitive antagonist at mu, delta, and kappa opioid receptors.
These compounds stimulate anabolism and inhibit catabolism. They stimulate the development of muscle mass, strength, and power.
Use of electric potential or currents to elicit biological responses.
A statistical technique that isolates and assesses the contributions of categorical independent variables to variation in the mean of a continuous dependent variable.
DNA sequences which are recognized (directly or indirectly) and bound by a DNA-dependent RNA polymerase during the initiation of transcription. Highly conserved sequences within the promoter include the Pribnow box in bacteria and the TATA BOX in eukaryotes.
Drugs that bind to and block the activation of MINERALOCORTICOID RECEPTORS by MINERALOCORTICOIDS such as ALDOSTERONE.
Specific proteins found in or on cells of progesterone target tissues that specifically combine with progesterone. The cytosol progesterone-receptor complex then associates with the nucleic acids to initiate protein synthesis. There are two kinds of progesterone receptors, A and B. Both are induced by estrogen and have short half-lives.
Compounds containing 1,3-diazole, a five membered aromatic ring containing two nitrogen atoms separated by one of the carbons. Chemically reduced ones include IMIDAZOLINES and IMIDAZOLIDINES. Distinguish from 1,2-diazole (PYRAZOLES).
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The measurement of an organ in volume, mass, or heaviness.
Drugs that bind to and block the activation of ADRENERGIC BETA-2 RECEPTORS.
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Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system. (1/288)

Advanced prostate cancer is treated by androgen ablation and/or androgen receptor (AR) antagonists. In order to investigate the mechanisms relevant to the development of therapy-resistant tumours, we established a new tumour model which closely resembles the situation in patients who receive androgen ablation therapy. Androgen-sensitive LNCaP cells were kept in androgen-depleted medium for 87 passages. The new LNCaP cell subline established in this manner, LNCaP-abl, displayed a hypersensitive biphasic proliferative response to androgen until passage 75. Maximal proliferation of LNCaP-abl cells was achieved at 0.001 nM of the synthetic androgen methyltrienolone (R1881), whereas 0.01 nM of this compound induced the same effect in parental cells. At later passages (> 75), androgen exerted an inhibitory effect on growth of LNCaP-abl cells. The non-steroidal anti-androgen bicalutamide stimulated proliferation of LNCaP-abl cells. AR protein expression in LNCaP-abl cells increased approximately fourfold. The basal AR transcriptional activity was 30-fold higher in LNCaP-abl than in LNCaP cells. R1881 stimulated reporter gene activity in LNCaP-abl cells even at 0.01 nM, whereas 0.1 nM of R1881 was needed for induction of the same level of reporter gene activity in LNCaP cells. Bicalutamide that acts as a pure antagonist in parental LNCaP cells showed agonistic effects on AR transactivation activity in LNCaP-abl cells and was not able to block the effects of androgen in these cells. The non-steroidal AR blocker hydroxyflutamide exerted stimulatory effects on AR activity in both LNCaP and LNCaP-abl cells; however, the induction of reporter gene activity by hydroxyflutamide was 2.4- to 4-fold higher in the LNCaP-abl subline. The changes in AR activity were associated neither with a new alteration in AR cDNA sequence nor with amplification of the AR gene. Growth of LNCaP-abl xenografts in nude mice was stimulated by bicalutamide and repressed by testosterone. In conclusion, our results show for the first time that the nonsteroidal anti-androgen bicalutamide acquires agonistic properties during long-term androgen ablation. These findings may have repercussions on the natural course of prostate cancer with androgen deprivation and on strategies of therapeutic intervention.  (+info)

Inhibition of p160-mediated coactivation with increasing androgen receptor polyglutamine length. (2/288)

Normal polymorphic size variation of the exon 1 CAG microsatellite of the androgen receptor (AR) is associated with prostate cancer, benign prostatic hyperplasia and male infertility. Furthermore, abnormal expansion of the satellite leads to Kennedy's disease. We have shown recently that the AR N-terminal domain (NTD), which contains the polyglutamine (polyQ) stretch (encoded by the CAG repeat), functionally interacts with the C-termini of p160 coactivators. In the present study we explored possible AR CAG size effects on the p160 coactivator-mediated transactivation activity of the receptor. First, we mapped the p160 coactivator interaction on the AR NTD and found an interaction surface between amino acids 351 and 537. Although this region is 'downstream' from the polyQ stretch, it is still within the AR NTD, is implicated in constitutive transactivation activity of the receptor, and thus might be subject to polyQ size modulation. Indeed, cotrans- fection experiments in cultured prostate epithelial cells, using AR constructs of varying CAG sizes and p160 coactivator expression vectors, revealed that increased polyQ length, up to a size of 42 repeats, inhibited both basal and coactivator-mediated AR transactivation activity. AR expression in these cells, on the other hand, was unaffected by the same increased CAG repeat size range. We conclude that the AR NTD contributes to AR transactivation activity via functional interactions with p160 coactivators and that increasing polyQ length negatively affects p160-mediated coactivation of the AR. This molecular mechanism thus might explain, at least in part, the observed phenotypic effects of the AR CAG size polymorphism.  (+info)

Acute impairment of relaxation by low levels of testosterone in porcine coronary arteries. (3/288)

OBJECTIVES: While there are many suggested reasons for the marked gender bias in cardiovascular events, much of the available data indicate that circulating estrogens are cardioprotective. The possibility that endogenous androgens may be detrimental to the cardiovascular system has received relatively less attention. We investigated the short-term modulatory effects of various concentrations of testosterone on vascular function in isolated porcine coronary artery rings. RESULTS: The higher concentrations (> 1 microM) of testosterone relaxed U46619-contracted coronary artery rings in an endothelium-independent manner. This direct effect was insensitive to the testosterone receptor antagonists, flutamide and cyproterone acetate. Short-term exposure (20 min) to low levels of testosterone (1-100 nM), which were ineffective on their own on vascular function, significantly diminished relaxation to bradykinin and calcium ionophore A23187 but not those produced by levcromakalim and sodium nitroprusside. The inhibitory effect observed with 1 nM testosterone was only partially reversed by flutamide and cyproterone acetate and unaltered in the presence of actinomycin D and cycloheximide. CONCLUSIONS: These results demonstrate that acute treatment with testosterone, at concentrations that have no effect on their own, reduces vasorelaxation. Furthermore, they suggest that this modulatory action may be in part independent of the classical testosterone receptor since it was not completely sensitive to the anti-androgens and was not inhibited by the transcriptional and translational inhibitors. These findings support the postulation that testosterone may have unfavorable influences on vascular function.  (+info)

Differential effects of 17beta-estradiol and testosterone on the contractile responses of porcine coronary arteries. (4/288)

1. We investigated the effects of short-term exposure to physiological levels of 17beta-estradiol and testosterone on vasocontractile responses in porcine coronary artery rings. 2. Concentration-response curves to endothelin-1, 5-hydroxytryptamine, the thromboxane analogue U46619 and KCl were constructed in endothelium-intact and endothelium-disrupted artery rings. 3. Thirty minutes exposure to 17beta-estradiol (1 and 30 nM) significantly attenuated vasoconstriction to endothelin-1, 5-hydroxytryptamine and U46619. Conversely, the same concentrations of testosterone significantly potentiated responses elicited by these contractile agents. These inhibitory effects of 17beta-estradiol and enhancing actions of testosterone on contractions were endothelium-independent. KCl-mediated contractions were unaffected by the presence of either sex hormones. 4. The oestrogen receptor antagonists, tamoxifen (10 microM) and ICI 182,780 (10 microM), were unable to reverse the inhibitory influence 1 nM 17beta-estradiol had on the agonist-mediated contractile responses. Similarly, the androgen receptor antagonists, flutamide (10 microM) and cyproterone acetate (10 microM), failed to affect the potentiating activities of 1 nM testosterone. The alteration in vasoconstrictive responses observed following acute exposure to either 1 nM 17beta-estradiol and 1 nM testosterone were apparent even in the presence of the protein synthesis inhibitor cycloheximide (10 microM) and the transcription inhibitor actinomycin D (10 microM). 6. In conclusion, we report a unique type of sex hormone action on the coronary vasculature. These events occur at low nanomolar concentrations of 17beta-estradiol and testosterone, are insensitive to conventional sex hormone receptor antagonists, are not blocked by de novo protein synthesis inhibitors and have rapid time-courses that are uncharacteristic of classical genomic activities.  (+info)

Specific recognition of androgens by their nuclear receptor. A structure-function study. (5/288)

Androgens, like progestins, are 3-ketosteroids with structural differences restricted to the 17beta substituent in the steroid D-ring. To better understand the specific recognition of ligands by the human androgen receptor (hAR), a homology model of the ligand-binding domain (LBD) was constructed based on the progesterone receptor LBD crystal structure. Several mutants of residues potentially involved in the specific recognition of ligands in the hAR were constructed and tested for their ability to bind agonists. Their transactivation capacity in response to agonist (R1881) and antagonists (cyproterone acetate, hydroxyflutamide, and ICI 176344) was also measured. Substitution of His(874) by alanine, only marginally impairs the ligand-binding and transactivation capacity of the hAR receptor. In contrast, mutations of Thr(877) and, to a greater extent, Asn(705) perturb ligand recognition, alter transactivation efficiency, and broaden receptor specificity. Interestingly, the N705A mutant acquires progesterone receptor (PR) properties for agonist ligands but, unlike wild type AR and PR, loses the capacity to repress transactivation with nonsteroidal antagonists. Models of the hAR.LBD complexes with several ligands are presented, which suggests new directions for drug design.  (+info)

The RING finger protein SNURF modulates nuclear trafficking of the androgen receptor. (6/288)

The androgen receptor (AR) is a transcription factor that mediates androgen action. We have used the green fluorescent protein (GFP) technique to investigate dynamics of nuclear trafficking of human AR in living cells. In the absence of ligand, the GFP-AR fusion protein is distributed between cytoplasm and nuclei. Androgen exposure leads to a rapid and complete import of GFP-AR to nuclei of CV-1 cells (>=90% nuclear in 30 minutes), whereas a pure antiandrogen, Casodex, elicits a slower (<40% nuclear in 30 minutes) and incomplete transfer. Unliganded ARs with mutations in the basic amino acids of the bipartite nuclear localization signal (NLS) within the second zinc finger and the hinge region are predominantly cytoplasmic and their androgen-dependent nuclear import is severely compromised ((3/4)20% nuclear in 30 minutes). Interestingly, substitutions of the Leu residues flanking the bipartite NLS lead to inefficient nuclear transfer in response to androgen ((3/4)20% nuclear in 30 minutes). The ligand-binding domain of AR, which represses bipartite NLS activity, contains an agonist-specific NLS. The small nuclear RING finger protein SNURF, which interacts with AR through a region overlapping with the bipartite NLS, facilitates AR import to nuclei and retards its export on hormone withdrawal. More AR is associated with the nuclear matrix in the presence than absence of coexpressed SNURF. We suggest that the SNURF-mediated tethering of AR in nuclei represents a novel mechanism for activating steroid receptor functions.  (+info)

Antiandrogenic effects of novel androgen synthesis inhibitors on hormone-dependent prostate cancer. (7/288)

We have found that in addition to being potent inhibitors of 17alpha-hydroxylase/C17,20-lyase and/or 5alpha-reductase, some of our novel androgen synthesis inhibitors also interact with the mutated androgen receptor (AR) expressed in LNCaP prostate cancer cells and the wild-type AR expressed in hormone-dependent prostatic carcinomas. The effects of these compounds on the proliferation of hormone-dependent human prostatic cancer cells were determined in vitro and in vivo. L-2 and L-10 are delta4-3-one-pregnane derivatives. L-35 and L-37 are delta5-3beta-ol-androstane derivatives, and L-36 and L-39 are delta4-3-one-androstane-derived compounds. L-2, L-10, and L-36 (L-36 at low concentrations) stimulated the growth of LNCaP cells, indicating that they were interacting agonistically with the mutated AR expressed in LNCaP cells. L-35, L-37, and L-39 acted as LNCaP AR antagonists. To determine whether the growth modulatory effects of our novel compounds were specific for the mutated LNCaP AR, competitive binding studies were performed with LNCaP cells and PC-3 cells stably transfected with the wild-type AR (designated PC-3AR). Regardless of AR receptor type, all of our novel compounds were effective at preventing binding of the synthetic androgen methyl-trienolone[17alpha-methyl-(3H)-R1881 to both the LNCaP AR and the wildtype AR. L-36, L-37, and L-39 (5.0 microM) prevented binding by >90%, whereas L-35 inhibited binding by 30%. To determine whether the compounds were acting as agonists or antagonists, LNCaP cells and PC-3AR cells were transfected with the pMAMneoLUC reporter gene. When luciferase activity was induced by dihydrotestosterone, all of the compounds were found to be potent inhibitors of transcriptional activity, and the pattern of inhibition was similar for both receptor types. However, L-2, L-10, and L-36 were determined to be AR agonists, and L-35, L-37, and L-39 were wild-type AR antagonists. When tested in vivo, L-39 was the only AR antagonist that proved to be effective at inhibiting the growth of LNCaP prostate tumor growth. L-39 slowed tumor growth rate in LNCaP tumors grown in male SCID mice to the same level as orchidectomy, significantly reduced tumor weights (P < 0.05), significantly lowered serum levels of prostate-specific antigen (P < 0.02), and significanty lowered serum levels of testosterone (P < 0.05). L-39 also proved to be effective when tested against the PC-82 prostate cancer xenograft that expresses wild-type AR. These results show that some of our compounds initially developed to be inhibitors of androgen synthesis also interact with the human AR and modulate the proliferation of hormone-dependent prostatic cancer cells. Therefore, compounds such as L-39, which have multifunctional activities, hold promise for the treatment of androgen-dependent prostate tumors.  (+info)

Androgen receptor antagonism by the organophosphate insecticide fenitrothion. (8/288)

Organophosphate insecticides represent one of the most widely used classes of pesticides with high potential for human exposure in both rural and residential environments. We investigated the interaction of the organophosphothioate pesticide fenitrothion (O,O-dimethyl O-(4-nitro-m-tolyl) phosphorothioate) with the human androgen receptor (AR). Fenitrothion blocked dihydrotestosterone-dependent AR activity in a concentration-dependent and competitive manner in HepG2 human hepatoma liver cells transiently transfected with human AR and an AR-dependent luciferase reporter gene. Schild regression analysis yielded an equilibrium dissociation constant value of 2.18 x 10(-8) M. To determine the antiandrogenic potential of fenitrothion in vivo, 7-week-old castrated Sprague-Dawley rats were dosed once a day for 7 days with testosterone propionate (50 microg/day, sc) plus gavage doses of either corn oil vehicle or fenitrothion (15 or 30 mg/kg/day). An additional group of rats was given testosterone propionate and flutamide (50 mg/kg/day). Motor activity and acetylcholinesterase activity in whole blood and brain were also assessed. Both fenitrothion and the reference antiandrogen flutamide caused significant decreases in the ventral prostate, seminal vesicle, and levator ani plus bulbocavernosus muscles tissue weights. In contrast, blood acetylcholinesterase activity, a standard biomarker of organophosphate poisoning, was only inhibited at the higher dose of fenitrothion (30 mg/kg). Our results demonstrate that fenitrothion is a competitive AR antagonist, comparable in potency to the pharmaceutical antiandrogen flutamide and more potent, based on in vitro assays, than the known environmental antiandrogens linuron and p,p'-, 2,2-bis(p-hydroxyphenyl)-1,1-dichloroethylene ( p,p'-DDE).  (+info)

Endogenous testosterone and estradiol are thought to be cardio-protective in men. We wanted to determine the effects of 2 different anti-androgen therapies on arterial stiffness as one suppresses (goserelin--a gonadotrophin-releasing hormone analog) while the other increases (bicalutamide--an androgen receptor blocker) both testosterone and estradiol. We conducted a randomized trial on 43 men (mean age, 71.2 +/- 6.2 years) with localized prostate cancer. They received either goserelin or bicalutamide for 24 weeks. Carotid-femoral (C-F) and carotid-radial (C-R) pulse wave velocities (PWVs) were measured. Twenty age- and disease-matched men with prostate cancer on no active treatment were studied in a similar manner. After 12 weeks of goserelin, radial artery PWV increased significantly from baseline and a nonsignificant increase was observed in femoral PWV (change from baseline radial: +1.4 m/s, P = .002, femoral: +0.9 m/s, P = .127) Both PWV measures increased significantly with bicalutamide ...
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Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.
A novel oxachrysenone series (2) of nonsteroidal selective androgen receptor modulators (SARM) was developed based on the 6-aryl-2-quinolinones (1). Synthesis and preliminary SAR results based on in vitro assays are discussed. In the cotransfection assay, lead compound 5d showed AR agonist activity …
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SARMs might fall into the same category as Steroids, a class drug, amid the latest crackdowns on its sale. The two are similar in some way but not exactly.
Contents1Intro2What are SARMs?3SARMs VS Steroids4Kinds of SARMs4.1GW501516-Cardarine:4.2SR9009-Stenabolic:4.3MK677-Nutrobal:4.4S4-Andarine:4.5LGD4033-Ligandrol-Anabolicum:4.6MK2866-Ostarine-Ostabolic:4.7RAD140-Testolone:5How to stack SARMs5.1Fat loss:5.2Endurance:5.3Recovery:5.4Strength and lean muscle gains:5.5Healing injuries:6Stacking with Anabolics6.1The harsh ones...6.2Without ...
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Inhibition of C5aR activity by CHIPS variants with C-terminal truncation. Fluo-3AM labeled U937/C5aR transfectants were preincubated with CHIPS variants and sti
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Androgen receptor antagonists: Drugs that bind directly to and block the AR.[66][67] These drugs include the steroidal ... Androgen receptor; Progesterone receptor; Estrogen receptor; GnRH receptor; 5α-Reductase; CYP17A1 (17α-hydroxylase/. 17,20- ... Androgen receptor degraders[edit]. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ...
Ran F, Xing H, Liu Y, Zhang D, Li P, Zhao G (2015). "Recent Developments in Androgen Receptor Antagonists". Archiv der ... RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was ... RU-59063 has high affinity for the human androgen receptor (AR) (Ki = 2.2 nM; Ka = 5.4 nM) and 1,000-fold selectivity for the ... Liu B, Su L, Geng J, Liu J, Zhao G (2010). "Developments in nonsteroidal antiandrogens targeting the androgen receptor". ...
They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Hirawat S, Budman DR, Kreis W (June 2003). "The androgen receptor: structure, mutations, and antiandrogens". Cancer Invest. 21 ... In addition, although CPA reduces androgen production in the gonads, it can increase the production of adrenal androgens, in ... and Its Receptor: Actions, Signal Transduction Pathways and Phenotypes Observed in PRL Receptor Knockout Mice". Endocrine ...
They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like ... There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ...
"Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211-47. doi:10.2174/ ... of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone receptors. ... synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): ...
321-. ISBN 978-1-901865-55-4. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...
Similarly to flutamide, AA560 is a selective antagonist of the androgen receptor (AR) and consequently shows progonadotropic ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ...
CPA is a potent competitive antagonist of the androgen receptor (AR), the biological target of androgens such as testosterone ... ISBN 978-1-4496-8695-6. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... its potency as an androgen receptor antagonist is quite weak. In order to take full advantage of its antiandrogenic activity, ... It has been said that in combined androgen blockade regimens with castration and CPA as the AR antagonist for prostate cancer, ...
Antiandrogens that directly block the androgen receptor are known as androgen receptor antagonists or blockers, while ... nonsteroidal antiandrogens are highly selective for the androgen receptor and act as pure androgen receptor antagonists. ... It works as an antiandrogen mainly by acting as an androgen receptor antagonist. The medication is also a weak steroidogenesis ... In addition to its actions as an antigonadotropin, cyproterone acetate is an androgen receptor antagonist. However, this action ...
Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding ... "Characterization of androgen receptors after photoaffinity labelling with [3H]methyltrienolone (R1881)". Journal of Steroid ... "Towards the mapping of the progesterone and androgen receptors". J. Steroid Biochem. 27 (1-3): 255-69. doi:10.1016/0022-4731(87 ...
It is a selective antagonist of the androgen receptor and consequently has progonadotropic effects by increasing gonadotropin ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... "Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3): 367-400. doi:10.1016/0163-7258(84)90010-x. PMID ... Thomson, D. S. (1989). "Pharmacology of Anti-androgens in the Skin". Pharmacology of the Skin II. Handbook of Experimental ...
... acts as a selective antagonist of the androgen receptor (AR), preventing the effects of androgens like testosterone ... 11-. ISBN 978-981-256-920-2. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ... a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133-8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358. ... "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen receptor stabilization". Urology. 48 (1): ...
The medication is a silent antagonist of the androgen receptor. RU-56187 is 3- to 10-fold more potent as an antiandrogen than ... RU-57073 RU-58642 RU-59063 Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Distinguishing androgen receptor agonists and antagonists: distinct mechanisms of activation by medroxyprogesterone acetate and ... of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone receptors. ...
Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ... ISBN 978-1-60327-829-4. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Androgen receptor antagonists for prostate cancer therapy". Endocrine-Related Cancer. 21 (4): T105-18. doi:10.1530/ERC-13-0545 ... a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133-8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358. ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133-8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358. ... "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen receptor stabilization". Urology. 48 (1): ... It has been reported to possess an IC50 of 700 nM for the androgen receptor (AR), which is about 4-fold less than that of ...
"Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor". The Journal of ... Kawahara T, Minamoto H (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical Immunology, ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... It works by blocking the androgen receptor (AR), the biological target of the androgen sex hormones testosterone and ...
Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... 53-. ISBN 978-3-642-88429-0. Jost A (1971). "Use of androgen antagonists and antiandrogens in studies on sex differentiation". ... to be due to marked suppression of total and free androgen levels as well as additional blockade of the androgen receptor. CPA ... These conditions are worsened by the presence of androgens, and by suppressing androgen levels and blocking their actions, CPA ...
ISBN 978-3-527-30247-5. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... Eunuchs, owing to their low androgen levels and small sebaceous glands, do not develop seborrheic dermatitis. In addition to ... Zouboulis, Christos C.; Degitz, Klaus (2004). "Androgen action on human skin - from basic research to clinical significance". ...
Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... List of androgens/anabolic steroids R.A. Hill; H.L.J. Makin; D.N. Kirk; G.M. Murphy (23 May 1991). Dictionary of Steroids. CRC ...
Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Rosterolone is a derivative of mesterolone, which, in contrast, is an androgen and anabolic steroid. Steroidal antiandrogen ...
Non-steroidal selective androgen receptor antagonists, developed as a treatment for androgen-sensitive prostate cancer, are ... Enzalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Enzalutamide acts as a selective silent antagonist of the androgen receptor (AR), the biological target of androgens like ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ...
... is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Apalutamide acts as a selective competitive silent antagonist of the androgen receptor (AR), via the ligand-binding domain, and ... Kawahara, Takashi; Miyamoto, Hiroshi (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical ... "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): 43-9. doi:10.1097/PPO. ...
... - AdisInsight Research programme: androgen receptor antagonists (EM-4350, EM-5855, EM-6537) - AdisInsight v t e v t e. ... Gauthier S, Martel C, Labrie F (October 2012). "Steroid derivatives as pure antagonists of the androgen receptor". J. Steroid ... The drug acts as a potent and selective competitive antagonist of the androgen receptor (AR). Unlike other steroidal ... Fujii S, Kagechika H (June 2019). "Androgen receptor modulators: a review of recent patents and reports (2012-2018)". Expert ...
Non-steroidal selective androgen receptor antagonists, developed as a treatment for androgen-sensitive prostate cancer, are ... ANDROGEN RECEPTOR BLOCKERS: Androgen receptor blockers bind directly to the androgen receptor and either competitively inhibit ... Gauthier S, Martel C, Labrie F (October 2012). "Steroid derivatives as pure antagonists of the androgen receptor". The Journal ... ISBN 978-3-662-45138-0. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...
H2 receptor antagonists on androgen action in vivo and dihydrotestosterone binding to the rat prostate androgen receptor in ... the first H2 receptor antagonist. Burimamide, a specific competitive antagonist at the H2 receptor, 100 times more potent than ... 351-. ISBN 978-0-08-049451-7. Cimetidine is a weak androgen receptor antagonist. A controlled clinical study has not found ... The first breakthrough was Nα-guanylhistamine, a partial H2 receptor antagonist. From this lead, the receptor model was further ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... In accordance with the involvement of androgens in seborrhoea, antiandrogens, such as cyproterone acetate,[30] spironolactone,[ ... Zouboulis, Christos C.; Degitz, Klaus (2004). "Androgen action on human skin - from basic research to clinical significance". ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... "Androgen Physiology, Pharmacology and Abuse". PMID 25905231.. *^ Kenneth L. Becker (2001). Principles and Practice of ... In accordance with the involvement of androgens in seborrhoea, antiandrogens, such as cyproterone acetate,[27] spironolactone,[ ...
"An androgen receptor N-terminal domain antagonist for treating prostate cancer". J. Clin. Invest. 123 (7): 2948-60. doi:10.1172 ... McEwan, Iainj; Monaghan, Amye (2016). "A sting in the tail: The N-terminal domain of the androgen receptor as a drug target". ... Maughan BL, Antonarakis ES (2015). "Clinical Relevance of Androgen Receptor Splice Variants in Castration-Resistant Prostate ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... ER RBA = Relative binding affinity to estrogen receptors of rat uterine cytosol. Uterine weight = Percentage change in uterine ... Antagonists. *(R,R)-THC. *7β-Hydroxy-DHEA. *Chloroindazole. *Cytestrol acetate. *EM-800 (SCH-57050) ...
Flutamide, a pure antagonist of the androgen receptor, is effective in treating acne in women.[112][120] It appears to reduce ... a pure androgen receptor antagonist with the same mechanism as flutamide and with comparable or superior antiandrogenic ... is an aldosterone antagonist and is a useful acne treatment due to its ability to additionally block the androgen receptor at ... C. acnes' ability to bind and activate a class of immune system receptors known as toll-like receptors (TLRs), especially TLR2 ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor modulators. Estrogen receptor modulators. ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ...
D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Higher androgen levels lead to increased expression of androgen receptor. Fusion of myoblasts generates myotubes, in a process ... Androgens have also been found to signal through membrane androgen receptors, which are distinct from the classical nuclear ...
Androgen receptor antagonistsEdit. Androgens and anti-. androgens at the AR[82][83]. Compound. RBA (%). ... Androgen receptor degradersEdit. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... Androgen receptor antagonists: drugs that bind directly to and block the AR.[57][58] These drugs include the steroidal ... AR antagonists may not bind to or block membrane androgen receptors (mARs), which are distinct from the classical nuclear AR.[ ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Estrogen receptor modulators. Androgens and antiandrogens. Progestogens and antiprogestogens. List of estrogens. ... GnRH antagonists (e.g., cetrorelix). *Progestogens (e.g., chlormadinone acetate, cyproterone acetate, gestonorone caproate, ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... "In vivo estrogen bioactivities and in vitro estrogen receptor binding and transcriptional activities of anticoagulant synthetic ... Antagonists. *(R,R)-THC. *7β-Hydroxy-DHEA. *Chloroindazole. *Cytestrol acetate. *EM-800 ...
D2 receptor antagonists (prolactin releasers) (incl., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... GnRH and gonadotropin receptor modulators. Androgens and antiandrogens. Estrogens and antiestrogens. Progestogens and ... See also: Receptor/signaling modulators • Signaling peptide/protein receptor modulators • GnRH and gonadotropins ... Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide) ...
What is more clear is that DDE is a weak androgen receptor antagonist and can produce male genital tract abnormalities.[16][17] ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ...
Leukotriene antagonists For endocrine problemsEdit. androgens, antiandrogens, estrogens, gonadotropin, corticosteroids, human ... H2-receptor antagonists, cytoprotectants, prostaglandin analogues. *Lower digestive tract: laxatives, antispasmodics, ... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ... General: β-receptor blockers ("beta blockers"), calcium channel blockers, diuretics, cardiac glycosides, antiarrhythmics, ...
LNCaP cells express androgen receptor (AR), but PC-3 and DU-145 cells express very little or no AR. AR, an androgen-activated ... Bishayee K, Khuda-Bukhsh AR (September 2013). "5-lipoxygenase antagonist therapy: a new approach towards targeted cancer ... the androgen receptor, and the vitamin D receptor.[26] TMPRSS2-ETS gene family fusion, specifically TMPRSS2-ERG or TMPRSS2-ETV1 ... "Role of androgen receptor in the progression of human prostate tumor cells to androgen independence and insensitivity". The ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ... "Redirecting abiraterone metabolism to fine-tune prostate cancer anti-androgen therapy" (PDF). Nature. 533 (7604): 547-51. doi ...
Calcitriol, the hormonally active form of vitamin D, acting through the vitamin D receptor (VDR), has, like the androgens, been ... as evidenced by the findings that progesterone receptor (PR) knockout mice or mice treated with the PR antagonist mifepristone ... "Androgen receptor genotypes predict response to endocrine treatment in breast cancer patients". Br. J. Cancer. 105 (11): 1676- ... In complete androgen insensitivity syndrome, a condition in which the AR is defective and insensitive to androgens, there is ...
Receptor antagonists. *ERA (Atrasentan). *Retinoid X receptor (Bexarotene). *Sex steroid (Testolactone). Other/ungrouped. * ... primarily estrogens for breast cancer and androgens for prostate cancer) is known as hormonal therapy, while the inhibition of ... Active targeting uses biological molecules (antibodies, proteins, DNA and receptor ligands) to preferentially target the ... other growth-promoting influences (especially those associated with receptor tyrosine kinases) is known as targeted therapy. ...
Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor modulators. Estrogen receptor modulators. ... Levonorgestrel is a progestogen, i.e. progesterone-receptor agonist. The hormonal IUD's primary mechanism of action is to ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Antagonists. *(R,R)-THC. *7β-Hydroxy-DHEA. *Chloroindazole. *Cytestrol acetate. *EM-800 ...
Nuclear receptor. *Steroids: Sex steroids: Androgens (AR). *Estrogens (ER). *Progestogens (PR); Corticosteroids: ... Antagonists: 20-Carboxy-LTB4. *Amelubant. *CGS-23131 (LY-223982). *CGS-25019C ... an activator of a subfamily of transient receptor potential canonical (TRPC) cation channels, TRPC3/6/7. ... "Insulin receptor Thr1160 phosphorylation mediates lipid-induced hepatic insulin resistance". Journal of Clinical Investigation ...
Caplea A, Seachrist D, Dunphy G, Ely D (April 2001). "Sodium-induced rise in blood pressure is suppressed by androgen receptor ... Currently, the RAS is targeted pharmacologically by ACE inhibitors and angiotensin II receptor antagonists, also known as ... Baroreceptors in low pressure receptor zones (mainly in the venae cavae and the pulmonary veins, and in the atria) result in ... angiotensin receptor blockers (ARBs). The aldosterone system is directly targeted by spironolactone, an aldosterone antagonist ...
Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Estrogen receptor modulators. Androgens and antiandrogens. Progestogens and antiprogestogens. List of estrogens. ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Parthasarathy HK, MacDonald TM (2007). "Mineralocorticoid receptor antagonists". Curr. Hypertens. Rep. 9 (1): 45-52. PMID ... 7α-TS and 7α-TMS have been found to possess approximately equivalent affinity for the rat ventral prostate androgen receptor ( ... Yang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin ...
GnRH antagonist. *GnRH agonist (inducing an initial stimulation (flare up) followed by permanent blockage of the GnRH pituitary ... LH supports theca cells in the ovaries that provide androgens and hormonal precursors for estradiol production. At the time of ... Often, HCG medication is used as an LH substitute because it activates the same receptor. Medically used hCG is derived from ... Gonadal steroids (estrogens and androgens) generally have negative feedback effects on GnRH-1 release at the level of the ...
DES has been identified as an antagonist of all three isotypes of the estrogen-related receptors (ERRs), the ERRα, ERRβ, and ... as well as significant antagonism of the androgen, progesterone, and mineralocorticoid receptors (75%, 85%, and 50% inhibition ... It suppresses gonadal androgen production and hence circulating androgen levels due to its antigonadotropic effects; it ... DES is an estrogen; specifically, it is a highly potent full agonist of both of the estrogen receptors (ERs).[55][56] It has ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ... Hackenberg, Reinhard; Turgetto, Inga; Filmer, Angelika; Schulz, Klaus-Dieter (1993). "Estrogen and androgen receptor mediated ...
Fiorucci S, Zampella A, Distrutti E (2012). "Development of FXR, PXR and CAR agonists and antagonists for treatment of liver ... The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member ... "Farnesoid X Receptor (NR1H4)". Nuclear Receptor Resource.. *farnesoid+X-activated+receptor at the US National Library of ... thyroid hormone receptor activity. • bile acid binding. • protein binding. • ligand-dependent nuclear receptor binding. • ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ... Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor modulators. Estrogen receptor modulators. ...
... that act selectively as agonists or antagonists on the estrogen receptors throughout the body. The most commonly prescribed ... An effect of natural menopause on circulating androgen levels has not been observed.[54] Thus specific tissue effects of ... Selective estrogen receptor modulators[edit]. SERMs are a category of drugs, either synthetically produced or derived from a ... Raloxifene exhibits oestrogen agonist activity on bone and lipids, and antagonist activity on breast and the endometrium.[79] ...
Androgen receptor (Androgen insensitivity syndrome). *general: Hypogonadism (Delayed puberty). *Hypergonadism *Precocious ... and mineralocorticoid antagonists. RAAS inhibition has been proven to be the most effective therapy to slow the progression of ... An important way AGEs exert their effect is through a receptor-mediated mechanism, most importantly by the receptor for ... Angiotensin-converting-enzyme inhibitors (ACEi), as well as angiotensin II receptor blockers (ARBs), are particularly helpful ...
Receptor/signaling modulators. Estrogens and antiestrogens. Androgen receptor modulators. Progesterone receptor modulators. ... CCL18 has been identified as an endogenous antagonist of the GPER.[16] ... mineralocorticoid receptor activity. • steroid binding. • G-protein coupled receptor activity. • steroid hormone receptor ... G protein-coupled estrogen receptor 1 (GPER), also known as G protein-coupled receptor 30 (GPR30), is a protein that in humans ...
Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ...
Receptor/signaling modulators. GABA receptor modulators. GABAA receptor positive modulators. Ionotropic glutamate receptor ... Faure N, Labrie F, Lemay A, Bélanger A, Gourdeau Y, Laroche B, Robert G (March 1982). "Inhibition of serum androgen levels by ... CB1 receptor antagonists. *Glycine receptor agonists. *Ketones. *Neurosteroids. *Pregnane X receptor agonists ... Nuclear receptor activity[edit]. Pregnenolone has been found to act as an agonist of the pregnane X receptor.[13] ...
Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor. J Biol Chem. ... An androgen receptor N-terminal domain antagonist for treating prostate cancer. Jae-Kyung Myung,1 Carmen A. Banuelos,1 Javier ... The androgen receptor co-activator CBP is up-regulated following androgen withdrawal and is highly expressed in advanced ... Androgen receptor regulates a distinct transcription program in androgen-independent prostate cancer. Cell. 2009;138(2):245-256 ...
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... which is an androgen receptor antagonist and an estrogen receptor agonist.. ... which is an androgen receptor antagonist and an estrogen receptor agonist. ... Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, ... Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide ...
Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists.. [ ...
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists ... Androgen receptor / NR3C4 - data and references - Guide to Pharmacology. Miscellaneous. *TESTOSTERONE - Hazardous Substances ... Analogues inhibit AR-mediated reporter gene expression and bind to AR as potently as or better than any known AR antagonists. ... antiandrogenic pharmacophore has been discovered using cell-based cotransfection assays with human androgen receptor (hAR). ...
A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2 ... Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2- ... Androgen Antagonists/chemical synthesis*. *Androgen Antagonists/pharmacology. *Androgen Receptor Antagonists*. *Androgens/ ...
... is androgen-receptor inhibitor. Highly recommended inhibitor in AR research. Find all the information about MDV3100 ( ... Related Androgen Receptor Products. * Darolutamide (ODM-201) New Darolutamide (ODM-201) is a novel androgen receptor (AR) ... which is an androgen receptor antagonist and an estrogen receptor agonist. ... Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, ...
... mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy. ... antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for ... mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy.. ... Accordingly, antagonists to the androgen receptor which do not display cross-reactivity with other intracellular receptors (e.g ...
... but inhibits androgen binding to the androgen receptor, androgen-induced transcriptional activity, and androgen action in ... Persistent DDT metabolite p,p-DDE is a potent androgen receptor antagonist Nature. 1995 Jun 15;375(6532):581-5. doi: 10.1038/ ... they are also consistent with inhibition of androgen receptor-mediated events. Here we report that the major and persistent DDT ... DDE and related environmental chemicals may be mediated at the level of the androgen receptor. ...
Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer.. Youzhi Tong, Chunyun ... Androgen Receptor (AR) antagonists have been used in clinic to treat prostate cancer. One example is bicalutamide (Casodex®), ... Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. [abstract]. In: Proceedings of the ... Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. ...
Bradykinin Receptor Antagonists. Class Summary. Bradykinin receptor antagonists such as icatibant inhibit bradykinin from ... Androgens. Class Summary. Oral androgens have provided the most successful preventive therapy. Synthetic attenuated androgens ( ... Icatibant, a new bradykinin-receptor antagonist, in hereditary angioedema. N Engl J Med. 2010 Aug 5. 363(6):532-41. [Medline]. ... Icatibant is a bradykinin B2 receptor antagonist indicated for acute attacks of HAE. ...
Flutamide (60 mg/kg), GABA-A receptor antagonist bicuculline (5 mg/kg), and GABA-B receptor antagonist CGP 55845 (10 mg/kg) ... We found that the GABA-A competitive receptor antagonist bicuculline rather than the GABA-B competitive receptor antagonist CGP ... and/or with GABA-A receptor antagonist bicuculline (5 mg/kg) or GABA-B receptor antagonist CGP 55845 (10 mg/kg) daily since ... Drug safety is a barrier to the discovery and development of new androgen receptor antagonists. Prostate 71, 480-488 (2011).. ...
Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. Cancer Res 1999; 59: 2511-5. ... Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor. J Biol Chem ... The mechanisms by which androgen receptor (AR) antagonists inhibit AR activity, and how their antagonist activity may be ... antagonist. Introduction. The androgen receptor (AR) plays a central role in prostate cancer development and progression, and ...
... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ...
The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... The ligand-activated human androgen receptor (AR) supports the growth of the prostate gland. Inhibition of human AR by androgen ... This androgen antagonistic activity is receptor specific and does not inhibit the closely related glucocorticoid or ...
The effects of natural ligands of hormone receptors and their antagonists on telomerase activity in the androgen sensitive ... The effects of natural ligands of hormone receptors and their antagonists on telomerase activity in the androgen sensitive ... 50 microM of bicalutamide down-regulated the levels of the androgen receptor, the proliferating cell nuclear antigen and ... antagonists tamoxifen and bicalutamide on telomerase activity and expression of cell cycle related proteins in the androgen- ...
Androgen receptor antagonists: Drugs that bind directly to and block the AR.[66][67] These drugs include the steroidal ... Androgen receptor; Progesterone receptor; Estrogen receptor; GnRH receptor; 5α-Reductase; CYP17A1 (17α-hydroxylase/. 17,20- ... Androgen receptor degraders[edit]. Selective androgen receptor degraders (SARDs) are another new type of antiandrogen that has ... Receptor/signaling modulators. Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. ...
... steroidal androgen receptor antagonists (like the androgens themselves)andnon-steroidal androgen receptor antagon... ... The androgen receptor antagonists are divided between:. *steroidal androgen receptor antagonists (like the androgens themselves ... Non-steroidal androgen receptor antagonists: The non-steroidal androgen receptor antagonists have common structural elements ... Enzalutamide, a 2nd generation androgen receptor antagonist , inhibits the androgen receptor signaling path... ...
... and progestins in higher dosages can block the androgen receptor. The main function of the androgen receptor is as a DNA- ... The androgen receptor is most closely related to the progesterone receptor, ... Androgen regulated genes are critical for the development and maintenance of the male sexual phenotype. Mutations in this gene ... Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, ...
Development of β-amino-carbonyl compounds as androgen receptor antagonists * ...research; Zhi-yun ZHANG, Yan-hui ZHU, and Yun- ... Rights & permissionsfor article Development of β-amino-carbonyl compounds as androgen receptor antagonists . Opens in a new ... Involvement of estrogen receptor-β in farrerol inhibition of rat thoracic aorta vascular smooth muscle cell proliferation * ... Rights & permissionsfor article Involvement of estrogen receptor-β in farrerol inhibition of rat thoracic aorta vascular smooth ...
A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic mice. Oct 15, 2008. ... Pharmacological Actions : Androgen Antagonists, Antiproliferative , Wnt/β-catenin signaling pathway modulation. Additional ... 6 Abstracts with Androgen Antagonists Research. Filter by Study Type. Animal Study. ... A compound within Pygeum bark antagonizes human androgen receptor in the prostate gland. Sep 23, 2009. ...
Fingerprint Dive into the research topics of Combination therapy with a second-generation androgen receptor antagonist and a ... T1 - Combination therapy with a second-generation androgen receptor antagonist and a metastasis vaccine improves survival in a ... Combination therapy with a second-generation androgen receptor antagonist and a metastasis vaccine improves survival in a ... Combination therapy with a second-generation androgen receptor antagonist and a metastasis vaccine improves survival in a ...
Novel Androgen Receptor Antagonists. Modern treatments for prostate cancer also include the use of androgen receptor ... Hormone therapy is best used in combination with other treatments such as radiotherapy, chemotherapy, and androgen receptor- ... Tagged androgen deprivation therapy erectile dysfunction oncology prostate cancer radiation therapy SD ... Radiotherapy (RT) and Androgen Deprivation Therapy (ADT). RT and ADT are the primary treatments used in the management of ...
Androgens. Finasteride. Hormones. Hormones, Hormone Substitutes, and Hormone Antagonists. Physiological Effects of Drugs. 5- ... androgen receptor gene polymorphism Medication response will be assessed according to androgen receptor genotype ... Androgen sensitivity in the cell is determined by the number of Cytosine-Adenine-Guanine repeats in the Androgen Receptor gene ... pharmacogenomics, androgen receptor gene, androgen sensitivity, CAG repeats, androgenetic alopecia. Pharmacogenomics in ...
Hormones, Hormone Substitutes, and Hormone Antagonists. Physiological Effects of Drugs. Androgen Antagonists. Hormone ... Assessing Induction of Double Strand Breaks With Androgen Receptor Partial Agonist in Patients on Androgen Suppression. The ... Randomized Trial Assessing Induction of Double Strand Breaks With Androgen Receptor Partial Agonist in Patients on Androgen ... The patient has decided to undergo brachytherapy plus androgen suppression as treatment modality for his prostate cancer (with ...
Androgen antagonist synonyms, Androgen antagonist pronunciation, Androgen antagonist translation, English dictionary definition ... of Androgen antagonist. n. A substance that inhibits the biological effects of androgenic hormones ... Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist.. Molecular alterations during ... 18) Low androgen levels, such as in those who are androgen deficient or using androgen antagonists, can result in reduced ...
... can mimic natural hormone to interact with receptors in the endocrine system and thus disrupt the functions of the endocrine ... Receptors, Androgen / metabolism* Substances * Androgen Receptor Antagonists * Androgens * Endocrine Disruptors * Receptors, ... EDCs that binding androgen receptor have been reported associated with diabetes mellitus in in vitro, animal, and clinical ... Endocrine Disrupting Chemicals Mediated through Binding Androgen Receptor Are Associated with Diabetes Mellitus Int J Environ ...
androgen receptor antagonist or. to androgen suppresses.. The third section offers an update on the physiological effects of ... androgen receptor antagonist or. to androgen suppresses sexual.Guyton and Hall Textbook of Medical Physiology, 12th edition pdf ... Add-on histamine receptor-3 antagonist (1). Drug-induced sleep endoscopy.Analysis of the link between androgen receptor. ... The selective androgen receptor.. are effective to prevent glucocorticoid-induced decrease in. receptor antagonist is. ...
Testosterone and GnRH Analogues (Agonists and Antagonists). *GnRH/Gonadotropin Vaccines. *Selective Androgen Receptor ... Selective Androgen Receptor Modulators Selective androgen receptor modulators or SARMs mimic the central and peripheral ...
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... In accordance with the involvement of androgens in seborrhoea, antiandrogens, such as cyproterone acetate,[30] spironolactone,[ ... Zouboulis, Christos C.; Degitz, Klaus (2004). "Androgen action on human skin - from basic research to clinical significance". ...
  • The androgen receptor (AR) plays a central role in prostate cancer development and progression, and androgen deprivation therapy by suppression of testicular androgen production (surgical castration or administration of luteinizing hormone-releasing hormone superagonists), or by treatment with AR antagonists (flutamide or bicalutamide), is still the standard systemic treatment. (aacrjournals.org)
  • One mechanism that may contribute to AR reactivation is increased accumulation or synthesis of androgens by prostate cancer cells, and a subset of patients who relapse after castration or luteinizing hormone-releasing hormone agonist treatment will respond to secondary hormonal therapies with AR antagonists such as bicalutamide or to treatments that suppress residual adrenal androgen production such as ketoconozole. (aacrjournals.org)
  • A new nonsteroidal antiandrogenic pharmacophore has been discovered using cell-based cotransfection assays with human androgen receptor (hAR). (nih.gov)
  • A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethylpyrido[3,2-g]quin olines was synthesized. (nih.gov)
  • The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate cancer cell growth. (curehunter.com)
  • The ligand-activated human androgen receptor (AR) supports the growth of the prostate gland. (curehunter.com)
  • A compound within Pygeum bark antagonizes human androgen receptor in the prostate gland. (greenmedinfo.com)
  • Several analogues also showed excellent in vivo activity in classic rodent models of AR antagonism, inhibiting growth of rat ventral prostate and seminal vesicles, without accompanying increases in serum gonadotropin and testosterone levels, as is seen with other AR antagonists. (nih.gov)
  • Antiandrogens , also known as androgen antagonists or testosterone blockers , are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. (wikipedia.org)
  • [1] [2] They can be thought of as the functional opposites of AR agonists , for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm . (wikipedia.org)
  • Androgens like testosterone and particularly DHT are importantly involved in the development and progression of prostate cancer. (wikipedia.org)
  • Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. (raystarbio.cn)
  • Antagonists work by blocking the effect of testosterone, which can have a negative effect on libido and function. (globalrph.com)
  • When the testosterone and androgen levels are too. (tylerweitzman.tk)
  • Selective androgen receptor modulators or SARMs mimic the central and peripheral androgenic and anabolic effects of testosterone and are being trialed for treatment of prostate disease. (medscape.com)
  • LH acts on the Leydig cells to stimulate de novo sythesis of androgens (mainly testosterone). (flashcardmachine.com)
  • Limited efficacy when androgen receptor antagonists are used alone because of a compensatory increase in LH secretion stimulates higher serum concentrations of testosterone. (flashcardmachine.com)
  • I feel that once you consider all of the effects of testosterone on muscle cells you come to realize that when you eventually stop growing (or grow more slowly) it is not because there is a reduction in the number of androgen receptors. (anabolicminds.com)
  • Ka = 5.4 nM) and 1,000-fold selectivity for the AR over other nuclear steroid hormone receptors, including the PR, ER, GR, and MR. It shows 3- and 8-fold higher affinity than testosterone for the rat and human AR, respectively, and up to 100-fold higher affinity for the rat AR than the first-generation NSAAs flutamide, nilutamide, and bicalutamide. (wikipedia.org)
  • It acts by blocking androgen receptors which prevents androgens from binding to them and suppresses luteinizing hormone (which in turn reduces testosterone levels). (drugbank.ca)
  • The androgen receptor (AR), also known as NR3C4 (nuclear receptor subfamily 3, group C, member 4), is a type of nuclear receptor that is activated by binding any of the androgenic hormones, including testosterone and dihydrotestosterone in the cytoplasm and then translocating into the nucleus. (wikipedia.org)
  • In some cell types, testosterone interacts directly with androgen receptors, whereas, in others, testosterone is converted by 5-alpha-reductase to dihydrotestosterone, an even more potent agonist for androgen receptor activation. (wikipedia.org)
  • Testosterone appears to be the primary androgen receptor-activating hormone in the Wolffian duct, whereas dihydrotestosterone is the main androgenic hormone in the urogenital sinus, urogenital tubercle, and hair follicles. (wikipedia.org)
  • They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). (wikipedia.org)
  • The CYP17A enzyme family is involved in the biosynthesis of androgens in the testes and adrenals, culminating in the weak androgens dehydroepiandrosterone (DHEA) and androstenedione, that further undergo metabolism in peripheral tissues (and in prostate cancer cells) to form potent androgens, such as testosterone and its active metabolite dihydotestosterone (DHT). (news-medical.net)
  • One promising drug in this family is abiraterone acetate, which shows good activity against androgens and especially lowers testosterone levels, however, disease progression has not been affected. (news-medical.net)
  • Since the most potent androgen, DHT, is synthesized from testosterone in peripheral tissues by 5α reductase, any therapy that inhibits this enzyme would be potentially useful as an antiandrogen. (news-medical.net)
  • An androgen that is produced from testosterone in the body and is important in the formation of the male reproductive organs and in the development of male secondary sex characteristics. (thefreedictionary.com)
  • The hemizygous mutations in the AR (Xq11.2-q12) encoding AR are associated with X-linked androgen insensitivity, and bi-allelic mutations in SRD5A2 cause enzyme deficiency, converting testosterone (T) to dihydrotestosterone (DHT). (thefreedictionary.com)
  • Natural hormone testosterone (T) and dihydrotestosterone (DHT), known as androgens, are the endogenous ligands of AR. (thefreedictionary.com)
  • Taking only an anti-androgen incurs risk of serious bone density loss, and taking only estrogen does not significantly lower testosterone levels. (trans-health.com)
  • Promising results for cancer immunotherapy in the clinic have led to attempts to combine immunotherapy with standard-of-care therapies, such as androgen deprivation therapy (ADT) for prostate cancer. (sciencemag.org)
  • Surgical and medical androgen deprivation therapy (ADT) is a cornerstone for prostate cancer treatment, but relapse usually occurs. (sciencemag.org)
  • The mechanisms by which androgen receptor (AR) antagonists inhibit AR activity, and how their antagonist activity may be abrogated in prostate cancer that progresses after androgen deprivation therapy, are not clear. (aacrjournals.org)
  • Additional mechanisms that may contribute to AR reactivation after androgen deprivation therapy are increased AR expression, including AR gene amplification that occurs in approximately one third of patients, and AR mutations that can enhance responses to nonandrogen steroids and to antagonists ( 6 - 9 ). (aacrjournals.org)
  • [13] In accordance, therapeutic modalities that reduce androgen signaling in the prostate gland, referred to collectively as androgen deprivation therapy , are able to significantly slow the course of prostate cancer and extend life in men with the disease. (wikipedia.org)
  • [13] Although antiandrogens are effective in slowing the progression of prostate cancer, they are not generally curative, and with time, the disease adapts and androgen deprivation therapy eventually becomes ineffective. (wikipedia.org)
  • The most common methods of androgen deprivation therapy currently employed to treat prostate cancer are castration (with a GnRH modulator or orchiectomy ), nonsteroidal antiandrogens, and the androgen synthesis inhibitor abiraterone acetate . (wikipedia.org)
  • This new drug is the latest breakthrough for the treatment of advanced cases and is the first-in-class intracrine androgen antagonist for patients whose cancer has stopped responding to androgen deprivation therapy (ADT). (thefreedictionary.com)
  • Therefore, androgen deprivation therapy and inhibition of the AR-signaling by AR antagonists are the major forms of PCa hormone therapy. (biomedcentral.com)
  • Is Gleason Grade 5 Prostate Cancer Resistant to Conventional Androgen Deprivation Therapy? (harvard.edu)
  • ORLANDO -- Intermittent androgen deprivation therapy guided by cancer-related biomarkers appears to be just as effective for treatment following prostate cancer therapy as continuous hormonal treatment, researchers said here. (medpagetoday.com)
  • This therapy is known as Androgen Deprivation Therapy or ADT. (fda.gov)
  • His lab developed methods to analyze advanced metastatic PCa through the use of bone marrow biopsies and showed that one mechanism for disease progression after androgen deprivation therapy was through mutations in the androgen receptor (AR). (bidmc.org)
  • In subsequent studies his lab has further established a critical role for AR in PCa that relapses after androgen deprivation therapy, and identified mechanisms that mediate AR reactivation (including enhanced androgen synthesis by tumor cells). (bidmc.org)
  • Androgen deprivation therapy remains the gold standard treatment, but it is not curative, and eventually the disease will return as lethal castration-resistant prostate cancer. (bcgsc.ca)
  • Ishizaki et al (2013) Androgen deprivation promotes intratumoral synthesis of dihydrotestosterone from androgen metabolites in prostate cancer. (tocris.com)
  • A Novel GPCR Target in correlation with Androgen Deprivation Therapy for Prostate Cancer Drug Discovery. (physiciansweekly.com)
  • Few mechanistic studies, however, have examined the vascular effects of androgens in humans, although we have recently demonstrated an association between androgen deprivation and enhanced endothelial function in older men consistent with a deleterious effect of androgens on vascular reactivity. (ahajournals.org)
  • Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist. (selleckchem.com)
  • Elevated AR expression in tumor cells correlates with a change in the functional activity of bicalutamide from antagonist to agonist, suggesting that prostate tumors may adapt to survive on any residual agonism. (aacrjournals.org)
  • Recent studies show that AR antagonists (including the clinically used drug bicalutamide) can enhance AR recruitment of corepressor proteins [nuclear receptor corepressor (NCoR) and silencing mediator of retinoid and thyroid receptors (SMRT)] and that loss of corepressors may enhance agonist activity and be a mechanism of antagonist failure. (aacrjournals.org)
  • We first show that the agonist activities of weak androgens and an AR antagonist (cyproterone acetate) are still dependent on the AR NH 2 /COOH-terminal interaction and are enhanced by steroid receptor coactivator (SRC)-1, whereas the bicalutamide-liganded AR did not undergo a detectable NH 2 /COOH-terminal interaction and was not coactivated by SRC-1. (aacrjournals.org)
  • Taken together, these results indicate that bicalutamide lacks agonist activity and functions as an AR antagonist due to ineffective recruitment of coactivator proteins and that enhanced coactivator recruitment, rather than loss of corepressors, may be a mechanism contributing to bicalutamide resistance. (aacrjournals.org)
  • Increased AR expression can enhance the growth of prostate cancer xenografts in castrated mice and has been reported to enhance the agonist activity of the AR antagonist bicalutamide ( 10 ). (aacrjournals.org)
  • Surprisingly, ABT263 lacks senolytic effect in both AR agonist- and antagonist-pretreated cells. (biomedcentral.com)
  • These data indicate a difference in the agonist- or antagonist-induced cellular senescence and suggest a novel role of MK2206 as a senolytic agent preferentially for AR antagonist-treated cells. (biomedcentral.com)
  • Taken together, our data suggest that both AR agonist and antagonist induce cellular senescence but differentially upregulate a pro-survival signaling which preferentially sensitize androgen-sensitive PCa LNCaP cells to a specific senolytic compound. (biomedcentral.com)
  • It has been shown that when taking a beta agonist such as Clenbuterol, the number of beta-receptors on target cells begins to decrease. (anabolicminds.com)
  • R )-Butaprost is a selective EP 2 prostanoid receptor agonist. (sigmaaldrich.com)
  • Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. (sigmaaldrich.com)
  • Synthetic attenuated androgens (eg, danazol, oxandrolone) taken prophylactically increase the serum concentration of C1 inhibitor (C1INH), presumably by enhancing the function of the C1INH gene ( SERPING1 ). (medscape.com)
  • Currently approved drugs aimed at androgen signaling axis include the AR antagonist bicalutamide and the CYP17 inhibitor abiraterone[ 7 ]. (biomedcentral.com)
  • Recent data report that abiraterone acetate, a specific inhibitor of CYP17 that is key to androgen and estrogen synthesis, improves survival in metastatic castration-resistant prostate cancer (CRPC), confirming the continued dependency of CRPC on the androgen receptor (AR) signaling pathway. (aacrjournals.org)
  • The goal of this clinical study is to determine the safety and efficacy of VT-464, a lyase-selective inhibitor of CYP17, in patients with castration-resistant prostate cancer (CRPC) who have been previously treated with Enzalutamide, Androgen Receptor Positive Triple-Negative Breast Cancer Patients, and Men with ER positive Breast Cancer. (clinicaltrials.gov)
  • Crystal structures of AKR1C3 containing an N-(aryl)amino-benzoate inhibitor and a bifunctional AKR1C3 inhibitor and androgen receptor antagonist. (rcsb.org)
  • We exploited the observation that some flufenamic acid analogs also act as AR antagonists and synthesized a second generation inhibitor, 3-((4-nitronaphthalen-1-yl)amino)benzoic acid (2). (rcsb.org)
  • Aragon's lead product candidate is a second generation androgen receptor signaling inhibitor, ARN-509, in Phase 2 development for castration resistant prostate cancer (CRPC). (bio-medicine.org)
  • The second generation androgen receptor antagonists (enzalutamide and apalutamide) have the highest affinity to the androgen receptor. (altmeyers.org)
  • Modeling Acquired Resistance to the Second-Generation Androgen Receptor Antagonist Enzalutamide in the TRAMP Model of Prostate Cancer. (bvsalud.org)
  • Enzalutamide (MDV3100) is a potent second-generation androgen receptor antagonist approved for the treatment of castration -resistant prostate cancer (CRPC) in chemotherapy -naïve as well as in patients previously exposed to chemotherapy . (bvsalud.org)
  • Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. (sigmaaldrich.com)
  • Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydrop. (nih.gov)
  • [5] These include AR antagonists , androgen synthesis inhibitors , and antigonadotropins . (wikipedia.org)
  • [5] AR antagonists work by directly blocking the effects of androgens, while androgen synthesis inhibitors and antigonadotropins work by lowering androgen levels. (wikipedia.org)
  • Nonsteroidal androgen synthesis inhibitors like ketoconazole can also be described as "NSAAs", although the term is usually reserved to describe AR antagonists. (wikipedia.org)
  • While other compounds also suppress androgen synthesis, such as glucocorticoids, aminoglutethimide and ketoconazole, these are not considered antiandrogens as their mechanism of action does not involve the AR, but rather various routes of synthesis. (news-medical.net)
  • Reduce hepatic cholesterol synthesis, lowering intracellular cholesterol, which stimulates upregulation of LDL receptor and increases the uptake of non-HDL particles from the systemic circulation. (flashcardmachine.com)
  • We report here the design and synthesis of novel androgen antagonists bearing carborane. (semanticscholar.org)
  • Design and synthesis of nonsteroidal progesterone receptor antagonists based on C,C'-diphenylcarborane scaffold as a hydrophobic pharmacophore. (semanticscholar.org)
  • Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. (semanticscholar.org)
  • The effects of the 17beta-estradiol, dihydrotestosterone and hormone antagonists tamoxifen and bicalutamide on telomerase activity and expression of cell cycle related proteins in the androgen-sensitive prostatic cancer cell line LNCaP were studied. (uni-regensburg.de)
  • 17beta-estradiol stimulated cell growth more effectively than dihydrotestosterone whereas hormone antagonists tamoxifen and bicalutamide caused a significant decrease in cell viability. (uni-regensburg.de)
  • It inhibited 5α-dihydrotestosterone stimulated AR reporter gene activity with an IC(50)=4.7 μM and produced a concentration dependent reduction in androgen receptor levels in prostate cancer cells. (rcsb.org)
  • The direct antiandrogenic effect of cyproterone is blockage of the binding of dihydrotestosterone to the specific receptors in the prostatic carcinoma cell. (drugbank.ca)
  • We therefore studied the effects of the nonaromatizable androgen dihydrotestosterone (DHT) on human monocyte adhesion to human endothelial cells and on endothelial cell-surface expression of adhesion molecules. (ahajournals.org)
  • Molecules based on this series of compounds have the potential to provide unique and effective clinical opportunities for treatment of prostate cancer and other androgen-dependent diseases. (nih.gov)
  • Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. (patentgenius.com)
  • Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy. (patentgenius.com)
  • Thus, this study provides a molecular insight for AA as a natural anti-androgenic compound and may serve as a basis for AA derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases . (curehunter.com)
  • Low-level exposure to endocrine-disrupting compounds can induce functional, developmental, behavioral, and transgenerational disturbances, as shown after low-level exposure to the fungicide vin-clozolin, which acts as an androgen antagonist in rats and mice (Anway et al. (thefreedictionary.com)
  • Interaction of organophosphate pesticides and related compounds with the androgen receptor. (thefreedictionary.com)
  • Some compounds are known to interact with multiple hormone receptors simultaneously. (wellnessresources.com)
  • TORONTO--(BUSINESS WIRE)--Aug 25, 2010 - Afferent Pharmaceuticals, a clinical-stage biopharmaceutical company developing first-in-class, small molecule compounds that target P2X3 receptors, today announced preclinical in vivo results demonstrating that an investigational P2X3 receptor antagonist reduced experimentally induced bladder hyperactivity. (drugs.com)
  • Afferent Pharmaceuticals is a clinical-stage biopharmaceutical company developing first-in-class, small molecule compounds that target P2X3 receptors for the treatment of chronic pain and irritative conditions. (drugs.com)
  • The Company currently has compounds in clinical and preclinical studies, in addition to a substantial and diverse library of small molecules that selectively target P2X3 receptors. (drugs.com)
  • Dose dependent effects measured in panel of AR antagonist compounds.The differential effects of various antagonist compounds on AR nuclear translocation, nuclear hyperspeckling, and transcriptional reporter gene activity in HeLa GFP-AR are plotted. (nih.gov)
  • In the course of screening for a new AR antagonist, we isolated novel compounds, antarlides A-E, from the Streptomyces sp. (nii.ac.jp)
  • MDV3100, a more potent AR antagonist (∼5x vs bicalutamide) without residual agonism, has demonstrated excellent efficacy in CRPC patients and has been approved by FDA for treating CRPC in clinic. (aacrjournals.org)
  • However, these responses are usually partial and transient, with AR activity becoming resistant to even high doses of the AR antagonist bicalutamide through unclear mechanisms ( 5 ). (aacrjournals.org)
  • Mutant ARs that are strongly stimulated by the AR antagonist flutamide have been found in approximately one third of patients who relapse after combination therapy with flutamide, and a distinct mutant AR that is strongly stimulated by bicalutamide has been found in long-term bicalutamide-treated patients, but such mutations are uncommon in patients treated with surgical or medical castration monotherapy ( 9 , 11 ). (aacrjournals.org)
  • 50 microM of bicalutamide down-regulated the levels of the androgen receptor, the proliferating cell nuclear antigen and telomerase activity, and up-regulated the expression of p27(Kip1). (uni-regensburg.de)
  • Bicalutamide , a nonsteroidal antiandrogen and the most widely used androgen receptor antagonist in the treatment of prostate cancer . (wikipedia.org)
  • All test systems showed that bicalutamide and hydroxyflutamide act as potent androgen antagonists (Ma et al. (thefreedictionary.com)
  • [13] [15] When castration is combined with a nonsteroidal antiandrogen like bicalutamide , this strategy is referred to as combined androgen blockade (also known as complete or maximal androgen blockade). (wikipedia.org)
  • MDV3100 also binds to the androgen receptor with a greater relative affinity than the clinically used antiandrogen bicalutamide (Casodex), Dr. Sawyers and colleagues said. (medpagetoday.com)
  • Various relevant study results support the importance of the androgen receptor signaling pathway in the treatment of prostate cancer. (altmeyers.org)
  • This stage, often referred to as castration-resistant prostate cancer (CRPC), is associated with an active androgen receptor (AR)-signaling pathway. (biomedcentral.com)
  • The influence of androgen and its receptor signaling pathway on sebaceous glands and sebum secretion is one of the important factors causing acne vulgaris. (biospace.com)
  • It competitively inhibits the binding of androgen in the skin tissue to the androgen receptor and can locally control the activation of the receptor signaling pathway caused by androgen hyperactivity without changing the activity of the androgen receptor signaling pathway in the human body. (biospace.com)
  • Flutamide (molecular formula: C11H11F3N2O3) is an oral, non-steroidal anti-androgen agent (androgen recepto. (altmeyers.org)
  • This is a prospective, single-center, two-phase study to assess the efficacy of single pulsed-dose flutamide in creating double strand breaks (DSBs) in prostate cancer within patients receiving central androgen suppression and brachytherapy. (clinicaltrials.gov)
  • To confirm DNA double strand breaks occur in prostate cancer tissue following pulse-dose flutamide administration in patients who are androgen suppressed, as compared to control patients receiving placebo. (clinicaltrials.gov)
  • It is used along with long-acting gonadotropin antagonists such as leuprolide as an effective and less toxic alternative to flutamide, and has now become the most commonly used, with a single daily dose protocol. (news-medical.net)
  • These mutations occur specifically in patients treated with an AR antagonist, flutamide, and are the result of strong selective pressure exerted by this drug. (bidmc.org)
  • Pharmalogical advances have led to the development of small molecule inhibitors of these receptors. (mskcc.org)
  • Using selective inhibitors we can gain a better understanding of the roles of these receptors. (mskcc.org)
  • The androgen receptor dimer binds to a specific sequence of DNA known as a hormone response element. (wikipedia.org)
  • INSL3 binds to its receptor in the gubernaculum and pulls the testis from the kidney position to the lower part of abdomen ( 5 ). (frontiersin.org)
  • Bisphenol A (BPA) or its analogs can bind both estrogen receptors (ESR1 and ESR2) and estrogen-related receptors (ERR1-3), which blocks LC gene expression, binds to androgen receptor (NR3C4) as an antagonist to block the activation of LC genes. (frontiersin.org)
  • 4-Hydroxytamoxifen (4-HT) is the active metabolite of tamoxifen which binds estrogen receptors (ER) and estrogen-related receptors (ERR) with estrogenic and anti-estrogenic effects. (sigmaaldrich.com)
  • All current androgen receptor-targeting therapies inhibit the growth of prostate cancer by blocking the ligand-binding domain, where androgen binds to activate the receptor. (bcgsc.ca)
  • Ketoconazole binds to and antagonizes Pregnane X Receptor (PXR) activation. (jove.com)
  • Coupled cistrome and transcriptome profiling upon small molecule antagonism led to the identification of a core set of AR direct effector genes that are most likely to mediate the activities of targeted agents: unbiased pathway mapping revealed that AR is a key modulator of steroid metabolism by forming a tightly controlled feedback loop with other nuclear receptor family members and this oncogenic effect can be relieved by antagonist treatment. (biomedcentral.com)
  • Kintor Pharmaceuticals is developing and commercializing a robust pipeline of small molecule and biological drugs for androgen-receptor-related disease areas with unmet medical needs, including COVID-19, prostate, breast and liver cancer, alopecia and acne. (biospace.com)
  • Here we investigated EPI-001, a small-molecule antagonist of AR NTD that inhibits protein-protein interactions necessary for AR transcriptional activity. (bcgsc.ca)
  • and d) select standard reference doses of TP and FLU for future studies with weakly potent agonists, antagonists, and nonandrogenic test substances. (thefreedictionary.com)
  • Interestingly, cellular senescence in prostate cancer (PCa) cells can be induced by either androgen receptor (AR) agonists at supraphysiological androgen level (SAL) used in bipolar androgen therapy or by AR antagonists. (biomedcentral.com)
  • In alternative embodiments, provided are selective agonists having a high affinity for the alpha7 nicotinic acetylcholine receptor (.alpha.7 nAChR), assays for. (patents.com)
  • A small screen of AR-binding ligands, including known agonists, antagonists, and endocrine disruptors, demonstrated that nuclear translocation and nuclear "speckling" were linked with transcriptional output, and specific ligands were noted to differentially affect measurements for wild type versus mutant AR, suggesting differing mechanisms of action. (nih.gov)
  • Understanding how androgen receptor (AR) function is modulated by exposure to steroids, growth factors or small molecules can have important mechanistic implications for AR-related disease therapies (e.g., prostate cancer, androgen insensitivity syndrome, AIS), and in the analysis of environmental endocrine disruptors. (nih.gov)
  • The non-steroidal androgen receptor antagonists have common structural elements with the exception of darolutamide. (altmeyers.org)
  • Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. (selleckchem.com)
  • Amajor metabolite of Enzalutamide (MDV3100) which is an androgen-receptor (AR) antagonist for treatment of prostate cancer. (raystarbio.cn)
  • MDV3100 is a novel antagonist of AR that is also in phase III clinical trials. (aacrjournals.org)
  • Despite encouraging clinical results with next generation drugs (MDV3100 and abiraterone) that inhibit androgen receptor (AR) signaling in patients with castration-resistant prostate cancer (CRPC), responses are variable and short-lived. (biomedsearch.com)
  • However, the AR and AR-regulated genes are still expressed at high levels in androgen-independent prostate cancer, indicating that AR transcriptional activity is reactivated in these tumors and that AR remains as a potential therapeutic target ( 1 - 4 ). (aacrjournals.org)
  • UT-34 is a selective androgen receptor degrader (SARD) ligand.Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer. (raystarbio.cn)
  • Given the critical role of AR in prostate cancer progression and particularly the late stages of the disease, additional therapeutic approaches are under development to target the receptor. (biomedcentral.com)
  • The postchemotherapy study of abiraterone acetate was recently reported and confirmed that targeting of the androgen receptor (AR) is a valid therapeutic strategy in CRPC, imparting overall survival (OS) benefit in advanced prostate cancer. (aacrjournals.org)
  • What are some therapeutic uses of androgens? (flashcardmachine.com)
  • Therapeutic used of anti-androgens? (flashcardmachine.com)
  • Therapeutic uses for androgen receptor antagonists? (flashcardmachine.com)
  • The androgen receptor is a transcription factor and validated therapeutic target for prostate cancer. (bcgsc.ca)
  • This review presents an overview of androgen receptor-related mechanisms of resistance as well as novel therapeutic agents to overcome resistance that is linked to the expression of androgen receptor splice variants in castration-resistant prostate cancer. (bcgsc.ca)
  • Therapeutic antibodies targeting the extracellular domains of these receptors have been successful in the treatment of cancer. (mskcc.org)
  • Based on these and other promising data, Afferent is planning a clinical trial of its lead P2X3 antagonist, AF-219, in patients with chronic bladder pain syndrome, a prevalent and painful condition with currently limited therapeutic options. (drugs.com)
  • Identification of the specific factors and molecular mechanisms that contribute to the tissue-specific actions and aberrant pathological effects of steroid receptors is critical for developing therapeutic agents. (keystonesymposia.org)
  • Some examples, including BCR-Abl, EML4-ALK, and the androgen receptor, contain mutations in the target itself, which hamper binding and inhibitory functions of therapeutic agents. (frontiersin.org)
  • Activity of cabazitaxel in patients with metastatic castration-resistant prostate cancer after treatment with single or dual regimens of novel androgen receptor-targeting agents. (urotoday.com)
  • The purpose of this study was to evaluate the efficacy of cabazitaxel for patients with metastatic castration-resistant prostate cancer (mCRPC) after sequential therapy with docetaxel (DTX) and single or dual regimens of novel androgen receptor-axis-targeted (ARAT) agents. (urotoday.com)
  • Metabolomic profiling to evaluate the efficacy of proxalutamide, a novel androgen receptor antagonist, in prostate cancer cells. (physiciansweekly.com)
  • One misunderstood principle of steroid physiology is the concept of androgen receptors (AR), sometimes called 'steroid receptors', and the effects of steroid use on their regulation. (anabolicminds.com)
  • In addition, steroid receptors regulate non‐transcriptional events. (embopress.org)
  • The steroidal antiandrogens bind not only the AR but also other steroid receptors, such as those for glucocorticoids and progestin, leading to nonspecific effects. (news-medical.net)
  • Steroid receptors are hormone-regulated transcription factors that control a diverse array of physiological processes. (keystonesymposia.org)
  • Recent studies have (1) revealed new mechanisms by which steroid receptors modulate transcription and activate cell signaling pathways, (2) identified molecules with diverse functions that regulate steroid receptor action, and (3) elucidated roles for steroid receptors in both normal physiological processes and disease states, including cancer. (keystonesymposia.org)
  • Steroid receptors regulate gene expression in a ligand-dependent manner by binding specific DNA sequences. (rupress.org)
  • Orphan receptors are a subset of receptors that were cloned prior to the discovery of their endogenous ligands. (keystonesymposia.org)
  • The identification of ligands for orphan receptors and the elucidation of their biological functions have led to the discovery of new hormone signaling pathways that control growth, development, and cell and tissue homeostasis. (keystonesymposia.org)
  • This yeast-based genetic method discovers novel nuclear receptor interactions with ligands that associate with surface binding sites. (jove.com)
  • These gender differences are mediated, at least in part, by effects of androgens. (jimmunol.org)
  • 1 2 Although there is a growing abundance of clinical and basic science data supporting a favorable effect of estrogen and perhaps progesterone on female cardiovascular risk and atherogenic processes, 3 4 5 6 there are comparatively few data on the possible proatherogenic effects of androgens. (ahajournals.org)
  • Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. (aacrjournals.org)
  • Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. (aacrjournals.org)
  • Oral androgens have provided the most successful preventive therapy. (medscape.com)
  • Inhibition of human AR by androgen ablation therapy and by applying synthetic anti- androgens is therefore the primary goal in treatment of patients. (curehunter.com)
  • Hormone therapy is best used in combination with other treatments such as radiotherapy, chemotherapy, and androgen receptor-targeted agents. (globalrph.com)
  • Given that polymorphisms of the androgen receptor gene which confer androgen sensitivity impact male response to finasteride therapy, it was hypothesized that the same polymorphism in women may identify the group that will respond. (clinicaltrials.gov)
  • Other forms of therapy include androgen antagonist drugs such as ketoconazole, finasteride and insulin-sensitizing drugs such as metformin. (thefreedictionary.com)
  • By selectively occupying the strongest binding sites, AR signaling remains active even when androgen levels are low, as is characteristic of first-line androgen ablation therapy. (biomedcentral.com)
  • While androgen ablation therapy is a standard first-line treatment, the vast majority of prostate tumors eventually become hormone refractory and continue to proliferate even with very low levels of androgen. (biomedcentral.com)
  • Not as effective for MTF hormone therapy, because it can potentially stimulate androgen production. (trans-health.com)
  • Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist, displays a strong local antiandrogenic activity in hamster's flank organ test, does not exhibit antiandrogenic activity after subcutaneous injection in vivo. (raystarbio.cn)
  • Antiandrogens are one of three types of sex hormone antagonists , the others being antiestrogens and antiprogestogens . (wikipedia.org)
  • Antiandrogens are used to treat an assortment of androgen-dependent conditions . (wikipedia.org)
  • [4] In women, antiandrogens are used to treat acne , seborrhea , excessive hair growth , scalp hair loss, and high androgen levels , such as those that occur in polycystic ovary syndrome (PCOS). (wikipedia.org)
  • In women, antiandrogens are much better tolerated , and antiandrogens that work only by directly blocking androgens are associated with minimal side effects. (wikipedia.org)
  • However, because estrogens are made from androgens in the body, antiandrogens that suppress androgen production can cause low estrogen levels and associated symptoms like hot flashes, menstrual irregularities , and osteoporosis in premenopausal women. (wikipedia.org)
  • Antiandrogens are used in the treatment of an assortment of androgen-dependent conditions in both males and females. (wikipedia.org)
  • The representatives of the family of non-steroidal antiandrogens are potent antagonists at the androgen receptor. (altmeyers.org)
  • Antiandrogens are used in the treatment of an assortment of androgen-dependent conditions in both men and women. (wikipedia.org)
  • For these reasons, they have improved efficacy and selectivity as antiandrogens and do not lower androgen levels, instead acting solely by directly blocking the actions of androgens at the level of their biological target, the AR. (wikipedia.org)
  • Antiandrogens are a group of medications which bind to intracellular androgen receptors (AR) to prevent androgen effects on organs such as the testes, the hair follicles, the hypothalamus, pituitary, ovaries and the prostate gland, which are targets of endogenous androgens. (news-medical.net)
  • Antiandrogens are molecules that compete with androgens to bind in the ligand binding site of the AR. (news-medical.net)
  • Topics presented in this meeting will include structure function relationships, the role of orphan receptors in development and metabolism, genome-wide analysis of receptor function, coactivators and corepressors, and drug discovery. (keystonesymposia.org)
  • Oral curcumin intake could inhibit androgen receptor expression and probably PSA activity. (greenmedinfo.com)
  • Upon binding the hormone ligand, the receptor dissociates from accessory proteins, translocates into the nucleus, dimerizes, and then stimulates transcription of androgen responsive genes. (raystarbio.cn)
  • AR, a member of the nuclear receptor (NR) superfamily, functions mainly as a ligand-dependent transcription factor. (biomedcentral.com)
  • Persuasive evidence supports the concept that constitutively active androgen receptor splice variants lacking the ligand-binding domain are one of the resistant mechanisms underlying advanced disease. (bcgsc.ca)
  • Hormone therapies for advanced prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD), but these ultimately fail and the disease progresses to lethal castration-resistant prostate cancer (CRPC). (bcgsc.ca)
  • Androgen receptor functional analyses by high throughput imaging: determination of ligand, cell cycle, and mutation-specific effects. (nih.gov)
  • The androgen receptor (AR) is a ligand-dependent transcription factor of the steroid receptor (SR) subfamily of nuclear receptors. (rupress.org)
  • Purpose: Enzalutamide, a second-generation androgen antagonist, was approved by the U.S. Food and Drug Administration (FDA) for castration-resistant prostate cancer (CRPC) treatment. (elsevier.com)
  • Androgen receptor targeted therapies in castration-resistant prostate cancer: Bench to clinic. (bcgsc.ca)
  • Castration-resistant prostate cancer is an untreatable form of prostate cancer, which bypassed the normal dependence on androgens for growth and survival. (aacrjournals.org)
  • A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic mice. (greenmedinfo.com)
  • The compound, being developed by Medivation, of San Francisco, blocks the androgen receptor and also inhibits androgen receptor function by preventing nuclear translocation of the receptor and DNA binding. (medpagetoday.com)
  • 1991. Effects of polychlorinated biphenyls with Ah receptor affinity on lymphoid development in the thymus and the bursa of Fabricius on chick embryos in ovo and in mouse thymus anlagen in vitro . (cdc.gov)
  • Here we report that the major and persistent DDT metabolite, p,p'-DDE (1,1-dichloro-2,2-bis(p-chlorophenyl)ethylene), has little ability to bind the oestrogen receptor, but inhibits androgen binding to the androgen receptor, androgen-induced transcriptional activity, and androgen action in developing, pubertal and adult male rats. (nih.gov)
  • Transcriptional activity of the androgen receptor requires a functional AF-1 region in its N-terminal domain. (bcgsc.ca)
  • In addition, antarlide B inhibited the transcriptional activity of not only wild type AR but also mutant ARs, which are seen in patients with acquired resistance to clinically used AR antagonists.We next observed that xanthohumol (XN), a prenylated chalcone, modulates autophagy. (nii.ac.jp)
  • This androgen antagonistic activity is receptor specific and does not inhibit the closely related glucocorticoid or progesterone receptors . (curehunter.com)
  • The androgen receptor is most closely related to the progesterone receptor, and progestins in higher dosages can block the androgen receptor. (raystarbio.cn)
  • Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR variants in prostate cancer, little or no inhibition or induction of cytochrome P450 enzymes, and little or no central nervous system distribution. (wikipedia.org)
  • Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system distribution, and no induction of seizures in animals. (wikipedia.org)
  • Importantly, AA is able to efficiently repress the growth of both the androgen-dependent LNCaP and also the androgen-independent C4-2 Pca cells but not that of PC3 or CV1 cells lacking AR. (curehunter.com)
  • Here, we first induced cellular senescence by treating androgen-sensitive PCa LNCaP cells with either SAL or the AR antagonist Enzalutamide (ENZ). (biomedcentral.com)
  • Treatment of human prostate carcinoma‐derived LNCaP cells with androgen or oestradiol triggers simultaneous association of androgen receptor and oestradiol receptor β with Src, activates the Src/Raf‐1/Erk‐2 pathway and stimulates cell proliferation. (embopress.org)
  • Androgen antagonists prevent the growth of prostate cancer cells and induce a G1 cell cycle arrest. (mskcc.org)
  • The androgen receptor plays a critical role throughout the progression of prostate cancer and is an important drug target for this disease. (biomedcentral.com)
  • We aim to evaluate a tumor-suppressive function of FLII in regulating androgen receptor (AR) in prostate cancer progression. (aacrjournals.org)
  • Spearmint herbal tea has significant anti-androgen effects in polycystic ovarian syndrome. (greenmedinfo.com)
  • BPA has estrogen and anti-androgen effects, thereby destroying the development and function of Leydig cells and causing related reproductive diseases such as testicular dysgenesis syndrome, delayed puberty, and subfertility/infertility. (frontiersin.org)
  • As has been also found for other steroid hormone receptors such as estrogen receptors, androgen receptors can have actions that are independent of their interactions with DNA. (wikipedia.org)
  • The nuclear hormone receptors are a superfamily of transcription factors that play important roles in both physiology and disease. (keystonesymposia.org)
  • It acts as a selective antagonist of the androgen receptor. (news-medical.net)
  • The study, co-authored by Anthony Ford, Ph.D., Founder and Chief Scientific Officer of Afferent Pharmaceuticals, was highlighted in a poster presentation titled, "Selective Blockade of Spinal P2X3 and P2X2/3 Receptors with a Novel and Selective Antagonist, AF-742, Reveals Central Endogenous Purinergic Regulation of Bladder Activity. (drugs.com)
  • Peppermint tea has an anti-androgen effect in rats. (greenmedinfo.com)
  • Androgen Optimization Simple.A receptor antagonist is a. in skeletal muscle encoded by a. rats and which increases muscle mass. (tylerweitzman.tk)
  • We herein show that orchiectomy synergizes with immunotherapy, whereas the more widely used treatment of medical ADT involving androgen receptor (AR) antagonists suppresses immunotherapy. (sciencemag.org)
  • to androgen suppresses sexual.Guyton and Hall Textbook of Medical Physiology, 12th edition pdf and chm free download.Transcriptional profiling identifies gene expression changes induced in HCV-subgenomic. (tylerweitzman.tk)
  • Whereas the role of androgens has not been addressed in detail, estrogens appear to equivocally influence lung injury outcomes depending on the model ( 3 , 4 , 5 , 6 ). (jimmunol.org)
  • Whereas estrogens were recently shown to at least partially regulate the acute inflammatory response to LPS in mice ( 10 ), the potential role of androgens has not been examined. (jimmunol.org)
  • Castration, therefore, does not suppress adrenal androgens and achieves a "hormone-reduced" rather than a "hormone-free" state, hence, the recent renaming of this stage of the disease as castration-resistant in preference to hormone-refractory. (aacrjournals.org)
  • The mainstay of first-line treatment for patients with metastatic prostate cancer is suppression of gonadal androgens by medical or surgical castration, a strategy that was described 7 decades ago by Charles Huggins and colleagues ( 1 ). (aacrjournals.org)
  • What is used with androgen receptor antagonists to treat metastatic prostate cancers? (flashcardmachine.com)
  • Seragon will be focused primarily on Aragon's Selective Estrogen Receptor Degrader or SERD platform, including ARN-810, its lead SERD currently being evaluated in a Phase I trial for estrogen receptors + metastatic breast cancer. (rttnews.com)
  • These are used along with chemical or surgical castration to remove all chances of exposure of prostate cancer cells to androgens from the adrenal gland, rather than removing the adrenal gland which could result in fatal or debilitating outcomes, such as hypoadrenalism. (news-medical.net)
  • Glucocorticoids such as prednisone, exert a negative feedback mechanism on central stimulation of steroid production, thus preventing adrenal androgen production. (news-medical.net)
  • be useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism. (raystarbio.cn)
  • Anti-androgen can be used in the treatment of benign prostatic hyperplasia, acne, hirsutism, and androgenic alopecia. (springer.com)
  • RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was never marketed. (wikipedia.org)
  • Pyrilutamide, a topical AR antagonist with a specific target, can inhibit the combination of androgen receptor and androgen in hair follicle sebaceous glands, thereby treating acne vulgaris. (biospace.com)
  • This belief has persisted despite the fact that there is no scientific evidence to date that shows that increased levels of androgens down regulates the androgen receptor in muscle tissue. (anabolicminds.com)
  • This increased activity is independent of androgens and explains the poor correlation between systemic levels of androgens and the severity of acne lesions. (thefreedictionary.com)
  • ht1a receptor: 2.83125914921958: 14: virulent e:. also induced: 2.08550653694701: 8: the ceria.Another common term used to refer to this treatment is androgen. (tylerweitzman.tk)
  • Expanding on previous observations, we first show that prostate-specific membrane antigen (PSMA) is repressed by androgen treatment in multiple models of AR-positive prostate cancer in an AR-dependent manner. (biomedsearch.com)
  • Which medications in the drug class Angiotensin II receptor antagonists are used in the treatment of IgA Nephropathy? (medscape.com)
  • Adverse effects of synthetic androgen treatment? (flashcardmachine.com)
  • Adverse effects of synthetic androgen treatment in women and children? (flashcardmachine.com)
  • Inhibition of androgen biosynthesis and/or AR antagonism should be efficacious in the treatment of CRPC. (rcsb.org)
  • Bryant HU, et al, An estrogen receptor basis for. (tylerweitzman.tk)
  • Activation of the Estrogen Receptor by estra-2-diol results in sustained binding and the previously described cyclical response kinetics are likely an artefact of observing a highly variable process without replicates. (elifesciences.org)
  • It is a cell permeable, selective estrogen receptor modulator (SERM). (sigmaaldrich.com)