5 alpha dihydroprogesterone. Medical search

Plasma glycoprotein member of the serpin superfamily which inhibits TRYPSIN; NEUTROPHIL ELASTASE; and other PROTEOLYTIC ENZYMES.

One of the two major pharmacological subdivisions of adrenergic receptors that were originally defined by the relative potencies of various adrenergic compounds. The alpha receptors were initially described as excitatory receptors that post-junctionally stimulate SMOOTH MUSCLE contraction. However, further analysis has revealed a more complex picture involving several alpha receptor subtypes and their involvement in feedback regulation.

Hypoxia-inducible factor 1, alpha subunit is a basic helix-loop-helix transcription factor that is regulated by OXYGEN availability and is targeted for degradation by VHL TUMOR SUPPRESSOR PROTEIN.

A member of the NICOTINIC ACETYLCHOLINE RECEPTOR subfamily of the LIGAND-GATED ION CHANNEL family. It consists entirely of pentameric a7 subunits expressed in the CNS, autonomic nervous system, vascular system, lymphocytes and spleen.

Cell surface receptor for LAMININ, epiligrin, FIBRONECTINS, entactin, and COLLAGEN. Integrin alpha3beta1 is the major integrin present in EPITHELIAL CELLS, where it plays a role in the assembly of BASEMENT MEMBRANE as well as in cell migration, and may regulate the functions of other integrins. Two alternatively spliced isoforms of the alpha subunit (INTEGRIN ALPHA3), are differentially expressed in different cell types.

An integrin alpha subunit that is unique in that it does not contain an I domain, and its proteolytic cleavage site is near the middle of the extracellular portion of the polypeptide rather than close to the membrane as in other integrin alpha subunits.

An integrin alpha subunit that primarily associates with INTEGRIN BETA1 or INTEGRIN BETA4 to form laminin-binding heterodimers. Integrin alpha6 has two alternatively spliced isoforms: integrin alpha6A and integrin alpha6B, which differ in their cytoplasmic domains and are regulated in a tissue-specific and developmental stage-specific manner.

An integrin found in FIBROBLASTS; PLATELETS; MONOCYTES, and LYMPHOCYTES. Integrin alpha5beta1 is the classical receptor for FIBRONECTIN, but it also functions as a receptor for LAMININ and several other EXTRACELLULAR MATRIX PROTEINS.

Integrin alpha4beta1 is a FIBRONECTIN and VCAM-1 receptor present on LYMPHOCYTES; MONOCYTES; EOSINOPHILS; NK CELLS and thymocytes. It is involved in both cell-cell and cell- EXTRACELLULAR MATRIX adhesion and plays a role in INFLAMMATION, hematopoietic cell homing and immune function, and has been implicated in skeletal MYOGENESIS; NEURAL CREST migration and proliferation, lymphocyte maturation and morphogenesis of the PLACENTA and HEART.

An interleukin-1 subtype that occurs as a membrane-bound pro-protein form that is cleaved by proteases to form a secreted mature form. Unlike INTERLEUKIN-1BETA both membrane-bound and secreted forms of interleukin-1alpha are biologically active.

An integrin found on fibroblasts, platelets, endothelial and epithelial cells, and lymphocytes where it functions as a receptor for COLLAGEN and LAMININ. Although originally referred to as the collagen receptor, it is one of several receptors for collagen. Ligand binding to integrin alpha2beta1 triggers a cascade of intracellular signaling, including activation of p38 MAP kinase.

A subclass of alpha-adrenergic receptors that mediate contraction of SMOOTH MUSCLE in a variety of tissues such as ARTERIOLES; VEINS; and the UTERUS. They are usually found on postsynaptic membranes and signal through GQ-G11 G-PROTEINS.

This integrin alpha subunit combines with INTEGRIN BETA1 to form a receptor (INTEGRIN ALPHA5BETA1) that binds FIBRONECTIN and LAMININ. It undergoes posttranslational cleavage into a heavy and a light chain that are connected by disulfide bonds.

Integrin alpha1beta1 functions as a receptor for LAMININ and COLLAGEN. It is widely expressed during development, but in the adult is the predominant laminin receptor (RECEPTORS, LAMININ) in mature SMOOTH MUSCLE CELLS, where it is important for maintenance of the differentiated phenotype of these cells. Integrin alpha1beta1 is also found in LYMPHOCYTES and microvascular endothelial cells, and may play a role in angiogenesis. In SCHWANN CELLS and neural crest cells, it is involved in cell migration. Integrin alpha1beta1 is also known as VLA-1 and CD49a-CD29.

A subclass of alpha-adrenergic receptors found on both presynaptic and postsynaptic membranes where they signal through Gi-Go G-PROTEINS. While postsynaptic alpha-2 receptors play a traditional role in mediating the effects of ADRENERGIC AGONISTS, the subset of alpha-2 receptors found on presynaptic membranes signal the feedback inhibition of NEUROTRANSMITTER release.

A cell surface receptor mediating cell adhesion to the EXTRACELLULAR MATRIX and to other cells via binding to LAMININ. It is involved in cell migration, embryonic development, leukocyte activation and tumor cell invasiveness. Integrin alpha6beta1 is the major laminin receptor on PLATELETS; LEUKOCYTES; and many EPITHELIAL CELLS, and ligand binding may activate a number of signal transduction pathways. Alternative splicing of the cytoplasmic domain of the alpha6 subunit (INTEGRIN ALPHA6) results in the formation of A and B isoforms of the heterodimer, which are expressed in a tissue-specific manner.

The sequence of PURINES and PYRIMIDINES in nucleic acids and polynucleotides. It is also called nucleotide sequence.

This intrgrin is a key component of HEMIDESMOSOMES and is required for their formation and maintenance in epithelial cells. Integrin alpha6beta4 is also found on thymocytes, fibroblasts, and Schwann cells, where it functions as a laminin receptor (RECEPTORS, LAMININ) and is involved in wound healing, cell migration, and tumor invasiveness.

The alpha subunits of integrin heterodimers (INTEGRINS), which mediate ligand specificity. There are approximately 18 different alpha chains, exhibiting great sequence diversity; several chains are also spliced into alternative isoforms. They possess a long extracellular portion (1200 amino acids) containing a MIDAS (metal ion-dependent adhesion site) motif, and seven 60-amino acid tandem repeats, the last 4 of which form EF HAND MOTIFS. The intracellular portion is short with the exception of INTEGRIN ALPHA4.

A family of transmembrane glycoproteins (MEMBRANE GLYCOPROTEINS) consisting of noncovalent heterodimers. They interact with a wide variety of ligands including EXTRACELLULAR MATRIX PROTEINS; COMPLEMENT, and other cells, while their intracellular domains interact with the CYTOSKELETON. The integrins consist of at least three identified families: the cytoadhesin receptors(RECEPTORS, CYTOADHESIN), the leukocyte adhesion receptors (RECEPTORS, LEUKOCYTE ADHESION), and the VERY LATE ANTIGEN RECEPTORS. Each family contains a common beta-subunit (INTEGRIN BETA CHAINS) combined with one or more distinct alpha-subunits (INTEGRIN ALPHA CHAINS). These receptors participate in cell-matrix and cell-cell adhesion in many physiologically important processes, including embryological development; HEMOSTASIS; THROMBOSIS; WOUND HEALING; immune and nonimmune defense mechanisms; and oncogenic transformation.

An integrin alpha subunit that binds COLLAGEN and LAMININ though its I domain. It combines with INTEGRIN BETA1 to form the heterodimer INTEGRIN ALPHA1BETA1.

Brain waves characterized by a relatively high voltage or amplitude and a frequency of 8-13 Hz. They constitute the majority of waves recorded by EEG registering the activity of the parietal and occipital lobes when the individual is awake, but relaxed with the eyes closed.

An integrin alpha subunit that occurs as alternatively spliced isoforms. The isoforms are differentially expressed in specific cell types and at specific developmental stages. Integrin alpha3 combines with INTEGRIN BETA1 to form INTEGRIN ALPHA3BETA1 which is a heterodimer found primarily in epithelial cells.

Deficiency of the protease inhibitor ALPHA 1-ANTITRYPSIN that manifests primarily as PULMONARY EMPHYSEMA and LIVER CIRRHOSIS.

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.

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.

One of the two major classes of cholinergic receptors. Nicotinic receptors were originally distinguished by their preference for NICOTINE over MUSCARINE. They are generally divided into muscle-type and neuronal-type (previously ganglionic) based on pharmacology, and subunit composition of the receptors.

Drugs that selectively bind to and activate alpha adrenergic receptors.

A nuclear transcription factor. Heterodimerization with RETINOID X RECEPTOR GAMMA is important to metabolism of LIPIDS. It is the target of FIBRATES to control HYPERLIPIDEMIAS.

A naturally occurring prostaglandin that has oxytocic, luteolytic, and abortifacient activities. Due to its vasocontractile properties, the compound has a variety of other biological actions.

Drugs that bind to but do not activate alpha-adrenergic receptors thereby blocking the actions of endogenous or exogenous adrenergic agonists. Adrenergic alpha-antagonists are used in the treatment of hypertension, vasospasm, peripheral vascular disease, shock, and pheochromocytoma.

Proteins prepared by recombinant DNA technology.

Hepatocyte nuclear factor 1-alpha is a transcription factor found in the LIVER; PANCREAS; and KIDNEY that regulates HOMEOSTASIS of GLUCOSE.

The parts of a macromolecule that directly participate in its specific combination with another molecule.

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.

Glycoprotein found in alpha(1)-globulin region in human serum. It inhibits chymotrypsin-like proteinases in vivo and has cytotoxic killer-cell activity in vitro. The protein also has a role as an acute-phase protein and is active in the control of immunologic and inflammatory processes, and as a tumor marker. It is a member of the serpin superfamily.

An EPIDERMAL GROWTH FACTOR related protein that is found in a variety of tissues including EPITHELIUM, and maternal DECIDUA. It is synthesized as a transmembrane protein which can be cleaved to release a soluble active form which binds to the EGF RECEPTOR.

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.

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.

The rate dynamics in chemical or physical systems.

Endogenous substances, usually proteins, which are effective in the initiation, stimulation, or termination of the genetic transcription process.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-1 RECEPTORS.

Nucleocytoplasmic transport molecules that bind to the NUCLEAR LOCALIZATION SIGNALS of cytoplasmic molecules destined to be imported into the CELL NUCLEUS. Once attached to their cargo they bind to BETA KARYOPHERINS and are transported through the NUCLEAR PORE COMPLEX. Inside the CELL NUCLEUS alpha karyopherins dissociate from beta karypherins and their cargo. They then form a complex with CELLULAR APOPTOSIS SUSCEPTIBILITY PROTEIN and RAN GTP-BINDING PROTEIN which is exported to the CYTOPLASM.

Compounds and molecular complexes that consist of very large numbers of atoms and are generally over 500 kDa in size. In biological systems macromolecular substances usually can be visualized using ELECTRON MICROSCOPY and are distinguished from ORGANELLES by the lack of a membrane structure.

Serum glycoprotein produced by activated MACROPHAGES and other mammalian MONONUCLEAR LEUKOCYTES. It has necrotizing activity against tumor cell lines and increases ability to reject tumor transplants. Also known as TNF-alpha, it is only 30% homologous to TNF-beta (LYMPHOTOXIN), but they share TNF RECEPTORS.

A selective adrenergic alpha-1 antagonist used in the treatment of HEART FAILURE; HYPERTENSION; PHEOCHROMOCYTOMA; RAYNAUD DISEASE; PROSTATIC HYPERTROPHY; and URINARY RETENTION.

The physiologically active and stable hydrolysis product of EPOPROSTENOL. Found in nearly all mammalian tissue.

Single chains of amino acids that are the units of multimeric PROTEINS. Multimeric proteins can be composed of identical or non-identical subunits. One or more monomeric subunits may compose a protomer which itself is a subunit structure of a larger assembly.

The insertion of recombinant DNA molecules from prokaryotic and/or eukaryotic sources into a replicating vehicle, such as a plasmid or virus vector, and the introduction of the resultant hybrid molecules into recipient cells without altering the viability of those cells.

The relationship between the dose of an administered drug and the response of the organism to the drug.

Any detectable and heritable change in the genetic material that causes a change in the GENOTYPE and which is transmitted to daughter cells and to succeeding generations.

Strains of mice in which certain GENES of their GENOMES have been disrupted, or "knocked-out". To produce knockouts, using RECOMBINANT DNA technology, the normal DNA sequence of the gene being studied is altered to prevent synthesis of a normal gene product. Cloned cells in which this DNA alteration is successful are then injected into mouse EMBRYOS to produce chimeric mice. The chimeric mice are then bred to yield a strain in which all the cells of the mouse contain the disrupted gene. Knockout mice are used as EXPERIMENTAL ANIMAL MODELS for diseases (DISEASE MODELS, ANIMAL) and to clarify the functions of the genes.

The phenotypic manifestation of a gene or genes by the processes of GENETIC TRANSCRIPTION and GENETIC TRANSLATION.

The biosynthesis of RNA carried out on a template of DNA. The biosynthesis of DNA from an RNA template is called REVERSE TRANSCRIPTION.

Regulatory proteins that act as molecular switches. They control a wide range of biological processes including: receptor signaling, intracellular signal transduction pathways, and protein synthesis. Their activity is regulated by factors that control their ability to bind to and hydrolyze GTP to GDP. EC 3.6.1.-.

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.

The level of protein structure in which combinations of secondary protein structures (alpha helices, beta sheets, loop regions, and motifs) pack together to form folded shapes called domains. Disulfide bridges between cysteines in two different parts of the polypeptide chain along with other interactions between the chains play a role in the formation and stabilization of tertiary structure. Small proteins usually consist of only one domain but larger proteins may contain a number of domains connected by segments of polypeptide chain which lack regular secondary structure.

The introduction of a phosphoryl group into a compound through the formation of an ester bond between the compound and a phosphorus moiety.

The order of amino acids as they occur in a polypeptide chain. This is referred to as the primary structure of proteins. It is of fundamental importance in determining PROTEIN CONFORMATION.

An imidazoline sympatholytic agent that stimulates ALPHA-2 ADRENERGIC RECEPTORS and central IMIDAZOLINE RECEPTORS. It is commonly used in the management of HYPERTENSION.

A polypeptide substance comprising about one third of the total protein in mammalian organisms. It is the main constituent of SKIN; CONNECTIVE TISSUE; and the organic substance of bones (BONE AND BONES) and teeth (TOOTH).

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.

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.

A plant alkaloid with alpha-2-adrenergic blocking activity. Yohimbine has been used as a mydriatic and in the treatment of ERECTILE DYSFUNCTION.

The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain).

Proteins which bind to DNA. The family includes proteins which bind to both double- and single-stranded DNA and also includes specific DNA binding proteins in serum which can be used as markers for malignant diseases.

Recombinant proteins produced by the GENETIC TRANSLATION of fused genes formed by the combination of NUCLEIC ACID REGULATORY SEQUENCES of one or more genes with the protein coding sequences of one or more genes.

Domesticated bovine animals of the genus Bos, usually kept on a farm or ranch and used for the production of meat or dairy products or for heavy labor.

A soluble factor produced by MONOCYTES; MACROPHAGES, and other cells which activates T-lymphocytes and potentiates their response to mitogens or antigens. Interleukin-1 is a general term refers to either of the two distinct proteins, INTERLEUKIN-1ALPHA and INTERLEUKIN-1BETA. The biological effects of IL-1 include the ability to replace macrophage requirements for T-cell activation.

A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).

Compounds that bind to and activate ADRENERGIC ALPHA-2 RECEPTORS.

The degree of similarity between sequences of amino acids. This information is useful for the analyzing genetic relatedness of proteins and species.

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.

A family of heterotrimeric GTP-binding protein alpha subunits that were originally identified by their ability to inhibit ADENYLYL CYCLASES. Members of this family can couple to beta and gamma G-protein subunits that activate POTASSIUM CHANNELS. The Gi-Go part of the name is also spelled Gi/Go.

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.

Electrophoresis in which a polyacrylamide gel is used as the diffusion medium.

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)

Different forms of a protein that may be produced from different GENES, or from the same gene by ALTERNATIVE SPLICING.

Drugs that bind to and block the activation of ADRENERGIC ALPHA-2 RECEPTORS.

Elements of limited time intervals, contributing to particular results or situations.

Short sequences (generally about 10 base pairs) of DNA that are complementary to sequences of messenger RNA and allow reverse transcriptases to start copying the adjacent sequences of mRNA. Primers are used extensively in genetic and molecular biology techniques.

Peptide elongation factor 1 is a multisubunit protein that is responsible for the GTP-dependent binding of aminoacyl-tRNAs to eukaryotic ribosomes. The alpha subunit (EF-1alpha) binds aminoacyl-tRNA and transfers it to the ribosome in a process linked to GTP hydrolysis. The beta and delta subunits (EF-1beta, EF-1delta) are involved in exchanging GDP for GTP. The gamma subunit (EF-1gamma) is a structural component.

A cell line derived from cultured tumor cells.

Partial proteins formed by partial hydrolysis of complete proteins or generated through PROTEIN ENGINEERING techniques.

A subfamily of nuclear receptors that regulate GENETIC TRANSCRIPTION of a diverse group of GENES involved in the synthesis of BLOOD COAGULATION FACTORS; and in GLUCOSE; CHOLESTEROL; and FATTY ACIDS metabolism.

Structurally related forms of an enzyme. Each isoenzyme has the same mechanism and classification, but differs in its chemical, physical, or immunological characteristics.

Models used experimentally or theoretically to study molecular shape, electronic properties, or interactions; includes analogous molecules, computer-generated graphics, and mechanical structures.

Cell surface proteins which bind GAMMA-AMINOBUTYRIC ACID and contain an integral membrane chloride channel. Each receptor is assembled as a pentamer from a pool of at least 19 different possible subunits. The receptors belong to a superfamily that share a common CYSTEINE loop.

(9 alpha,11 alpha,13E,15S)-9,11,15-Trihydroxyprost-13-en-1-oic acid (PGF(1 alpha)); (5Z,9 alpha,11,alpha,13E,15S)-9,11,15-trihydroxyprosta-5,13-dien-1-oic acid (PGF(2 alpha)); (5Z,9 alpha,11 alpha,13E,15S,17Z)-9,11,15-trihydroxyprosta-5,13,17-trien-1-oic acid (PGF(3 alpha)). A family of prostaglandins that includes three of the six naturally occurring prostaglandins. All naturally occurring PGF have an alpha configuration at the 9-carbon position. They stimulate uterine and bronchial smooth muscle and are often used as oxytocics.

Histochemical localization of immunoreactive substances using labeled antibodies as reagents.

Conversion of an inactive form of an enzyme to one possessing metabolic activity. It includes 1, activation by ions (activators); 2, activation by cofactors (coenzymes); and 3, conversion of an enzyme precursor (proenzyme or zymogen) to an active enzyme.

Genetically engineered MUTAGENESIS at a specific site in the DNA molecule that introduces a base substitution, or an insertion or deletion.

A subfamily in the family MURIDAE, comprising the hamsters. Four of the more common genera are Cricetus, CRICETULUS; MESOCRICETUS; and PHODOPUS.

A condition of decreased oxygen content at the cellular level.

Single-stranded complementary DNA synthesized from an RNA template by the action of RNA-dependent DNA polymerase. cDNA (i.e., complementary DNA, not circular DNA, not C-DNA) is used in a variety of molecular cloning experiments as well as serving as a specific hybridization probe.

A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances.

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.

Antibodies produced by a single clone of cells.

The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups.

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.

A family of heterotrimeric GTP-binding protein alpha subunits that activate ADENYLYL CYCLASES.

A positive regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.

Drugs that bind to and activate nicotinic cholinergic receptors (RECEPTORS, NICOTINIC). Nicotinic agonists act at postganglionic nicotinic receptors, at neuroeffector junctions in the peripheral nervous system, and at nicotinic receptors in the central nervous system. Agents that function as neuromuscular depolarizing blocking agents are included here because they activate nicotinic receptors, although they are used clinically to block nicotinic transmission.

Heparin-binding proteins that exhibit a number of inflammatory and immunoregulatory activities. Originally identified as secretory products of MACROPHAGES, these chemokines are produced by a variety of cell types including NEUTROPHILS; FIBROBLASTS; and EPITHELIAL CELLS. They likely play a significant role in respiratory tract defenses.

Specific cell surface receptors which bind to FIBRONECTINS. Studies have shown that these receptors function in certain types of adhesive contact as well as playing a major role in matrix assembly. These receptors include the traditional fibronectin receptor, also called INTEGRIN ALPHA5BETA1 and several other integrins.

The sequence of carbohydrates within POLYSACCHARIDES; GLYCOPROTEINS; and GLYCOLIPIDS.

A 38-kDa mitogen-activated protein kinase that is abundantly expressed in a broad variety of cell types. It is involved in the regulation of cellular stress responses as well as the control of proliferation and survival of many cell types. The kinase activity of the enzyme is inhibited by the pyridinyl-imidazole compound SB 203580.

Enzymes catalyzing the transfer of fucose from a nucleoside diphosphate fucose to an acceptor molecule which is frequently another carbohydrate, a glycoprotein, or a glycolipid molecule. Elevated activity of some fucosyltransferases in human serum may serve as an indicator of malignancy. The class includes EC 2.4.1.65; EC 2.4.1.68; EC 2.4.1.69; EC 2.4.1.89.

The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells.

An enzyme that catalyzes the active transport system of sodium and potassium ions across the cell wall. Sodium and potassium ions are closely coupled with membrane ATPase which undergoes phosphorylation and dephosphorylation, thereby providing energy for transport of these ions against concentration gradients.

In vitro method for producing large amounts of specific DNA or RNA fragments of defined length and sequence from small amounts of short oligonucleotide flanking sequences (primers). The essential steps include thermal denaturation of the double-stranded target molecules, annealing of the primers to their complementary sequences, and extension of the annealed primers by enzymatic synthesis with DNA polymerase. The reaction is efficient, specific, and extremely sensitive. Uses for the reaction include disease diagnosis, detection of difficult-to-isolate pathogens, mutation analysis, genetic testing, DNA sequencing, and analyzing evolutionary relationships.

A family of heterotrimeric GTP-binding protein alpha subunits that activate TYPE C PHOSPHOLIPASES dependent signaling pathways. The Gq-G11 part of the name is also spelled Gq/G11.

Serum proteins that have the most rapid migration during ELECTROPHORESIS. This subgroup of globulins is divided into faster and slower alpha(1)- and alpha(2)-globulins.

Differentiation antigens residing on mammalian leukocytes. CD stands for cluster of differentiation, which refers to groups of monoclonal antibodies that show similar reactivity with certain subpopulations of antigens of a particular lineage or differentiation stage. The subpopulations of antigens are also known by the same CD designation.

Laboratory mice that have been produced from a genetically manipulated EGG or EMBRYO, MAMMALIAN.

The GTPase-containing subunits of heterotrimeric GTP-binding proteins. When dissociated from the heterotrimeric complex these subunits interact with a variety of second messenger systems. Hydrolysis of GTP by the inherent GTPase activity of the subunit causes it to revert to its inactive (heterotrimeric) form. The GTP-Binding protein alpha subunits are grouped into families according to the type of action they have on second messenger systems.

Glycoproteins found on the surfaces of cells, particularly in fibrillar structures. The proteins are lost or reduced when these cells undergo viral or chemical transformation. They are highly susceptible to proteolysis and are substrates for activated blood coagulation factor VIII. The forms present in plasma are called cold-insoluble globulins.

The movement of cells from one location to another. Distinguish from CYTOKINESIS which is the process of dividing the CYTOPLASM of a cell.

Members of the class of compounds composed of AMINO ACIDS joined together by peptide bonds between adjacent amino acids into linear, branched or cyclical structures. OLIGOPEPTIDES are composed of approximately 2-12 amino acids. Polypeptides are composed of approximately 13 or more amino acids. PROTEINS are linear polypeptides that are normally synthesized on RIBOSOMES.

Connective tissue cells which secrete an extracellular matrix rich in collagen and other macromolecules.

Collagen receptors are cell surface receptors that modulate signal transduction between cells and the EXTRACELLULAR MATRIX. They are found in many cell types and are involved in the maintenance and regulation of cell shape and behavior, including PLATELET ACTIVATION and aggregation, through many different signaling pathways and differences in their affinities for collagen isoforms. Collagen receptors include discoidin domain receptors, INTEGRINS, and glycoprotein VI.

A PERTUSSIS TOXIN-sensitive GTP-binding protein alpha subunit. It couples with a variety of CELL SURFACE RECEPTORS, has been implicated in INTERLEUKIN-12 production, and may play a role in INFLAMMATORY BOWEL DISEASES.

The species Oryctolagus cuniculus, in the family Leporidae, order LAGOMORPHA. Rabbits are born in burrows, furless, and with eyes and ears closed. In contrast with HARES, rabbits have 22 chromosome pairs.

CELL LINE derived from the ovary of the Chinese hamster, Cricetulus griseus (CRICETULUS). The species is a favorite for cytogenetic studies because of its small chromosome number. The cell line has provided model systems for the study of genetic alterations in cultured mammalian cells.

Detection of RNA that has been electrophoretically separated and immobilized by blotting on nitrocellulose or other type of paper or nylon membrane followed by hybridization with labeled NUCLEIC ACID PROBES.

Precursor of epinephrine that is secreted by the adrenal medulla and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers and of the diffuse projection system in the brain arising from the locus ceruleus. It is also found in plants and is used pharmacologically as a sympathomimetic.

Proteins found in the nucleus of a cell. Do not confuse with NUCLEOPROTEINS which are proteins conjugated with nucleic acids, that are not necessarily present in the nucleus.

Progressive restriction of the developmental potential and increasing specialization of function that leads to the formation of specialized cells, tissues, and organs.

A benzodioxane-linked imidazole that has alpha-2 adrenoceptor antagonist activity.

Immunologic method used for detecting or quantifying immunoreactive substances. The substance is identified by first immobilizing it by blotting onto a membrane and then tagging it with labeled antibodies.

Non-antibody proteins secreted by inflammatory leukocytes and some non-leukocytic cells, that act as intercellular mediators. They differ from classical hormones in that they are produced by a number of tissue or cell types rather than by specialized glands. They generally act locally in a paracrine or autocrine rather than endocrine manner.

An alpha-1 adrenergic agonist used as a mydriatic, nasal decongestant, and cardiotonic agent.

A member of the serpin superfamily found in plasma that inhibits the lysis of fibrin clots which are induced by plasminogen activator. It is a glycoprotein, molecular weight approximately 70,000 that migrates in the alpha 2 region in immunoelectrophoresis. It is the principal plasmin inactivator in blood, rapidly forming a very stable complex with plasmin.

Eukaryotic initiation factor of protein synthesis. In higher eukaryotes the factor consists of three subunits: alpha, beta, and gamma. As initiation proceeds, eIF-2 forms a ternary complex with Met-tRNAi and GTP.

Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders).

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.

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).)

A negative regulatory effect on physiological processes at the molecular, cellular, or systemic level. At the molecular level, the major regulatory sites include membrane receptors, genes (GENE EXPRESSION REGULATION), mRNAs (RNA, MESSENGER), and proteins.

An integrin that binds to a variety of plasma and extracellular matrix proteins containing the conserved RGD amino acid sequence and modulates cell adhesion. Integrin alphavbeta3 is highly expressed in OSTEOCLASTS where it may play role in BONE RESORPTION. It is also abundant in vascular smooth muscle and endothelial cells, and in some tumor cells, where it is involved in angiogenesis and cell migration. Although often referred to as the vitronectin receptor there is more than one receptor for vitronectin (RECEPTORS, VITRONECTIN).

Established cell cultures that have the potential to propagate indefinitely.

The sum of the weight of all the atoms in a molecule.

Processes that stimulate the GENETIC TRANSCRIPTION of a gene or set of genes.

A basic helix-loop-helix transcription factor that plays a role in APOPTOSIS. It is composed of two subunits: ARYL HYDROCARBON RECEPTOR NUCLEAR TRANSLOCATOR and HYPOXIA-INDUCIBLE FACTOR 1, ALPHA SUBUNIT.

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.

A basic element found in nearly all organized tissues. It is a member of the alkaline earth family of metals with the atomic symbol Ca, atomic number 20, and atomic weight 40. Calcium is the most abundant mineral in the body and combines with phosphorus to form calcium phosphate in the bones and teeth. It is essential for the normal functioning of nerves and muscles and plays a role in blood coagulation (as factor IV) and in many enzymatic processes.

A stable prostaglandin endoperoxide analog which serves as a thromboxane mimetic. Its actions include mimicking the hydro-osmotic effect of VASOPRESSIN and activation of TYPE C PHOSPHOLIPASES. (From J Pharmacol Exp Ther 1983;224(1): 108-117; Biochem J 1984;222(1):103-110)

Proteins which are found in membranes including cellular and intracellular membranes. They consist of two types, peripheral and integral proteins. They include most membrane-associated enzymes, antigenic proteins, transport proteins, and drug, hormone, and lectin receptors.

A characteristic feature of enzyme activity in relation to the kind of substrate on which the enzyme or catalytic molecule reacts.

The arrangement of two or more amino acid or base sequences from an organism or organisms in such a way as to align areas of the sequences sharing common properties. The degree of relatedness or homology between the sequences is predicted computationally or statistically based on weights assigned to the elements aligned between the sequences. This in turn can serve as a potential indicator of the genetic relatedness between the organisms.

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 fission of a CELL. It includes CYTOKINESIS, when the CYTOPLASM of a cell is divided, and CELL NUCLEUS DIVISION.

Positively charged particles composed of two protons and two NEUTRONS, i.e. equivalent to HELIUM nuclei, which are emitted during disintegration of heavy ISOTOPES. Alpha rays have very strong ionizing power, but weak penetrability.

The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.

Transport proteins that carry specific substances in the blood or across cell membranes.

Diffusible gene products that act on homologous or heterologous molecules of viral or cellular DNA to regulate the expression of proteins.

Body organ that filters blood for the secretion of URINE and that regulates ion concentrations.

A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain.

The first continuously cultured human malignant CELL LINE, derived from the cervical carcinoma of Henrietta Lacks. These cells are used for VIRUS CULTIVATION and antitumor drug screening assays.

A group of enzymes with the general formula CMP-N-acetylneuraminate:acceptor N-acetylneuraminyl transferase. They catalyze the transfer of N-acetylneuraminic acid from CMP-N-acetylneuraminic acid to an acceptor, which is usually the terminal sugar residue of an oligosaccharide, a glycoprotein, or a glycolipid. EC 2.4.99.-.

A non-fibrillar collagen found in the structure of BASEMENT MEMBRANE. Collagen type IV molecules assemble to form a sheet-like network which is involved in maintaining the structural integrity of basement membranes. The predominant form of the protein is comprised of two alpha1(IV) subunits and one alpha2(IV) subunit, however, at least six different alpha subunits can be incorporated into the heterotrimer.

Neurotoxic proteins from the venom of the banded or Formosan krait (Bungarus multicinctus, an elapid snake). alpha-Bungarotoxin blocks nicotinic acetylcholine receptors and has been used to isolate and study them; beta- and gamma-bungarotoxins act presynaptically causing acetylcholine release and depletion. Both alpha and beta forms have been characterized, the alpha being similar to the large, long or Type II neurotoxins from other elapid venoms.

The commonest and widest ranging species of the clawed "frog" (Xenopus) in Africa. This species is used extensively in research. There is now a significant population in California derived from escaped laboratory animals.

Immunoglobulin molecules having a specific amino acid sequence by virtue of which they interact only with the ANTIGEN (or a very similar shape) that induced their synthesis in cells of the lymphoid series (especially PLASMA CELLS).

Carbohydrates consisting of between two (DISACCHARIDES) and ten MONOSACCHARIDES connected by either an alpha- or beta-glycosidic link. They are found throughout nature in both the free and bound form.

Extrachromosomal, usually CIRCULAR DNA molecules that are self-replicating and transferable from one organism to another. They are found in a variety of bacterial, archaeal, fungal, algal, and plant species. They are used in GENETIC ENGINEERING as CLONING VECTORS.

The process by which two molecules of the same chemical composition form a condensation product or polymer.

Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment.

Small double-stranded, non-protein coding RNAs (21-31 nucleotides) involved in GENE SILENCING functions, especially RNA INTERFERENCE (RNAi). Endogenously, siRNAs are generated from dsRNAs (RNA, DOUBLE-STRANDED) by the same ribonuclease, Dicer, that generates miRNAs (MICRORNAS). The perfect match of the siRNAs' antisense strand to their target RNAs mediates RNAi by siRNA-guided RNA cleavage. siRNAs fall into different classes including trans-acting siRNA (tasiRNA), repeat-associated RNA (rasiRNA), small-scan RNA (scnRNA), and Piwi protein-interacting RNA (piRNA) and have different specific gene silencing functions.

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)

A ubiquitously expressed family of heterotrimeric GTP-binding protein alpha subunits that signal through interactions with a variety of second messengers as GTPASE-ACTIVATING PROTEINS; GUANINE NUCLEOTIDE EXCHANGE FACTORS; and HEAT SHOCK PROTEINS. The G12-G13 part of the name is also spelled G12/G13.

Female germ cells derived from OOGONIA and termed OOCYTES when they enter MEIOSIS. The primary oocytes begin meiosis but are arrested at the diplotene state until OVULATION at PUBERTY to give rise to haploid secondary oocytes or ova (OVUM).

Nicotine is highly toxic alkaloid. It is the prototypical agonist at nicotinic cholinergic receptors where it dramatically stimulates neurons and ultimately blocks synaptic transmission. Nicotine is also important medically because of its presence in tobacco smoke.

A C19 norditerpenoid alkaloid (DITERPENES) from the root of ACONITUM plants. It activates VOLTAGE-GATED SODIUM CHANNELS. It has been used to induce ARRHYTHMIAS in experimental animals and it has antiinflammatory and antineuralgic properties.

Technique using an instrument system for making, processing, and displaying one or more measurements on individual cells obtained from a cell suspension. Cells are usually stained with one or more fluorescent dyes specific to cell components of interest, e.g., DNA, and fluorescence of each cell is measured as it rapidly transverses the excitation beam (laser or mercury arc lamp). Fluorescence provides a quantitative measure of various biochemical and biophysical properties of the cell, as well as a basis for cell sorting. Other measurable optical parameters include light absorption and light scattering, the latter being applicable to the measurement of cell size, shape, density, granularity, and stain uptake.

The part of CENTRAL NERVOUS SYSTEM that is contained within the skull (CRANIUM). Arising from the NEURAL TUBE, the embryonic brain is comprised of three major parts including PROSENCEPHALON (the forebrain); MESENCEPHALON (the midbrain); and RHOMBENCEPHALON (the hindbrain). The developed brain consists of CEREBRUM; CEREBELLUM; and other structures in the BRAIN STEM.

The characteristic 3-dimensional shape of a carbohydrate.

DNA sequences encoding the alpha chain of the T-cell receptor. The genomic organization of the TcR alpha genes is essentially the same in all species and is similar to the organization of Ig genes.

One of the mechanisms by which CELL DEATH occurs (compare with NECROSIS and AUTOPHAGOCYTOSIS). Apoptosis is the mechanism responsible for the physiological deletion of cells and appears to be intrinsically programmed. It is characterized by distinctive morphologic changes in the nucleus and cytoplasm, chromatin cleavage at regularly spaced sites, and the endonucleolytic cleavage of genomic DNA; (DNA FRAGMENTATION); at internucleosomal sites. This mode of cell death serves as a balance to mitosis in regulating the size of animal tissues and in mediating pathologic processes associated with tumor growth.

Cholestanes substituted in any position with one or more hydroxy groups. They are found in feces and bile. In contrast to bile acids and salts, they are not reabsorbed.

An serine-threonine protein kinase that requires the presence of physiological concentrations of CALCIUM and membrane PHOSPHOLIPIDS. The additional presence of DIACYLGLYCEROLS markedly increases its sensitivity to both calcium and phospholipids. The sensitivity of the enzyme can also be increased by PHORBOL ESTERS and it is believed that protein kinase C is the receptor protein of tumor-promoting phorbol esters.

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 family of DNA-binding transcription factors that contain a basic HELIX-LOOP-HELIX MOTIF.

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.

Test for tissue antigen using either a direct method, by conjugation of antibody with fluorescent dye (FLUORESCENT ANTIBODY TECHNIQUE, DIRECT) or an indirect method, by formation of antigen-antibody complex which is then labeled with fluorescein-conjugated anti-immunoglobulin antibody (FLUORESCENT ANTIBODY TECHNIQUE, INDIRECT). The tissue is then examined by fluorescence microscopy.

The biosynthesis of PEPTIDES and PROTEINS on RIBOSOMES, directed by MESSENGER RNA, via TRANSFER RNA that is charged with standard proteinogenic AMINO ACIDS.

Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).

Any of various enzymatically catalyzed post-translational modifications of PEPTIDES or PROTEINS in the cell of origin. These modifications include carboxylation; HYDROXYLATION; ACETYLATION; PHOSPHORYLATION; METHYLATION; GLYCOSYLATION; ubiquitination; oxidation; proteolysis; and crosslinking and result in changes in molecular weight and electrophoretic motility.

Any of the processes by which nuclear, cytoplasmic, or intercellular factors influence the differential control of gene action in enzyme synthesis.

A family of DNA binding proteins that regulate expression of a variety of GENES during CELL DIFFERENTIATION and APOPTOSIS. Family members contain a highly conserved carboxy-terminal basic HELIX-TURN-HELIX MOTIF involved in dimerization and sequence-specific DNA binding.

A class of saturated compounds consisting of two rings only, having two or more atoms in common, containing at least one hetero atom, and that take the name of an open chain hydrocarbon containing the same total number of atoms. (From Riguady et al., Nomenclature of Organic Chemistry, 1979, p31)

An alpha integrin with a molecular weight of 160-kDa that is found in a variety of cell types. It undergoes posttranslational cleavage into a heavy and a light chain that are connected by disulfide bonds. Integrin alphaV can combine with several different beta subunits to form heterodimers that generally bind to RGD sequence-containing extracellular matrix proteins.

An interleukin receptor subunit with specificity for INTERLEUKIN-13. It dimerizes with the INTERLEUKIN-4 RECEPTOR ALPHA SUBUNIT to form the TYPE II INTERLEUKIN-4 RECEPTOR which has specificity for both INTERLEUKIN-4 and INTERLEUKIN-13. Signaling of this receptor subunit occurs through the interaction of its cytoplasmic domain with JANUS KINASES such as the TYK2 KINASE.

A species of gram-negative, facultatively anaerobic, rod-shaped bacteria (GRAM-NEGATIVE FACULTATIVELY ANAEROBIC RODS) commonly found in the lower part of the intestine of warm-blooded animals. It is usually nonpathogenic, but some strains are known to produce DIARRHEA and pyogenic infections. Pathogenic strains (virotypes) are classified by their specific pathogenic mechanisms such as toxins (ENTEROTOXIGENIC ESCHERICHIA COLI), etc.

T-cell receptors composed of CD3-associated alpha and beta polypeptide chains and expressed primarily in CD4+ or CD8+ T-cells. Unlike immunoglobulins, the alpha-beta T-cell receptors recognize antigens only when presented in association with major histocompatibility (MHC) molecules.

A dsRNA-activated cAMP-independent protein serine/threonine kinase that is induced by interferon. In the presence of dsRNA and ATP, the kinase autophosphorylates on several serine and threonine residues. The phosphorylated enzyme catalyzes the phosphorylation of the alpha subunit of EUKARYOTIC INITIATION FACTOR-2, leading to the inhibition of protein synthesis.

A category of nucleic acid sequences that function as units of heredity and which code for the basic instructions for the development, reproduction, and maintenance of organisms.

Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed.

Differential modulation of the gamma-aminobutyric acid type C receptor by neuroactive steroids. (1/29)

Gamma-aminobutyric acid type C receptor channels (GABA(C)Rs) composed of rho subunits are pharmacologically distinct from GABA(A) receptor channels (GABA(A)Rs). This difference is illustrated by the insensitivity of homo-oligomeric rho(1) receptor channels to many known modulators of GABA(A)Rs, such as barbiturates and benzodiazepines. A number of endogenous metabolites of corticosterone and progesterone, known as neuroactive steroids, compose yet another class of compounds that can modulate GABA(A)Rs. Here, several neuroactive steroids are shown to also modulate the rho(1) receptor channel. 5alpha-Pregnane-3alpha,21-diol-20-one (allotetrahydrodeoxycorticosterone), 5alpha-pregnane-3alpha-ol-11, 20-dione (alphaxalone), and 5alpha-pregnane-3alpha-ol-20-one (allopregnanolone) potentiated the GABA-evoked currents from rho(1) receptor channels and concomitantly altered the deactivation kinetics by prolonging the decay time. In contrast, 5beta-pregnane-3alpha-ol-20-one (pregnanolone), 5beta-pregnane-3, 20-dione (5beta-dihydroprogesterone), and 5beta-pregnane-3alpha, 21-diol-20-one (tetrahydrodeoxycorticosterone), all potentiators of GABA(A)Rs, inhibited the GABA-elicited currents of the rho(1) receptor channel. In comparison to GABA(A)Rs, the modulation of rho(1) receptor channels by these neuroactive compounds occurred with relatively high concentrations of the neuroactive steroids and was more prominent in the presence of low concentrations of GABA, equivalent to fractions of the EC(50) value of the rho(1) receptor channel. Structural comparison of these six neuroactive steroids reveals that the key parameter in determining the mode of modulation for the rho(1) receptor channel is the position of the hydrogen atom bound to the fifth carbon, imposing a trans- or cis-configuration in the backbone structure. This is the first demonstration of isomeric compounds that can differentially modulate the activity of the rho(1) receptor channel. (+info)

Self-augmentation effect of male-specific products on sexually differentiated progesterone metabolism in adult male rat liver microsomes. (2/29)

It is well known that several 3-keto-4-ene steroids such as progesterone and testosterone are metabolized in a gender-specific or -predominant manner by adult rat liver microsomes. In the male, these steroids are primarily metabolized into two oxidized (16alpha-hydroxyl and 6beta-hydroxyl) products mainly by the respective, male-specific cytochrome P450 subforms, CYP2C11 and CYP3A2, while they are primarily metabolized into the 5alpha-reduced products by female-predominant 5alpha-reductase in the female. These sexually differentiated enzyme activities are largely regulated at the transcription level under endocrine control. In the present study, we show that unlabeled 16alpha-hydroxyprogesterone and 6beta-hydroxyprogesterone inhibited the 5alpha-reductive [(3)H]progesterone metabolism by adult male rat liver microsomes without significantly inhibiting the CYP2C11 and CYP3A2 activities producing themselves, whereas 3alpha-hydroxy-5alpha-pregnan-20-one and 5alpha-pregnane-3,20-dione not only stimulated the 5alpha-reductive metabolism producing themselves but also inhibited the male-specific oxidative metabolism. This finding compels us to propose a novel hypothesis that adult male rat liver microsomes may possess a self-augmentation system regulated by the male-specific products on sexually differentiated steroid metabolism, besides regulation by gene expressions of the related enzymes. (+info)

Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. (3/29)

In this report, we compared kinetic constants and products in the reduction of the neurosteroids, 3alpha,5alpha-tetrahydroprogesterone (3alpha,5alpha THP) and 3alpha,5alpha-tetrahydrodeoxycorticosterone (3alpha,5alpha-THDOC), and their precursors, 5alpha-dihydroprogesterone (5alpha-DHP), 5alpha-dihydrodeoxycorticosterone (5alpha-DHDOC) and progesterone, by three isoenzymes (AKR1C1, AKR1C2 and AKR1C3) of human 3alpha-hydroxysteroid dehydrogenase. AKR1C1 efficiently reduced 3alpha,5alpha-THP, 5alpha-DHP and progesterone to their 20alpha-hydroxy metabolites, and slowly converted 5alpha-DHDOC to 3alpha,5alpha-THDOC. AKR1C2 exhibited low 20-ketoreductase activity for 3alpha,5alpha-THP and moderate 3-ketoreductase activity for 5alpha-DHP and 5alpha-DHDOC. 3alpha,5alpha-THDOC was not reduced by the two isoenzymes. No significant activity for the steroids was detected with AKR1C3. The results suggest that AKR1C2 is involved in the neurosteroid synthesis, but AKR1C1 decreases the neurosteroid concentrations in human brain by inactivating 3alpha,5alpha-THP and eliminating the precursors from the synthetic pathways. In addition, we found that the several benzodiazepines inhibited the three isoenzymes noncompetitively with respect to the substrate. Although cloxazolam was a potent and specific inhibitor of AKR1C3, diazepam, estazolam, flunitrazepam, medazepam and nitrazepam, that inhibited AKR1C1 and AKR1C2, may influence the neurosteroid metabolism. (+info)

Branched fatty acids in dairy and beef products markedly enhance alpha-methylacyl-CoA racemase expression in prostate cancer cells in vitro. (4/29)

An enzyme previously identified as alpha-methylacyl-CoA racemase (AMACR) is overexpressed in high-grade prostatic intraepithelial neoplasia and in a majority (60-100%) of prostate cancers (CaPs) as compared with normal and benign hyperplastic lesions of the prostate, where it is minimally expressed. This enzyme is required for the beta-oxidation of branched-chain fatty acids, which include phytanic acid and its alpha-oxidation product, pristanic acid. Interestingly, there is an established correlation between CaP risk and the consumption of dairy and beef products, which also contain marked quantities of these two phytols. In this context, it has also been reported that sex steroids influence lipogenesis through the induction of fatty acid synthase in CaP-derived cell lines and CaP tissues. These findings indicate a potential role for AMACR and the possible influence of sex steroids in both the early development and subsequent progression of CaP. Despite the recent interest in AMACR as a histological marker for CaP, little is known about the regulation of this enzyme and its role in CaP development. To identify potential AMACR-regulating factors, we treated LNCaP cells (an androgen-responsive CaP-derived cell line) and NPrEC cells (a normal prostate basal epithelial cell line) with increasing concentrations of pristanic acid, phytanic acid, 5alpha-dihydrotestosterone, and 17beta-estradiol. Neither the biologically potent androgen 5alpha-dihydrotestosterone nor 17beta-estradiol had any apparent effect on AMACR expression at the protein or transcriptional levels in either cell line. Conversely, pristanic acid and, to a much lesser extent, phytanic acid markedly increased AMACR protein levels selectively in the LNCaP cell line, but not the NPrEC cell line. However, no change was measured at the transcriptional level in either cell line. AMACR is therefore significantly increased at the protein level in CaP cells, through what appears to be the stabilizing effect of the same fatty acids that are present at appreciable concentrations in beef and dairy products, which have been associated with CaP risk. Our findings therefore provide a link between the consumption of dietary fatty acids and the enhanced expression of AMACR, an enzyme that may play an important role in genesis and progression of CaP. (+info)

Androgen inhibition of MAP kinase pathway and Elk-1 activation in proliferating osteoblasts. (5/29)

Non-aromatizable androgens have significant beneficial effects on skeletal homeostasis independently of conversion to estradiol, but the effects of androgens on bone cell metabolism and cell proliferation are still poorly understood. Using an osteoblastic model with enhanced androgen responsiveness, MC3T3-E1 cells stably transfected with androgen receptor (AR) under the control of the type I collagen promoter (colAR-MC3T3), the effects of androgens on mitogenic signaling were characterized. Cultures were treated with the non-aromatizable androgen 5alpha-dihydrotestosterone (DHT) and the effects on osteoblast viability were determined as measured by an MTT assay. A complex response was observed in that continuous short-term DHT treatment enhanced osteoblast viability, but with longer-term DHT treatment inhibition was observed. The inhibition by DHT was prevented by the specific AR antagonist hydroxyflutamide, and was also observed in primary cultures of normal rat calvarial osteoblasts. In order to identify potential mediators of this effect, mitogenic pathway-specific cDNA microarrays were interrogated. Reduced hybridization of several genes important in MAP kinase-mediated signaling was observed, with the most dramatic effect on Elk-1 expression. Analysis of phosphorylation cascades demonstrated that DHT treatment inhibited phosphoERK1/2 levels, MAP kinase activation of Elk-1, Elk-1 protein and phosphoElk-1 levels, and downstream AP-1/luciferase reporter activity. Together, these data provide the first evidence that androgen inhibition of the MAP kinase signaling pathway is a potential mediator of osteoblast growth, and are consistent with the hypothesis that the MAP cascade may be a specific downstream target of DHT. (+info)

Insight into the mechanism of action of neuroactive steroids. (6/29)

Rho(1) receptor-channels (rho(1)Rs) are GABA-gated chloride channels that exhibit slow kinetics, little desensitization, and inert pharmacology to most anesthetics, except for neuroactive steroids (NSs). NSs differentially modulate rho(1)Rs dependent on the steric arrangement of the hydrogen atom at the fifth carbon position. In particular, the NS allotetrahydrodeoxycorticosterone (5alpha-THDOC) potentiates, whereas 5beta-pregnane-3alpha-ol-20-one (pregnanolone) and 5beta-dihydroprogesterone (5beta-DHP) inhibit rho(1) GABA currents. Here, we used Xenopus laevis oocytes expressing rho(1)Rs as a model system to study the mechanism of NS modulation. The second transmembrane residue, Ile307, was mutated to 16 amino acids. Subsequent testing of these mutants with 5alpha- and 5beta-NSs, at equivalent GABA activity, showed the following paradigm. For 5beta-DHP, Ile307 mutation either altered the degree of inhibition or entirely reversed the direction of modulation, rendering 5beta-DHP a potentiator. Dependent on the mutation, pregnanolone remained an inhibitor, transformed into a potentiator, or converted to inhibitor and potentiator based on concentration. The extent of mode reversal for both 5beta compounds showed a correlation with the side-chain hydrophilicity of the 307 residue. In contrast, Ile307 substitutions did not alter the direction of modulation for 5alpha-THDOC but caused a significant increase in the level of potentiation. Paradoxical to their impact on the mode and/or the degree of modulation, none of the mutations altered the concentration range producing the response significantly for any of the above NSs. Moreover, preincubation of Ile307 mutants with 5alpha or 5beta alone produced an equivalent effect on the activation time course. Based on the above data, a universal model is presented wherein anesthetic compounds like NSs can potentiate or inhibit the activity of ligand-gated ion channels distinct from interaction with alternative binding sites. (+info)

Modulation of the firing activity of female dorsal raphe nucleus serotonergic neurons by neuroactive steroids. (7/29)

Important gender differences in mood disorders result in a greater susceptibility for women. Accumulating evidence suggests a reciprocal modulation between the 5-hydroxytryptamine (5-HT) system and neuroactive steroids. Previous data from our laboratory have shown that during pregnancy, the firing activity of 5-HT neurons increases in parallel with progesterone levels. This study was undertaken to evaluate the putative modulation of the 5-HT neuronal firing activity by different neurosteroids. Female rats received i.c.v. for 7 days a dose of 50 micro g/kg per day of one of the following steroids: progesterone, pregnenolone, 5beta-pregnane-3,20-dione (5beta-DHP), 5beta-pregnan-3alpha-ol,20-one, 5beta-pregnan-3beta-ol,20-one, 5alpha-pregnane-3,20-dione, 5alpha-pregnan-3alpha-ol,20-one (allopregnanolone, 3alpha,5alpha-THP), 5alpha-pregnane-3beta-ol,20-one and dehydroepiandrosterone (DHEA). 5beta-DHP and DHEA were also administered for 14 and 21 days (50 micro g/kg per day, i.c.v.) as well as concomitantly with the selective sigma 1 (sigma1) receptor antagonist NE-100. In vivo, extracellular unitary recording of 5-HT neurons performed in the dorsal raphe nucleus of these rats revealed that DHEA, 5beta-DHP and 3alpha,5alpha-THP significantly increased the firing activity of the 5-HT neurons. Interestingly, 5beta-DHP and DHEA showed different time-frames for their effects with 5beta-DHP having its greatest effect after 7 days to return to control values after 21 days, whereas DHEA demonstrated a sustained effect over the 21 day period. NE-100 prevented the effect of DHEA but not of 5beta-DHP, thus indicating that its sigma1 receptors mediate the effect of DHEA but not that of 5beta-DHP. In conclusion, our results offer a cellular basis for potential antidepressant effects of neurosteroids, which may prove important particularly for women with affective disorders. (+info)

Fine tuning of the specificity of an anti-progesterone antibody by first and second sphere residue engineering. (8/29)

The specificity of anti-progesterone P15G12C12G11 antibody was improved by combination of in vitro scanning saturation mutagenesis and error-prone PCR. The most evolved mutant is able to discriminate against 5beta- or 5alpha-dihydroprogesterone, 23 and 15 times better than the starting antibody, while maintaining the affinity for progesterone that remains in the picomolar range. The high level of homology with anti-progesterone monoclonal antibody DB3 allowed the construction of three-dimensional models of P15G12C12G11 based on the structures of DB3 in complex with various steroids. These models together with binding data, derived from site-directed mutagenesis, were used to build a phage library in which five first sphere positions in complementarity-determining regions 2H and 3L were varied. Variants selected by an initial screening in competition against a large excess of 5beta- or 5alpha-dihydroprogesterone were characterized by a convergent amino acid signature different from that of the wild-type antibody and had lower cross-reactivity. Binding properties of this first set of mutants were further improved by the addition of second sphere mutations selected independently from an error-prone library. The three-dimensional models of the best variant show changes in the antigen binding site that explain well the increase in selectivity. The improvements are partly linked to a change in the canonical class of the light chain third hypervariable loop. (+info)

I. C21 steroids: progesterone, 16 alpha-hydroxyprogesterone, 17 alpha-hydroxyprogesterone, 20 alpha-dihydroprogesterone, delta ... I. C21 steroids: progesterone, 16ά-hydroxyprogesterone, 17ά -hydroxy-progesterone, 20ά-dihydroprogesterone, ∆5-pregnenolone, ∆5 ... Nov; 56 (5): 649-655, 1980. Buster JE, Chang RJ, Preston DL, Elashoff RM, Cousins LM, Abraham GE, Hobel CJ, Marshall JR: ... Nov;46 (5): 811-813, 1986. Carson SA, Buster JE: Ectopic pregnancy. N Engl J Med. Oct; 329 (16): 1174-1181, 1993. Buster JE, ...

https://en.wikipedia.org/wiki/John_Buster

20-alpha-dihydroprogesterone MeSH D06.472.334.851.687.750.099 - 5-alpha-dihydroprogesterone MeSH D06.472.334.851.687.750.478 - ... alpha subunit MeSH D06.472.351.576.463 - luteinizing hormone MeSH D06.472.351.576.463.249 - glycoprotein hormones, alpha ... alpha-msh MeSH D06.472.699.631.525.690.583.075 - beta-msh MeSH D06.472.699.631.525.690.583.115 - gamma-msh MeSH D06.472.699.631 ... alpha-msh MeSH D06.472.734.525.690.583.075 - beta-msh MeSH D06.472.734.525.690.583.115 - gamma-msh MeSH D06.472.734.525.883 - ...

https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D06)

20-alpha-dihydroprogesterone MeSH D04.808.745.745.654.829.395 - hydroxyprogesterones MeSH D04.808.745.745.654.829.395.400 - 17- ... MeSH D04.345.051.500 - crown ethers MeSH D04.345.103.222 - alpha-cyclodextrins MeSH D04.345.103.333 - beta-cyclodextrins MeSH ... alpha-hydroxyprogesterone MeSH D04.808.745.745.654.829.614 - medroxyprogesterone MeSH D04.808.745.745.654.829.614.500 - ... medroxyprogesterone 17-acetate MeSH D04.808.745.745.725 - pregnenolone MeSH D04.808.745.745.725.395 - 17-alpha- ...

https://en.wikipedia.org/wiki/List_of_MeSH_codes_(D04)

"PAQR7 - Membrane progestin receptor alpha - Homo sapiens (Human) - PAQR7 gene & protein". www.uniprot.org. Retrieved 2015-10-30 ... "PAQR7 - Membrane progestin receptor alpha - Homo sapiens (Human) - PAQR7 gene & protein". www.uniprot.org. Retrieved 2015-10-27 ... Thomas P (May 2008). "Characteristics of membrane progestin receptor alpha (mPRalpha) and progesterone membrane receptor ... Membrane progesterone receptor alpha (mPRα) is a protein that in humans is encoded by the PAQR7 gene. It is a steroid receptor ...

https://en.wikipedia.org/wiki/Membrane_progesterone_receptor

"Reduction of predator odor-induced anxiety in mice by the neurosteroid 3 alpha-hydroxy-4-pregnen-20-one (3 alpha HP)". Brain ... Unlike 3α-dihydroprogesterone (3α-DHP), 3β-DHP does not act as a positive allosteric modulator of the GABAA receptor, which is ... 3β-Dihydroprogesterone (3β-DHP), also known as 3β-hydroxyprogesterone, or pregn-4-en-3β-ol-20-one (4-pregnenolone, δ4- ... 5α-Dihydroprogesterone 5β-Dihydroprogesterone 3β-Androstanediol Pregnenolone Progesterone 3-acetyl enol ether Quingestrone ...

https://en.wikipedia.org/wiki/3β-Dihydroprogesterone

"Reduction of predator odor-induced anxiety in mice by the neurosteroid 3 alpha-hydroxy-4-pregnen-20-one (3 alpha HP)". Brain ... 3α-Dihydroprogesterone (3α-DHP), also known as 3α-hydroxyprogesterone, as well as pregn-4-en-3α-ol-20-one, is an endogenous ... 3β-Dihydroprogesterone 5α-Dihydroprogesterone 5β-Dihydroprogesterone Pregnanolone Pregnenolone Neurosteroids and Brain Function ... Unlike the case of most other inhibitory neurosteroids, 3α-DHP production is not blocked by 5α-reductase inhibitors like ...

https://en.wikipedia.org/wiki/3α-Dihydroprogesterone

Zander J, Forbes TR, Von Munstermann AM, Neher R (April 1958). "Delta 4-3-Ketopregnene-20 alpha-ol and delta 4-3-ketopregnene- ... 20β-Dihydroprogesterone (20β-DHP), also known as 20β-hydroxyprogesterone (20β-OHP), is an endogenous metabolite of progesterone ... 20α-Dihydroprogesterone 17α-Hydroxyprogesterone 16α-Hydroxyprogesterone 5α-Dihydroprogesterone 11-Deoxycorticosterone Bertram G ...

https://en.wikipedia.org/wiki/20β-Dihydroprogesterone

Zander J, Forbes TR, Von Munstermann AM, Neher R (April 1958). "Delta 4-3-Ketopregnene-20 alpha-ol and delta 4-3-ketopregnene- ... 20α-Dihydroprogesterone (20α-DHP), also known as 20α-hydroxyprogesterone (20α-OHP), is a naturally occurring, endogenous ... Nowak FV (April 2002). "Distribution and metabolism of 20 alpha-hydroxylated progestins in the female rat". J. Steroid Biochem ... 20β-Dihydroprogesterone 17α-Hydroxyprogesterone 16α-Hydroxyprogesterone 5α-Dihydroprogesterone 11-Deoxycorticosterone Beranič N ...

https://en.wikipedia.org/wiki/20α-Dihydroprogesterone

5S,8R,9S,10S,13S,14S,17S)-17-acetyl-10,13-dimethyl-1,2,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-3- ... a model to study the putative role of allopregnanolone and 5alpha-dihydroprogesterone in psychiatric disorders". Brain Res. ... 5α-Dihydroprogesterone (5α-DHP), also known as allopregnanedione,[1] as well as 5α-pregnane-3,20-dione, is an endogenous ... 5α-DHP is an agonist of the progesterone receptor and a positive allosteric modulator of the GABAA receptor (albeit with an ...

https://en.wikipedia.org/wiki/5-alpha-dihydroprogesterone

"Brain 5alpha-dihydroprogesterone and allopregnanolone synthesis in a mouse model of protracted social isolation". Proceedings ... alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines" (pdf). Biological & Pharmaceutical ... 25 (4): 441-5. doi:10.1248/bpb.25.441. PMID 11995921. Akk G, Shu HJ, Wang C, Steinbach JH, Zorumski CF, Covey DF, Mennerick S ( ... 5: 65. doi:10.3389/fphys.2014.00065. ISSN 1664-042X. PMC 3935357. PMID 24616704. Paul, S. M.; Doherty, J. J.; Robichaud, A. J ...

https://en.wikipedia.org/wiki/Neurosteroid

This is in accordance with other 3β-hydroxy steroids, including isopregnanolone, epipregnanolone, 3β-dihydroprogesterone, and 3 ... A positional isomer of androstenol, 3β-androstenol (5α-androst-16-en-3β-ol), is also endogenous to humans (as well as to pigs ... Androstenol, also known as 5α-androst-16-en-3α-ol (shortened to 3α,5α-androstenol or 3α-androstenol), is a steroidal pheromone ... 5 alpha-androst-16-en-3 alpha-ol) is a neurosteroid positive modulator of GABAA receptors". The Journal of Pharmacology and ...

https://en.wikipedia.org/wiki/Androstenol

... alpha -substrate}+NADP+}}} 5α-DHP is a major hormone in circulation of normal cycling and pregnant women. 5α-Reductase is most ... 5alpha-reductase enzyme isoforms I and II reduce progesterone to dihydroprogesterone (DHP) and deoxycorticosterone to ... This exists as a monomer with a seven alpha-helix transmembrane structure housing a hydrophobic pocket that holds cofactor ... Allopregnanolone 3β-Dihydroprogesterone → Isopregnanolone Deoxycorticosterone → 5α-Dihydrodeoxycorticosterone Corticosterone → ...

https://en.wikipedia.org/wiki/5α-Reductase

Ozeki T, Takahashi Y, Nakayama K, Kamataki T (September 2002). "Hepatocyte nuclear factor (HNF)-4 alpha/gamma, HNF-1 alpha, and ... "Hepatocyte nuclear factor-4 alpha/gamma and hepatocyte nuclear factor-1 alpha as causal factors of interindividual difference ... Binstock JM, Iyer RB, Hamby CV, Fried VA, Schwartz IS, Weinstein BI, Southren AL (September 1992). "Human hepatic 3 alpha- ... Khanna M, Qin KN, Cheng KC (June 1995). "Distribution of 3 alpha-hydroxysteroid dehydrogenase in rat brain and molecular ...

https://en.wikipedia.org/wiki/3α-Hydroxysteroid_dehydrogenase

150 (5): 933.e1-933.e7. doi:10.1016/j.ahj.2005.06.005. PMID 16290967.. ... This fear of viral resistance caused a lot of users to be wary of the drug.[5] ... 5] They were the ones who started the process of research and development into protease inhibitors and its relation to the ... 5] Other researchers claim that this study helped determine the future trajectory of the development of the inhibitor. After ...

https://en.wikipedia.org/wiki/Indinavir

91 (5): 1729-34. doi:10.1210/jc.2005-2400. PMID 16507633.. *^ Dietlein M, Wegscheider K, Vaupel R, Schmidt M, Schicha H (2007 ... ISBN 978-0-495-39184-5.. *^ Kendall EC (1915). "The isolation in crystalline form of the compound containing iodin, which ... InChI=1S/C15H11I4NO4/c16-8-4-7(5-9(17)13(8)21)24-14-10(18)1-6(2-11(14)19)3-12(20)15(22)23/h1-2,4-5,12,21H, 3,20H2, (H, 22,23)/ ... 5] Levothyroxine is available as a generic medication.[1] The wholesale cost in the developing world is about 0.58 to 12.28 USD ...

https://en.wikipedia.org/wiki/Levothyroxine

2S,16Z,18E,20S,21S,22R,23R,24R,25S,26S,27S,28E)-5,6,21,23,25-pentahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-( ... 66 (12): 2850-5. doi:10.1093/jac/dkr377. PMID 21948965.. *^ Nelson RL, Suda KJ, Evans CT (March 2017). "Antibiotic treatment ... 4,5-e]pyrido[1,2-a]-benzimida-zole-1,15(2H)-dione,25-acetate ... Alpha-Lipoic acid. *Ambrisentan. *AMI-193. *Amlodipine besylate ... Rifaximin may be used to treat and prevent traveler's diarrhea.[4][5] ...

https://en.wikipedia.org/wiki/Rifaximin

Archived from the original on 5 April 2013. Retrieved 14 April 2013.. ... 5] In the United States, a course of treatment typically costs less than $25.[6] In 2016, it was the 148th most prescribed ... 5,7-8,10-11H2,1-3H3/t12-,14-,15-,17-,19+,20-,21-,22-/m0/s1 Y ... Alpha-Lipoic acid. *Ambrisentan. *AMI-193. *Amlodipine besylate ...

https://en.wikipedia.org/wiki/Solu-Medrol

13 (5): 247-52. doi:10.1097/00008571-200305000-00002. PMID 12724615.. *^ a b Stedman CA, Barclay ML (August 2000). "Review ... 36 (5): 405-413. doi:10.1111/j.1365-2036.2012.05201.x.. *^ Neal, Keith; Logan, Richard (2001). "Potential gastrointestinal ... InChI=1S/C17H19N3O3S/c1-10-8-18-15(11(2)16(10)23-4)9-24(21)17-19-13-6-5-12(22-3)7-14(13)20-17/h5-8H,9H2,1-4H3,(H,19,20) Y ... When omeprazole is stopped, baseline stomach acid secretory activity returns after 3 to 5 days. The inhibitory effect of ...

https://en.wikipedia.org/wiki/Prilosec

114 (5): e84-231. doi:10.1161/CIRCULATIONAHA.106.176857. PMID 16880336.. *^ JA Mohr. (1979). Nafcillin-associated hypokalemia. ... 2S,5R,6R)-6-[(2-ethoxy-1-naphthoyl)amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid ...

https://en.wikipedia.org/wiki/Nafcillin

"Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ... Pregnanes: 3α-Dihydroprogesterone. *3β-Dihydroprogesterone. *5α-Dihydrocorticosterone. *5α-Dihydroprogesterone ... Androstenediol, or 5-androstenediol (abbreviated as A5 or Δ5-diol), also known as androst-5-ene-3β,17β-diol, is an endogenous ... Androstenediol, also known as androst-5-ene-3β,17β-diol, is a naturally occurring androstane steroid.[5] It is closely related ...

https://en.wikipedia.org/wiki/5-Androstenediol

InChI=1S/C21H20Cl2O3/c1-21(2)17(12-18(22)23)19(21)20(24)25-13-14-7-6-10-16(11-14)26-15-8-4-3-5-9-15/h3-12,17,19H,13H2,1-2H3 ... Permethrin was discovered in 1973.[5] It is on the World Health Organization's List of Essential Medicines, the most effective ...

https://en.wikipedia.org/wiki/Permethrin

"Docetaxel serum protein binding with high affinity to alpha 1-acid glycoprotein". Invest New Drugs. 14 (2): 147-51. doi:10.1007 ... 5: 357-65. doi:10.2147/CMAR.S49321. PMC 3798099. PMID 24143122.. *^ a b c d e f g Anonymous. Drugdex Evaluations: Docetaxel. ... 1,7β,10β-trihydroxy-9-oxo-5β,20-epoxytax-11-ene-2α,4,13α-triyl 4-acetate 2-benzoate 13-{(2R,3S)-3-[(tert-butoxycarbonyl)amino]- ... Renal impairment is unlikely to affect metabolism or excretion of docetaxel as renal excretion contributes less than 5% of ...

https://en.wikipedia.org/wiki/Docetaxel

2Z,4S,4aR,5S,5aR,12aS)-2-[amino(hydroxy)methylene]-4-(dimethylamino)-5,10,11,12a-tetrahydroxy-6-methylene-4a,5a,6,12a- ...

https://en.wikipedia.org/wiki/Metacycline

The use of methoxychlor as a pesticide was banned in the United States in 2003[5] and in the European Union in 2002.[6] ... InChI=1S/C16H15Cl3O2/c1-20-13-7-3-11(4-8-13)15(16(17,18)19)12-5-9-14(21-2)10-6-12/h3-10,15H,1-2H3 Y ...

https://en.wikipedia.org/wiki/Methoxychlor

Pregnanes: 3α-Dihydroprogesterone. *3β-Dihydroprogesterone. *5α-Dihydrocorticosterone. *5α-Dihydroprogesterone ... 1-[(3R,5R,8R,9S,10S,13S,14S,17S)-3-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a] ... Eltanolone; 5β-Pregnan-3α-ol-20-one; 3α-Hydroxy-5β-pregnan-20-one; 3α,5β-Tetrahydroprogesterone; 3α,5β-THP; 3α-Hydroxy-5β- ... During pregnancy, pregnanolone and allopregnanolone are involved in sedation and anesthesia of the fetus.[5][6

https://en.wikipedia.org/wiki/Eltanolone

Ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate ... 5] Loratadine is available as a generic medication.[1] The wholesale cost in the developing world is about US$0.01 to 0.06 per ... ISBN 978-0-683-30737-5.. CS1 maint: Uses editors parameter (link) ...

https://en.wikipedia.org/wiki/Alavert

... , also called 5,7-dihydroxyflavone,[1] is a flavone found in honey, propolis, the passion flowers, Passiflora caerulea ... InChI=1S/C15H10O4/c16-10-6-11(17)15-12(18)8-13(19-14(15)7-10)9-4-2-1-3-5-9/h1-8,16-17H Y ... 4 (5): 337-44. doi:10.12980/APJTB.4.2014C1262. PMC 3985046. PMID 25182716.. ...

https://en.wikipedia.org/wiki/Chrysin

Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... doi:10.1007/s00213-005-0210-5. PMID 16292591.. *^ a b c d Samuels BA, Nautiyal KM, Kruegel AC, Levinstein MR, Magalong VM, ... 336 (5): 478-482. doi:10.1007/bf00169302. PMID 3437921.. *^ Oluyomi, AO; Datla, KP; Curzon, G (March 1997). "Effects of the ... 5 December 2011. Retrieved 2 December 2013.. *^ Schruers, K; Griez, E (December 2004). "The effects of tianeptine or paroxetine ...

https://en.wikipedia.org/wiki/Tianeptine

alpha-cypermethrin in the Pesticide Properties DataBase (PPDB). *zeta-cypermethrin in the Pesticide Properties DataBase (PPDB) ... 13 (5): 341-345. doi:10.1002/jat.2550130508. PMID 8258631.. *^ Amer, S.M.; E.I. Aboulela (1985). "Cytogenetic effects of ... It may cause allergic skin reactions in humans.[5] Excessive exposure can cause nausea, headache, muscle weakness, salivation, ...

https://en.wikipedia.org/wiki/Cypermethrin

5] The British group mentions antifungal properties with no mention of HMG-CoA reductase inhibition. ... 4-5,7,10-13H2,1-3H3/t14-,15-,17+,18+,19-,20-,22-/m0/s1 Y ... Alpha-Lipoic acid. *Ambrisentan. *AMI-193. *Amlodipine besylate ...

https://en.wikipedia.org/wiki/Mevastatin

McLean PJ, Farb DH, Russek SJ (Aug 1995). "Mapping of the alpha 4 subunit gene (GABRA4) to human chromosome 4 defines an alpha ... Gamma-aminobutyric acid receptor subunit alpha-4 is a protein that in humans is encoded by the GABRA4 gene.[5][6] ... Mu W, Cheng Q, Yang J, Burt DR (2002). "Alternative splicing of the GABA(A) receptor alpha 4 subunit creates a severely ... Yang W, Drewe JA, Lan NC (1996). "Cloning and characterization of the human GABAA receptor alpha 4 subunit: identification of a ...

https://en.wikipedia.org/wiki/GABRA4

6 (5): a022780. doi:10.1101/cshperspect.a022780. PMC 4852797. PMID 26801895.. *^ Dailey JW, Reith ME, Steidley KR, Milbrandt JC ... doi:10.1016/s0014-2999(97)83041-5. PMID 9218697.. *^ Kawata Y, Okada M, Murakami T, Kamata A, Zhu G, Kaneko S (June 2001). " ... doi:10.15844/pedneurbriefs-10-3-5.. *^ Powell G, Saunders M, Rigby A, Marson AG (December 2016). "Immediate-release versus ... Alpha lipoic acid. *Benfotiamine. *Botulinum toxin A. *Bupropion. *Cannabinoids (e.g., cannabis, dronabinol, nabilone) ...

https://en.wikipedia.org/wiki/Tegretol

GREENBLATT RB (1956). "The progestational activity of 17-alpha-ethinyl-19-nortestosterone". J. Clin. Endocrinol. Metab. 16 (7 ... Progesterone derivatives: 3β-Dihydroprogesterone. *5α-Dihydroprogesterone. *9α-Bromo-11-ketoprogesterone ... 978-1-59745-150-5. .. *^ a b c d e Lara Marks (2010). Sexual Chemistry: A History of the Contraceptive Pill. Yale University ... 5 (6): 435-41. doi:10.2165/00128071-200405060-00008. PMID 15663340.. *^ a b Pochi PE, Strauss JS (1965). "Lack of androgen ...

https://en.wikipedia.org/wiki/Norethindrone

3β-Dihydroprogesterone (pregn-4-en-3β-ol-20-one) is an isomer of pregnenolone in which the C5 double bond has been replaced ... Pregnenolone (P5), or pregn-5-en-3β-ol-20-one, is an endogenous steroid and precursor/metabolic intermediate in the ... Pregnenolone is an allosteric endocannabinoid, as it is a negative allosteric modulator of the CB1 receptor.[4][5] Pregnenolone ... Pregnenolone is also known chemically as pregn-5-en-3β-ol-20-one.[27][28] Like other steroids, it consists of four ...

https://en.wikipedia.org/wiki/Pregnenolone

"Evaluation of ligand selectivity using reporter cell lines stably expressing estrogen receptor alpha or beta". Biochemical ... Pregnanes: 3α-Dihydroprogesterone. *3β-Dihydroprogesterone. *5α-Dihydrocorticosterone. *5α-Dihydroprogesterone ... 978-3-527-33527-5. .. *^ a b c Escande A, Pillon A, Servant N, Cravedi JP, Larrea F, Muhn P, Nicolas JC, Cavaillès V, Balaguer ... 978-0-19-977158-5. .. *^ N. S. Assali (3 September 2013). The Maternal Organism. Elsevier. pp. 341-. ISBN 978-1-4832-6380-9. . ...

https://en.wikipedia.org/wiki/Estriol

Alpha-1 blockers (e.g., prazosin). *Alpha-2 agonists (e.g., clonidine, dexmedetomidine, guanfacine) ... doi:10.1016/S1054-3589(10)58002-5. ISBN 9780123786470. PMID 20655477.. *^ Bowery NG, Hill DR, Hudson AL (1983). " ... Phenibut is a derivative of the inhibitory neurotransmitter GABA.[5] Hence, it is a GABA analogue.[5] Phenibut is specifically ... Phenibut is generally well-tolerated.[6][5] Possible side effects may include sedation, somnolence, nausea, irritability, ...

https://en.wikipedia.org/wiki/Phenibut

GABA is not an alpha amino acid, meaning the amino group is not attached to the alpha carbon. Nor is it incorporated into ... By convention the term "amino acid", when used without a qualifier, refers specifically to an alpha amino acid. ... 5-88. ISBN 978-1498754286. .. *^ a b c Kuriyama K, Sze PY (January 1971). "Blood-brain barrier to H3-γ-aminobutyric acid in ... 58 (5): 317-322. doi:10.2170/physiolsci.rp006208. PMID 18834560.. *^ The Brain, the Nervous System, and Their Diseases [3 ...

https://en.wikipedia.org/wiki/Gamma-Aminobutyric_acid

Retinol (ജീവകം എ) • B vitamins: തയാമിൻ (B1) • Riboflavin (B2) • Niacin (B3) • Pantothenic acid (B5) • Pyridoxine (B6) • Biotin ...

https://ml.wikipedia.org/wiki/ഹൈപെരികം_പെർഫൊറാറ്റം

... brand names Ell-Cranell Alpha, Pantostin) is a topical 5-ARI used to treat pattern hair loss in Europe.[17][18] An extract of ... 16 (5): 4806-12. PMID 19796455.. *^ Chu FM, Sartor O, Gomella L, Rudo T, Somerville MC, Hereghty B, Manyak MJ (2015). "A ... 177 (5): 691-692. doi:10.1001/jamainternmed.2017.0096. PMID 28319227.. *^ Malde S, Cartwright R, Tikkinen KA (January 2018). " ... Substrate + NADPH + H+ → 5α-substrate + NADP+. Beyond being a catalyst in the rate-limiting step in testosterone reduction, 5α- ...

https://en.wikipedia.org/wiki/5α-Reductase_inhibitor

It inhibits production of interleukin (IL)-12, interferon (IFN)-gamma, IFN-alpha, and tumor-necrosis-factor (TNF)-alpha by ... Pregnanes: 3α-Dihydroprogesterone. *3β-Dihydroprogesterone. *5α-Dihydrocorticosterone. *5α-Dihydroprogesterone ... 5. New York: Alan R. Liss. p. 200.. *^ a b c Fairchild SS, Shannon K, Kwan E, Mishell RI (February 1984). "T cell-derived ... 25 (5): 831-66. doi:10.1210/er.2003-0031. PMID 15466942.. *^ van Staaveren, N., Teixeira, D.L., Hanlon, A. and Boyle, L.A. ( ...

https://en.wikipedia.org/wiki/Cortisol

... brand names Ell-Cranell Alpha, Pantostin) is a topical 5-ARI used to treat pattern hair loss in Europe.[17][18] An extract of ... 16 (5): 4806-12. PMID 19796455.. *^ Chu FM, Sartor O, Gomella L, Rudo T, Somerville MC, Hereghty B, Manyak MJ (2015). "A ... 177 (5): 691-692. doi:10.1001/jamainternmed.2017.0096. PMID 28319227.. *^ Locci A, Pinna G (2017). "Neurosteroid biosynthesis ... Substrate + NADPH + H+ → 5α-substrate + NADP+. Beyond being a catalyst in the rate-limiting step in testosterone reduction, 5α- ...

https://en.wikipedia.org/wiki/5-alpha-reductase_inhibitor

Text is available under the Creative Commons Attribution-ShareAlike License; additional terms may apply. By using this site, you agree to the Terms of Use and Privacy Policy. Wikipedia® is a registered trademark of the Wikimedia Foundation, Inc., a non-profit organization ...

https://en.wikipedia.org/wiki/Template:Xenobiotic-sensing_receptor_modulators

... is usually used 5 times daily for 14 days for oral thrush, twice daily for 2 to 8 weeks for skin infections, and ... 5] In 2016 Canesten was one of the biggest selling branded over-the-counter medications sold in Great Britain, with sales of £ ... InChI=1S/C22H17ClN2/c23-21-14-8-7-13-20(21)22(25-16-15-24-17-25,18-9-3-1-4-10-18)19-11-5-2-6-12-19/h1-17H Y ...

https://en.wikipedia.org/wiki/Clotrimazole

Branched fatty acids in dairy and beef products markedly enhance alpha-methylacyl-CoA racemase expression in prostate cancer ... A biologically active 5-alpha-reduced metabolite of plasma PROGESTERONE. It is the immediate precursor of 5-alpha-pregnan-3- ... alpha-ol-20-one (ALLOPREGNANOLONE), a neuroactive steroid that binds with GABA(A) RECEPTOR. ... "5-alpha-Dihydroprogesterone" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH ( ...

https://profiles.umassmed.edu/display/105347

5-alpha-Dihydroprogesterone 566-65-4 Suppliers,provide 5-alpha-Dihydroprogesterone 566-65-4 product and the products related ... 5-alpha-Dihydroprogesterone 566-65-4 Zhejiang J&C Biological Technology Co.,Limited China (Mainland) ... 5-alpha-Dihydroprogesterone CAS NO.566-65-4. FOB Price: USD 10.00-10.00 /Gram Get Latest Price. Min.Order Quantity: 1 Gram. ... Zhejiang J&C Biological Technology Co.,Limited5-alpha-Dihydroprogesterone//www.lookchem.com/300w//2010/0622/566-65-4.jpg ...

https://www.lookchem.com/product_5-alpha-Dihydroprogesterone/2196061.html

https://en.wikipedia.org/wiki/5-alpha-dihydroprogesterone

20-alpha-dihydroprogesterone. A biologically active 20-alpha-reduced metabolite of PROGESTERONE. It is converted from ... 17-alpha-hydroxy-progesterone caproate, Castor Oil (Placebo). Location. Desert Good Samaritan Hospital. Mesa. Arizona. United ... Treatment of Preterm Labor With 17 Alpha-Hydroxyprogesterone Caproate. The goal of our research will be to determine the ... It is not known whether 17-alpha-hydroxyprogesterone caproate (17OHP-C) is effective for preventing preterm delivery with an ...

https://www.bioportfolio.com/resources/trial/65146/Progesterone-17OHP-for-Prolongation-of-Pregnancy-in-Women-With-Preterm-Rupture-of.html

It is converted from progesterone to 20-alpha-hydroxypregn-4-en-3-one by the 20-ALPHA-HYDROXYSTEROID DEHYDROGENASE in the ... A biologically active 20-alpha-reduced metabolite of PROGESTERONE. ... 20-alpha-Dihydroprogesterone. Known as: 20-alpha-Hydroxyprogesterone, Pregn-4-en-3-one, 20-alpha-hydroxy-, 20alpha Hydroxypregn ... The development of a sensitive enzyme-immunoassay for 20 alpha-dihydroprogesterone (20 alpha-DHP) and its use in determining… ( ...

https://www.semanticscholar.org/topic/20-alpha-Dihydroprogesterone/1515082

https://en.wikipedia.org/wiki/20%CE%B1-Dihydroprogesterone

Chemical supplier listed by chemBlink - Shaoyang Kerey Chemicals Co., Ltd.: phone and fax numbers, website URL, online contact form and page 1 of product list.

https://www.chemblink.com/webs/www.kery-pharm.com.htm

... α-dihydroprogesterone (5α-DHP) is a major hormone in the circulation of both normal cycling and pregnant women [31]. 5α- ... 1-5 μM. 5α-R2 has a lower turnover number (. ) and a higher substrate affinity, as indicated by = 0.004-1 μM for T. Under ... Isozymes are different proteins that perform the same function:(a)5α-R1 and 5α-R2,(b)5α-R3,(c)GPSN2 and GPSN2L proteins. ... They detected 5α-R2 only in fetal genital skin. Lunacek et al. [55] studied the expression of 5α-R 1 and 5α-R2 at the mRNA (RT- ...

https://www.hindawi.com/journals/au/2012/530121/

https://en.wikipedia.org/wiki/3%CE%B2-Dihydroprogesterone

20«alpha»-Dihydroprogesterone, MO-TMS. *Formula: C25H43NO2Si ... 20«alpha»-hydroxy-pregn-4-en-3-one, MO-TMS, anti. *20«alpha»- ...

https://webbook.nist.gov/cgi/cbook.cgi?ID=R421948

... pregnanolone and 5 alpha-dihydroprogesterone (5α-DHP). [ Time Frame: Outcome will be assessed at several time points for each ...

https://clinicaltrials.gov/show/NCT00656318

3 alpha, 5 alpha-tetrahydrodesoxycorticosterone, 3 alpha-hydroxy-5 alpha-dihydro-progesterone, 17-hydroxyprogesterone, and 17- ... 5. Azcoitia I, Arevalo MA, De Nicola AF, Garcia-Segura LM. Neuroprotective actions of estradiol revisited. Trends Endocrinol ... Wang JJ, Klein R, Smith W, Klein BE, Tomany S, Mitchell P. Cataract surgery and the 5-years incidence of late-stage age-related ... Aust N Z J Ophthalmol (1997) 25(Suppl 1):S13-5. doi:10.1111/j.1442-9071.1997.tb01745.x ...

https://www.frontiersin.org/articles/10.3389/fendo.2018.00066/full

Betacellulin (BTC), Growth hormone (GH), Growth hormone releasing factor (GHRF), Transforming growth factor alpha (TGF α), ... and 20β-dihydroprogesterone, 5α-pregnan-3β-ol-20-one, 5α-androstene-3β17β-diol, 5α-androstan-3β-ol-17-one, androstenedione, ... Estrogens (Estrone, Estradiol-17β, Estriol and Estrone sulfate), Progesterone, 20 alpha-dihydropregnenolone, 5α androstanedione ... February 21, 2014 at 5:23 pm MST. said: Dr. Cordain is one of my Paleo heros along with Rob Wolfe and Mark Sisson but not to ...

https://thepaleodiet.com/kefir-consumption-ill-founded-at-best/

5alpha-dihydroprogesterone had an ED50 of 2.9 mg/kg against generalized kindled convulsions and an ED50 of 4.3 mg/kg against ... 5alpha-dihydroprogesterone is considerably more potent than progesterone. At low, nonsedative doses, it was effective against ... 5alpha-dihydroprogesterone did not produce sedation 15 min after injection, or at any later time interval. ... The anticonvulsant effects of progesterone and 5alpha-dihydroprogesterone on amygdala-kindled seizures in rats.. Lonsdale D1, ...

https://www.ncbi.nlm.nih.gov/pubmed/14636318?dopt=Abstract

20-alpha-Dihydroprogesterone Medicine & Life Sciences * Angiotensin II Medicine & Life Sciences * Pregnant Women Medicine & ... In seven women who had developed PIH and who had lost their refractoriness to A-II, the infusion of 5α-pregnan-3,20-dione (5α- ... In seven women who had developed PIH and who had lost their refractoriness to A-II, the infusion of 5α-pregnan-3,20-dione (5α- ... In seven women who had developed PIH and who had lost their refractoriness to A-II, the infusion of 5α-pregnan-3,20-dione (5α- ...

https://utsouthwestern.pure.elsevier.com/en/publications/modification-of-vascular-responsiveness-to-angiotensin-ii-in-preg

Gamma-aminobutyric acidA receptors mediate 3 alpha-hydroxy-5 alpha-pregnan-20-one-induced gonadotropin secretion. - PubMed - ... dihydroprogesterone (5α-pregnane-3,20-dione) and 5α-pregnane-17α-ol-3,20-dione, are then readily catalyzed by reductive 3αHSDs ... Dihydroprogesterone and Allo are excellent substrates for the 17α-hydroxylase activity of P450c17, and 17OH-Allo is the most ... dihydroprogesterone (5α-pregnane-3,20-dione) and 5α-pregnane-17α-ol-3,20-dione, are then readily catalyzed by reductive 3αHSDs ...

https://raypeatforum.com/community/threads/5a-dihydroprogesterone-5a-dhp-is-androgen-progesterone-agonist-and-pro-hormone-for-dht.13741/

20beta-dihydroprogesterone (DHP)-promoting activity with associated oocyte maturation. Two-dimensional chromatography ( ... Production of 17 alpha-hydroxy-20 beta-dihydroprogesterone, testosterone, and 17 beta-estradiol by various components of the ... I. Production of 17 alpha-hydroxy,20 beta-dihydroprogesterone, testosterone, and 17 beta-estradiol by prematurational follicles ... 20β-dihydroprogesterone (DHP), testosterone (T), and 17β-estradiol (E2) generated after follicle culture at 25°C for 24 h and ...

https://rbej.biomedcentral.com/articles/10.1186/1477-7827-2-14

5α-dihydroprogesterone concentrations and synthesis in non-pregnant mares. Conley, A. J., Scholtz, E. L., Legacki, E. L., ...

https://ucdavis.pure.elsevier.com/en/persons/benjamin-moeller

Equine 5α-reductase activity and expression in epididymis. C. J. Corbin, E. L. Legacki, B. A. Ball, K. E. Scoggin, Scott D ... Fingerprint Dive into the research topics of Equine 5α-reductase activity and expression in epididymis. Together they form a ...

https://ucdavis.pure.elsevier.com/en/publications/equine-5%CE%B1-reductase-activity-and-expression-in-epididymis/fingerprints/

Use methylene blue, vitamin C, vitamin K2, CoQ10, alpha lipoic acid (ALA), vitamin E, PQQ and succinic acid to promote proper ... I prefer a mixed tocopherol high in alpha-tocopherol, such as wheat germ extract. ... Best 15 must-eat foods to increase DHT for more Alpha Energy ... 5 Tribulus terrestris. Im personally a huge fan of this herb. ... 5α-DHP is twice as effective as progesterone at lowering prolactin, but if you apply the progesterone on the skin, most of it ...

https://men-elite.com/2017/08/30/lower-prolactin-for-men-5-most-effective-strategies-with-supplements/

Caseins in CM (and also in goats milk) are divided into: alphaS1, alphaS2, beta and kappa.2 ... and 20β-dihydroprogesterone, 5α-pregnan-3β-ol-20-one, 5α-androstene-3β17β-diol, 5α-androstan-3β-ol-17-one, androstenedione, ... Hormi K, Lehy T. Developmental expression of transforming growth factor-alpha and epidermal growth factor receptor proteins in ... Betacellulin (BTC), Growth hormone (GH), Growth hormone releasing factor (GHRF), Transforming growth factor alpha (TGF α), ...

https://thepaleodiet.com/tag/dairy/

3 alpha-hydroxysteroid dehydrogenase, 3 alphaHD, 3-alpha-HSD, 3alpha-HSD, 3alpha-HSD/CR, 3alpha-HSOR, 3alpha-hydroxysteroid ... 5alpha-dihydroprogesterone 3alpha-hydroxysteroid oxidoreductase, AKR1C, AKR1C1-4, AKR1C17, AKR1C2, AKR1C3, AKR1C4, AKR1C9, aldo ... 5alpha-dihydroprogesterone 3alpha-hydroxysteroid oxidoreductase, prostaglandin F2alpha-synthase, PT3HSD, sterognost 3alpha ... type 5 17beta-hydroxysteroid dehydrogenase, type I 3alpha-HSD ...

http://www.brenda-enzymes.org/all_enzymes.php?ecno=1.1.1.50&table=Storage_Stability

"Moreover, while less DHT is made, more dihydroprogesterone (DHP; 5a-pregnane-3,20dione) is made. DHP competes with the residual ... Klein, ""Progesterone is the chief inhibitor of an enzyme called 5-alpha reductase. Progesterone inhibits the body from ... 5-AR is the enzyme that converts human serum to testosterone, then into DHT, which is the compound thought to be responsible ... converting testosterone to di-hydrotestosterone (DHT) by binding to 5 alpha reductase; ...

https://hairsite.com/baldness-encyclopedia/progesterone-and-hair-loss/

Dihydroprogesterone. 20-alpha-Dihydroprogesterone. Hydroxypregnenolone. 17-alpha-Hydroxypregnenolone. Prasterone. ... 5,8,11,14,17-Eicosapentaenoic Acid. Eicosapentaenoic Acid. D12 - AMINO ACIDS, PEPTIDES, AND PROTEINS. Mercaptopropionylglycine ...

http://decs2007.bvsalud.org/I/rep_i2004.htm

Dihydroprogesterone. 20-alpha-Dihydroprogesterone. Hydroxypregnenolone. 17-alpha-Hydroxypregnenolone. Prasterone. ...

http://decs2015.bvsalud.org/I/rep_i2004.htm

A biologically active 5-alpha-reduced metabolite of plasma PROGESTERONE. (umassmed.edu)
5α-Dihydroprogesterone ( 5α-DHP ), also known as allopregnanedione , [1] as well as 5α-pregnane-3,20-dione , is an endogenous progestogen and neurosteroid that is synthesized from progesterone . (wikipedia.org)
A biologically active 20-alpha-reduced metabolite of PROGESTERONE. (semanticscholar.org)
Progesterone, 20 alpha-dihydroprogesterone and 20 beta-dihydroprogesterone in mother and child at birth. (semanticscholar.org)
Unlike 3α-dihydroprogesterone (3α-DHP), 3β-DHP does not act as a positive allosteric modulator of the GABAA receptor, which is in accordance with the fact that other 3β-hydroxylated progesterone metabolites such as isopregnanolone and epipregnanolone similarly do not act as potentiators of this receptor and instead inhibit it as well as reverse the effects of potentiators like allopregnanolone. (wikipedia.org)
The anticonvulsant effects of progesterone and 5alpha-dihydroprogesterone on amygdala-kindled seizures in rats. (nih.gov)
The purpose of the present study was to investigate the anticonvulsant actions of progesterone and its primary metabolite 5alpha-dihydroprogesterone in the amygdala kindling model. (nih.gov)
Multiple doses of progesterone and 5alpha-dihydroprogesterone were then tested for anticonvulsant activity against focal electrographic and generalized convulsive kindled seizures. (nih.gov)
5alpha-dihydroprogesterone is considerably more potent than progesterone. (nih.gov)
In this backdoor pathway, progesterone is first acted upon by the enzyme 5-AR and that generates the steroid 5α-Dihydroprogesterone (5α-DHP). (raypeatforum.com)
However, when supplied in sufficient quantities these progesterone metabolites (i.e. 5α-DHP or allopregnanolone) can serve as significant sources of androgen synthesis as apparently they are the preferred raw material (substrate) for some of the androgen-synthesizing enzymes. (raypeatforum.com)
A search into the endocrine pathways that lead from cholesterol through five enzymatic steps to dihydrotestosterone (DHT) revealed that Dr. Darling's hormones (progesterone, 5α-A and 5α-P) were all part of the DHT production pathway ( Fig. 1 ) and so could conceivably be metabolized to DHT right in the pilosebaceous unit, if the necessary enzymes were present. (raypeatforum.com)
According to Dr. Klein, ""Progesterone is the chief inhibitor of an enzyme called 5-alpha reductase. (hairsite.com)
Medroxyprogesterone acetate and dexamethasone, but not progesterone, dose dependently increases alpha-ENaC and sgk1 mRNA in M-1 and in Madin-Darby canine kidney-C7 cells, both collecting duct cell lines. (selleckchem.com)
1986. Microsonal $20{\alpha}$ -atiol and $20{\alpha}$ -hydroxysteroid dehydrogenase activity for progesterone in human placenta. (koreascience.or.kr)
1970. The roles of pregn- 5-ene- $3{\beta}$ , $20{\alpha}$ -atiol and $20{\alpha}$ -hydroxysteroid dehydro-genase in the control of progesterone synthesis preceding parturition and lactogenesis in the rat. (koreascience.or.kr)
[8] Beyond reducing testosterone to dihydrotestosterone, 5alpha-reductase enzyme isoforms I and II reduce progesterone to dihydroprogesterone (DHP) and deoxycorticosterone to dihydrodeoxycorticosterone (DHDOC). (wikidoc.org)
Progesterone and its metabolites 5-dihydroprogesterone and 5-3-tetrahydroprogesterone decrease LPS-induced NO release in the murine microglial cell line, BV-2. (nel.edu)
Müller E, Kerschbaum H. Progesterone and its metabolites 5-dihydroprogesterone and 5-3-tetrahydroprogesterone decrease LPS-induced NO release in the murine microglial cell line, BV-2. (nel.edu)
[7] [8] They include 3β-hydroxy-Δ5 derivatives, such as pregnenolone (PREG) and dehydroepiandrosterone (DHEA), their sulfates, and reduced metabolites such as the tetrahydro derivative of progesterone 3α-hydroxy-5α-pregnane-20-one (3α,5α-THPROG). (wikia.org)
P4 and ALLO also signal through a number of membrane receptors (progesterone receptor membrane component 1, and membrane progesterone receptors (mPRs) alpha, beta, gamma, delta, and epsilon) in the brain that are distinct from Pgr, although the role of these receptors in the normal brain and in the therapeutic response to P4 and ALLO following TBI is unclear. (frontiersin.org)
In contrast to the A ring-reduced metabolites and analogues of progesterone and deoxycorticosterone, glucocorticoids had no effect on muscimol-stimulated 36Cl- uptake in cerebral cortical synaptoneurosomes at concentrations between 20 nM and 5 microM. (muscimol.xyz)
The enzyme 17-beta,10-alpha-hydroxysteroid dehydrogenase may play an important role in increasing the estrogen-progesterone ratio in fetal membranes at the time of parturition. (readabstracts.com)
A study examined the activity of 17-beta,10-alpha-hydroxysteroid dehydrogenase and its affect on the estrogen-progesterone ratio in fetal membranes. (readabstracts.com)
Estradiol is the most potent form of naturally occurring estrogen, and 20-alpha-dihydroprogesterone is a weak form of progesterone. (readabstracts.com)
1975). Progesterone, 20 alpha-dihydroprogesterone and 20 beta-dihydroprogesterone in mother and child at birth. (core.ac.uk)

Brain 5alpha-dihydroprogesterone and allopregnanolone synthesis in a mouse model of protracted social isolation. (semanticscholar.org)
5alpha-dihydroprogesterone had an ED50 of 2.9 mg/kg against generalized kindled convulsions and an ED50 of 4.3 mg/kg against focal afterdischarge 15 min after injection. (nih.gov)
5alpha-dihydroprogesterone did not produce sedation 15 min after injection, or at any later time interval. (nih.gov)
Medroxyprogesterone acetate (MPA) inhibits the enzyme 3-hydroxyste-roid dehydrogenase, involved in the reversible conversion between 5alpha-dihydroprogesterone (DHP) and 3alpha, 5alpha-tetrahydroprogesterone (THP), and therefore may affect the local actions of DHP and THP in the brain. (selleckchem.com)
In addition, ALLO is metabolized to another compound, 5alpha-dihydroprogesterone, which binds Pgr, suggesting ALLO actions may involve signaling through Pgr as well as the aforementioned mechanisms of action. (frontiersin.org)

Despite the discovery of 5 alpha-reduction as an enzymatic step in steroid metabolism in 1951, and the discovery that dihydrotestosterone is more potent than testosterone in 1968, the significance of 5 alpha-reduced steroids in human diseases was not appreciated until the discovery of 5 alpha-reductase type 2 deficiency in 1974. (hindawi.com)
So, given the benefits of androgens and progestogens on health and metabolism 5α-DHP may be unique among steroids (except maybe allopregnanolone) in conferring the benefits of both worlds. (raypeatforum.com)
5α-Reductases act on 3-oxo (3-keto), Δ 4,5 C19/C21 steroids as its substrates. (wikidoc.org)
Outside of dihydrotestosterone, much of the physiological role of 5α-reduced steroids is unknown. (wikidoc.org)
Several of these steroids, including 3 alpha-hydroxy-5 alpha-pregnan-20-one (3 alpha-OH-DHP) and 3 alpha,21-dihydroxy-5 alpha-pregnan-20-one (THDOC), increase the potency of muscimol to stimulate 36Cl- uptake in a concentration-dependent and stereospecific manner. (muscimol.xyz)
Only two steroids were found: 17 alpha,20 beta-dihydroxy-4-pregnen-3-one, the presence of which has already been firmly established, and 17 alpha,20 beta, 21-trihydroxy-4-pregnen-3-one, which has not been previously identified in rainbow trout. (ualg.pt)
The focus of this review is on peripheral anti-nociceptive properties of 5α- and 5β-reduced neuroactive steroids with either selective or combined modulatory action on GABA A and T-type Ca 2+ neurotransmission. (pubmedcentralcanada.ca)

It is the immediate precursor of 5-alpha-pregnan-3-alpha-ol-20-one (ALLOPREGNANOLONE), a neuroactive steroid that binds with GABA(A) RECEPTOR. (umassmed.edu)
The 5α-DHP then gets metabolized into allopregnanolone, and allopreganolon can get converted into androsterone and other androgenic intermediates that serve as precursors to DHT. (raypeatforum.com)
[4] [5] Ganaxolone , an analog of the endogenous neurosteroid allopregnanolone , is under investigation for the treatment of epilepsy. (wikia.org)
If DHT is high, then you don't have to focus on boosting DHT, but maybe rather allopregnanolone through increasing 5-AR type 1. (men-elite.com)

Intracellular T is converted to dihydrotestosterone (DHT), the preferred ligand for androgen receptor (AR) transactivation, by the enzyme 5 alpha-reductase (5 α -R). Upon ligand binding and transactivation, the DHT-AR complex translocates from cytoplasm to nucleus and activates the transcription of certain genes (the androgen receptor-regulated genes, ARRG). (hindawi.com)
A 3-hydroxysteroid dehydrogenase which catalyzes the reversible reduction of the active androgen, DIHYDROTESTOSTERONE to 5 ALPHA-ANDROSTANE-3 ALPHA,17 BETA-DIOL. (bvsalud.org)
Human steroid 5α-reductase 2 (SRD5α2) as a critical integral membrane enzyme in steroid metabolism catalyzes testosterone to dihydrotestosterone. (cdc.gov)
(a ) 5α-reduction reaction of the Δ , double bond of testosterone catalyzed by SRD5α2 to generate dihydrotestosterone (DHT). (cdc.gov)

As such, a steroid such as 5α-DHP may be used to raise DHT levels without incurring the typical risks of negative feedback such as other steroid synthesis inhibition as a compensatory mechanism. (raypeatforum.com)
synthesis of bile (5β-R specifically), which is essential for the digestion of fat and absorption of fat-soluble vitamins. (men-elite.com)

5-AR is the enzyme that converts human serum to testosterone, then into DHT, which is the compound thought to be responsible for damaging hair follicles and an important factor in hair loss. (hairsite.com)
Finasteride is a 5-alpha reductase inhibitor and this blocks the conversion of testosterone to DHT. (men-elite.com)
Structural analysis together with computational and mutagenesis studies reveals molecular mechanisms for the 5α-reduction of testosterone and the finasteride inhibition involving residues E57 and Y91. (cdc.gov)

1981. Purification of $20{\alpha}$ hydroxysteroid oxidoreductase from bovine fetal erythrocytes. (koreascience.or.kr)

The reaction involves a stereospecific and permanent break of the Δ 4,5 with the help of NADPH as a cofactor. (wikidoc.org)

3β-Dihydroprogesterone (3β-DHP), also known as 3β-hydroxyprogesterone, or pregn-4-en-3β-ol-20-one (4-pregnenolone, δ4-pregnenolone), is an endogenous steroid. (wikipedia.org)

Several compounds have been developed to inhibit the 5 alpha-reductase isozymes and they play an important role in the prevention and treatment of many common diseases. (hindawi.com)
This review describes the basic biochemical properties, functions, tissue distribution, chromosomal location, and clinical significance of the 5 alpha-reductase isozyme family. (hindawi.com)
Only one 5 beta-reductase (5 β -R) enzyme has been identified. (hindawi.com)
There are three isoenzymes of 5α-reductase, SRD5A1 , SRD5A2 , and SRD5A3 , which vary in different tissues with age. (wikidoc.org)
[3] [4] There are three isoenzymes of 5α-reductase: steroid 5α-reductase 1, 2, and 3 ( SRD5A1 , SRD5A2 and SRD5A3 ). (wikidoc.org)
The pseudohermaphrodites described in this 1974 study were born with a rare congenital 5 alpha-reductase deficiency . (tophairlosstreatments.com)
Propecia works by inhibiting 5 alpha-reductase activity. (tophairlosstreatments.com)
Finasteride is a competitive inhibitor of 5 alpha-reductase enzyme, and is used for treatment of benign prostatic hyperplasia and androgenetic alopecia. (propeciahelp.com)
Mutations on its gene have been linked to 5α-reductase deficiency and prostate cancer. (cdc.gov)
In particular, 5β-dihydroprogesterone formation by aldo-keto reductase 1D1 appears to play an important role in maintaining uterine quiescence. (nih.gov)

20α-Dihydroprogesterone (20α-DHP), also known as 20α-hydroxyprogesterone (20α-OHP), is a naturally occurring, endogenous progestogen. (wikipedia.org)
But efficient though it is in reducing endogenous DHT, the 5α-P and 5α-A in dairy products provide the prostate's intracrine system with DHT precursors that are already 5α-reduced . (raypeatforum.com)

Three isozymes of 5 α -R are known to exist (5 α -R1-3) [ 7 ] and two other proteins exhibit 5-alpha reducing capabilities, glycoprotein synaptic 2 (GPSN2), and glycoprotein synaptic 2-like (GPSN2L) proteins. (hindawi.com)

Radioimmunoassays, combined with thin-layer chromatography, have been used to test for the presence of 17 alpha,20 beta-dihydroxy-4-pregnen-3-one, 17 alpha,20 beta,21-trihy-droxy-4-pregnen-3-one, and 20 beta-hydroxy-4-pregnen-3-one, and for the presence of their 5-pregnene and 5 alpha-pregnane analogs, in the blood and ovarian incubation media of maturing/ovulating female rainbow trout (Salmo gairdneri). (ualg.pt)

The role of DHT was discovered after the description of 5 α -R2 deficiency in a group of males from the Dominican Republic [ 4 ]. (hindawi.com)

File:Steroidogenesis.svg 5α-reductases , also known as 3-oxo-5α-steroid 4-dehydrogenases , are enzymes involved in steroid metabolism. (wikidoc.org)
Thus, the two substrates of these enzymes are a 3-oxo-5α-steroid and acceptor, whereas its two products are 3-oxo-Δ4-steroid and a reduced acceptor. (wikidoc.org)

Measurement of urinary oestrogens and 20 alpha-dihydroprogesterone during ovarian cycles of black (Diceros bicornis) and white (Ceratotherium simum) rhinoceroses. (semanticscholar.org)
Inhibition of rat ovarian 3 beta-hydroxysteroid dehydrogenase (3 beta-HSD), 17 alpha-hydroxylase and 17,20 lyase by progestins and danazol. (semanticscholar.org)
1990. Participation of ovarian $20{\alpha}$ -hydroxysteroid dehydrogenase in luteotrophic and luteolytic processes during rat pseudopregnancy. (koreascience.or.kr)
1994. Molecular cloning of cDNA for rat ovarian 20 alpha-hydroxysteroid dehydrogenase (HSD1). (koreascience.or.kr)

The blood oxaloacetate, alpha-ketoglutarate, malate and citrate concentrations and citrate excretion with the urine were studied in 86 patients with diabetes mellitus. (statescale.cf)

The studies below, and the attached screenshots, describe the pathways and mechanisms through which 5α-DHP can serve as a quite effective pro-hormone for potent androgens such as DHT, androsterone, androstanedione and androstanediol. (raypeatforum.com)

The presence of a nitro group at position 5 of the furan ring in most of the 2 furylethylenes reported in literature until the 1980's, limited the use of these compounds because the aromatic nitro compounds in general, and nitrofurans in particular, have mutagenic and carcinogenic properties 5-6 . (uninet.edu)
Subsequent studies opened a novel opportunity for these compounds, because it demonstrated that the presence of a nitro group at position 5 of the furan ring is not a necessary condition for the development of the antimicrobial activity of such chemicals 7-8 . (uninet.edu)

20β-Dihydroprogesterone 17α-Hydroxyprogesterone 16α-Hydroxyprogesterone 5α-Dihydroprogesterone 11-Deoxycorticosterone Beranič N, Gobec S, Rižner TL (2011). (wikipedia.org)

5-alpha-Dihydroprogesterone" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (umassmed.edu)

10,000 µM)), with approximately six-fold lower potency relative to its 5β-isomer, 5β-dihydroprogesterone . (wikipedia.org)
DHT has 2-5 times higher binding affinity for AR than T, and 10-fold higher potency of inducing AR signaling than T [ 5 ], which means that their effects are different but complementary [ 6 ]. (hindawi.com)

Anion-exchange and hydrophobic-interaction chromatography (HIC) yielded two distinct peaks of 17beta-estradiol (E 2 )- and 17alpha-hydroxy,20beta-dihydroprogesterone (DHP)-promoting activity with associated oocyte maturation. (biomedcentral.com)
Around this time, its activity resulted in the net production of estradiol and 20-alpha-dihydroprogesterone. (readabstracts.com)

1994. - 5. (kiev.ua)
1994. Identification of a major prolactin-regulated protein as 20 alpha-hydroxysteroid dehydrogenase: coordinate regulation of its activity, protein content, and messenger ribonucleic acid expression. (koreascience.or.kr)

The subjects were kindled to 30 stage 5 seizures and stability tested. (nih.gov)

Expression cloning and characterization of human 17 beta-hydroxysteroid dehydrogenase type 2, a microsomal enzyme possessing 20 alpha-hydroxysteroid dehydrogenase activity. (semanticscholar.org)
The amounts of 17 alpha,20 beta, 21-trihydroxy-4-pregnen-3-one found in vivo and in vitro were, however, only 1-1.5% of those of 17 alpha,20 beta-dihydroxy-4-pregnen-3-one, and therefore seem unlikely to play a significant role in the induction of oocyte final maturation. (ualg.pt)
The activity of 17-beta,10-alpha-hydroxysteroid dehydrogenase changed at the time of parturition. (readabstracts.com)
A study was conducted to determine the role of 5(beta)-dihyhydroprogesterone, acting through the nuclear receptor pregnane X receptor (PXR), in regulating uterine contractility. (readabstracts.com)

In the presence of Streptavidin-coated Alpha Donor beads, biotinylated Corticosterone-BSA complex binds to the Streptavidin-coated Alpha Donor beads. (perkinelmer.com)

Moreover, they are produced, not only by the gonads, but also by other organs ( 3 , 4 ), including the central nervous system (CNS) in which estrogens are thought to exert a neuroprotective role ( 5 , 6 ). (frontiersin.org)

2002. Jana 5(3): 15-24). (thepaleodiet.com)

5α-R2 is expressed in prostate, seminal vesicles, epididymis, liver, and to a lesser extent the scalp and skin. (wikidoc.org)

accumulation of fat in the liver and the progression of fatty liver ( R ). Cortisol antagonist can help reverse some of these effects, which just indicate that 5-AR can prevent fatty liver by deactivating cortisol. (men-elite.com)

The first of these to be introduced was hydroxydione, which is the esterified 21-hydroxy derivative of 5β-pregnanedione. (wikia.org)

In socially isolated mice, 5α-R1 is specifically down-regulated in glutamatergic pyramidal neurons that converge on the amygdala from cortical and hippocampal regions. (wikidoc.org)

5α-R1 is expressed in fetal scalp and nongenital skin of the back, anywhere from 5 to 50 times less than in the adult. (wikidoc.org)
5α-R2 is expressed in fetal prostates similar to adults. (wikidoc.org)
5α-R1 is expressed mainly in the epithelium and 5α-R2 the stroma of the fetal prostate. (wikidoc.org)

Branched fatty acids in dairy and beef products markedly enhance alpha-methylacyl-CoA racemase expression in prostate cancer cells in vitro. (umassmed.edu)
De uheldige kvinner som av en eller annen grunn, har vanskeligheter med å bli gravid naturlig og trenger in vitro fertilisering (IVF) vil også trenge progesteron fra tidspunktet for implantasjon inntil morkaken produserer nok progesteron til å holde på fosteret. (tjenester.org)

Hepatic expression of both 5α-R1 and 2 is immediate, but disappears in the skin and scalp at month 18. (wikidoc.org)
Using existing patient outcome data, we demonstrate a strong correlation between TACE and TGF{alpha} expression in human breast cancers that is predictive of poor prognosis. (unt.edu)

It also has activity towards other 3-alpha-hydroxysteroids and on 9-, 11- and 15- hydroxyprostaglandins. (bvsalud.org)
[2] Medroxyprogesterone acetate (MPA) and dexamethasone dose dependently increases alpha-ENaC promoter-driven luciferase activity in M-1 cells, which is not inhibited by Org31710, indicating that Medroxyprogesterone acetate regulates alpha-ENaC in a PR-independent manner. (selleckchem.com)
Alpha-carotene and gamma-carotene also have a single retinyl group, which give them some vitamin activity. (ffl.org)
Also has 20-alpha-HSD activity. (uniprot.org)

Anatomy22

Organisms12

Diseases3

Chemicals and Drugs141

Analytical, Diagnostic and Therapeutic Techniques and Equipment25

Phenomena and Processes51

Disciplines and Occupations1

Information Science4

Differential modulation of the gamma-aminobutyric acid type C receptor by neuroactive steroids. (1/29)

Self-augmentation effect of male-specific products on sexually differentiated progesterone metabolism in adult male rat liver microsomes. (2/29)

Substrate specificity of human 3(20)alpha-hydroxysteroid dehydrogenase for neurosteroids and its inhibition by benzodiazepines. (3/29)

Branched fatty acids in dairy and beef products markedly enhance alpha-methylacyl-CoA racemase expression in prostate cancer cells in vitro. (4/29)

Androgen inhibition of MAP kinase pathway and Elk-1 activation in proliferating osteoblasts. (5/29)

Insight into the mechanism of action of neuroactive steroids. (6/29)

Modulation of the firing activity of female dorsal raphe nucleus serotonergic neurons by neuroactive steroids. (7/29)

Fine tuning of the specificity of an anti-progesterone antibody by first and second sphere residue engineering. (8/29)

alpha 1-Antitrypsin

Receptors, Adrenergic, alpha

Hypoxia-Inducible Factor 1, alpha Subunit

alpha7 Nicotinic Acetylcholine Receptor

Integrin alpha3beta1

Integrin alpha4

Integrin alpha6

Integrin alpha5beta1

Integrin alpha4beta1

Interleukin-1alpha

Integrin alpha2beta1

Receptors, Adrenergic, alpha-1

Integrin alpha5

Integrin alpha1beta1

Receptors, Adrenergic, alpha-2

Integrin alpha6beta1

Base Sequence

Integrin alpha6beta4

Integrin alpha Chains

Integrins

Integrin alpha1

Alpha Rhythm

Integrin alpha3

alpha 1-Antitrypsin Deficiency

Protein Binding

Molecular Sequence Data

Receptors, Nicotinic

Adrenergic alpha-Agonists

PPAR alpha

Dinoprost

Adrenergic alpha-Antagonists

Recombinant Proteins

Hepatocyte Nuclear Factor 1-alpha

Binding Sites

Transfection

alpha 1-Antichymotrypsin

Transforming Growth Factor alpha

Signal Transduction

Gene Expression Regulation

Kinetics

Transcription Factors

Adrenergic alpha-1 Receptor Antagonists

alpha Karyopherins

Macromolecular Substances

Tumor Necrosis Factor-alpha

Prazosin

6-Ketoprostaglandin F1 alpha

Protein Subunits

Cloning, Molecular

Mice, Inbred C57BL

Dose-Response Relationship, Drug

Mutation

Mice, Knockout

Gene Expression

Transcription, Genetic

GTP-Binding Proteins

Blotting, Western

Protein Structure, Tertiary

Phosphorylation

Amino Acid Sequence

Clonidine

Collagen

Promoter Regions, Genetic

Tumor Cells, Cultured

Yohimbine

Protein Conformation

DNA-Binding Proteins

Recombinant Fusion Proteins

Cattle

Interleukin-1

DNA

Adrenergic alpha-2 Receptor Agonists

Sequence Homology, Amino Acid

Rats, Sprague-Dawley

GTP-Binding Protein alpha Subunits, Gi-Go

Reverse Transcriptase Polymerase Chain Reaction

Electrophoresis, Polyacrylamide Gel

Ligands

Protein Isoforms

Adrenergic alpha-2 Receptor Antagonists