Pawlowski JE, Ertel JR, Allen MP, Xu M, Butler C, Wilson EM, Wierman ME (June 2002). "Liganded androgen receptor interaction ... a nuclear beta-catenin-associated antagonist of the Wnt/Wingless pathway". Nature. 422 (6934): 905-909. Bibcode:2003Natur.422.. ... Androgen receptor, CBY1, CDH1, CDH2, CDH3, CDK5R1, CHUK, CTNND1, CTNNA1, EGFR, Emerin ESR1 FHL2, GSK3B, HER2/neu, HNF4A, IKK2, ... "Functional localization and competition between the androgen receptor and T-cell factor for nuclear beta-catenin: a means for ...

... shows reduced affinity for the androgen receptor relative to normethandrone. Its affinity for the androgen receptor is ... by combined administration of GnRH antagonist and 19-nortestosterone cannot be maintained by this non-aromatizable androgen ... It is also a synthetic AAS and hence is an agonist of the androgen receptor, the biological target of androgens like ... "Towards the mapping of the progesterone and androgen receptors". Journal of Steroid Biochemistry. 27 (1-3): 255-269. doi: ...

... nicotinic acetylcholine receptor antagonist, 5-HT2A receptor antagonist, α1-adrenergic receptor antagonist, weak serotonin ... PDE5 inhibitor and androgen receptor agonist Sildenafil/testosterone - Emotional Brain - AdisInsight TGFK09SD - 5-HT1A receptor ... 5-HT1A receptor partial agonist and androgen receptor agonist Buspirone/testosterone - Emotional Brain - AdisInsight ... selective androgen receptor modulatorOPK 88004 - AdisInsight Testosterone low-dose intranasal (MPP-14, TBS-2, Noseafix, Tefina ...

Other nuclear receptor targets of DHEA besides the androgen and estrogen receptors include the PPARα, PXR, and CAR. However, ... it can actually behave more like an antagonist depending on circulating testosterone and dihydrotestosterone (DHT) levels, and ... Women with complete androgen insensitivity syndrome (CAIS), who have a non-functional androgen receptor (AR) and are immune to ... weak partial agonist of the androgen receptor (AR). However, its intrinsic activity at the receptor is quite weak, and on ...

In addition to the mineralocorticoid receptor, mexrenone also binds to the glucocorticoid, androgen, and progesterone receptors ... A potent mineralocorticoid antagonist with reduced affinity for the 5 alpha-dihydrotestosterone receptor of human and rat ... Hofmann LM, Weier RM, Suleymanov OD, Pedrera HA (June 1977). "Mexrenoate potassium: a steroidal aldosterone antagonist and ... Cutler GB, Sauer MA, Loriaux DL (April 1979). "SC 25152: a potent mineralocorticoid antagonist with decreased antiandrogenic ...

Kolkhof P, Bärfacker L (2017). "30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of ... 7α-TS and 7α-TMS have been found to possess approximately equivalent affinity for the rat ventral prostate androgen receptor ( ... Maron BA, Leopold JA (2008). "Mineralocorticoid receptor antagonists and endothelial function". Curr Opin Investig Drugs. 9 (9 ... Parthasarathy HK, MacDonald TM (2007). "Mineralocorticoid receptor antagonists". Curr. Hypertens. Rep. 9 (1): 45-52. doi: ...

... it is an antagonist of the sigma σ1 receptor, a negative allosteric modulator of nicotinic acetylcholine receptors, and, via ... Progesterone does not interact significantly with the androgen receptor (AR) or with the estrogen receptor (ER). In addition to ... It is also a potent antimineralocorticoid (antagonist of the mineralocorticoid receptor (MR)), as well as a very weak ... Parthasarathy, Saudhamini; Chin, Andrea; Malloy, Virginia; Matias, Jonathan (1988). "In Vitro Androgen Receptor Binding ...

... in the presence of mifepristone via its N and C termini revealing a novel molecular mechanism for androgen receptor antagonists ... Nuclear receptor co-repressor 1 has been shown to interact with: Androgen receptor, CHD1, Calcitriol receptor GPS2, ... "Inhibition of the dihydrotestosterone-activated androgen receptor by nuclear receptor corepressor". Mol. Endocrinol. 16 (7): ... "The androgen receptor recruits nuclear receptor CoRepressor (N-CoR) ...

Kolkhof P, Bärfacker L (2017). "30 YEARS OF THE MINERALOCORTICOID RECEPTOR: Mineralocorticoid receptor antagonists: 60 years of ... 7α-TS and 7α-TMS have been found to possess approximately equivalent affinity for the rat ventral prostate androgen receptor ( ... Maron BA, Leopold JA (2008). "Mineralocorticoid receptor antagonists and endothelial function". Curr Opin Investig Drugs. 9 (9 ... Yang J, Young MJ (2016). "Mineralocorticoid receptor antagonists-pharmacodynamics and pharmacokinetic differences". Curr Opin ...

Prostate cells contain an Androgen Receptor (AR), that when stimulated by androgens like testosterone, promotes growth and ... whereas LHRH antagonists decrease directly the amount of testosterone. LHRH agonists and antagonists used in androgen ... Androgen deprivation therapy (ADT), also called androgen ablation therapy or androgen suppression therapy, is an antihormone ... Prostate cancer cells usually require androgen hormones, such as testosterone, to grow. ADT reduces the levels of androgen ...

... is an androgen receptor (AR) inhibitor and shows strong and specific antiandrogenic activity in vitro (e.g., ... However, its mechanism of action and effects differ from those of conventional antiandrogens; it is not an antagonist of the AR ... Shi Q, Shih CC, Lee KH (2009). "Novel anti-prostate cancer curcumin analogues that enhance androgen receptor degradation ... "New therapeutic approach to suppress castration-resistant prostate cancer using ASC-J9 via targeting androgen receptor in ...

Classes of selective receptor modulators include: Selective androgen receptor modulator (SARM) Selective estrogen receptor ... Hence selective receptor modulators are sometimes referred to as tissue selective drugs or mixed agonists / antagonists. This ... Agonist-antagonist Selective glucocorticoid receptor agonist (SEGRA) Smith CL, O'Malley BW (February 2004). "Coregulator ... In the field of pharmacology, a selective receptor modulator or SRM is a type of drug that has different effects in different ...

"Tip60 and histone deacetylase 1 regulate androgen receptor activity through changes to the acetylation status of the receptor ... characterization of new antagonists". Molecular Pharmacology. 50 (4): 923-30. PMID 8863838. Fu M, Wang C, Reutens AT, Wang J, ... Together with GRM6, GRM7 and GRM8 it belongs to group III of the metabotropic glutamate receptor family. Group III receptors ... "p300 and p300/cAMP-response element-binding protein-associated factor acetylate the androgen receptor at sites governing ...

... including androgen receptors into the nucleus), thus, a potential anti-androgen agent. The transport of viral particles ( ... 4 July 2012). "Orally Bioavailable Tubulin Antagonists for Paclitaxel-Refractory Cancer". Pharmaceutical Research. 29 (11): ... in Men With Metastatic Castration-Resistant Prostate Cancer with Progression on an Androgen Receptor Targeting Agent". Clinical ...

... in Men With Metastatic Castration-Resistant Prostate Cancer with Progression on an Androgen Receptor Targeting Agent". Clinical ... 4 July 2012). "Orally Bioavailable Tubulin Antagonists for Paclitaxel-Refractory Cancer". Pharmaceutical Research. 29 (11): ... and receptor-modulating compounds. Pivotal Phase III trials assess whether a candidate drug has efficacy specifically against a ... binds to the soluble human complement split product C5a after cleavage from C5 to block its interaction with the C5a receptor, ...

Another monoclonal antibody, bimagrumab, works as an antagonist of the ACVR2 and ACVR2B receptors, preventing myostatin and ... YK-11, a selective androgen receptor modulator, is also a myostatin inhibitor. Resistance training reduces myostatin activity ... Reduction of myostatin expression is one of the mechanisms for the effects of androgens in promoting muscle growth. Androgens ... "Exploring the polymorphism of selective androgen receptor modulator YK11". Journal of Molecular Structure. 1273: 134281. doi: ...

... and glucocorticoid receptor (GR), and poor affinity for the estrogen receptor (ER). As an androgen, danazol is described as ... The drug can act as both an agonist and antagonist of the PR depending on the bioassay, indicating that it could be regarded as ... Danazol is described as a possessing high affinity for the androgen receptor (AR), moderate affinity for the progesterone ... Danazol has a complex mechanism of action, and is characterized as a weak androgen and anabolic steroid, a weak progestogen, a ...

In addition to the mineralocorticoid receptor, prorenone also binds to the glucocorticoid, androgen, and progesterone receptors ... September 1987). "Aldosterone antagonists. 2. Synthesis and biological activities of 11,12-dehydropregnane derivatives". ... "Relative inhibitory potency of five mineralocorticoid antagonists on aldosterone biosynthesis in vitro". Biochemical ...

... acting as a weak partial agonist of the androgen receptor. However, due to its lower intrinsic activity in comparison, in the ... August 2004). "Partial agonist/antagonist properties of androstenedione and 4-androsten-3beta,17beta-diol". The Journal of ... Androgens and anabolic steroids, Androstanes, Estrogens, Androgen esters, All stub articles, Steroid stubs, Genito-urinary ... "Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta". ...

Spironolactone is an antagonist of the AR, the biological target of androgens like testosterone and DHT. Its affinity for the ... It works by binding to the AR and displacing androgens like testosterone and DHT from the receptor, thereby reducing its ... Breiner M, Romalo G, Schweikert HU (1986). "Inhibition of androgen receptor binding by drugs in cultured human genital skin ... Breiner M, Romalo G, Schweikert HU (August 1986). "Inhibition of androgen receptor binding by natural and synthetic steroids in ...

Interactions of ZEN and its metabolite with human androgen receptors (hAR) have also been documented. Zearalenone has two major ... exceeding that of well known antagonists such as bisphenol A and DDT. Studies have been performed that strongly suggest a ... Mycoestrogens act as agonists of the estrogen receptors, ERα and ERβ. Mycoestrogens are produced by various strains of fungi, ... Mycoestrogens mimic natural estrogen in the body by acting as estrogen receptor (ER) ligands. Mycoestrogens have been ...

Ghrelin and ghrelin receptor agonist Anabolic catabolic transforming agents such as MT-102 Selective androgen receptor ... Anti-emetics such as 5-HT3 antagonists are also commonly used in cancer cachexia if nausea is a prominent symptom. Anabolic- ... NF-κB is a known regulator of the genes that encode cytokines and cytokine receptors. The increased production of cytokines ... Thalidomide Cytokine antagonists Cannabinoids Omega-3 fatty acids, including eicosapentaenoic acid (EPA) Non-steroidal anti- ...

Androgens and anabolic steroids, Androstanes, GABAA receptor negative allosteric modulators, Glycine receptor antagonists, ... Mo Q, Lu SF, Simon NG (2006). "Dehydroepiandrosterone and its metabolites: differential effects on androgen receptor ... The routine use of DHEA-S and other androgens is discouraged in the treatment of women with low androgen levels due to ... DHEA-S has also been found to inhibit the TRPV1 and TRPC5 transient receptor potential channels and to inhibit the P2X receptor ...

They are synthetic androgens and anabolic steroids and hence are agonists of the androgen receptor (AR), the biological target ... Brueggemeier RW (September 16, 2006). "Sex Hormones (Male): Analogs and Antagonists". In Meyers RA (ed.). Encyclopedia of ... comparison of the binding to the androgen receptors in skeletal muscle and in prostate, as well as to sex hormone-binding ... which has both reduced affinity for the androgen receptor (AR) relative to nandrolone in vitro and weaker AR agonistic potency ...

... form of the nuclear receptor (or possibly antagonist bound receptor). CtBP 602618 SIN3A (associates with class II histone ... Examples include: ARA (androgen receptor associated protein) ARA54 (RNF14) ARA55 (TGFB1I1) ARA70 (NCOA4) AIRE BCAS3 (breast ... Nuclear receptors bind to coactivators in a ligand-dependent manner. A common feature of nuclear receptor coactivators is that ... "Nuclear Receptor Signaling Atlas (Receptors, Coactivators, Corepressors and Ligands)". The NURSA Consortium. Retrieved 2008-02- ...

Androgen receptor antagonist (Ki = 240 nM) Estrogen receptor agonist (Ki > 5 μM; EC50 > 5 μM) Farnesoid X receptor antagonist ( ... Mineralocorticoid receptor antagonist (Ki = 39 nM) Progesterone receptor partial agonist (Ki = 201 nM) Glucocorticoid receptor ... In humans, it acts as an antagonist of the farnesoid X receptor, which was once believed to result in decreased cholesterol ... Pregnane X receptor agonists, Pregnanes, Progestogens, Selective progesterone receptor modulators, Steroidal antiandrogens). ...

... s act as antagonists of the estrogen receptors, ERα and ERβ. The first nonsteroidal antiestrogen was discovered by ... and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues. Estrogen receptors (ER) like ERα ... the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant, aromatase inhibitors (AIs) like ... Amenyogbe E, Chen G, Wang Z, Lu X, Lin M, Lin AY (2020-02-07). "A Review on Sex Steroid Hormone Estrogen Receptors in Mammals ...

... a nuclear protein that interacts with and regulates transcriptional activity of androgen receptor and glucocorticoid receptor ... Dexamethasone and other corticosteroids are agonists, while mifepristone and ketoconazole are antagonists of the GR. Anabolic ... The glucocorticoid receptor (GR or GCR) also known as NR3C1 (nuclear receptor subfamily 3, group C, member 1) is the receptor ... The unbound receptor resides in the cytosol of the cell. After the receptor is bound to glucocorticoid, the receptor- ...

The medication is a synthetic androgen and anabolic steroid and hence is an agonist of the androgen receptor (AR), the ... by combined administration of GnRH antagonist and 19-nortestosterone cannot be maintained by this non-aromatizable androgen ... As such, it is an androgen and anabolic steroid, or an agonist of the AR, the biological target of androgens like testosterone ... Nandrolone esters can be used as a form of androgen replacement therapy for treatment of androgen deficiency in men. However, ...

... for the rat ventral prostate androgen receptor (AR), which is similar to that of spironolactone and its active metabolite 7α- ... A potent mineralocorticoid antagonist with reduced affinity for the 5 alpha-dihydrotestosterone receptor of human and rat ...