Mediates androgen receptor antagonists. Medical search. Frequent questions

Here, we show that (+)-JJ-74-138 is more potent than JJ-450 in the inhibition of androgen-independent AR activity in enzalutamide-resistant LN95 cells. (aacrjournals.org)
Cell lines with experimentally derived AR gene rearrangements displayed high expression of tumor-specific AR-Vs andwere resistant to endocrine therapies, including the AR antagonist enzalutamide. (wustl.edu)
We analyzed here the molecular mechanism of the interaction between the human AR Ligand Binding Domain (hAR-LBD) and two environmental pollutants, linuron (a herbicide) and procymidone (a pesticide), and compared with the steroid agonist dihydrotestosterone (DHT) and well-known hAR antagonists bicalutamide and enzalutamide. (iste.edu.tr)
Reporter assay with MDA-kb2 cells showed that linuron, procymidone, bicalutamide and enzalutamide can inhibit androgen mediated activation of luciferase activity. (iste.edu.tr)
Moreover, recipient cells acquiring mesenchymal traits displayed enhanced migratory and invasive features as well as increased resistance to the androgen receptor antagonist, enzalutamide. (elsevierpure.com)
on androgen synthesis and/or AR signaling such as for example abiraterone and MDV3100/enzalutamide respectively demonstrate medical advantage to CRPC individuals[20-22]. (buyresearchchemicalss.net)

The mechanism by which the androgen receptor (AR) distinguishes between agonist and antagonist ligands is poorly understood. (rcsb.org)
To investigate why subtle structural changes to both the ligand and the receptor (i.e. mutations) result in drastic changes in activity, we studied structure-activity relationships for nonsteroidal AR ligands through crystallography and site-directed mutagenesis, comparing bound conformations of R-bicalutamide, hydroxyflutamide, and two previously reported nonsteroidal androgens, S-1 and R-3. (rcsb.org)
rather, they are synthetic ligands that bind to androgen receptors. (swolverine.com)
Unique interactions of SARM ligands with androgen receptor result in specific conformational change in the androgen receptor protein, recruitment of a unique repertoire of co-regulator proteins thus contributing to their tissue-specific transcriptional regulation of gene expression. (swolverine.com)
Paradoxes exist in that endogenous ligands testosterone (T) and 5α-dihydrotestosterone (DHT) have differential effects on male sexual development while binding to the same receptor and transcriptional specificity is achieved even though the androgen response elements (AREs) are identical to those seen for the progesterone, glucocorticoid and mineralocorticoid receptors. (bvsalud.org)
Despite the growing interest in FXR ligands in drug discovery, little is known with regard to the roles of FXR in mediating or protecting xenobiotic-induced toxicity. (nature.com)
The diversified effects of cannabinoids are now known to be mediated through the activation of G-protein-coupled receptors that are normally bound by a family of endogenous ligands, the endocannabinoids ( 1 ). (aacrjournals.org)
In case you aren't familiar with sarms, they're a class of androgen receptor ligands. (seattlecovenant.org)

Clinically approved AR antagonists compete with dihydrotestosterone (DHT) for binding to the ligand-binding domain (LBD) of AR, and patients eventually develop resistance to these treatments. (aacrjournals.org)
The MoA of KX-826 for treatment of AGA is to locally block the androgen mediated signaling by competing with Dihydrotestosterone (DHT), limit the miniaturization of hair follicles and promote the growth of terminal hairs. (biospace.com)
Dihydrotestosterone (DHT, 5α-dihydrotestosterone, 5α-DHT, androstanolone or stanolone) is an endogenous androgen sex hormone. (mynutritiontipsblog.com)
A decrease in sebum could be achieved by obstructing dihydrotestosterone binding towards the androgen receptor within sebocytes and inhibiting androgen-induced sebocyte proliferation [16, 17]. (bioinbrief.com)
2]The premise of androgen ablationrelies on growth of most prostate carcinomacells being androgen-dependent.The androgen receptor expressedby these cells binds dihydrotestosterone,which is then transported intothe nucleus, leading to a cascade ofevents that induces cellular growth. (cancernetwork.com)
The androgen receptor (AR)[14] can be a ligand-dependent transcription element that upon binding towards the androgen dihydrotestosterone (DHT) goes through Ibuprofen Lysine (NeoProfen) a conformational modification resulting in homodimerization nuclear translocation and upregulation of gene transcription. (buyresearchchemicalss.net)
Antiandrogens bind to androgen receptors and competitively inhibit their interaction with testosterone and dihydrotestosterone. (medscape.com)

Andarine is a partial agonist of the androgen receptor. (mynutritiontipsblog.com)
Relative to testosterone, DHT is considerably more potent as an agonist of the androgen receptor. (mynutritiontipsblog.com)
S-4 is a full androgen receptor agonist in muscle tissue, and a partial agonist in the prostate [ R ]. Thus, S-4 potently stimulates muscle growth, but is unable to maintain prostate size. (mynutritiontipsblog.com)
Studies have shown S-4 is a full androgen receptor agonist in muscle tissue, and a partial agonist in the prostate [ R ], making it an ideal candidate as an alternative to steroidal androgen receptor agonists (i.e., testosterone and DHT), due to associated adverse effects on liver, heart, and fertility. (mynutritiontipsblog.com)
To the end right here we display that coupling a hydrophobic label for an androgen receptor agonist changes it to a powerful Selective Androgen Receptor Degrader (SARD) with the capacity of inducing >50% of AR degradation (DC50) at 1 μM. (buyresearchchemicalss.net)
Furthermore in CRPC the first-generation anti-androgen medicines such as for example bicalutamide[19] and flutamide[18] may screen AR agonist activity. (buyresearchchemicalss.net)
To do this we designed some selective androgen receptor degraders (SARDs) predicated on the high affinity AR agonist RU59063[24] linked via a brief PEG linker for an adamantyl group (Shape 1A) a hydrophobic degron been shown to be effective inside our previous use Halotag fusion proteins. (buyresearchchemicalss.net)
A) Constructions of Selective Androgen Receptor Degraders (SARDs) predicated on the androgen receptor agonist RU59063. (buyresearchchemicalss.net)
SARD-mediated AR degradation needs direct discussion with AR since co-incubation using the competitive AR agonist RU59063 clogged the experience of SARD279 (not really shown). (buyresearchchemicalss.net)

Anti-androgen flutamide suppresses hepatocellular carcinoma cell proliferation via the aryl hydrocarbon receptor mediated induction of transforming growth factor-β1. (oregonstate.edu)
As an anti-androgen and potential inhibitor of sebogenesis, spironolactone SCR7 supplier represents a feasible alternative to dental isotretinoin and mixed dental contraceptives (COCs), the just licensed anti-acne medicines that considerably decrease sebum secretion, but which might be associated with severe adverse effects in a few individuals [20, 21]. (bioinbrief.com)
lt;p>Investigators at the National Institutes of Health (NIH) have discovered compounds that have potential as novel anti-androgen therapeutics. (nih.gov)

Recently, our laboratory discovered selective androgen receptor modulators, which structurally resemble the nonsteroidal AR antagonists bicalutamide and hydroxyflutamide but act as agonists for the androgen receptor in a tissue-selective manner. (rcsb.org)
SARMS or selective androgen receptor modulators are highly bioavailable investigational non-steroidal alternatives to anabolic steroids, made to help mitigate the long-term side effects. (swolverine.com)
In this series, we will be comprehensively discussing individual selective androgen receptor modulators (SARMS), their uses, benefits, and preclinical as well as clinical data. (swolverine.com)
Selective androgen receptor modulators (SARMS) are non-steroidal compounds that promote anabolic and androgenic effects, that bind to selective androgen receptors. (swolverine.com)
The AR is a drug target for selective androgen receptor modulators (SARMS) that either have anabolic or androgenic effects. (bvsalud.org)
One of the most common S-4 (andarine), also known as Gtx-007, is an investigational compound, specifically selective androgen receptor modulator (SARM), originally developed for muscle wasting, osteoporosis, and benign prostatic hypertrophy. (mynutritiontipsblog.com)
S-4, marketed as andarine, is an orally bioavailable, non-steroidal selective androgen receptor modulator (SARM). (mynutritiontipsblog.com)
In spite of the fact that it is often associated to SARMS (selective androgen receptor modulators), it is actually not a SARM (it's not even hormonal). (seattlecovenant.org)
Yk11 is a selective androgen receptor (sarm). (seattlecovenant.org)

Castration of normal male mice induces expansion of the bone marrow B cell population, an effect that can be reversed by androgen replacement. (jci.org)

It is thus in a selective manner, that SARMS modulate or mediate coregulators and transcription factors or signaling cascade proteins to promote anabolic activity. (swolverine.com)
Unlike anabolic steroids which bind to androgen receptors in many tissues all over the body, individual SARMs selectively bind to androgen receptors in certain tissues, but not in others. (swolverine.com)
All SARMS bind to androgen receptors and display tissue-selective activation of androgenic signaling. (swolverine.com)
S-4 like other SARMS were developed in the early 2000s, in an attempt to overcome the pharmacologic and pharmacokinetic limitations of steroidal androgen receptor agonists (i.e., testosterone and DHT), which have known associations with liver and heart disease [ R ]. (mynutritiontipsblog.com)
The development of SARMS for clinical and therapeutic use as an androgen alternative, is promising based on preclinical data. (mynutritiontipsblog.com)
This methodology and study design, effectively allows researchers to investigate how potent and efficacious exogenous androgens and SARMS can be to selectively transcribe and exhibit androgenic and anabolic activity. (mynutritiontipsblog.com)

Novel targeted agents to treat CRPC have been developed that inhibit either androgen receptor (AR)-mediated signaling (AR antagonists and inhibitors of androgen synthesis) or non-AR-mediated signaling (inhibitors of Src, mammalian target of rapamycin, chaperone proteins, insulin-like growth factor-1 receptor, vascular endothelial growth factor, and endothelin-A receptor) pathways. (escholarship.org)
With the goal of finding potential therapeutic compounds that inhibit the FKBP52-mediated activation of AR, several small molecules were tested and found to be antagonists of FKBP52 and to inhibit AR activity in prostate cells. (nih.gov)
2004). Glucocorticoid-mediated GR activation is certainly associated with cancers cell level of resistance in preclinical versions EGT1442 by activating the appearance of genes whose proteins products considerably inhibit chemotherapy-induced apoptosis (Skor et al. (bioxorio.com)

The preservation of sexual desire and function with NSAA monotherapy may be related to testosterone metabolites such as estradiol and the 3α-androstanediol maintaining these functions rather than the androgen receptor or to bicalutamide and other NSAAs possibly incompletely blocking the androgen receptor in the brain. (wikipedia.org)
For instance Ibuprofen Lysine (NeoProfen) androgen deprivation therapy[15] coupled with AR antagonists (we.e. anti-androgens) such as for example bicalutamide[16] continues to be used like a first-line treatment for early stage prostate tumor for many years. (buyresearchchemicalss.net)

The presentation will highlight preclinical data in prostate cancer cell lines that demonstrate the company's glucocorticoid receptor (GR) antagonist, ORIC-101, reversing GR-mediated resistance to an androgen receptor (AR) degrader. (oricpharma.com)
ORIC's lead product candidate, ORIC-101, is a potent and selective small molecule antagonist of the glucocorticoid receptor, which has been linked to resistance to multiple classes of cancer therapeutics across a variety of solid tumors. (oricpharma.com)
the glucocorticoid receptor (GR) another steroid receptor not really identified by the mother or father ligand RU59063 isn't degraded in LNCaP cells under circumstances that bring about near-complete degradation from the androgen receptor. (buyresearchchemicalss.net)
History The glucocorticoid receptor (GR) is certainly expressed in a substantial subset of individual breasts malignancies (Conzen 2008). (bioxorio.com)
Mifepristone is certainly a powerful glucocorticoid receptor (GR) and progesterone receptor (PR) antagonist, and a weakened androgen receptor (AR) antagonist (Tune et al. (bioxorio.com)

Options forandrogen blockade primarily include orchiectomy, luteinizing hormone-releasing agonists and antagonists, and nonsteroidal antiandrogens.There is some controversy regarding combined androgen blockade,intermittent androgen blockade, and the question of whether earlyandrogen blockade is superior to delayed therapy. (cancernetwork.com)
The predomination of an androgen-independent phenotype canoccur approximately 1 to 2 years afterthe initiation of androgen deprivation.Multiple strategies have been usedto induce serum levels of testosteronesimilar to those following castration.Traditional treatment options for androgenblockade include orchiectomy,luteinizing hormone-releasing hormone(LHRH) agonists and antagonists,nonsteroidal antiandrogens, andestrogens. (cancernetwork.com)
Antiandrogens, or androgen receptor (AR) antagonists, include the fungicide vinclozolin, the DDT metabolite p,p′-DDE, certain phthalates (a group of chemicals used to soften polyvinyl chloride plastics), and certain other PCBs. (desdaughter.com)

In addition to many other compounds that have been shown to alter androgen signaling, several environmental pollutants are known to disrupt androgen signaling via binding to androgen receptor (AR) or indirectly affecting the androgen synthesis. (iste.edu.tr)
The systemic ramifications of SCR7 supplier spironolactone on adrenal synthesis of androgen precursors could also contribute to medical effectiveness, although at restorative dosages this can be improbable [18]. (bioinbrief.com)
Some have been shown to act via non-receptor-mediated mechanisms, for example by interfering with hormone synthesis. (desdaughter.com)
Have hcg and classic estrogen receptor antagonist androgen receptor acts as transcription regulatory element by binding to specific DNA response elements in target gene promoters, causing activation or repression of transcription and subsequently protein synthesis. (flourandwaterpizzeria.com)

The most-studied and best known are the environmental estrogens, which mimic estradiol and bind to estrogen receptors (ERs). (desdaughter.com)
Nuclear receptor coactivators associate in a ligand-dependent manner with estrogen receptors (ER) and other nuclear receptors, and they enhance ligand-dependent transcriptional activation. (bioone.org)

Identification of novel androgen receptor (AR) antagonists may lead to urgently needed new treatments for patients with prostate cancer resistant to current AR antagonists. (aacrjournals.org)
Flutamide is an androgen receptor (AR) antagonist approved by the United States Food and Drug Administration for the treatment of prostate cancer. (oregonstate.edu)
AR antagonists are currently used to treat prostate cancer. (rcsb.org)
Castration-resistant prostate cancer (CRPC) is a lethal stage of the disease that emerges when endocrine therapies are no longer effective at suppressing activity of the androgen receptor (AR) transcription factor. (wustl.edu)
Kintor Pharmaceutical Limited is developing and commercializing a robust pipeline of innovative small molecule and biological therapeutics for oncology and androgen-receptor-related disease areas with unmet medical needs, including COVID-19, prostate cancer, alopecia, acne, liver and breast cancers. (biospace.com)
Consequently, prostate weight, semi vesicle weight, and muscle tissue all decline along with androgen levels in parallel. (mynutritiontipsblog.com)
In this study, we assessed the effects of the extracellular vesicles released by these cells on recipient androgen-dependent epithelial VCaP prostate cancer cells. (elsevierpure.com)
Our results suggest a previously unappreciated role for Mes-PCa secreted vesicles in cancer promotion by transferring cell-mediated signals and promoting phenotypic changes in recipient prostate cancer cells. (elsevierpure.com)
In this study, we investigated the growth inhibitory, antiandrogenic, and pro-apoptotic effects of 13 pure compounds found in the pomegranate in androgen-dependent LNCaP human prostate cancer cells. (nih.gov)
These four pomegranate compounds inhibited DHT-stimulated androgen receptor nuclear accumulation and the expression of the androgen receptor-dependent genes prostate specific antigen and steroid 5α-reductase type 1 at concentrations ≥10 μM. (nih.gov)
The immunophilin protein FKBP52 is part of a protein complex that helps fold the androgen receptor (AR) protein, a target for treating prostate cancer, and enhances its activity. (nih.gov)
in androgen-dependent prostate tumor cell lines. (buyresearchchemicalss.net)
These outcomes claim that selective AR degradation could be an effective restorative prostate Ibuprofen Lysine (NeoProfen) tumor technique in the framework of AR mutations that confer level of resistance to third era AR antagonists. (buyresearchchemicalss.net)
While essential for the standard advancement and maintenance of the prostate AR-mediated gene manifestation remains a significant drivers throughout prostate tumor progression. (buyresearchchemicalss.net)

As a whole, these studies provide critical new insight for receptor-based drug design of nonsteroidal AR agonists and antagonists. (rcsb.org)

1991. Effects of polychlorinated biphenyls with Ah receptor affinity on lymphoid development in the thymus and the bursa of Fabricius on chick embryos in ovo and in mouse thymus anlagen in vitro . (cdc.gov)
S-4 has a high androgen receptor (AR) binding affinity. (mynutritiontipsblog.com)
The selective binding effects of S-4, and it high androgen binding affinity, can increase muscle tissue and size. (mynutritiontipsblog.com)
Spironolactone, a artificial 17-lactone steroid, functions as a nonselective mineralocorticoid receptor antagonist with moderate affinity for both progesterone and androgen receptors [15]. (bioinbrief.com)
The various EDCs differ greatly in their potencies relative to natural hormones, and in their affinity for target receptors. (desdaughter.com)

Bipolar T treatment and NTD-antagonists could surmount these resistance mechanisms, respectively. (bvsalud.org)

Protstate cancer is treated with androgen deprivation therapy or by the use of AR antagonists that bind to the LBD. (bvsalud.org)

Androgens are the main physiologic anabolic steroid hormones and normal testosterone levels are necessary for a range of developmental and biological processes, including maintenance of muscle mass. (frontiersin.org)
Moreover, because testosterone (T) can be aromatized into estrogen in the hypothalamus ( Lephart, 1996 ) and because the androgen receptor is not expressed in MNCs, it is conceivable that effects of T could also be mediated through ER-β. (jneurosci.org)
Sixty-day-old Sprague Dawley males were castrated and implanted with SILASTIC capsules containing testosterone (T) or nothing, and osmotic minipumps continuously infusing MK-801, a noncompetitive NMDA receptor antagonist, or saline. (jneurosci.org)
GnRH agonists bind to the GnRH receptors on pituitary gonadotropin-producing cells, causing an initial release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) and consequently a rise in testosterone levels for a few weeks. (medscape.com)
These reproductive glands-the testes in males and the ovaries in females, and, to a lesser extent, the suprarenal (adrenal) glands -secrete androgens (including testosterone) and estrogens. (medscape.com)

The pleiotropic harmful effects of EDCs act through hormone-dependent downstream signaling pathways responsible for gonad development either through direct interaction with steroid hormone receptor or via epigenetic regulation. (intechopen.com)
breasts cancers cells by preventing stress-mediated cell survival pathways that could in any other case counteract chemotherapy-induced apoptosis in tumor cells. (bioxorio.com)
EDCs include a spectrum of substances that can be loosely classified according to their known or suspected activity in relation to sex hormone receptors and pathways. (desdaughter.com)
In particular we are studying the role of eicosanoids in normal pregnancy and preeclampsia, the contribution of a purinergic receptor to the release of the cytokine interleukin-1beta in pregnancy as well as investigation of the inflammasome in coordinating inflammatory pathways coupled to cytokine release. (nottingham.ac.uk)

Furthermore, the antiandrogen through the androgen receptor (AR). (cdc.gov)
Nilutamide is a nonsteroidal antiandrogen that behaves as a competitive antagonist of the androgen receptors and is proposed in the treatment of metastatic prostatic carcinoma. (mcmaster.ca)

Because endogenous chemicals bind and activate FXR, it is important to examine which xenobiotic compounds would disrupt normal receptor function. (nature.com)
Structure-activity relationships of FXR-active compounds revealed by this screening were then compared against the androgen receptor, estrogen receptor α, peroxisome proliferator-activated receptors δ and γ and the vitamin D receptor. (nature.com)
Moreover, FKBP52 is also implicated in the regulation of other hormone receptors so these compounds could be used to treat other hormone-dependent diseases such as diabetes or even used as contraceptives. (nih.gov)
Cannabinoid refers to a group of chemicals naturally found in the marijuana plant Cannabis sativa L. and includes compounds that are either structurally or pharmacologically similar to Δ(9)-tetrahydrocannabinol or those that bind to the cannabinoid receptors. (aacrjournals.org)

ORIC-101 was shown to completely reverse these effects and block tumor cell growth and androgen-regulated gene expression. (oricpharma.com)
Small Indels in the Androgen Receptor Gene: Phenotype Implications and Mechanisms of Mutagenesis. (medscape.com)

In fact, we demonstrated that an antagonist of ER-β prevents estradiol (E 2 ) inhibition of stimulated VP release from explants of the hypothalamo-neurohypophyseal system (HNS) ( Somponpun and Sladek, 2002 ). (jneurosci.org)

Because of the eminent role of receptors for mediating the biological effects of steroid hormones, changes in receptor expression could alter responsiveness of the target cells and determine the physiological circumstances in which gonadal steroids become important regulators of cell function. (jneurosci.org)

Hypothesizing that improved AR amounts may drive the introduction of CRPC and taking into consideration Ibuprofen Lysine (NeoProfen) the medical success from the selective estrogen receptor degrader (SERD) fulvestrant[23] we wanted to induce AR degradation via our hydrophobic tagging strategy. (buyresearchchemicalss.net)

However, the pathophysiological mechanisms underlying this muscle syndrome and its relationship with plasma level of androgens are not completely understood. (frontiersin.org)
Uncovering the mechanisms underlying sexual dimorphism in immunity is essential to understand both infectious and immune-mediated diseases, as well as to better design, optimize and individualize immunomodulatory therapies. (scilifelab.se)
In conclusion, punicic acid, the main constituent of pomegranate seed (70-80%), exhibited potent growth inhibitory activities in androgen-dependent LNCaP cells, which appear to be mediated by both antiandrogenic and pro-apoptotic mechanisms. (nih.gov)
So the two variants shared two distinct 3′-end processing mechanisms: canonical polyadenylation for NEAT1_v1 and RNase P-mediated cleavage for NEAT1_v2. (biomedcentral.com)

One approach that has drawn recent attention is supplementation with androgens, hormones with anabolic properties whose levels naturally decline with age ( 9 - 12 ). (frontiersin.org)
Androgen receptors are ubiquitous in muscle tissue and bone, thus making them highly receptive to activate or be inhibited my anabolic agents, creating undesirable systemic effects. (swolverine.com)

When an animal is castrated, endogenous androgen levels rapidly decline, due to the inability to produce them. (mynutritiontipsblog.com)
These results suggest that androgen affects the size of SNB motoneurons by influencing their expression of the NMDA receptor, and therefore the response of the motoneurons to endogenous glutamate. (jneurosci.org)

The morphology of SNB motoneurons is maintained by testicular androgens secreted in adulthood. (jneurosci.org)

The interaction of these proteoforms in multiprotein complexes with co-activators and co-repressors driven by interdomain coupling mediates the AR transcriptional output. (bvsalud.org)

We employed in vitro cultures and two in vivo models to investigate whether androgens exert these effects directly on marrow lymphoid precursors or whether actions on marrow stromal elements are required. (jci.org)

Interestingly, androgens act elsewhere, primarily on the BC/LA target muscles, to increase dendritic outgrowth of SNB motoneurons, probably via a retrograde axonal signal ( Rand and Breedlove, 1995 ). (jneurosci.org)

The Androgen Receptor (AR) is a ligand (androgen) activated transcription factor and a member of the nuclear receptor (NR) superfamily. (bvsalud.org)

Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)
This transformation was accompanied by a modulation of androgen receptor signaling and activation of TGFβ signaling pathway. (elsevierpure.com)

The stromal cell requirement for androgen-mediated effects was confirmed in vivo by experiments using chimeric animals created by bone marrow transplantation in which androgen receptor expression was restricted to either the stromal or lymphoid cells of the bone marrow. (jci.org)

However, therapeutic effects of nilutamide are overshadowed by the occurrence of several adverse reactions mediated by toxic mechanism(s), which remain(s) poorly investigated. (mcmaster.ca)

Immature B cells from normal mouse bone marrow were not responsive to the suppressive effect of androgens unless they were cocultured with marrow stromal cells or with supernatants from androgen-treated stromal cells, suggesting that the androgen effects are exerted through marrow stromal elements by production of a diffusible mediator. (jci.org)
These experiments suggest that effects of androgens on developing B cells are mediated through androgen receptors in bone marrow stromal cells. (jci.org)
Androgens also exert effects on B cell development in bone marrow. (jci.org)
1994. Ah receptor in embryonic mouse palate and effects of TCDD on receptor expression. (cdc.gov)
Studies targeted at establishing such effects at cellular level and their correlations with in vivo models, will broaden our understanding of the roles played by androgens on skeletal muscle function in elderly. (frontiersin.org)
The concomitant inclusion of the "pure" estrogen antagonist, ICI 182, 780, did not alter the inhibitive effects of HPTE, suggesting that the effects of HPTE are not mediated through the estrogen receptor (ER) pathway. (cdc.gov)
selective antagonism of the NMDA receptor attenuates these effects. (jneurosci.org)
Although anticancer effects of cannabinoids were shown as early as 1975 in Lewis lung carcinoma (ref. 1 and references therein), renewed interest was generated little after the discovery of the cannabinoid system and cloning of the specific cannabinoid receptors ( 1 ). (aacrjournals.org)
Insulin signaling through the insulin receptor increases linear growth through effects on bone and the GH-IGF-1 axis. (medscape.com)

An androgen-independentphenotype can occur by wayof androgen-resistant clones that surviveand proliferate, their growth beingstimulated by mitogenic growthfactors. (cancernetwork.com)
Thus, androgens appear to increase soma size through a direct action on SNB motoneurons where functional androgen receptors are necessary for the response to occur. (jneurosci.org)
Cope with the aches and choose to filter by low price and british dragon (Moderate) Changes in insulin sensitivity or glycemic control may occur in patients treated with androgens. (flourandwaterpizzeria.com)

Immunocytochemistry demonstrated that the decrease in ER-β mRNA was translated into depletion of receptor protein content in hyper-osmotic animals. (jneurosci.org)
G protein-coupled receptors (GPCRs) belong to the largest class of drug targets. (mdpi.com)

The aryl hydrocarbon receptor (AhR) is a ligand-activated transcription factor and a member of the basic helix-loop-helix PER/ARNT/SIM family of chemosensors and developmental regulators. (oregonstate.edu)
AR is a transcription factor (TF) belonging to the nuclear steroid hormone receptor family. (biomedcentral.com)

Anatomy12

Organisms4

Diseases10

Chemicals and Drugs133

Analytical, Diagnostic and Therapeutic Techniques and Equipment13

Psychiatry and Psychology1

Phenomena and Processes20

Disciplines and Occupations1

Information Science2

Health Care1

Enzalutamide6

Ligands8

Dihydrotestosterone7

Agonist9

Anti-androgen3

Selective androgen receptor9

Reversed by androgen replacement1

SARMS6

Inhibit3

Bicalutamide2

Glucocorticoid5

Antiandrogens3

Synthesis4

Estrogen receptors2

Prostate14

Agonists and antagonists1

Affinity5

Resistance1

Deprivation therapy1

Testosterone5

Pathways4

Antiandrogen2

Compounds4

Gene2

Estradiol1

Steroid hormones1

Degrader1

Mechanisms4

Anabolic2

Endogenous2

Testicular1

Transcriptional1

Vitro1

Interestingly1

Nuclear receptor1

Activation2

Lymphoid1

Therapeutic1

Effects9

Occur3

Protein2

Transcription factor2