Androgen Receptor Antagonists
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.
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.
Interleukin 1 Receptor Antagonist Protein
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.
Neurokinin-1 Receptor Antagonists
Dose-Response Relationship, Drug
Purinergic P1 Receptor Antagonists
Histamine H2 Antagonists
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.
Serotonin 5-HT3 Receptor Antagonists
Excitatory Amino Acid Antagonists
Angiotensin Receptor Antagonists
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.
Serotonin 5-HT2 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Adenosine A1 Receptor Antagonists
Purinergic P2 Receptor Antagonists
Histamine H1 Antagonists
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.
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.
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.
GABA-A Receptor Antagonists
Nuclear Receptor Coactivators
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.
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)
Nuclear Receptor Coactivator 2
Receptor, Endothelin A
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.
Serotonin 5-HT1 Receptor Antagonists
Gene Expression Regulation, Neoplastic
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.
Muscular Disorders, Atrophic
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.
Reverse Transcriptase Polymerase Chain Reaction
Adrenergic alpha-1 Receptor Antagonists
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).)
Prostatic Neoplasms, Castration-Resistant
Tumor Cells, Cultured
Serotonin Receptor Agonists
Histamine H3 Antagonists
Bulbo-Spinal Atrophy, X-Linked
Adrenergic alpha-2 Receptor Antagonists
Disease Models, Animal
Molecular Sequence Data
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.
Cholestenone 5 alpha-Reductase
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.
Estrogen Receptor beta
GABA-B Receptor Antagonists
5-alpha Reductase Inhibitors
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.
Receptor, Endothelin B
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)
Adenosine A3 Receptor Antagonists
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.
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.
Gene Expression Regulation
Purinergic P2X Receptor Antagonists
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.
Estrogen Receptor alpha
Serotonin 5-HT4 Receptor Antagonists
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)
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.
Receptor, Cannabinoid, CB1
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.
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.
Receptors, Dopamine D2
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.
Cannabinoid Receptor Antagonists
Analysis of Variance
Promoter Regions, Genetic
Mineralocorticoid Receptor Antagonists
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.
Gonadal Steroid Hormones
Adrenergic beta-2 Receptor Antagonists
An octapeptide that is a potent but labile vasoconstrictor. It is produced from angiotensin I after the removal of two amino acids at the C-terminal by ANGIOTENSIN CONVERTING ENZYME. The amino acid in position 5 varies in different species. To block VASOCONSTRICTION and HYPERTENSION effect of angiotensin II, patients are often treated with ACE INHIBITORS or with ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS.
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)
Effect of androgen suppression compared with androgen receptor blockade on arterial stiffness in men with prostate cancer :...
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 ...
Androgen receptor blockade | OncologyPRO
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Addressing the conundrum of male predominance in mantle cell lymphoma using androgen receptor blockade
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Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. |...
Sigma-Aldrich offers abstracts and full-text articles by [Isao Kinoyama, Nobuaki Taniguchi, Toru Yoden, Hiroshi Koutoku, Takashi Furutani, Masafumi Kudoh, Minoru Okada].
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Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists...
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Androgen Receptor Antagonists
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... 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 ... "Espacenet - Original document". Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate ... Kawahara, Takashi; Miyamoto, Hiroshi (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical ...
... - 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 ...
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 ...
"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 ...
... for the rat ventral prostate androgen receptor (AR), which is similar to that of spironolactone and its active metabolite 7α- ... A potent mineralocorticoid antagonist with reduced affinity for the 5 alpha-dihydrotestosterone receptor of human and rat ...
... is a strong dopamine receptor antagonist (D2 (Ki 0.027 nM) and D4 (Ki 0.066 nM)) with weaker serotonin receptor ... as an alternative to anti-androgen drugs such as cyproterone acetate. Benperidol was discovered by Janssen Pharmaceutica in ... "Endocrine changes in male sexual deviants after treatment with anti-androgens, oestrogens or tranquillizers". The Journal of ...
Mifepristone is a powerful glucocorticoid type II receptor antagonist and, since it does not interfere with normal cortisol ... oligomenorrhea and infertility in women due to elevations in androgens. Studies have also shown that the resultant amenorrhea ... This atrophy is associated with areas of high glucocorticoid receptor concentrations such as the hippocampus and correlates ... can act on the melanocortin 1 receptor. A variant of Cushing's disease can be caused by ectopic, i.e. extra pituitary, ACTH ...
... a nuclear protein that interacts with and regulates transcriptional activity of androgen receptor and glucocorticoid receptor ... Dexamethasone and other corticosteroids are agonists, while mifepristone and ketoconazole are antagonists of the GR. ... The glucocorticoid receptor (GR, or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor ... The unbound receptor resides in the cytosol of the cell. After the receptor is bound to glucocorticoid, the receptor- ...
"DU-145 and PC-3 human prostate cancer cell lines express androgen receptor: implications for the androgen receptor functions ... "5-lipoxygenase antagonist therapy: a new approach towards targeted cancer chemotherapy". Acta Biochimica et Biophysica Sinica. ... Some androgen-independent LNCaP sublines have been developed from the ATCC androgen-dependent LNCaP cells after androgen ... "Role of androgen receptor in the progression of human prostate tumor cells to androgen independence and insensitivity". The ...
Index of biochemistry articles
... receptor (biochemistry) - receptor antagonist - receptor protein-tyrosine kinase - recombinant fusion protein - recombinant ... androgen receptor - angiotensin - angiotensin II - angiotensin receptor - ankyrin - annexin II - antibiotic - antibody - ... interleukin receptor - interleukin-1 receptor - interleukin-2 receptor - interleukin-3 - interleukin-3 receptor - intermediate ... G protein-coupled receptor - G3P - GABA - GABA receptor - GABA-A receptor - gag-onc fusion protein - galanin - gamete - gamma- ...
... such as the androgen receptor, estrogen receptors, glucocorticoid receptor, and progesterone receptor. It has been noted that ... Binding of antagonist ligands to nuclear receptors in contrast induces a conformation of the receptor that preferentially binds ... for example the retinoic acid receptor, retinoid X receptor and thyroid hormone receptor. Type III nuclear receptors ( ... Orphan receptors are found amongst all six subfamilies of nuclear receptors, while ligand-dependent receptors are found amongst ...
Effects of hormones on sexual motivation
Androgen receptor antagonists such as flutamide and bicalutamide cause little to no decrease in sexual desire in women. Low ... High-dosage monotherapy with an androgen receptor antagonist such as bicalutamide or enzalutamide, which preserves testosterone ... 2010). "Nonsteroidal selective androgen receptor modulators enhance female sexual motivation". The Journal of Pharmacology and ... and marked androgen receptor antagonism with high-dosage cyproterone acetate monotherapy causes profound sexual dysfunction in ...
Drugs and sexual desire
It compiles a serotonin 1A receptor agonist and a serotonin 2A receptor antagonist. and is an antidepressant that was ... In addition to this mechanism, it also competes for the androgen receptors against testosterone and dihydrotestosterone, ... Steroidal anti-androgens are a class of steroid drugs that inhibit the actions of androgens. Cyproterone acetate, a 17- ... The melanocortin receptor agonist proposes to activate multiple receptor subtypes nonselectively, with the highest affinity ...
The drug is a high-affinity antagonist of the androgen receptor (AR) with a Ki value of 26 nM and has been found to inhibit ... Gao W, Kim J, Dalton JT (2006). "Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands". Pharm. Res. ... Nyrönen TH, Söderholm AA (2010). "Structural basis for computational screening of non-steroidal androgen receptor ligands". ... "Selective androgen receptor modulators". Expert Opinion on Therapeutic Patents. 13 (1): 59-66. doi:10.1517/13543718.104.22.168. ...
Estrogen receptor beta
October 2000). "Steroid-induced androgen receptor-oestradiol receptor beta-Src complex triggers prostate cancer cell ... "Differential response of estrogen receptor alpha and estrogen receptor beta to partial estrogen agonists/antagonists". ... nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor-a nuclear receptor which is ... ERβ is a member of the family of estrogen receptors and the superfamily of nuclear receptor transcription factors. The gene ...
... a fourth generation GnRH antagonist, induces apoptosis in hormone refractory androgen receptor negative prostate cancer cells ... Gonadotropin-releasing hormone receptor § Antagonists "Ozarelix - AdisInsight". Festuccia C, Dondi D, Piccolella M, Locatelli A ... Ozarelix (developmental code names D-63153, SPI-153) is a peptide gonadotropin-releasing hormone antagonist (GnRH antagonist) ... GnRH antagonists, Hormonal antineoplastic drugs, Peptides, All stub articles, Genito-urinary system drug stubs, Systemic ...
1990) suggests that when a vasopressin receptor antagonist is injected into the anterior hypothalamus of the resident male, the ... Androgens in particular have well documented effects on enhancing aggression in male rodents, and testosterone injections into ... This antagonist has been known to decrease the tendency of offensive aggression via injections into the ventrolateral ... It is hypothesized[by whom?] that serotonin acts as an antagonist to vasopressin by eliciting its effects on vasopressin- ...
Diindolylmethane is a strong androgen antagonist in human prostate cancer cells". The Journal of Biological Chemistry. 278 (23 ... a bitter-taste receptor gene". American Journal of Human Genetics. 74 (4): 637-46. doi:10.1086/383092. PMC 1181941. PMID ...
Hydrocodone is a full agonist of the opioid receptors with a higher affinity for the mu-opioid receptor. Upon binding, ... Mixed agonist/antagonist and partial agonist opioids may reduce the analgesic effect of benzhydrocodone/APAP or cause ... Chronic hydrocodone use can lead to androgen deficiency, which may result in low libido, impotence, erectile dysfunction, ... Mu-opioid receptor agonists, Catechol ethers, Semisynthetic opioids, Benzoate esters). ...
In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors ... A Potent Mineralocorticoid Antagonist with Reduced Affinity for the 5α-Dihydrotestosterone Receptor of Human and Rat Prostate ... Cutler GB, Sauer MA, Loriaux DL (1979). "SC 25152: a potent mineralocorticoid antagonist with decreased antiandrogenic activity ... Hofmann LM, Weier RM, Suleymanov OD, Pedrera HA (1977). "Mexrenoate potassium: a steroidal aldosterone antagonist and ...
Gonadotropin-releasing hormone agonist
v t e Hormone levels with GnRH agonists and antagonists Testosterone levels during the first month of androgen deprivation ... is achieved through receptor downregulation by internalization of receptors. Generally this induced and reversible hypogonadism ... Agonists do not quickly dissociate from the GnRH receptor. As a result, initially there is an increase in FSH and LH secretion ... They are agonists of the GnRH receptor and work by increasing or decreasing the release of gonadotropins and the production of ...
The H2-receptor antagonist cimetidine causes an increase in the plasma concentration of metformin by reducing clearance of ... androgen excess, and oligomenorrhea in adolescence". The Journal of Clinical Endocrinology and Metabolism. 96 (8): E1262-7. doi ... but differ by the site of binding to the intended receptor and the drugs' affinities to the receptor. As a result, they have a ... In short GnRH-antagonist protocols metformin may reduce live birth rates with uncertainty on its effect on clinical pregnancy ...
Pharmacology of bicalutamide
... bicalutamide acts as a selective antagonist of the androgen receptor (AR), the biological target of androgens like testosterone ... "Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor". The Journal of ... Bicalutamide acts as a highly selective competitive silent antagonist of the androgen receptor (AR) (IC50 = 159-243 nM), the ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ...
It is a steroidal antimineralocorticoid of the spirolactone group and a selective aldosterone receptor antagonist (SARA). ... Eplerenone is more selective than spironolactone at the mineralocorticoid receptor relative to binding at androgen, progestogen ... Eplerenone is an antimineralocorticoid, or an antagonist of the mineralocorticoid receptor (MR). Eplerenone is also known ... LoSalt Advisory Statement (PDF) Delyani JA (April 2000). "Mineralocorticoid receptor antagonists: the evolution of utility and ...
... is an estrogen, specifically an agonist of the estrogen receptors ERα and ERβ. It is a far less potent estrogen than is ... Lundström E, Conner P, Naessén S, Löfgren L, Carlström K, Söderqvist G (2015). "Estrone - a partial estradiol antagonist in the ... though they can also be formed from adrenal androgens in adipose tissue. Relative to estradiol, both estrone and estriol have ... In contrast to estradiol and estriol, estrone is not a ligand of the G protein-coupled estrogen receptor (affinity >10,000 nM ...
Some steroid antagonists: Androgen: cyproterone acetate Progestins: mifepristone, gestrinone Steroid hormones are transported ... Then the steroid binds to a specific steroid hormone receptor, also known as a nuclear receptor, which is a large ... Upon steroid binding, many kinds of steroid receptors dimerize: two receptor subunits join together to form one functional DNA- ... They can pass through the cell membrane as they are fat-soluble, and then bind to steroid hormone receptors (which may be ...
Valproic acid has been found to be an antagonist of the androgen and progesterone receptors, and hence as a nonsteroidal ... Valproic acid has been found to directly stimulate androgen biosynthesis in the gonads via inhibition of histone deacetylases ... Death AK, McGrath KC, Handelsman DJ (December 2005). "Valproate is an anti-androgen and anti-progestin". Steroids. 70 (14): 946 ...
What is more clear is that DDE is a weak androgen receptor antagonist and can produce male genital tract abnormalities. ...
... estrogen receptor antagonists such as fulvestrant, aromatase inhibitors such as anastrozole and exemestane, gonadotropin- ... Androgen-dependent condition Estrogen insensitivity syndrome "Estrogen: Hormone, Function, Levels & Imbalances". Cleveland ... Such conditions may be treated with drugs with antiestrogen actions, including selective estrogen receptor modulators(SERMs) ...
In addition, it has also been found to act as a competitive antagonist of the androgen receptor (AR), with potency reportedly ... "Redirecting abiraterone metabolism to fine-tune prostate cancer anti-androgen therapy" (PDF). Nature. 533 (7604): 547-51. ...
Other nuclear receptor targets of DHEA besides the androgen and estrogen receptors include the PPARα, PXR, and CAR. However, ... it can actually behave more like an antagonist depending on circulating testosterone and dihydrotestosterone (DHT) levels, and ... Women with complete androgen insensitivity syndrome (CAIS), who have a non-functional androgen receptor (AR) and are immune to ... weak partial agonist of the androgen receptor (AR). However, its intrinsic activity at the receptor is quite weak, and on ...
... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ...
Acne Vulgaris Medication: Topical Products, Retinoid-like Agents, Antibiotics, Estrogens/Progestins, Aldosterone Antagonists,...
... which suppress ovarian androgen production as well as androgen receptor blockers that block the effect of androgens ... Topical Androgen Receptor Inhibitors. Class Summary. These agents compete with androgens, specifically dihydrotestosterone, for ... Aldosterone antagonists may reduce free testosterone levels and compete with androgens binding at the sebaceous gland. ... Clascoterone cream targets androgen receptors in the skin to reduce cutaneous 5-alpha dihydrotestosterone. Favorable results, ...
Gender Dysphoria Medication: Progestins, Gonadotropin-Releasing Hormone Agonists, Aldosterone Antagonists, Selective,...
Androgen receptor repeat length polymorphism associated with male-to-female transsexualism. Biol Psychiatry. 2009 Jan 1. 65(1): ... Androgens. Class Summary. Androgens are used for replacement therapy in hypogonadism associated with a deficiency or absence of ... Spironolactone is an aldosterone antagonist that competes with testosterone and dihydrotestosterone receptor sites. It also ... Flutamide is a nonsteroidal antiandrogen that inhibits androgen uptake or binding of androgen to target tissues. ...
Androgen Antagonists | GreenMedInfo | Pharmacological Action
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. ...
Functional analysis of androgen receptor mutations that confer anti-androgen resistance identified in circulating cell-free DNA...
All current non-steroidal AR antagonists, such as hydroxyflutamide, bicalutamide, and enzalutamide, target the androgen binding ... site of the receptor, competing with endogenous androgenic steroids. Several AR mutations in this binding site have been ... The androgen receptor (AR) is a pivotal drug target for the treatment of prostate cancer, including its lethal castration- ... Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. Cancer Res. 1999;59:2511-5. ...
Synthesis and preliminary investigations into novel 1,2,3-triazole-derived androgen receptor antagonists inspired by...
A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, six 1 ... N2 - A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, ... AB - A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this methodology, ... abstract = "A versatile and high yielding synthesis of novel androgen receptor (AR) antagonists is presented. Using this ...
Bicalutamide (Casodex®) in the treatment of prostate cancer | Semantic Scholar
Development of a Benzopyran‐Containing Androgen Receptor Antagonist to Treat Antiandrogen‐Resistant Prostate Cancer. *Sangmi Oh ... MDM2 antagonists boost antitumor effect of androgen withdrawal: implications for therapy of prostate cancer. *C. Tovar, B. ... Since majority of prostate tumors express wild-type p53, its activation by MDM2 antagonists in combination with androgen ... competitive androgen receptor blockers in male precocious peripheral puberty, firstly employed in male MAS, and contributes to ...
Biblio | Page 7 | Linus Pauling Institute | Oregon State University
Prostate Cancer - Results from #140
a) Prior treatment with androgen receptor antagonists; (b) Treatment with gonadotropin-releasing hormone analog (GnRHa) prior ... Cognitive Effects of Androgen Receptor (AR) Directed Therapies for Advanced Prostate Cancer. Condition: Castration-Resistant ... Ongoing androgen deprivation therapy (ADT) with luteinizing hormone-releasing hormone (LHRH) agonist or antagonist or bilateral ... Phase IIIb Randomized Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH ...
Androgen Receptor Inhibitor. LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. ... Androgen Receptor Inhibitor. LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. ... Androgen Receptor Inhibitor. LHRH antagonist. No 2003. 2005. Jan. 1, 2005 No Longer Used. ... Androgen Receptor Inhibitor. CYP17 Inhibitor. Yes 2011. In Use. NA. Acalabrutinib Calquence. 100 mg. Chemotherapy Tyrosine ...
News for Medical Independent Sales Representatives and Medical Distributors: Bayer and Orion Expand Clinical Development...
Phase III study to be initiated in metastatic hormone-sensitive prostate cancer assessing the androgen-receptor antagonist in ... BAY-1841788 (ODM-201) is an investigational oral androgen receptor (AR) antagonist. In preclinical studies, BAY-1841788 and its ... oration today announced the expansion of the global clinical development program for the investigational androgen receptor (AR ... The Phase III study ARASENS will evaluate the compound in combination with standard androgen deprivation therapy (ADT) and the ...
Gonadal Hormones: Androgens Flashcards by Nicole Pritchard | Brainscape
Androgens flashcards from Nicole Pritchard's St. Georges University class online, or in Brainscape's iPhone or Android ... Androgens (Testosterone). Antiandrogens. --receptor antagonists: flutamide. ---5 alpha reductase inhibitor: Finasteride --- ... Its an androgen derivative, a partial agonist of progestin and glucocorticoid receptors Used in endometriosis and fibrocystic ... Gonadal Hormones: Androgens Flashcards Preview Pharm: Final Exam Drugs , Gonadal Hormones: Androgens , Flashcards ...
Histone methyltransferase DOT1L coordinates AR and MYC stability in prostate cancer | Nature Communications
... the authors report that DOTL1 inhibition suppresses both androgen receptor and MYC pathways in a negative feed forward manner ... Genetic and chemical inhibition of DOT1L selectively impaired the viability of androgen receptor (AR)-positive PCa cells and ... Shen, H. C. & Balk, S. P. Development of androgen receptor antagonists with promising activity in castration-resistant prostate ... Increased androgen receptor activity and altered c-myc expression in prostate cancer cells after long-term androgen deprivation ...
Frontiers | Endocrine Therapy for the Functional Recovery of Spinal Cord Injury
... the neuroprotective and neurotherapeutic effects of testosterone are significantly inhibited by androgen receptor antagonists. ... 2016). Unexpected central role of the androgen receptor in the spontaneous regeneration of myelin. Proc. Natl. Acad. Sci. U S A ... 2013). The neural androgen receptor: a therapeutic target for myelin repair in chronic demyelination. Brain 136(Pt 1), 132-146 ... The neuroprotective effect of testosterone on nerve diseases has mainly been confirmed by the activation of androgen receptors ...
Drug CategoriesBrowse DrugBank Categories | DrugBank Online
Androgen Receptor Antagonists. Not Available. 5. 36. Details. Androgen Receptor Inhibitors. Not Available. 7. 58. Details. ... Androgens. Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the ef... more. 18. 180. Details. ... Androgens for Topical Use. Not Available. 1. 0. Details. Androstadienes. Derivatives of the steroid androstane having two ... A subclass of analgesic agents that typically do not bind to OPIOID RECEPTORS and are n... more. 172. 813. Details. ...
The AMEDEO Literature Guide
Combination therapy with novel androgen receptor antagonists and statin for castration-resistant prostate cancer.. Prostate. ... Abiraterone switches castration-resistant prostate cancer dependency from adrenal androgens towards androgen receptor variants ... Immune checkpoint B7-H3 protein expression is associated with poor outcome and androgen receptor status in prostate cancer.. ... Regulatory mechanism of androgen receptor on NCAPD3 gene expression in prostate cancer.. Prostate. 2021 Sep 30. doi: 10.1002/ ...
KEGG DRUG: Apalutamide
DG01591 Androgen receptor antagonist. D11040 Apalutamide. Target-based classification of drugs [BR:br08310]. Nuclear receptors ... DG01591 Androgen receptor antagonist. DG01624 Flutamide-type antiandrogen. Metabolizing enzyme substrate. DG02918 CYP2C8 ... DG01591 Androgen receptor antagonist. DG01624 Flutamide-type antiandrogen. D11040 Apalutamide. Metabolizing enzyme substrate. ... L02B HORMONE ANTAGONISTS AND RELATED AGENTS. L02BB Anti-androgens. L02BB05 Apalutamide. D11040 Apalutamide (JAN/INN) ,JP/US,. ...
Diagnosis and Treatment of Acne | AAFP
Spironolactone (Aldactone) is an androgen receptor antagonist with unclear effectiveness in the treatment of acne. It is ... Use of androgens, adrenocorticotropic hormone, bromides, corticosteroids, oral contraceptives, iodides, isoniazid, lithium, ... in which androgens have an important role; (2) hyperkeratinization of the follicle, leading to a microcomedo that eventually ...
Sadar Lab | Genome Sciences Centre
An androgen receptor N-terminal domain antagonist for treating prostate cancer. The Journal of clinical investigation, 2013 ... Combination therapy with androgen receptor N-terminal domain antagonist EPI-7170 and enzalutamide yields synergistic activity ... Sintokamide A Is a Novel Antagonist of Androgen Receptor That Uniquely Binds Activation Function-1 in Its Amino-terminal Domain ... Androgen receptor (AR) is a member of the steroid receptor family and a therapeutic target for all stages of prostate cancer. ...
Differential induction of the androgen receptor transcriptional activity by selective androgen receptor coactivators<...
Androgen Antagonists Medicine & Life Sciences 100% * Androgen Receptors Medicine & Life Sciences 81% ... Differential induction of the androgen receptor transcriptional activity by selective androgen receptor coactivators. In: Keio ... Differential induction of the androgen receptor transcriptional activity by selective androgen receptor coactivators. Keio ... Differential induction of the androgen receptor transcriptional activity by selective androgen receptor coactivators. / Yeh, ...
Proscillaridin A induces apoptosis, inhibits STAT3 activation and augments doxorubicin toxicity in prostate cancer cells
A bufadienolide derived androgen receptor antagonist with inhibitory activities against prostate cancer cells. Chem Biol ... In contrast to death receptor pathway, mitochondrial apoptosis pathway is initiated by various non-receptor mediated stimuli. ... we demonstrated for the first time that PSN-A inhibits STAT3 activation both in androgen-dependent and androgen-independent ... This differential effect of PSN-A might be associated with androgen sensitivity. Further study is needed to find out the exact ...
Xenoestrogen Action in Prostate Cancer: Pleiotropic Effects Dependent on Androgen Receptor Status | Cancer Research | American...
Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. Cancer Res ... Persistent DDT metabolite p,p′-DDE is a potent androgen receptor antagonist. Nature ... Mutations in the androgen receptor gene are associated with progression of human prostate cancer to androgen independence. Clin ... Androgen receptor mutations in androgen-independent prostate cancer: Cancer and Leukemia Group B Study 9663. J Clin Oncol ...
Androgen receptor and antiandrogen therapy in male breast cancer<...
Androgen Antagonists Medicine & Life Sciences 92% * Androgen Receptors Medicine & Life Sciences 75% ... keywords = "Androgen receptor, Androgens, Anti-androgen therapy, Gonadotropin-releasing hormone analogs, Male breast cancer", ... Androgen receptor and antiandrogen therapy in male breast cancer. Luigi Di Lauro, Maddalena Barba, Laura Pizzuti, Patrizia Vici ... Androgen receptor and antiandrogen therapy in male breast cancer. / Di Lauro, Luigi; Barba, Maddalena; Pizzuti, Laura et al. ...
Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines<...
Androgens Medicine & Life Sciences 15% * Gene Rearrangement Medicine & Life Sciences 9% * Androgen Antagonists Medicine & Life ... Li, Y., Chan, S. C., Brand, L. J., Hwang, T. H., Silverstein, K. A. T., & Dehm, S. M. (2013). Androgen receptor splice variants ... Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines. Cancer ... Androgen receptor splice variants mediate enzalutamide resistance in castration-resistant prostate cancer cell lines. In: ...
NCCN Announces Funding for Prostate Cancer Research Projects, in Collaboration with Pfizer and Astellas
Flutamide (Eulexin) is a nonsteroidal androgen re-ceptor antagonist that inhibits androgen binding to its nuclear receptor. It ... Androgen Receptor Antagonists. Spironolactone (Aldactone) is a compound originally developed as a mineralocorticoid antagonist ... at high doses spironolactone binds to the androgen receptor. In clinical practice it is a weak an-drogen antagonist used to ... Cyproterone acetate is a progestational antiandro-gen that blocks androgen receptor binding and sup-presses androgen-sensitive ...
Dryad Data -- Identification of the additional mitochondrial liabilities of 2-hydroxyflutamide when compared to its parent...
Integrative Analysis of lncRNA-mRNA Signature Reveals a Functional lincRNA in Triple-negative Breast Cancer | Research Square
The LAR subtype is characterized by androgen receptor (AR) signaling and sensitive to AR antagonist . Then, the sensitivity ... The high expression of ELK4 showed favorable prognosis of patients with basal-like 1 subtype and luminal androgen receptor ... and luminal androgen receptor (LAR) subtype. Furthermore, the relationship between the expression of ELK4 and different ... progesterone receptor (PgR) and ErbB-2/human epidermal growth factor receptor 2 (Her2) . It has been well known that TNBC is ...
DeprivationBicalutamideInhibitorsAntiandrogensEnzalutamideSecond-generation androgen-receptorFlutamideTranscriptional activityLuteinizing hormoneInhibits androgenAnti-androgensLevels of androgensInhibitorSelectiveCompoundsOvarianBlock androgenDihydrotestosteroneMechanismLHRHInhibit androgenTarget tissuesTumorMDV3100PathwayLigand-bindinLNCaPSpironolactoneBlockadeTissuesGenesEndocrineBindsDiseaseHydroxyflutamideClinicalAntineoplasticTherapyNuclear ReceptorsEstrogen receptorSpliceT877ARats2002DependentTherapiesOralSuppressionTherapeuticTNBCTranscriptionExpression
- The Phase III study ARASENS will evaluate the compound in combination with standard androgen deprivation therapy (ADT) and the chemotherapy docetaxel in men with newly diagnosed metastatic hormone-sensitive prostate cancer (mHSPC), who are starting first line hormone therapy. (salesandmarketingnetwork.com)
- ARASENS (A Randomized, double-blind, placebo-controlled Phase III study of ODM-201 versus placebo in addition to standard Androgen deprivation therapy and docetaxel in patients with metastatic castration SENSitive prostate cancer) is planned to be initiated towards the end of 2016. (salesandmarketingnetwork.com)
- PSA provocation by bipolar androgen therapy may predict duration of response to first-line androgen deprivation: Updated results from the BATMAN study. (amedeo.com)
- Prostate tumor RON receptor signaling mediates macrophage recruitment to drive androgen deprivation therapy resistance through Gas6-mediated Axl and RON signaling. (amedeo.com)
- Increased cytokine gene expression and cognition risk associated with androgen deprivation therapy. (amedeo.com)
- At present, surgery, radiotherapy, androgen deprivation therapy (ADT) and chemotherapy are the available treatment options for prostate cancer [ 1 ]. (medsci.org)
- For patients with metastatic castration-resistant prostate cancer who experience disease progression on novel hormonal agents (NHAs) and androgen deprivation therapy, it is important to consider when the NHA was received and whether docetaxel has been administered, as these factors affect downstream options and sequencing. (onclive.com)
- The results of the ARCHES trial show that giving androgen receptor antagonist Xtandi (enzalutamide) on top of androgen deprivation therapy (ADT) met the main objective of the study by significantly reducing the risk of radiographic progression or death in men with metastatic, hormone-sensitive prostate cancer (mHSPC). (pharmaphorum.com)
- The second of our new Phase 2 trials will study MDV3100 in an even earlier-stage population - hormone naïve prostate cancer patients who are indicated for androgen deprivation therapy. (technologynetworks.com)
- Although androgen deprivation therapy (ADT) has been the standard treatment, Concepcion noted that new evidence suggests this patient could benefit from a more aggressive approach. (onclive.com)
- All current non-steroidal AR antagonists, such as hydroxyflutamide, bicalutamide, and enzalutamide, target the androgen binding site of the receptor, competing with endogenous androgenic steroids. (biomedcentral.com)
- In this study we have used the acute glucose or galactose-conditioning of HepG2 cells to compare the mitochondrial toxicity of flutamide, 2-hydroxyflutamide and the structurally-related, non-hepatotoxic androgen receptor antagonist, bicalutamide. (datadryad.org)
- Urologists quickly embraced the concept of combined androgen blockage/maximal androgen blockade (CAB/MAB) and became very comfortable prescribing flutamide and later nilutamide and bicalutamide. (canjurol.com)
- Anti-androgen drugs, such as bicalutamide (Casodex), suppress the growth of cancer cells temporarily, but in most patients, the cancer ultimately develops resistance to drugs. (uclahealth.org)
- Medivation, Inc. and Astellas Pharma Inc. have announced treatment of the first patient in the TERRAIN study, a Phase 2 comparison of the investigational drug MDV3100, a triple-acting oral androgen receptor antagonist, with bicalutamide, a commonly used anti-androgen, in the treatment of advanced prostate cancer patients who have progressed while on LHRH analogue therapy or following surgical castration. (technologynetworks.com)
- It has been demonstrated that mutations in the ABS of the AR can lead to its activation by weak adrenal androgens, steroidal and non-steroidal ligands, and by mutation-driven conversion of AR inhibitors into agonists [ 13 ]. (biomedcentral.com)
- This report provides further evidence of effectiveness and safety of combined third generation aromatase inhibitors - competitive androgen receptor blockers in male precocious peripheral puberty, firstly employed in male MAS, and contributes to expand the spectrum of disorders in which their employment may reveal promising. (semanticscholar.org)
- Here, we provide the first comparison between AR-NTD inhibitors and AR-LBD inhibitors on androgen-regulated gene expression in prostate cancer cells using cDNA arrays, GSEA, and RT-PCR. (bcgsc.ca)
- LBD inhibitors and NTD inhibitors largely overlapped in the profile of androgen-induced genes that they each inhibited. (bcgsc.ca)
- De-repression of the transcriptome of androgen-repressed genes showed profound variance between these two classes of inhibitors. (bcgsc.ca)
- Second, the development of aromatase inhibitors unexpectedly raised the need for neutralizing androgens in order to tackle endocrine feedback mechanisms responsible for acquired resistance. (elsevier.com)
- Recent success in retargeting persistent AR activity with next generation androgen/AR axis inhibitors such as enzalutamide (MDV3100) has validated AR as a master regulator during all stages of disease progression. (elsevier.com)
- We updated AR agonists , inhibitors, and antagonists. (bvsalud.org)
- Biological and theoretical evaluation demonstrated that the introduction of the triazole core in the scaffold of nonsteroidal antiandrogens allowed the development of small molecules with improved overall AR-antagonist activity, and compound 14d displayed promising in vitro antitumor activity. (semanticscholar.org)
- All clinically approved hormonal therapies target the AR LBD, either directly with antiandrogens and selective AR modulators or indirectly by reducing levels of androgens. (bcgsc.ca)
- These findings may not only help us to better understand the specificity of the sex hormones and antiandrogens, but also to facilitate the development of better antiandrogens or androgens to fight the androgen-related diseases, such as prostate cancer. (elsevier.com)
- However, selective knock-down of AR-V expression inhibited androgen-independent growth and restored responsiveness to androgens and antiandrogens. (elsevier.com)
- Potential clinical uses of antiandrogens include suppression of androgen excess and treatment of androgen-dependent tumors. (brainkart.com)
- Urologists have been using oral nonsteroidal antiandrogens (AA) for 30 years as a component of combined androgen blockade. (canjurol.com)
- MDV3100) is an androgen-receptor (AR) antagonist antihypertensives, antidepressants, antipsychotics and antiandrogens. (hewedi.com)
- Enzalutamide is a potent anti-androgen that competes with DHT and binds to the ABS, preventing AR transcriptional activation. (biomedcentral.com)
- Genetic and chemical inhibition of DOT1L selectively impaired the viability of androgen receptor (AR)-positive PCa cells and organoids, including castration-resistant and enzalutamide-resistant cells. (nature.com)
- In this study, we show that cells with AR gene rearrangements expressing both full-length and AR-Vs are androgen independent and enzalutamide resistant. (elsevier.com)
- Enzalutamide (ENZ) is a second-generation androgen receptor (AR) antagonist used for the treatment of castration-resistant prostate cancer (CRPC) and reportedly prolongs survival time within a year of starting therapy. (bvsalud.org)
- Here we used quantitative mass spectrometry to define the "lipidome" in prostate tumors with matched benign tissues (n=21), independent unmatched tissues (n=47), and primary prostate explants cultured with the clinical AR antagonist enzalutamide (n=43). (garvan.org.au)
- Hormone therapy consisted of a luteinizing hormone-releasing hormone agonist/antagonist with or without a second-generation androgen-receptor targeting agent. (renalandurologynews.com)
- Flutamide is a nonsteroidal antiandrogen that inhibits androgen uptake or binding of androgen to target tissues. (medscape.com)
- Flutamide ( Eulexin ) is a nonsteroidal androgen re-ceptor antagonist that inhibits androgen binding to its nuclear receptor. (brainkart.com)
- The androgen receptor antagonist, flutamide, is strongly associated with idiosyncratic drug-induced liver injury (DILI). (datadryad.org)
- Persistent androgen receptor (AR) transcriptional activity underlies resistance to AR-targeted therapy and progression to lethal castration-resistant prostate cancer (CRPC). (elsevier.com)
- Tyagi R.K. Mechanisms of inhibition of transcriptional activity of androgen receptor by antagonists/endocrine disruptors CSIR , (2003-2006). (jnu.ac.in)
- In the case of a newly diagnosed patient with hormone-naïve high-grade metastatic prostate cancer, initiating therapy with a luteinizing hormone-releasing hormone antagonist (LHRH) would be appropriate, said Renzulli. (onclive.com)
- A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic mice. (greenmedinfo.com)
- For maximum clinical effectiveness it has to be used in combination with a GnRH antagonist (e.g., leuprolide acetate) that inhibits androgen production. (brainkart.com)
- 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment. (semanticscholar.org)
- MDV3100 has been shown in preclinical studies to provide more complete suppression of the androgen receptor pathway than existing anti-androgens and the TERRAIN study provides the opportunity to investigate this finding further in a clinical setting," said Lynn Seely, M.D., chief medical officer of Medivation. (technologynetworks.com)
Levels of androgens3
- Pathological conditions related to AR dysfunction involve altered levels of androgens and structural alterations in the AR. (bcgsc.ca)
- The physiological levels of androgens, secreted by ovarian stromal cells, are greatly increased with hyperplastic or neoplastic transformation leading to possible clinical consequences.We report a case of a 56-year-old woman with type 2 diabetes presenting with hirsuitism and a history of male pattern hair loss over a two year period. (endocrine-abstracts.org)
- We have recently shown that exercise is also neuroprotective on motoneuron dendrites following partial motoneuron depletion, and circulating levels of androgens have previously been shown to increase following exercise. (atsbio.com)
- Apalutamide is a third generation, nonsteroidal androgen receptor inhibitor or antiandrogen that was FDA-approved on February 14, 2018 as the first medication specifically indicated for non-metastatic (M0) castrate resistant prostate cancer (CRPC). (canjurol.com)
- In August 2011, icatibant (Firazyr), a selective bradykinin B2 receptor antagonist, was approved for treatment of acute attacks of HAE in adults at a dose of 30 mg SC in the abdominal area. (medscape.com)
- Sarms stand for selective androgen receptor modulator. (jackwall.net)
- Ostarine is a type of drug called a selective androgen receptor modulator (sarm). (jackwall.net)
- Evaluation of these compounds for their anti-proliferative properties against androgen dependent (LNCaP) and independent (PC-3) cells showed promising IC 50 values of 34-45 μM and 29-151 μM, respectively. (edu.au)
- The data suggest that the latter compounds may be an excellent starting point for the development of prostate cancer therapeutics for both androgen dependent and independent forms of this disease. (edu.au)
- Docking of these compounds (each enantiomer) in silico into the T877A mutated androgen receptor, as possessed by LNCaP cells, was also undertaken. (edu.au)
- Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the ef. (drugbank.com)
- Together, these data show that BPA can serve as a potential "hormone sensitizer" of the mutant ARs present in advanced prostate adenocarcinomas, thereby possibly contributing toward therapeutic relapse in advanced prostate cancer patients and supporting the notion that nonsteroidal environmental compounds can alter the function of nuclear receptor complexes. (aacrjournals.org)
- In an article published April 9 in the advanced online edition of the journal Science, the scientists describe the development and testing of two novel compounds, MDV3100 and RD162, which block the androgen receptor (AR) in CRPC cells, and report results from clinical trials in which MDV3100 was found to lower prostate-specific antigen (PSA) levels - a marker for tumor growth - in men with CRPC. (uclahealth.org)
- For competitive switch to short-acting compounds which are chemically modified by the body to increase muscle mass or enhance androgen production, best legal supplements for muscle growth. (scorsesefilms.com)
- Compounds that bind to and inhibit the activation of ANDROGEN RECEPTORS . (bvsalud.org)
- Oral contraceptives inhibit ovarian androgen production and are probably the first choice for young women with hirsutism who do not want to become pregnant. (medscape.com)
- Spearmint herbal tea has significant anti-androgen effects in polycystic ovarian syndrome. (greenmedinfo.com)
- Extreme clinical examples of androgen excess include central precocious puberty, the adrenogenital syn-dromes, and androgen-secreting adrenal, ovarian, or testicular tumors. (brainkart.com)
- Aldosterone antagonist that inhibits ovarian and adrenal production of androgens. (medscape.com)
- Aldosterone antagonists may block androgen receptors. (medscape.com)
- Therapies for advanced prostate cancer aim to block androgen receptor (AR) action. (aacrjournals.org)
- Spironolactone is an aldosterone antagonist that competes with testosterone and dihydrotestosterone receptor sites. (medscape.com)
- Abiraterone inhibits cytochrome P450 17A1 (CYP17A1), an enzyme responsible for the synthesis of testosterone that, after conversion to dihydrotestosterone (DHT), binds to the androgen binding site (ABS) of the AR and activates the AR signaling axis. (biomedcentral.com)
- The male hormones testosterone and dihydrotestosterone, which are also known as androgens, spur the growth of prostate cells, and drugs that block the receptors for these hormones are the most common treatment for the disease in its advanced, metastatic stage. (uclahealth.org)
- and agents for the imaging of tumor expression of androgen and estrogen receptors, such as 16β- 18 F-fluoro-5α-dihydrotestosterone and 16α- 18 F-fluoro-17β-estradiol, respectively. (snmjournals.org)
- Competes with dihydrotestosterone binding at hormone receptor sites on hair follicle cells. (medscape.com)
- One mechanism of such reactivation occurs through AR mutations, rendering the receptor responsive to noncanonical ligands. (aacrjournals.org)
- Although androgen independence of prostate cancer growth is a known contributing factor to endocrine resistance, the mechanism of androgen receptor deregulation in endocrine resistance is still poorly understood. (oncotarget.com)
- Approximately 1,300 patients will be randomized (1:1 ratio) to receive either BAY-1841788 (ODM-201) or placebo in combination with an ADT of investigator's choice (LHRH agonist/antagonists or orchiectomy), started =12 weeks before randomization. (salesandmarketingnetwork.com)
- Oral curcumin intake could inhibit androgen receptor expression and probably PSA activity. (greenmedinfo.com)
- May inhibit androgen feedback on pituitary gland. (medscape.com)
- AR mediates the action of physiological and exogenous androgens to regulate the expression of a network of genes in target tissues that are essential for the development and maintenance of the male phenotype and reproductive function as well as the function of numerous other tissues in both males and females. (bcgsc.ca)
- Sarms with agonist activity in most target tissues but the prostate and other sarms with antagonist activity only in prostate are likely to fulfill important. (jackwall.net)
- We have shown previously that a known xenoestrogen, bisphenol A (BPA), activates a tumor-derived AR mutant ( T877A ), leading to androgen-independent prostate cancer cell proliferation. (aacrjournals.org)
- The new, small organic molecule MDV3100 was "designed as a very strong antagonist of the androgen receptor to stop the growth of any prostate cancer that requires the AR for propagation, which includes most forms of prostate cancer," said Michael Jung, UCLA professor of chemistry and biochemistry and a researcher at UCLA's Jonsson Comprehensive Cancer Center , whose research group synthesized both MDV3100 and RD162. (uclahealth.org)
- Of 30 men with anti-androgen-resistant prostate cancer who received low doses of MDV3100 in the multisite Phase 1/2 trial designed to evaluate safety, 22 showed a sustained decline in PSA levels, an indication that their cancer was responding favorably to the drug. (uclahealth.org)
- MDV3100 and RD162 are second-generation anti-androgen therapies that prevent male hormones from stimulating the growth of prostate cancer cells. (uclahealth.org)
- The mainstay treatment for advanced PCa involves targeting of the androgen receptor (AR) signaling pathway 15 . (nature.com)
- Hormonal therapies for prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD). (bcgsc.ca)
- Several new androgen receptor (AR) cofactors, associated to the ligand binding domain of AR, have been identified by our group and named AR associated protein (ARA)70, ARA55, and ARA54. (elsevier.com)
- We also show that higher concentrations of BPA block proliferation of AR-positive, androgen-dependent prostate adenocarcinoma cells (LNCaP and LAPC-4), with a more modest inhibitory effect on androgen-independent cells (22Rv-1). (aacrjournals.org)
- Therefore, the objective of this study was to define some of the cellular changes that are associated with BDO 2 toxicity in prostate cells under androgen sensitive (LNCaP(AR + )) and androgen insensitive DU-145 (DU145(AR − )) conditions. (scirp.org)
- We examined the effect of butadiene diepoxide in prostate by assessing its effect on the growth of LNCaP(AR + ) cells, production and secretion of prostate secretary protein, androgen receptor status, and induction of androgen dependent genes. (scirp.org)
- However, at high doses spironolactone binds to the androgen receptor. (brainkart.com)
- Potential sites of action include go-nadotropin suppression, inhibition of androgen synthe-sis, and androgen receptor blockade. (brainkart.com)
- Blockade of the androgen receptor at the target muscle prevents the neuroprotective effects on motoneuron dendrites in rats treated with supplemental androgens. (atsbio.com)
- In the present study, we examine whether blockade of androgen receptors at the target musculature would prevent the neuroprotective effects of exercise on dendrites following partial motoneuron depletion. (atsbio.com)
- Early data suggests that following partial motoneuron depletion, exercised males with androgen receptor blockade at the quadriceps show dendritic lengths that are significantly shorter than those of exercised males with no treatment, while dendritic lengths in exercised males with interscapular implants do not differ from those of exercised animals without implants. (atsbio.com)
- Cyproterone acetate is a progestational antiandro-gen that blocks androgen receptor binding and sup-presses androgen-sensitive tissues. (brainkart.com)
- In the majority of cases, CRPC is accompanied by reactivation of the AR signaling axis so that the receptor regulates its numerous target genes including PSA. (biomedcentral.com)
- Further, mitotic genes deemed previously to be unique ARV targets were found to be biphasic targets associated with a proliferative level of signaling output from either ARVs or androgen-stimulated AR. (elsevier.com)
- We then discuss androgens in the context of the endocrine networks nourishing male breast cancer. (elsevier.com)
- Due to the lack or poor expression of the estrogen receptor , human epidermal growth factor receptor 2, and progesterone receptor , TNBC is resistant to hormones and endocrine therapies . (bvsalud.org)
- Paricalcitol is a synthetic vitamin D analogue that binds and activates vitamin D receptors in the kidneys, parathyroid glands, intestines, and bones. (medscape.com)
- The drug binds to its receptors in the cytoplasm by passing through the cell membrane, and the drug-receptor complex enters the cell nucleus. (firedrug.com)
- Male breast cancer is a hormone-driven disease that often expresses the estrogen receptor, and antiestrogen therapy represents the mainstay of treatment. (elsevier.com)
- Simultaneously, some saporin-injected rats were given implants of the androgen receptor antagonist hydroxyflutamide, either directly at the quadriceps musculature or interscapularly as a systemic control. (atsbio.com)
- WHIPPANY, N.J., June 3, 2016 -- (Healthcare Sales & Marketing Network) -- Bayer and Orion Corp oration today announced the expansion of the global clinical development program for the investigational androgen receptor (AR) antagonist BAY-1841788 (ODM-201) in the area of prostate cancer. (salesandmarketingnetwork.com)
- In clinical practice it is a weak an-drogen antagonist used to treat hirsutism in women by blocking testosterone binding to androgen receptors in hair follicles. (brainkart.com)
- Our group provides a comprehensive review of the structure and function of the AR and clinical evidence for targeting the cell 's nuclear receptor in TNBC. (bvsalud.org)
- Apalutamide is a small molecule and androgen receptor (AR) antagonist with potential antineoplastic activity. (affygility.com)
- Unfortunately, patients with advanced PCa either do not respond to anti-androgen therapy due to pre-existing aberrations of CYP17, or AR or relapse to CRPC due to adaptive responses, or Darwinian selection of rare aberrations. (biomedcentral.com)
- Gene expression profiling following knock-down of full-length AR or AR-Vs showed that AR-Vs drive resistance to AR-targeted therapy by functioning as constitutive and independent effectors of the androgen/AR transcriptional program. (elsevier.com)
- Therefore, therapy should be monitored by x-ray this study to determine whether tracking levels of C-reactive winsol kan je terecht voor ramen en deuren, rolluiken, poorten,zonwering, terrasoverkaping en raamdecoratie. (dancetracksdigital.com)
- Table 2 Examples of the difference treatment with the IL-6 receptor antagonists tocilizumab and sarilumab improved rise in systolic blood pressure in the MENT group, but returned to normal post-therapy. (awnry.com)
- Studies to decipher the functional implications of nuclear receptors docking onto the mitotic chromatin" Council of Scientific and Industrial Research (CSIR) , (2010-13). (jnu.ac.in)
- Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)
- Triple-negative breast cancer (TNBC), which accounts for 15%-20% of breast cancer, is an aggressive subtype characterized by negative expression of estrogen receptor (ER), progesterone receptor (PgR) and ErbB-2/human epidermal growth factor receptor 2 (Her2) . (researchsquare.com)
- However, CRPC patients can develop ENZ resistance (ENZR), mainly driven by abnormal reactivation of AR signaling, involving increased expression of the full-length AR (ARfl) or dominantly active androgen receptor splice variant 7 (ARv7) and ARfl/ARv7 heterodimers. (bvsalud.org)
- Here, we show that BPA cooperates with androgen to activate AR-T877A as shown by both reporter assays and increased levels of prostate-specific antigen expression. (aacrjournals.org)
- Peppermint tea has an anti-androgen effect in rats. (greenmedinfo.com)
- Vinclozolin (Vin CAS 50471-44-8), a dicarboximide fungicide, has been reported be an antagonist of androgen receptor binding in rats, effects that could result in decreased fertility, defects in reproductive organs or cancer. (cdc.gov)
- In vitro studies in two preadipocyte cell lines (3T3-L1, 3T3-F442) suggest that p,p ´-DDT has the ability to alter adipocyte differentiation, and that these effects correlate with changes induced in the expression of C/EBPα (CCAAT/enhancer-binding protein α) and PPARγ (peroxisome proliferator-activated receptor γ), the main transcription factors regulating the adipogenic process ( Moreno-Aliaga and Matsumura 2002 ). (cdc.gov)
- The AR is a member of the nuclear receptor superfamily of ligand-dependent transcription factors, and the identification of AR antagonists is an important step in the development of therapeutic agents for the treatment of prostate cancer. (semanticscholar.org)
- that heightened sensitivity makes prostate cancer cells resistant to existing anti-androgen therapies. (uclahealth.org)
- Newly Developed Targeted Therapies Against the Androgen Receptor in Triple-Negative Breast Cancer: A Review. (bvsalud.org)
- The compound, BAY-1841788 (ODM-201), is an investigational oral AR-antagonist currently in Phase III development for high-risk non-metastatic castration-resistant prostate cancer (nmCRPC). (salesandmarketingnetwork.com)
- We tend to use an antagonist, in this case to get rapid suppression of testosterone within about 3 days, and then based on that, we watch for his PSA response and symptomatic response to that. (onclive.com)
- First, molecular characterization efforts pointed to the androgen receptor as a potential therapeutic target. (elsevier.com)
- Tyagi RK, Modulatory effects of herbal drug ingredient(s) on transcription factor Pregnane & Xenobiotic Receptor (PXR): Evaluation for therapeutic potency and health safety assessment. (jnu.ac.in)
- The high expression of ELK4 showed favorable prognosis of patients with basal-like 1 subtype and luminal androgen receptor subtype of TNBC. (researchsquare.com)
- Three principal characteristics of TNBC cells are (i) extreme aggressiveness, (ii) absence of hormones , and (iii) growth factor receptors . (bvsalud.org)
- therefore, inhibiting androgen signaling pathways holds promise for TNBC targeting. (bvsalud.org)