Androgens
Compounds that interact with ANDROGEN RECEPTORS in target tissues to bring about the effects similar to those of TESTOSTERONE. Depending on the target tissues, androgenic effects can be on SEX DIFFERENTIATION; male reproductive organs, SPERMATOGENESIS; secondary male SEX CHARACTERISTICS; LIBIDO; development of muscle mass, strength, and power.
Receptors, Androgen
Cyproterone Acetate
Dihydrotestosterone
Androgen Receptor Antagonists
Testosterone
A potent androgenic steroid and major product secreted by the LEYDIG CELLS of the TESTIS. Its production is stimulated by LUTEINIZING HORMONE from the PITUITARY GLAND. In turn, testosterone exerts feedback control of the pituitary LH and FSH secretion. Depending on the tissues, testosterone can be further converted to DIHYDROTESTOSTERONE or ESTRADIOL.
Testosterone Congeners
Metribolone
Hormone Antagonists
Androgen-Insensitivity Syndrome
A disorder of sexual development transmitted as an X-linked recessive trait. These patients have a karyotype of 46,XY with end-organ resistance to androgen due to mutations in the androgen receptor (RECEPTORS, ANDROGEN) gene. Severity of the defect in receptor quantity or quality correlates with their phenotypes. In these genetic males, the phenotypic spectrum ranges from those with normal female external genitalia, through those with genital ambiguity as in Reifenstein Syndrome, to that of a normal male with INFERTILITY.
Dopamine Antagonists
Drugs that bind to but do not activate DOPAMINE RECEPTORS, thereby blocking the actions of dopamine or exogenous agonists. Many drugs used in the treatment of psychotic disorders (ANTIPSYCHOTIC AGENTS) are dopamine antagonists, although their therapeutic effects may be due to long-term adjustments of the brain rather than to the acute effects of blocking dopamine receptors. Dopamine antagonists have been used for several other clinical purposes including as ANTIEMETICS, in the treatment of Tourette syndrome, and for hiccup. Dopamine receptor blockade is associated with NEUROLEPTIC MALIGNANT SYNDROME.
Excitatory Amino Acid Antagonists
Neurokinin-1 Receptor Antagonists
Histamine H2 Antagonists
Drugs that selectively bind to but do not activate histamine H2 receptors, thereby blocking the actions of histamine. Their clinically most important action is the inhibition of acid secretion in the treatment of gastrointestinal ulcers. Smooth muscle may also be affected. Some drugs in this class have strong effects in the central nervous system, but these actions are not well understood.
Dose-Response Relationship, Drug
Prostate
Interleukin 1 Receptor Antagonist Protein
Rats, Sprague-Dawley
Muscarinic Antagonists
Drugs that bind to but do not activate MUSCARINIC RECEPTORS, thereby blocking the actions of endogenous ACETYLCHOLINE or exogenous agonists. Muscarinic antagonists have widespread effects including actions on the iris and ciliary muscle of the eye, the heart and blood vessels, secretions of the respiratory tract, GI system, and salivary glands, GI motility, urinary bladder tone, and the central nervous system.
GABA Antagonists
Histamine H1 Antagonists
Drugs that selectively bind to but do not activate histamine H1 receptors, thereby blocking the actions of endogenous histamine. Included here are the classical antihistaminics that antagonize or prevent the action of histamine mainly in immediate hypersensitivity. They act in the bronchi, capillaries, and some other smooth muscles, and are used to prevent or allay motion sickness, seasonal rhinitis, and allergic dermatitis and to induce somnolence. The effects of blocking central nervous system H1 receptors are not as well understood.
Purinergic P1 Receptor Antagonists
Androstenedione
Histamine Antagonists
Nicotinic Antagonists
Neoplasms, Hormone-Dependent
Adenosine A2 Receptor Antagonists
Adrenergic alpha-1 Receptor Antagonists
Purinergic P2 Receptor Antagonists
Nandrolone
Androstane-3,17-diol
Dehydroepiandrosterone
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
Serotonin 5-HT3 Receptor Antagonists
Serotonin 5-HT2 Receptor Antagonists
3-Oxo-5-alpha-Steroid 4-Dehydrogenase
Rats, Wistar
Adenosine A1 Receptor Antagonists
Leukotriene Antagonists
Angiotensin Receptor Antagonists
Estradiol
Signal Transduction
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.
RNA, Messenger
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.
Binding, Competitive
Adrenergic alpha-2 Receptor Antagonists
Gonadotropin-Releasing Hormone
A decapeptide that stimulates the synthesis and secretion of both pituitary gonadotropins, LUTEINIZING HORMONE and FOLLICLE STIMULATING HORMONE. GnRH is produced by neurons in the septum PREOPTIC AREA of the HYPOTHALAMUS and released into the pituitary portal blood, leading to stimulation of GONADOTROPHS in the ANTERIOR PITUITARY GLAND.
Adrenergic Antagonists
GABA-A Receptor Antagonists
Nitriles
Testis
Adrenergic alpha-Antagonists
Cells, Cultured
Estrogen Antagonists
Radioligand Assay
Histamine H3 Antagonists
Ligands
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)
Steroid 17-alpha-Hydroxylase
A microsomal cytochrome P450 enzyme that catalyzes the 17-alpha-hydroxylation of progesterone or pregnenolone and subsequent cleavage of the residual two carbons at C17 in the presence of molecular oxygen and NADPH-FERRIHEMOPROTEIN REDUCTASE. This enzyme, encoded by CYP17 gene, generates precursors for glucocorticoid, androgen, and estrogen synthesis. Defects in CYP17 gene cause congenital adrenal hyperplasia (ADRENAL HYPERPLASIA, CONGENITAL) and abnormal sexual differentiation.
Dehydroepiandrosterone Sulfate
Aromatase
An enzyme that catalyzes the desaturation (aromatization) of the ring A of C19 androgens and converts them to C18 estrogens. In this process, the 19-methyl is removed. This enzyme is membrane-bound, located in the endoplasmic reticulum of estrogen-producing cells of ovaries, placenta, testes, adipose, and brain tissues. Aromatase is encoded by the CYP19 gene, and functions in complex with NADPH-FERRIHEMOPROTEIN REDUCTASE in the cytochrome P-450 system.
Receptors, Serotonin
Estrogens
Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds.
Receptors, Endothelin
Cholestenone 5 alpha-Reductase
Adrenergic beta-2 Receptor Antagonists
Receptors, N-Methyl-D-Aspartate
A class of ionotropic glutamate receptors characterized by affinity for N-methyl-D-aspartate. NMDA receptors have an allosteric binding site for glycine which must be occupied for the channel to open efficiently and a site within the channel itself to which magnesium ions bind in a voltage-dependent manner. The positive voltage dependence of channel conductance and the high permeability of the conducting channel to calcium ions (as well as to monovalent cations) are important in excitotoxicity and neuronal plasticity.
The effects of androgens and antiandrogens on hormone-responsive human breast cancer in long-term tissue culture. (1/1203)
We have examined five human breast cancer cell lines in continuous tissue culture for androgen responsiveness. One of these cell lines shows a 2- to 4-fold stimulation of thymidine incorporation into DNA, apparent as early as 10 hr following androgen addition to cells incubated in serum-free medium. This stimulation is accompanied by an acceleration in cell replication. Antiandrogens [cyproterone acetate (6-chloro-17alpha-acetate-1,2alpha-methylene-4,6-pregnadiene-3,20-dione) and R2956 (17beta-hydroxy-2,2,17alpha-trimethoxyestra-4,9,11-triene-1-one)] inhibit both protein and DNA synthesis below control levels and block androgen-mediated stimulation. Prolonged incubation (greater than 72 hr) in antiandrogen is lethal. The MCF- cell line contains high-affinity receptors for androgenic steroids demonstrable by sucrose density gradients and competitive protein binding analysis. By cross-competition studies, androgen receptors are distinguishable from estrogen receptors also found in this cell line. Concentrations of steroid that saturate androgen receptor sites in vitro are about 1000 times lower than concentrations that maximally stimulate the cells. Changes in quantity and affinity of androgen binding to intact cells at 37 degrees as compared with usual binding techniques using cytosol preparation at 0 degrees do not explain this difference between dissociation of binding and effect. However, this difference can be explained by conversion of [3H]-5alpha-dihydrotestosterone to 5alpha-androstanediol and more polar metabolites at 37 degrees. An examination of incubation media, cytoplasmic extracts and crude nuclear pellets reveals probable conversion of [3H]testosterone to [3H]-5alpha-dihydrotestosterone. Our data provide compelling evidence that some human breast cancer, at least in vitro, may be androgen dependent. (+info)Pharmacokinetics of flutamide in patients with renal insufficiency. (2/1203)
AIMS: The aim of this study was to determine the pharmacokinetic parameters of flutamide, a nonsteroidal antiandrogenic compound, and its pharmacologically active metabolite, hydroxyflutamide, in renal insufficiency. Haemodialysis (HD) clearance of flutamide and hydroxyflutamide was also determined. METHODS: Pharmacokinetic parameters were assessed for flutamide and hydroxyflutamide in 26 male subjects with normal renal function (creatinine clearance by 24 h urine collection, CLcr, greater than 80 ml min(-1) 1.73 m(-2); n=6) or reduced renal function; CLcr=50-80 (n=7), 30-49 (n=3), 5-29 (n=4), and <5 ml min(-1) 1.73 m(-2)-HD (n=6), following a single, oral 250 mg flutamide dose. Subjects undergoing HD received a second 250 mg dose of flutamide 4 h prior to HD; blood and dialysate were collected during HD to determine dialysability of flutamide and hydroxyflutamide. RESULTS: Cmax, tmax, AUC, t1/2, and renal clearance of flutamide and hydroxyflutamide did not differ between groups. Less than 1% of the dose appeared in dialysate as hydroxyflutamide. No serious adverse events were observed. CONCLUSIONS: Renal function did not affect flutamide nor hydroxyflutamide disposition. HD did not alter hydroxyflutamide pharmacokinetics. Dosing adjustments for renal impairment or HD are not indicated for flutamide. (+info)Androgen-independent induction of prostate-specific antigen gene expression via cross-talk between the androgen receptor and protein kinase A signal transduction pathways. (3/1203)
Transcription of the prostate-specific antigen (PSA) gene escapes regulation by androgens in advanced prostate cancer. To determine the molecular mechanism(s) of androgen-independent regulation of the PSA gene, the possibility that the androgen receptor (AR) is activated in the absence of androgen by stimulation of protein kinase A (PKA) was investigated. Activation of PKA by forskolin resulted in elevated expression of the PSA gene in androgen-depleted LNCaP cells, an effect that was blocked by the antiandrogen, bicalutamide. Further evidence that induction of PSA gene expression was dependent on AR was obtained from experiments using PC3 cells devoid of AR. Neither PSA, PB, nor ARR3 androgen-responsive reporters could be induced by activation of PKA in the absence of transfected AR. In addition, when nuclear AR from forskolin-treated LNCaP cells was incubated with oligonucleotides encoding an androgen response element of the PSA promoter and examined by electromobility shift assay, an increase in AR-androgen response element complex formation was observed. Lastly, cotransfection of an expression vector for a chimeric protein encoding the amino-terminal domain of the human AR linked to Gal4 and a 5xGal4UAS reporter gene construct resulted in activation of the amino-terminal domain of the AR by stimulation of PKA activity. These results demonstrate androgen-independent induction of PSA gene expression in prostate cancer cells by an AR-dependent pathway. (+info)Does androgen insufficiency cause lacrimal gland inflammation and aqueous tear deficiency? (4/1203)
PURPOSE: The current investigators have shown that androgen treatment suppresses inflammation and stimulates the function of lacrimal glands in mouse models of Sjogren's syndrome. Recently, others have hypothesized that androgen insufficiency induces an autoimmune process in lacrimal tissue, leading to inflammation, a Sjogren's syndrome-like pathology, and aqueous tear deficiency. The purpose of the present study was to test this hypothesis. METHODS: Lacrimal glands were obtained from adult testicular feminized (Tfm) and control mice; castrated rats, guinea pigs, and rabbits; and castrated rats without anterior or whole pituitary glands and were processed for histology and image analysis. Tear volumes were measured in mice, in patients taking antiandrogen medications, and in age-matched human control subjects. RESULTS: Tfm mice, which are completely resistant to classical androgen action, did not have increased lymphocyte infiltration in their lacrimal glands or decreased tear volumes. No inflammation was evident in lacrimal tissues of male or female rats, guinea pigs, or rabbits 12 to 31 days after castration, no inflammation existed in rat lacrimal glands 15 to 31 days after orchiectomy and pituitary removal, and no aqueous tear deficiency was apparent in patients receiving antiandrogen therapy. CONCLUSIONS: Androgen deficiency may promote the progression of Sjogren's syndrome and its associated lacrimal gland inflammation, meibomian gland dysfunction, and severe dry eye. However, androgen insufficiency alone does not cause lacrimal gland inflammation, a Sjogren's syndrome-like pathology in lacrimal tissue, or aqueous tear deficiency in nonautoimmune animals and humans. (+info)From HER2/Neu signal cascade to androgen receptor and its coactivators: a novel pathway by induction of androgen target genes through MAP kinase in prostate cancer cells. (5/1203)
Overexpression of the HER2/Neu protooncogene has been linked to the progression of breast cancer. Here we demonstrate that the growth of prostate cancer LNCaP cells can also be increased by the stable transfection of HER2/Neu. Using AG879, a HER2/Neu inhibitor, and PD98059, a MAP kinase inhibitor, as well as MAP kinase phosphatase-1 (MPK-1), in the transfection assay, we found that HER2/Neu could induce prostate-specific antigen (PSA), a marker for the progression of prostate cancer, through the MAP kinase pathway at a low androgen level. Reporter assays and mammalian two-hybrid assays further suggest this HER2/Neu-induced androgen receptor (AR) transactivation may function through the promotion of interaction between AR and AR coactivators, such as ARA70. Furthermore, we found this HER2/Neu --> MAP kinase --> AR-ARAs --> PSA pathway could not be blocked completely by hydroxyflutamide, an antiandrogen used in the treatment of prostate cancer. Together, these data provide a novel pathway from HER2/Neu to AR transactivation, and they may represent one of the reasons for the PSA re-elevation and hormone resistance during androgen ablation therapy in prostate cancer patients. (+info)Differentially expressed genes in hormone refractory prostate cancer: association with chromosomal regions involved with genetic aberrations. (6/1203)
Differential gene expression between the androgen sensitive human prostate cancer cell line LNCaP and an insensitive clonal variant, LNCaP-r, was demonstrated by suppression subtractive hybridization. Twenty-one sequences were identified of which 9 are homologous to known genes, 11 are represented by expressed sequence tags (ESTs), and 1 is novel. We present data for 5 of 7 sequences confirmed to be differentially expressed by Northern blot analysis and semiquantitative RT-PCR. Only one gene, fibronectin (FN), was highly overexpressed (>60-fold) in LNCaP-r cells, consistent with previously reported overexpression of FN in prostate cancer. Four sequences were down-regulated in LNCaP-r cells, including an inactive variant of the E2 ubiquitin conjugating enzyme (UEV-1), a novel metalloproteinase-related collagenase (PM5), and a potential tumor suppressor gene (breast basic conserved gene, BBC1). UEV-1 is multifunctional, regulates the cell cycle via cdk1, has homology to MMS2 and likewise functions as a DNA protection protein, and also has homology to TSG101. Aberrant splice variants of TSG101 occur frequently in both breast and prostate cancer, but its mechanism of action is unknown. FN, BBC1, and UEV-1 localize to regions of chromosomal aberration (2q3.4, 16q24.3, and 20q13.2, respectively) associated with advanced prostate cancer and thus may be highly relevant to disease progression. (+info)Overexpression of the cyclin-dependent kinase inhibitor p16 is associated with tumor recurrence in human prostate cancer. (7/1203)
The INK4A gene maps to the 9p21 region and was initially described [M. Serrano et al., Nature (Lond.), 366: 704-707, 1993; A. Kamb et al., Science (Washington DC), 264: 436-440, 1994] as encoding a 148-amino-acid protein termed p16. The p16 protein associates exclusively with Cdk4 and Cdk6, inhibiting their complexation with D-type cyclins and the consequent phosphorylation of pRb. This contributes to cell cycle arrest. The purpose of the present study was to evaluate patterns of p16 expression in a well-characterized cohort of prostatic adenocarcinomas while exploring potential associations between alterations of p16 and clinicopathological variables. Normal and malignant tissues from 88 patients with prostate carcinoma were examined. In situ hybridization and immunohistochemistry assays were used to determine the status of the INK4A exon 1alpha transcripts and levels of p16 protein, respectively. Associations between altered patterns of expression and clinicopathological variables, including pretreatment prostate-specific antigen (PSA) level, Gleason grade, pathological stage, and hormonal status, were evaluated using the Mantel-Haenszel chi2 test. Biochemical (PSA) relapse after surgery was evaluated using the Kaplan-Meier method and the log-rank test. Levels of p16 expression and INK4A exon 1alpha transcripts in normal prostate and benign hyperplastic tissues were undetectable. However, p16 nuclear overexpression was observed in 38 (43%) prostate carcinomas, whereas the remaining 50 (57%) cases showed undetectable p16 levels. Overexpression of p16 protein was found to correlate with increased INK4A exon 1alpha transcripts. Moreover, p16 overexpression was associated with a higher pretreatment PSA level (P = 0.018), the use of neoadjuvant androgen ablation (P = 0.001), and a sooner time to PSA relapse after radical prostatectomy (P = 0.002). These data suggest that p16 overexpression is associated with tumor recurrence and a poor clinical course in patients with prostate cancer. (+info)Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. (8/1203)
The role of androgen receptor (AR) mutations in androgen-independent prostate cancer (PCa) was determined by examining AR transcripts and genes from a large series of bone marrow metastases. Mutations were found in 5 of 16 patients who received combined androgen blockade with the AR antagonist flutamide, and these mutant ARs were strongly stimulated by flutamide. In contrast, the single mutant AR found among 17 patients treated with androgen ablation monotherapy was not flutamide stimulated. Patients with flutamide-stimulated AR mutations responded to subsequent treatment with bicalutamide, an AR antagonist that blocks the mutant ARs. These findings demonstrate that AR mutations occur in response to strong selective pressure from flutamide treatment. (+info)
Risk assessment among prostate cancer patients receiving primary androgen deprivation therapy<...
Intermittent or Continuous Androgen Suppression Produces Comparable Survival after Radical Therapy in Prostate Cancer - The...
Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer - Full Text View -...
Radiation Therapy With or Without Androgen-Deprivation Therapy in Treating Patients With Prostate Cancer - Full Text View -...
Intermittent androgen deprivation therapy appears viable for advanced prostate cancer | Urology Times
Bone mineral density in Nigerian men on androgen deprivation therapy for advanced prostate cancer | African Journal of Urology ...
Impact of androgen deprivation therapy on cardiovascular disease and diabetes
Combined androgen blockade achieved better oncological outcome in androgen deprivation therapy for prostate cancer: Analysis of...
Androgen-deprivation therapy in prostate cancer: A European expert panel review<...
Long-term follow-up comparing salvage radiation therapy and androgen-deprivation therapy for biochemical recurrence after...
Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus Flare...
Bone-Protecting Agents Shown to Reduce Fracture Rate in Men With Metastatic Prostate Cancer - The ASCO Post
Primary androgen deprivation therapy ineffective for most men with early prost... ( WASHINGTON A study of more than 150...)
Positive and negative mood in men with advanced prostate cancer undergoing androgen deprivation therapy: Considering the role...
Undertreatment of Men in Their Seventies with High-risk Nonmetastatic Prostate Cancer
For patients with localized prostate cancer, androgen deprivation therapy may be harmful - ONA
Purpose Principal androgen-deprivation therapy (PADT) is usually often used to take - Cisplatin Induced Nephrotoxicity in Mice
Thromboembolic Risk With Androgen Deprivation Therapy in Prostate Cancer | EDIZIONI SCRIPTA MANENT PLANET
The risk of prostate cancer mortality and cardiovascular mortality of nonmetastatic prostate cancer patients: A population...
Introduction Treatment of metastatic prostate cancer with androgen deprivation therapy (ADT) is effective, but can be...
Androgen deprivation therapy remains to be a critical element of treatment - Cisplatin Induced Nephrotoxicity in Mice
2 Information about enzalutamide | Enzalutamide for hormone-relapsed non-metastatic prostate cancer | Guidance | NICE
Phase I trial of tremelimumab in combination with short-term androgen deprivation in patients with PSA-recurrent prostate...
Understanding why thinking skills may change after Androgen Deprivation Therapy for prostate cancer. | Prostate Cancer UK
A Prospective Randomised Phase III Study of Androgen Deprivation Therapy (+/- Docetaxel) With or Without Local Radiotherapy...
Link Found Between Androgen Deprivation Therapy and Alzheimers Disease in Men with Prostate Cancer | ISSM Professionals
Aging | Androgen deprivation therapy increases brain ageing - Figure
Immune Responses Enhanced and Sustained When PROVENGE® (sipuleucel-T) is Given After Androgen Deprivation Therapy in...
Mushroom-supplemented soybean extract shows therapeutic promise for advanced prostate cancer
OPUS Würzburg | Search
OPUS Würzburg | Search
Higher Rates of Osteoporosis in Prostate Cancer Patients Using ADT | Imaging Technology News
Next Generation Androgen Deprivation Therapy | Grand Rounds in Urology
Adding Docetaxel to Androgen-Deprivation Therapy in Newly Diagnosed Metastatic Prostate Cancer | Gotoper.com
A Phase 1/2 Trial of Brief Androgen Suppression and Stereotactic Radiation Therapy (FASTR) for High-Risk Prostate Cancer ...
Zoledronate in Preventing Osteoporosis and Bone Fractures in Patients With Locally Advanced Nonmetastatic Prostate Cancer...
A Randomized, Double-Blind, Multicentre, Phase II Controlled Trial Assessing Zactima (Vandetanib) Against Placebo in Prolonging...
Multimodal therapy for locally advanced prostate cancer: the roles of radiotherapy, androgen deprivation therapy, and their...
Serum Lipids prior to Starting Androgen Deprivation Therapy and Risk of Castration Resistant Prostate Cancer and Metastasis:...
Risk factors of PSA progression and overall survival in patients with localized and locally advanced prostate cancer treated...
The Prevalence of Cardiac Risk Factors in Men with Localized Prostate Cancer Undergoing Androgen Deprivation Therapy in British...
Exercise medicine to arrest bone loss in men with prostate cancer undergoing androgen deprivation therapy: a 12-month...
Bone mass behavior after 1 year of different treatment strategies in prostate cancer patients subjected to androgen deprivation...
Plus it
Clinical Trial: Metformin In Patients Initiating Adt As Prevention And Intervention Of Metabolic Syndrome - Healthcare /...
ADT Plus Combination Therapy Improves Outcomes in Metastatic Prostate Cancer | Journal Of Clinical Pathways
Evaluation of Insulin-like Growth Factor Receptor 1 Inhibition as a Tr by Cale Fahrenholtz
How prostate cancer is diagnosed. Large print | Prostate Cancer UK
The Central Role of Radiation in Prolonging Survival for High-Risk Prostate Cancer | Gotoper.com
The Impact of Definitive Local Therapy for Lymph Node-Positive Prostate Cancer: A Population-Based Study (Journal Article) |...
Radiation Oncology Associates
Medical Students Share Original Research Study Results at Forum - Jacobs School of Medicine and Biomedical Sciences -...
Plus it
androgen deprivation therapy Archives | Prostate Cancer News Today
Early effects of androgen deprivation on bone and mineral homeostasis in adult men: a prospective cohort study in: European...
Safety and Efficacy Study of Hypofractionated Radiotherapy and Androgen Deprivation Therapy for Prostate Cancer
Functions of autophagy in lipid homeostasis and survival in androgen-d by Ramesh Kaini
Novel trifluoromethylated enobosarm analogues with potent antiandrogenic activity in vitro and tissue selectivity in vivo -ORCA
ADT May Reduce Survival in African American Men With Favorable-risk Prostate Cancer - ONA
U.S. FDA approves darolutamide, a new treatment for men with non-metastatic castration-resistant prostate cancer - Bayer News
Supplements - Prostate Cancer Canada Network - Toronto
Clinical and genomic insights into circulating tumor DNA-based alterations across the spectrum of metastatic hormone-sensitive...
Investigational approaches for the treatment of advanced prostate cancer
Abiraterone Added to ADT and Docetaxel Prolongs PFS in De Novo mCSPC
Moffitt researchers work to determine why some prostate cancer patients experience more hot flashes | EurekAlert! Science News
Updated Results of the SPARTAN Study Show 25 Percent Reduction in the Risk of Death in Patients with Non-Metastatic Castration...
A Randomized Phase III Study of Neo-Adjuvant Docetaxel and Androgen Deprivation Prior to Radical Prostatectomy Versus Immediate...
Hormone Therapy Offered Intermittently For Prostate Cancer Substandard To Continuous Therapy
Exosomes and Exosomal MicroRNAs in Prostate Cancer Radiation Therapy | Exosome RNA
Browse | JNCCN
Should docetaxel be standard of care for patients with metastatic hormone-sensitive prostate cancer? Pro and contra | Klinikai...
Norfolk and Norwich University Hospitals NHS Foundation Trust » Reducing the side effects of prostate hormone therapy with...
Buy Cheap Flutamide - Purchase Flutamide Tablet
Flutamide Cheap Price - Buy Flutamide Online Europe
Androgenic suppression combined with radiotherapy for the treatment of prostate adenocarcinoma: a systematic review | BMC...
XTANDI® (enzalutamide) Demonstrates Significant Improvement in Overall Survival in Phase 3 PROSPER Trial of Patients with nmCRPC
Group-based exercise in daily clinical practice to improve physical fitness in men with prostate cancer undergoing androgen...
Prostate Cancer Patients Improve Bone Health with Osteoporosis Drugs by Dr David Samadi
Efficacy of Local Treatment in Prostate Cancer Patients with Clinically Pelvic Lymph Node-positive Disease at Initial Diagnosis.
Plus it
Newswise
Antiandrogen
... s, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like ... N-Terminal domain antagonists[edit]. N-Terminal domain AR antagonists are a new type of AR antagonist that, unlike all ... Androgen antagonists; Androgen blockers; Testosterone blockers. Use. • Men and boys: Prostate cancer; Benign prostatic ... Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3 ...
Clascoterone
... is an antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such as ... Clascoterone is a steroidal antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such ... Lerner LJ (1975). "Androgen antagonists". Pharmacol Ther B. 1 (2): 217-31. doi:10.1016/0306-039x(75)90006-9. PMID 772705. "Drug ... is an Androgen Receptor Antagonist in Dermal Papilla Cells In Vitro". J Drugs Dermatol. 18 (2): 197-201. PMID 30811143. Rosette ...
11α-Hydroxyprogesterone
Tindall, D.J.; Chang, C.H.; Lobl, T.J.; Cunningham, G.R. (1984). "Androgen antagonists in androgen target tissues". ... Lerner, Leonard J. (1975). "Androgen antagonists". Pharmacology & Therapeutics B. 1 (2): 217-231. doi:10.1016/0306-039X(75) ... It was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, and ...
Benorterone
... is an antiandrogen, or an antagonist of the androgen receptor (AR), the biological target of the androgen sex ... ISBN 978-3-642-80859-3. Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues ... Thus we are left with CPA as the only anti-androgen that is already on the market in several countries. J. Elks (14 November ... ISBN 978-0-87489-225-3. Limited clinical experience also exists with benorterone, the first anti-androgen tried in man, and ...
RU-22930
"Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3): 367-400. doi:10.1016/0163-7258(84)90010-x. PMID ... It is a selective antagonist of the androgen receptor and consequently has progonadotropic effects by increasing gonadotropin ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... Thomson, D. S. (1989). "Pharmacology of Anti-androgens in the Skin". Pharmacology of the Skin II. Handbook of Experimental ...
RU-59063
Ran F, Xing H, Liu Y, Zhang D, Li P, Zhao G (2015). "Recent Developments in Androgen Receptor Antagonists". Archiv der ... RU-59063 is a nonsteroidal androgen or selective androgen receptor modulator (SARM) which was first described in 1994 and was ... RU-59063 has high affinity for the human androgen receptor (AR) (Ki = 2.2 nM; Ka = 5.4 nM) and 1,000-fold selectivity for the ... Liu B, Su L, Geng J, Liu J, Zhao G (2010). "Developments in nonsteroidal antiandrogens targeting the androgen receptor". ...
Nonsteroidal antiandrogen
They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... An over-the-counter histamine H2 receptor antagonist that also shows very weak activity as an AR antagonist. Also inhibits ...
Side effects of cyproterone acetate
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... In addition, although CPA reduces androgen production in the gonads, it can increase the production of adrenal androgens, in ... The use of CPA in men has been associated with cellulite, which has been attributed to androgen deficiency as well. CPA has ... Similar depressive changes have been observed with castration, and may be a consequence of androgen deprivation in men. In ...
Steroidal antiandrogen
They are typically antagonists of the androgen receptor (AR) and act both by blocking the effects of androgens like ... Specifically acts as an AR antagonist, weak antigonadotropin, and weak steroidogenesis inhibitor. Used for androgen-dependent ... There are many different androgen blockers used for transition care. Spironolactone, an aldosterone receptor antagonist, is ... ISBN 978-1-60761-471-5. Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure- ...
RU-57073
"Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr. Med. Chem. 7 (2): 211-47. doi:10.2174/ ... It shows 163% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone ... synthesis and biological profile of high-affinity ligands for the androgen receptor". J. Steroid Biochem. Mol. Biol. 48 (1): ...
Azasteroid
321-. ISBN 978-1-901865-55-4. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...
AA560
Similarly to flutamide, AA560 is a selective antagonist of the androgen receptor (AR) and consequently shows progonadotropic ... Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ...
Pharmacology of cyproterone acetate
CPA is a potent competitive antagonist of the androgen receptor (AR), the biological target of androgens such as testosterone ... It has been said that in combined androgen blockade regimens with castration and CPA as the AR antagonist for prostate cancer, ... Androgens: Pharmacodynamics and antagonists. Biochemical and biological studies with 4-aza-steroidal 5 alpha-reductase ... ISBN 978-1-4496-8695-6. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...
Feminizing hormone therapy
Antiandrogens that directly block the androgen receptor are known as androgen receptor antagonists or blockers, while ... nonsteroidal antiandrogens are highly selective for the androgen receptor and act as pure androgen receptor antagonists. ... It works as an antiandrogen mainly by acting as an androgen receptor antagonist. The medication is also a weak steroidogenesis ... In addition to its actions as an antigonadotropin, cyproterone acetate is an androgen receptor antagonist. However, this action ...
Metribolone
Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Ojasoo T, Delettré J, Mornon JP, Turpin-VanDycke C, Raynaud JP (1987). "Towards the mapping of the progesterone and androgen ... ISBN 978-1-4831-4566-2. R-2956 [41-43], a dimethyl derivative of an extremely potent androgen, R 1881 [44], is a powerful ... Takeda AN, Pinon GM, Bens M, Fagart J, Rafestin-Oblin ME, Vandewalle A (2007). "The synthetic androgen methyltrienolone (r1881 ...
Nilutamide
... acts as a selective antagonist of the androgen receptor (AR), preventing the effects of androgens like testosterone ... Nilutamide acts as a selective competitive silent antagonist of the AR (IC50 = 412 nM), which prevents androgens like ... Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... 11-. ISBN 978-981-256-920-2. Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists ( ...
RU-56187
The medication is a silent antagonist of the androgen receptor. RU-56187 is 3- to 10-fold more potent as an antiandrogen than ... RU-57073 RU-58642 RU-59063 Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Distinguishing androgen receptor agonists and antagonists: distinct mechanisms of activation by medroxyprogesterone acetate and ... It shows 92% of the affinity of testosterone for the androgen receptor and negligible affinity for other steroid hormone ...
Comparison of bicalutamide with other antiandrogens
Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ... ISBN 978-1-60327-829-4. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ... "Androgen receptor antagonists for prostate cancer therapy". Endocrine-Related Cancer. 21 (4): T105-18. doi:10.1530/ERC-13-0545 ...
Hydroxyflutamide
Kemppainen JA, Wilson EM (July 1996). "Agonist and antagonist activities of hydroxyflutamide and Casodex relate to androgen ... Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... a steroidal androgen receptor antagonist". J. Steroid Biochem. 33 (6): 1133-8. doi:10.1016/0022-4731(89)90420-2. PMID 2615358. ... Differential effects on high-androgen responder and low-androgen responder muscle groups". Endocrinology. 154 (12): 4594-606. ...
Bicalutamide
Masiello D, Cheng S, Bubley GJ, Lu ML, Balk SP (July 2002). "Bicalutamide functions as an androgen receptor antagonist by ... Kawahara T, Minamoto H (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical Immunology, ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... It works by blocking the androgen receptor (AR), the biological target of the androgen sex hormones testosterone and ...
Cyproterone acetate
53-. ISBN 978-3-642-88429-0. Jost A (1971). "Use of androgen antagonists and antiandrogens in studies on sex differentiation". ... Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... These conditions are worsened by the presence of androgens, and by suppressing androgen levels and blocking their actions, CPA ... Chemical Control of Androgen Action. Annual Reports in Medicinal Chemistry. 21. pp. 179-188. doi:10.1016/S0065-7743(08)61128-8 ...
Delanterone
ISBN 978-3-527-30247-5. Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): ...
Seborrhoeic dermatitis
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... Eunuchs, owing to their low androgen levels and small sebaceous glands, do not develop seborrheic dermatitis. In addition to ... Zouboulis, Christos C.; Degitz, Klaus (2004). "Androgen action on human skin - from basic research to clinical significance". ...
Ethyltestosterone
Singh SM, Gauthier S, Labrie F (2000). "Androgen receptor antagonists (antiandrogens): structure-activity relationships". Curr ... List of androgens/anabolic steroids R.A. Hill; H.L.J. Makin; D.N. Kirk; G.M. Murphy (23 May 1991). Dictionary of Steroids. CRC ...
Rosterolone
Singh SM, Gauthier S, Labrie F (February 2000). "Androgen receptor antagonists (antiandrogens): structure-activity ... Rosterolone is a derivative of mesterolone, which, in contrast, is an androgen and anabolic steroid. Steroidal antiandrogen ...
Enzalutamide
Non-steroidal selective androgen receptor antagonists, developed as a treatment for androgen-sensitive prostate cancer, are ... Enzalutamide is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Enzalutamide acts as a selective silent antagonist of the androgen receptor (AR), the biological target of androgens like ... Rathkopf D, Scher HI (2013). "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): ...
Apalutamide
... is an antiandrogen, and acts as an antagonist of the androgen receptor, the biological target of androgens like ... Apalutamide acts as a selective competitive silent antagonist of the androgen receptor (AR), via the ligand-binding domain, and ... Kawahara, Takashi; Miyamoto, Hiroshi (2014). "Androgen Receptor Antagonists in the Treatment of Prostate Cancer". Clinical ... "Androgen receptor antagonists in castration-resistant prostate cancer". Cancer Journal. 19 (1): 43-9. doi:10.1097/PPO. ...
Seborrhoeic dermatitis
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... In accordance with the involvement of androgens in seborrhoea, antiandrogens, such as cyproterone acetate,[30] spironolactone,[ ... Zouboulis, Christos C.; Degitz, Klaus (2004). "Androgen action on human skin - from basic research to clinical significance". ...
Seborrhoeic dermatitis
Singh, Shankar; Gauthier, Sylvain; Labrie, Fernand (2000). "Androgen Receptor Antagonists (Antiandrogens) Structure-Activity ... Seborrhoea is recognized as an androgen-sensitive condition - that is, it is caused or aggravated by androgen sex hormones such ... "Androgen Physiology, Pharmacology and Abuse". PMID 25905231.. *^ Kenneth L. Becker (2001). Principles and Practice of ... In accordance with the involvement of androgens in seborrhoea, antiandrogens, such as cyproterone acetate,[27] spironolactone,[ ...
4-Hydroxyestrone
Androgen receptor modulators. Progesterone receptor modulators. List of estrogens. This article about a steroid is a stub. You ... Antagonists. *(R,R)-THC. *7β-Hydroxy-DHEA. *Chloroindazole. *Cytestrol acetate. *EM-800 (SCH-57050) ...
Acne
Flutamide, a pure antagonist of the androgen receptor, is effective in treating acne in women.[112][120] It appears to reduce ... a pure androgen receptor antagonist with the same mechanism as flutamide and with comparable or superior antiandrogenic ... Both androgens and IGF-1 seem to be essential for acne to occur, as acne does not develop in individuals with complete androgen ... Rasmusson GH (1986). Chemical Control of Androgen Action. Annual Reports in Medicinal Chemistry. 21. pp. 179-188. doi:10.1016/ ...
Trenbolone hexahydrobenzylcarbonate
List of androgen esters § Trenbolone esters. References[edit]. *^ a b c d William Llewellyn (2011). Anabolics. Molecular ... GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ...
Androgen
GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... Soon after they differentiate, Leydig cells begin to produce androgens.. Androgen effects[edit]. The androgens function as ... This article is about androgens as natural hormones. For androgens as medications, see Anabolic steroid and Androgen ... Exogenous androgen supplements can be used as a male contraceptive. Elevated androgen levels caused by use of androgen ...
Antiandrogen
Androgen receptor antagonistsEdit. Androgens and anti-. androgens at the AR[82][83]. Compound. RBA (%). ... Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like ... N-Terminal domain antagonistsEdit. N-Terminal domain AR antagonists are a new type of AR antagonist that, unlike all currently ... androgen synthesis inhibitors, and antigonadotropins.[5] AR antagonists work by directly blocking the effects of androgens, ...
Acolbifene
GnRH antagonists (e.g., cetrorelix). *Progestogens (e.g., chlormadinone acetate, cyproterone acetate, gestonorone caproate, ... Certain androgens/anabolic steroids (e.g., testosterone, testosterone esters, methyltestosterone, metandienone, nandrolone ... Androgens/anabolic steroids (e.g., testosterone, testosterone esters, nandrolone esters, oxandrolone, fluoxymesterone) ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ...
Gonadotropin-releasing hormone agonist
Sex steroid antagonists (via disinhibition of the HPG axis): Antiandrogens (e.g., flutamide, bicalutamide, enzalutamide) ... Sex steroid agonists (via negative feedback on the HPG axis): Androgens/anabolic steroids (e.g., testosterone, nandrolone ... Usage of GnRH agonist for this purpose necessitates using a GnRH antagonist instead of a GnRH agonist for suppression of ... D2 receptor antagonists (prolactin releasers) (incl., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ...
Dichlorodiphenyldichloroethylene
What is more clear is that DDE is a weak androgen receptor antagonist and can produce male genital tract abnormalities.[16][17] ... Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ...
Medication
Leukotriene antagonists For endocrine problemsEdit. androgens, antiandrogens, estrogens, gonadotropin, corticosteroids, human ... dopamine antagonists, antihistamines, cholinergics, anticholinergics, emetics, cannabinoids, and 5-HT (serotonin) antagonists. ...
سرطان پروستات - ویکیپدیا، دانشنامهٔ آزاد
Some androgen-independent LNCaP sublines have been developed from the ATCC androgen-dependent LNCaP cells after androgen ... Bishayee K, Khuda-Bukhsh AR (September 2013). "5-lipoxygenase antagonist therapy: a new approach towards targeted cancer ... The paradox is that androgens inhibit the proliferation of these androgen-independent prostate cancer cells.[191][192][193] ... These androgen-independent LNCaP cells have elevated AR expression and express prostate specific antigen upon androgen ...
3-Keto-5α-abiraterone
Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ... "Redirecting abiraterone metabolism to fine-tune prostate cancer anti-androgen therapy" (PDF). Nature. 533 (7604): 547-51. doi ...
Breast development
In complete androgen insensitivity syndrome, a condition in which the AR is defective and insensitive to androgens, there is ... knockout mice or mice treated with the PR antagonist mifepristone show delayed (albeit eventually normal, due to estrogen ... Calcitriol, the hormonally active form of vitamin D, acting through the vitamin D receptor (VDR), has, like the androgens, been ... Women with CAIS, who are completely insensitive to the AR-mediated actions of androgens, have, as a group, above-average sized ...
Chemotherapy
... primarily estrogens for breast cancer and androgens for prostate cancer) is known as hormonal therapy, while the inhibition of ... Receptor antagonists. *ERA (Atrasentan). *Retinoid X receptor (Bexarotene). *Sex steroid (Testolactone). Other/ungrouped. * ...
Hormonal IUDs
Antagonists. *Mifepristone. See also. Receptor/signaling modulators. Progestogens and antiprogestogens. Androgen receptor ...
Estrobin
Androgen receptor modulators. Progesterone receptor modulators. List of estrogens. This drug article relating to the genito- ... Antagonists. *(R,R)-THC. *7β-Hydroxy-DHEA. *Chloroindazole. *Cytestrol acetate. *EM-800 ...
Diglyceride
Steroids: Sex steroids: Androgens (AR). *Estrogens (ER). *Progestogens (PR); Corticosteroids: Glucocorticoids (GR) ... Antagonists: 20-Carboxy-LTB4. *Amelubant. *CGS-23131 (LY-223982). *CGS-25019C ...
Blood pressure
Caplea A, Seachrist D, Dunphy G, Ely D (April 2001). "Sodium-induced rise in blood pressure is suppressed by androgen receptor ... Currently, the RAS is targeted pharmacologically by ACE inhibitors and angiotensin II receptor antagonists, also known as ... angiotensin receptor blockers (ARBs). The aldosterone system is directly targeted by spironolactone, an aldosterone antagonist ...
Hormone replacement therapy
Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... GnRH antagonists (e.g., cetrorelix). *Progestogens (e.g., chlormadinone acetate, cyproterone acetate, gestonorone caproate, ... Morley JE, Perry HM (May 2003). "Androgens and women at the menopause and beyond". J. Gerontol. A Biol. Sci. Med. Sci. 58 (5): ... Certain androgens/anabolic steroids (e.g., testosterone, testosterone esters, methyltestosterone, metandienone, nandrolone ...
7α-Thiomethylspironolactone
Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... Parthasarathy HK, MacDonald TM (2007). "Mineralocorticoid receptor antagonists". Curr. Hypertens. Rep. 9 (1): 45-52. PMID ... 7α-TS and 7α-TMS have been found to possess approximately equivalent affinity for the rat ventral prostate androgen receptor ( ... Cutler GB, Pita JC, Rifka SM, Menard RH, Sauer MA, Loriaux DL (1978). "SC 25152: A potent mineralocorticoid antagonist with ...
Luteinizing hormone
GnRH antagonist. *GnRH agonist (inducing an initial stimulation (flare up) followed by permanent blockage of the GnRH pituitary ... LH supports theca cells in the ovaries that provide androgens and hormonal precursors for estradiol production. At the time of ... Gonadal steroids (estrogens and androgens) generally have negative feedback effects on GnRH-1 release at the level of the ... In both males and females, LH works upon endocrine cells in the gonads to produce androgens. ...
Diethylstilbestrol
It suppresses gonadal androgen production and hence circulating androgen levels due to its antigonadotropic effects; it ... DES has been identified as an antagonist of all three isotypes of the estrogen-related receptors (ERRs), the ERRα, ERRβ, and ... Oral DES at 0.25 to 0.5 mg/day is effective in the treatment of hot flashes in men undergoing androgen deprivation therapy for ... In 1960, DES was found to be more effective than androgens in the treatment of advanced breast cancer in postmenopausal women.[ ...
Androstenediol
Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ... See also: List of androgens/anabolic steroids and List of androgen esters ... Androgens. (C-19: Androstane). 1. Dehydroepiandrosterone → Androstenedione → 5α-Androstanedione1 → Androsterone1. 2. ...
Progestin-induced virilisation
Maternal use of androgens or high doses of certain weakly androgenic synthetic progestogens (progestins) structurally related ... ISBN 0-07-142280-3. Schardein, James L. (2000). "Hormones and Hormone Antagonists". Chemically Induced Birth Defects (3rd ed ... The first drugs reported to cause fetal masculinization were the androgens methandriol and methyltestosterone in the mid 1950s ... On June 21, 1976, the FDA approved the androgen danazol (Danocrine), a derivative of ethisterone (17α-ethinyl-testosterone), ...
Farnesoid X receptor
Fiorucci S, Zampella A, Distrutti E (2012). "Development of FXR, PXR and CAR agonists and antagonists for treatment of liver ...
Norethisterone
Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... Raynaud JP, Ojasoo T (1986). "The design and use of sex-steroid antagonists". J. Steroid Biochem. 25 (5B): 811-33. doi:10.1016/ ... Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... Norethisterone is a potent progestogen and a weak androgen and estrogen.[4] That is, it is a potent agonist of the progesterone ...
Menopause
An effect of natural menopause on circulating androgen levels has not been observed.[54] Thus specific tissue effects of ... Raloxifene exhibits oestrogen agonist activity on bone and lipids, and antagonist activity on breast and the endometrium.[79] ... that act selectively as agonists or antagonists on the estrogen receptors throughout the body. The most commonly prescribed ... "Ovarian androgen production in postmenopausal women". The Journal of Clinical Endocrinology and Metabolism. 92 (8): 3040-3. ...
Diabetic nephropathy
... and mineralocorticoid antagonists. RAAS inhibition has been proven to be the most effective therapy to slow the progression of ... Androgen receptor (Androgen insensitivity syndrome). *general: Hypogonadism (Delayed puberty). *Hypergonadism *Precocious ...
Chlorodehydromethyltestosterone
Androgen receptor modulators. Estrogens and antiestrogens. Progestogens and antiprogestogens. List of androgens/anabolic ... GnRH antagonists (e.g., cetrorelix). *Progestogens (incl., chlormadinone acetate, cyproterone acetate, hydroxyprogesterone ... Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... D2 receptor antagonists (prolactin releasers) (e.g., domperidone, metoclopramide, risperidone, haloperidol, chlorpromazine, ...
GPER
CCL18 has been identified as an endogenous antagonist of the GPER.[16] ... "In vivo effects of a GPR30 antagonist". Nat. Chem. Biol. 5 (6): 421-7. doi:10.1038/nchembio.168. PMC 2864230. PMID 19430488 ...
4-Hydroxytestosterone
Androgens and antiandrogens. Estrogen receptor modulators. Progesterone receptor modulators. List of androgens/anabolic ... Antagonists. *Steroidal: 7α-Thioprogesterone. *7α-Thiospironolactone. *7α-Thiomethylspironolactone. *11α-Hydroxyprogesterone ...
Androgen Antagonists | GreenMedInfo | Pharmacological Action
Pharmacological Actions : Androgen Antagonists, Antiproliferative , Wnt/β-catenin signaling pathway modulation. Additional ... 6 Abstracts with Androgen Antagonists Research. Filter by Study Type. Animal Study. ... A novel dietary flavonoid fisetin inhibits androgen receptor signaling and tumor growth in athymic mice. Oct 15, 2008. ... A compound within Pygeum bark antagonizes human androgen receptor in the prostate gland. Sep 23, 2009. ...
Androgen antagonist - definition of Androgen antagonist by The Free Dictionary
Androgen antagonist synonyms, Androgen antagonist pronunciation, Androgen antagonist translation, English dictionary definition ... of Androgen antagonist. n. A substance that inhibits the biological effects of androgenic hormones ... 18) Low androgen levels, such as in those who are androgen deficient or using androgen antagonists, can result in reduced ... Androgen antagonist - definition of Androgen antagonist by The Free Dictionary https://www.thefreedictionary.com/Androgen+ ...
Androgen Antagonists - Pipeline Insights, 2017
Androgen Antagonists Overview. Androgen Antagonists Disease Associated. Androgen Antagonists Pipeline Therapeutics. Androgen ... Androgen Antagonists Assessment by Molecule Type. Androgen Antagonists Assessment by Stage and Molecule Type. Androgen ... Androgen Antagonists Assessment by Combination Products. Androgen Antagonists Assessment by Route of Administration. Androgen ... Androgen Antagonists Assessment by Combination Products. Androgen Antagonists Assessment by Route of Administration. Androgen ...
Androgen Antagonists | Harvard Catalyst Profiles | Harvard Catalyst
"Androgen Antagonists" by people in Harvard Catalyst Profiles by year, and whether "Androgen Antagonists" was a major or minor ... "Androgen Antagonists" is a descriptor in the National Library of Medicines controlled vocabulary thesaurus, MeSH (Medical ... Below are the most recent publications written about "Androgen Antagonists" by people in Profiles. ... Below are MeSH descriptors whose meaning is more general than "Androgen Antagonists". ...
JCI -
An androgen receptor N-terminal domain antagonist for treating prostate cancer
An androgen receptor N-terminal domain antagonist for treating prostate cancer. Jae-Kyung Myung,1 Carmen A. Banuelos,1 Javier ... Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptor. J Biol Chem. ... The androgen receptor co-activator CBP is up-regulated following androgen withdrawal and is highly expressed in advanced ... Androgen receptor regulates a distinct transcription program in androgen-independent prostate cancer. Cell. 2009;138(2):245-256 ...
Androgen Receptor Antagonists
BioVision develops and offers a wide variety of products including assay kits, antibodies, recombinant proteins & enzymes, and other innovative research tools for studying Apoptosis, Metabolism, Cell Proliferation, Cellular Stress, Cell Damage and Repair, Diabetes, Obesity and Metabolic Syndrome, Stem Cell Biology, Gene Regulation, Signal Transduction, etc. BioVisions products are currently being sold in more than 60 countries worldwide.
Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. |...
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists...
Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists ... Analogues inhibit AR-mediated reporter gene expression and bind to AR as potently as or better than any known AR antagonists. ... Androgen receptor / NR3C4 - data and references - Guide to Pharmacology. Miscellaneous. *TESTOSTERONE - Hazardous Substances ... A new nonsteroidal antiandrogenic pharmacophore has been discovered using cell-based cotransfection assays with human androgen ...
Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2...
A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2 ... Effects of isosteric pyridone replacements in androgen receptor antagonists based on 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2- ... Androgen Antagonists/chemical synthesis*. *Androgen Antagonists/pharmacology. *Androgen Receptor Antagonists*. *Androgens/ ...
Dehydroepiandrosterone (DHEA) | ≥99%(HPLC) | Selleck | Androgen Receptor antagonist
...
Galeterone (TOK-001) is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, ... Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide ... Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to ... Darolutamide (ODM-201, BAY-1841788) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki ...
Assays to Measure Estrogen and Androgen Agonists and Antagonists | Springer for Research & Development
1998) Assays to Measure Estrogen and Androgen Agonists and Antagonists. In: del Mazo J. (eds) Reproductive Toxicology. Advances ... Olea, N., Sakabe, K., Soto, A.M. and Sonnenschein, C., 1990, The proliferative effect of "anti-androgens" on the androgen- ... DDE is a potent androgen receptor antagonist, Nature. 375: 581.PubMedCrossRefGoogle Scholar ... Androgen-induced inhibition of proliferation in human breast cancer MCF7 cells transfected with androgen receptor, ...
Enzalutamide (MDV3100) | Androgen Receptor antagonist | Read Reviews & Product Use Citations
... is androgen-receptor inhibitor. Highly recommended inhibitor in AR research. Find all the information about MDV3100 ( ... Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, ... Darolutamide (ODM-201) is a novel androgen receptor (AR) antagonist that blocks AR nuclear translocation with Ki of 11 nM. ... Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. ...
Non-steroid androgen receptor antagonist compounds and methods - Patent # 5677336 - PatentGenius
... antagonists for the androgen receptor are disclosed. Also disclosed are methods for employing the disclosed compounds for ... modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy ... androgen receptor antagonist therapy.. Claim:. We claim:. 1. A method of antagonizing androgen activity comprising the in vivo ... steroid androgen receptor antagonist compounds disclosed can be readily utilized in pharmacological applications where androgen ...
Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. | Cancer Research
Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer.. Youzhi Tong, Chunyun ... Androgen Receptor (AR) antagonists have been used in clinic to treat prostate cancer. One example is bicalutamide (Casodex®), ... Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. [abstract]. In: Proceedings of the ... Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. ...
Pediatric Angioedema Medication: Androgens, Antifibrinolytic Agents, Blood Products, Sympathomimetic Agents, Kallikrein...
Bradykinin Receptor Antagonists. Class Summary. Bradykinin receptor antagonists such as icatibant inhibit bradykinin from ... Androgens. Class Summary. Oral androgens have provided the most successful preventive therapy. Synthetic attenuated androgens ( ... Icatibant, a new bradykinin-receptor antagonist, in hereditary angioedema. N Engl J Med. 2010 Aug 5. 363(6):532-41. [Medline]. ... Hepatotoxicity (more commonly observed in the group receiving 17 alpha alkylated androgen) has not been observed. Oxandrolone ...
Persistent DDT metabolite p,p'-DDE is a potent androgen receptor antagonist
... but inhibits androgen binding to the androgen receptor, androgen-induced transcriptional activity, and androgen action in ... Persistent DDT metabolite p,p-DDE is a potent androgen receptor antagonist Nature. 1995 Jun 15;375(6532):581-5. doi: 10.1038/ ... they are also consistent with inhibition of androgen receptor-mediated events. Here we report that the major and persistent DDT ... DDE and related environmental chemicals may be mediated at the level of the androgen receptor. ...
GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7...
GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7 ... GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7 ... GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7 ... GnRH Antagonists Have Direct Inhibitory Effects On Castration-Resistant Prostate Cancer Via Intracrine Androgen and AR-V7 ...
Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse | Science...
Drug safety is a barrier to the discovery and development of new androgen receptor antagonists. Prostate 71, 480-488 (2011).. ... Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse ... Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse ... Androgen receptor antagonists compromise T cell response against prostate cancer leading to early tumor relapse ...
Activity of Androgen Receptor Antagonist Bicalutamide in Prostate Cancer Cells Is Independent of NCoR and SMRT Corepressors |...
Selection for androgen receptor mutations in prostate cancers treated with androgen antagonist. Cancer Res 1999; 59: 2511-5. ... The mechanisms by which androgen receptor (AR) antagonists inhibit AR activity, and how their antagonist activity may be ... antagonist. Introduction. The androgen receptor (AR) plays a central role in prostate cancer development and progression, and ... Activity of Androgen Receptor Antagonist Bicalutamide in Prostate Cancer Cells Is Independent of NCoR and SMRT Corepressors. ...
Suberoylanilide hydroxamic acid (vorinostat) represses androgen receptor expression and acts synergistically with an androgen...
... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ... represses androgen receptor expression and acts synergistically with an androgen receptor antagonist to inhibit prostate cancer ...
Potent androgen antagonists based on carborane as a hydrophobic core structure. - Semantic Scholar
We report here the design and synthesis of novel androgen antagonists bearing carborane. The most potent compounds, the ... Further development of the potent carborane-containing androgen antagonists described here, having a new skeletal structure and ... as well as in cell growth inhibition assay using androgen-dependent SC-3 cells. ... unique characteristics, may yield novel therapeutic agents, especially selective androgen receptor modulators. ...
The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and...
The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate ... Inhibition of human AR by androgen ablation therapy and by applying synthetic anti-androgens is therefore the primary goal in ... Importantly, AA is able to efficiently repress the growth of both the androgen-dependent LNCaP and also the androgen- ...
Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus Flare...
Phase IIIb Randomized Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH ... The minimum duration of androgen deprivation with GnRH agonist or antagonist therapy is 18 months.. For each patient, the ... PEGASUS Trial Comparing Irradiation Plus Long Term Adjuvant Androgen Deprivation With GnRH Antagonist Versus GnRH Agonist Plus ... A non-steroidal anti-androgen (e. g. flutamide, bicalutamide) will be given orally one week before the first injection of the ...
R)-Bicalutamide | Androgen Areceptor Antagonist | MedChemExpress
... antagonist, with antineoplastic activity. (R)-Bicalutamide is widely used for the research of prostate cancer. - Mechanism of ... R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) ... R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, ... R)-Bicalutamide is the (R)-enantiomer of Bicalutamide (HY-14249). (R)-Bicalutamide is an androgen receptor (AR) antagonist, ...
The effects of natural ligands of hormone receptors and their antagonists on telomerase activity in the androgen sensitive...
The effects of natural ligands of hormone receptors and their antagonists on telomerase activity in the androgen sensitive ... The effects of natural ligands of hormone receptors and their antagonists on telomerase activity in the androgen sensitive ... antagonists tamoxifen and bicalutamide on telomerase activity and expression of cell cycle related proteins in the androgen- ... antagonists tamoxifen and bicalutamide on telomerase activity and expression of cell cycle related proteins in the androgen- ...
Antiandrogen - Wikipedia
Antiandrogens, also known as androgen antagonists or testosterone blockers, are a class of drugs that prevent androgens like ... N-Terminal domain antagonists[edit]. N-Terminal domain AR antagonists are a new type of AR antagonist that, unlike all ... Androgen antagonists; Androgen blockers; Testosterone blockers. Use. • Men and boys: Prostate cancer; Benign prostatic ... Tindall DJ, Chang CH, Lobl TJ, Cunningham GR (1984). "Androgen antagonists in androgen target tissues". Pharmacol. Ther. 24 (3 ...
Kinase Inhibitors | Sloan Kettering Institute
Nilandron
-
Androgen Antagonists, Antineoplastic Agents, ATC:L02BB02
Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or ... Prostate cancer is mostly androgen-dependent and can be treated with surgical or chemical castration. To date, antiandrogen ... glucocorticoid receptors). Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which ...
Androgen receptor antagonists - Altmeyers Encyclopedia - Department Internal medicine
... steroidal androgen receptor antagonists (like the androgens themselves)andnon-steroidal androgen receptor antagon... ... The androgen receptor antagonists are divided between:. *steroidal androgen receptor antagonists (like the androgens themselves ... Non-steroidal androgen receptor antagonists: The non-steroidal androgen receptor antagonists have common structural elements ... The second generation androgen receptor antagonists (enzalutamide and apalutamide) have the highest affinity to the androgen ...
Androgen Receptor (AR)|Inhibitors Agonists Modulators Antagonists|RayStarBio.com
The main function of the androgen receptor is as a DNA-binding transcription factor that regulates gene expression. Androgen ... and then stimulates transcription of androgen responsive genes. The androgen receptor is most closely related to the ... Mutations in this gene are also associated with complete androgen insensitivity (CAIS) ... Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones ...
ReceptorsDeprivationRequiring androgen receptorHuman androgen receptorTestosteroneCompoundsSecond generation androgen receptorEstrogenAgonistInhibitorsAgonistsAntiandrogensTherapyTherapeuticSteroidal androgen receptor antagonistsBicalutamideGnRHSynthesisMDV3100FlutamideDihydrotestosteroneSelectivePotent androgen receptorAntiandrogenMetabolismActions of androgensTreatment of androgen-dependent skinSteroidSmall moleculeEndogenousAbstractInhibitionInhibit androgen receptorSuppressesPathwayLNCaPCastration-resistant prostateAnti-androgen effectInhibits androgen receptorProstate cancer cellMeSHGrowth of prostate cancerActive androgen receptorEnzalutamide and apalutamideReceptor expressionAdrenalSyntheticTranscriptional activityLevels of androgensTumorRatsMetastatic
Receptors16
- Recent studies show that AR antagonists (including the clinically used drug bicalutamide) can enhance AR recruitment of corepressor proteins [nuclear receptor corepressor (NCoR) and silencing mediator of retinoid and thyroid receptors (SMRT)] and that loss of corepressors may enhance agonist activity and be a mechanism of antagonist failure. (aacrjournals.org)
- This androgen antagonistic activity is receptor specific and does not inhibit the closely related glucocorticoid or progesterone receptors . (curehunter.com)
- Nilutamide is a pure, nonsteroidal anti-androgen with affinity for androgen receptors (but not for progestogen, estrogen, or glucocorticoid receptors). (pharmacycode.com)
- Especialidad en Medicina Interna por el Hospital Universitario Dr.. catecholamines are powerful stimulators of vascular smooth muscle hypertrophy, acting via a1 receptors. (tylerweitzman.tk)
- Antiandrogens bind to androgen receptors and competitively inhibit their interaction with testosterone and dihydrotestosterone. (medscape.com)
- Androgen Receptors Downregulate? (anabolicminds.com)
- I started out with this article planning on giving some textbook style explanation as to why using steroids doesn t down regulate androgen receptors (AR). (anabolicminds.com)
- Androgen receptors down-regulate .Don t they? (anabolicminds.com)
- One misunderstood principle of steroid physiology is the concept of androgen receptors (AR), sometimes called 'steroid receptors', and the effects of steroid use on their regulation. (anabolicminds.com)
- Androgen receptors and adrenergic receptors are quite different. (anabolicminds.com)
- I feel that once you consider all of the effects of testosterone on muscle cells you come to realize that when you eventually stop growing (or grow more slowly) it is not because there is a reduction in the number of androgen receptors. (anabolicminds.com)
- They act as competitive antagonists at the GnRH receptors in the anterior pituitary. (flashcardmachine.com)
- Antiandrogens are a group of medications which bind to intracellular androgen receptors (AR) to prevent androgen effects on organs such as the testes, the hair follicles, the hypothalamus, pituitary, ovaries and the prostate gland, which are targets of endogenous androgens. (news-medical.net)
- In fact, when too many androgen receptors are present, he said, current antiandrogen drugs begin to stimulate cancer growth. (medpagetoday.com)
- Bisphenol A (BPA) or its analogs can bind both estrogen receptors (ESR1 and ESR2) and estrogen-related receptors (ERR1-3), which blocks LC gene expression, binds to androgen receptor (NR3C4) as an antagonist to block the activation of LC genes. (frontiersin.org)
- The results showed that two receptors, estrogen receptor alpha (ERα) and androgen receptor (AR), are affected by BPA in opposite direction. (pubmedcentralcanada.ca)
Deprivation34
- This new drug is the latest breakthrough for the treatment of advanced cases and is the first-in-class intracrine androgen antagonist for patients whose cancer has stopped responding to androgen deprivation therapy (ADT). (thefreedictionary.com)
- D'Amico AV. Post-operative salvage androgen deprivation and radiotherapy for prostate cancer. (harvard.edu)
- Serum Lipids prior to Starting Androgen Deprivation Therapy and Risk of Castration Resistant Prostate Cancer and Metastasis: Results from the SEARCH Database. (harvard.edu)
- The mechanisms by which androgen receptor (AR) antagonists inhibit AR activity, and how their antagonist activity may be abrogated in prostate cancer that progresses after androgen deprivation therapy, are not clear. (aacrjournals.org)
- The androgen receptor (AR) plays a central role in prostate cancer development and progression, and androgen deprivation therapy by suppression of testicular androgen production (surgical castration or administration of luteinizing hormone-releasing hormone superagonists), or by treatment with AR antagonists (flutamide or bicalutamide), is still the standard systemic treatment. (aacrjournals.org)
- Additional mechanisms that may contribute to AR reactivation after androgen deprivation therapy are increased AR expression, including AR gene amplification that occurs in approximately one third of patients, and AR mutations that can enhance responses to nonandrogen steroids and to antagonists ( 6 - 9 ). (aacrjournals.org)
- Promising results for cancer immunotherapy in the clinic have led to attempts to combine immunotherapy with standard-of-care therapies, such as androgen deprivation therapy (ADT) for prostate cancer. (sciencemag.org)
- Surgical and medical androgen deprivation therapy (ADT) is a cornerstone for prostate cancer treatment, but relapse usually occurs. (sciencemag.org)
- [13] In accordance, therapeutic modalities that reduce androgen signaling in the prostate gland, referred to collectively as androgen deprivation therapy , are able to significantly slow the course of prostate cancer and extend life in men with the disease. (wikipedia.org)
- [13] Although antiandrogens are effective in slowing the progression of prostate cancer, they are not generally curative, and with time, the disease adapts and androgen deprivation therapy eventually becomes ineffective. (wikipedia.org)
- The most common methods of androgen deprivation therapy currently employed to treat prostate cancer are castration (with a GnRH modulator or orchiectomy ), nonsteroidal antiandrogens, and the androgen synthesis inhibitor abiraterone acetate . (wikipedia.org)
- It is not yet known which regimen of radiation therapy with or without androgen-deprivation therapy is more effective for prostate cancer. (clinicaltrials.gov)
- PURPOSE: This randomized phase III trial is studying prostate radiation therapy to see how well it works compared with short-term androgen deprivation therapy given together with pelvic lymph node radiation therapy with or without prostate radiation therapy in treating patients with a rising PSA after surgery for prostate cancer. (clinicaltrials.gov)
- PBRT and short-term androgen deprivation [STAD]): Beginning 2 months before the start of PBRT, patients undergo STAD, using a combination of antiandrogen (AA) and LHRH agonist therapy, for a total of 4-6 months. (clinicaltrials.gov)
- This phase II trial studies how well androgen deprivation therapy and vorinostat followed by radical prostatectomy works in treating patients with prostate cancer that has not spread to other parts of the body. (clinicaltrials.gov)
- Giving androgen deprivation therapy and vorinostat before surgery may make the tumor smaller and reduce the amount of normal tissue that needs to be removed. (clinicaltrials.gov)
- Compare the survival of patients with metastatic stage IV prostate cancer responsive to combined androgen-deprivation therapy (CAD) treated with intermittent vs continuous CAD. (clinicaltrials.gov)
- Induction therapy: Patients receive combined androgen-deprivation (CAD) therapy comprising goserelin subcutaneously once a month and oral bicalutamide once daily for 8 courses (7 months). (clinicaltrials.gov)
- Therefore, androgen deprivation therapy and inhibition of the AR-signaling by AR antagonists are the major forms of PCa hormone therapy. (biomedcentral.com)
- BACKGROUND: There has been substantial increase in use of androgen deprivation therapy as adjuvant management of prostate cancer. (biomedsearch.com)
- However, all interventions to date have been of rehabilitative intent being implemented after a minimum of 3 months since initiation of androgen deprivation, by which time considerable physical and psychological health problems have manifested. (biomedsearch.com)
- The pressing question is whether it is more efficacious to commence exercise therapy at the same time as initiating androgen deprivation, so treatment induced adverse effects can be immediately attenuated or indeed prevented. (biomedsearch.com)
- METHODS/DESIGN: We are proposing a multi-site randomized controlled trial with partial crossover to examine the effects of timing of exercise implementation (immediate or delayed) on preserving long-term skeletal health, reversing short- and long-term metabolic and cardiovascular risk factors, and supporting mental health in men receiving androgen deprivation therapy. (biomedsearch.com)
- 124 men who are about to initiate androgen deprivation for prostate cancer will be randomized to immediate or delayed groups. (biomedsearch.com)
- DISCUSSION: This project is unique as it explores a fundamental question of when exercise implementation will be of most benefit and addresses both physical and psychological consequences of androgen deprivation initiation. (biomedsearch.com)
- The final outcome may be adjunct treatment which will reduce if not prevent the toxicities of androgen deprivation, ultimately resulting in reduced morbidity and mortality for men with prostate cancer. (biomedsearch.com)
- Cardiovascular risk patients under androgen deprivation therapy : Lower risk with GnRH antagonists compared to LHRH agonists? (urotoday.com)
- Androgen deprivation therapy (ADT) with gonadotropin-releasing hormone (GnRH) agonists or GnRH antagonists is the mainstay of treatment for metastatic prostate cancer (mCaP). (urotoday.com)
- Long-term Castration-related Outcomes in Patients With High-risk Localized Prostate Cancer Treated With Androgen Deprivation Therapy With or Without Docetaxel and Estramustine in the UNICANCER GETUG-12 Trial. (urotoday.com)
- Neoadjuvant chemotherapy with docetaxel and estramustine (DE) significantly improved relapse-free survival in patients with high-risk localized prostate cancer treated with androgen deprivation therapy (ADT) for 3 years and a local treatment in the GETUG-12 phase III trial. (urotoday.com)
- Is Gleason Grade 5 Prostate Cancer Resistant to Conventional Androgen Deprivation Therapy? (harvard.edu)
- ORLANDO -- Intermittent androgen deprivation therapy guided by cancer-related biomarkers appears to be just as effective for treatment following prostate cancer therapy as continuous hormonal treatment, researchers said here. (medpagetoday.com)
- Androgen deprivation therapy remains the gold standard treatment, but it is not curative, and eventually the disease will return as lethal castration-resistant prostate cancer. (bcgsc.ca)
- This therapy is known as Androgen Deprivation Therapy or ADT. (fda.gov)
Requiring androgen receptor1
- Also disclosed are methods for employing the disclosed compounds for modulating processes mediated by the androgen receptor and for treating patients requiring androgen receptor antagonist therapy. (patentgenius.com)
Human androgen receptor5
- A compound within Pygeum bark antagonizes human androgen receptor in the prostate gland. (greenmedinfo.com)
- A new nonsteroidal antiandrogenic pharmacophore has been discovered using cell-based cotransfection assays with human androgen receptor (hAR). (nih.gov)
- A series of nonsteroidal human androgen receptor (hAR) antagonists based on 8-substituted 1,2-dihydro- and 1,2,3,4-tetrahydro-2,2-dimethyl-6-trifluoromethylpyrido[3,2-g]quin olines was synthesized. (nih.gov)
- The natural compound atraric acid is an antagonist of the human androgen receptor inhibiting cellular invasiveness and prostate cancer cell growth. (curehunter.com)
- The ligand-activated human androgen receptor (AR) supports the growth of the prostate gland. (curehunter.com)
Testosterone19
- Several analogues also showed excellent in vivo activity in classic rodent models of AR antagonism, inhibiting growth of rat ventral prostate and seminal vesicles, without accompanying increases in serum gonadotropin and testosterone levels, as is seen with other AR antagonists. (nih.gov)
- Degarelix (Firmagon), a gonadotropin-releasing hormone (GnRH) receptor antagonist differs from luteinizing hormone-releasing hormone (LHRH) agonists by avoiding "testosterone flare" and lower follicle-stimulating hormone (FSH) levels. (aacrjournals.org)
- Antiandrogens , also known as androgen antagonists or testosterone blockers , are a class of drugs that prevent androgens like testosterone and dihydrotestosterone (DHT) from mediating their biological effects in the body. (wikipedia.org)
- [1] [2] They can be thought of as the functional opposites of AR agonists , for instance androgens and anabolic steroids (AAS) like testosterone, DHT, and nandrolone and selective androgen receptor modulators (SARMs) like enobosarm . (wikipedia.org)
- Androgens like testosterone and particularly DHT are importantly involved in the development and progression of prostate cancer. (wikipedia.org)
- Androgen receptor (AR) is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus. (raystarbio.cn)
- Antagonists work by blocking the effect of testosterone, which can have a negative effect on libido and function. (globalrph.com)
- When the testosterone and androgen levels are too. (tylerweitzman.tk)
- Clascoterone is an antiandrogen, or antagonist of the androgen receptor (AR), the biological target of androgens such as testosterone and dihydrotestosterone. (wikipedia.org)
- LH acts on the Leydig cells to stimulate de novo sythesis of androgens (mainly testosterone). (flashcardmachine.com)
- Limited efficacy when androgen receptor antagonists are used alone because of a compensatory increase in LH secretion stimulates higher serum concentrations of testosterone. (flashcardmachine.com)
- The CYP17A enzyme family is involved in the biosynthesis of androgens in the testes and adrenals, culminating in the weak androgens dehydroepiandrosterone (DHEA) and androstenedione, that further undergo metabolism in peripheral tissues (and in prostate cancer cells) to form potent androgens, such as testosterone and its active metabolite dihydotestosterone (DHT). (news-medical.net)
- One promising drug in this family is abiraterone acetate, which shows good activity against androgens and especially lowers testosterone levels, however, disease progression has not been affected. (news-medical.net)
- Since the most potent androgen, DHT, is synthesized from testosterone in peripheral tissues by 5α reductase, any therapy that inhibits this enzyme would be potentially useful as an antiandrogen. (news-medical.net)
- They are typically selective and full or silent antagonists of the androgen receptor (AR) and act by directly blocking the effects of androgens like testosterone and dihydrotestosterone (DHT). (wikipedia.org)
- An androgen that is produced from testosterone in the body and is important in the formation of the male reproductive organs and in the development of male secondary sex characteristics. (thefreedictionary.com)
- The hemizygous mutations in the AR (Xq11.2-q12) encoding AR are associated with X-linked androgen insensitivity, and bi-allelic mutations in SRD5A2 cause enzyme deficiency, converting testosterone (T) to dihydrotestosterone (DHT). (thefreedictionary.com)
- Natural hormone testosterone (T) and dihydrotestosterone (DHT), known as androgens, are the endogenous ligands of AR. (thefreedictionary.com)
- Taking only an anti-androgen incurs risk of serious bone density loss, and taking only estrogen does not significantly lower testosterone levels. (trans-health.com)
Compounds8
- Low-level exposure to endocrine-disrupting compounds can induce functional, developmental, behavioral, and transgenerational disturbances, as shown after low-level exposure to the fungicide vin-clozolin, which acts as an androgen antagonist in rats and mice (Anway et al. (thefreedictionary.com)
- Interaction of organophosphate pesticides and related compounds with the androgen receptor. (thefreedictionary.com)
- Compounds which inhibit or antagonize the biosynthesis or actions of androgens. (harvard.edu)
- Molecules based on this series of compounds have the potential to provide unique and effective clinical opportunities for treatment of prostate cancer and other androgen-dependent diseases. (nih.gov)
- Non-steroidal compounds which are high affinity, high specificity ligand antagonists for the androgen receptor are disclosed. (patentgenius.com)
- Thus, this study provides a molecular insight for AA as a natural anti-androgenic compound and may serve as a basis for AA derivatives as a new chemical lead structure for novel therapeutic compounds as AR antagonists, that can be used for prophylaxis or treatment of prostatic diseases . (curehunter.com)
- Some compounds showed very potent androgen-antagonistic activity. (elsevier.com)
- While other compounds also suppress androgen synthesis, such as glucocorticoids, aminoglutethimide and ketoconazole, these are not considered antiandrogens as their mechanism of action does not involve the AR, but rather various routes of synthesis. (news-medical.net)
Second generation androgen receptor4
- The second generation androgen receptor antagonists (enzalutamide and apalutamide) have the highest affinity to the androgen receptor. (altmeyers.org)
- Modeling Acquired Resistance to the Second-Generation Androgen Receptor Antagonist Enzalutamide in the TRAMP Model of Prostate Cancer. (bvsalud.org)
- Enzalutamide (MDV3100) is a potent second-generation androgen receptor antagonist approved for the treatment of castration -resistant prostate cancer (CRPC) in chemotherapy -naïve as well as in patients previously exposed to chemotherapy . (bvsalud.org)
- Aragon's lead product candidate is a second generation androgen receptor signaling inhibitor, ARN-509, in Phase 2 development for castration resistant prostate cancer (CRPC). (bio-medicine.org)
Estrogen8
- Dehydroepiandrosterone (DHEA, Prasterone, Dehydroisoandrosterone) is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist. (selleckchem.com)
- However, because estrogens are made from androgens in the body, antiandrogens that suppress androgen production can cause low estrogen levels and associated symptoms like hot flashes, menstrual irregularities , and osteoporosis in premenopausal women. (wikipedia.org)
- Recent data report that abiraterone acetate, a specific inhibitor of CYP17 that is key to androgen and estrogen synthesis, improves survival in metastatic castration-resistant prostate cancer (CRPC), confirming the continued dependency of CRPC on the androgen receptor (AR) signaling pathway. (aacrjournals.org)
- EDCs can exert endocrine disrupting activity on more than just estrogen, androgen, and thyroid hormone action. (wellnessresources.com)
- Metabolite of the chemotherapeutic drug tamoxifen, exhibiting more potent estrogen agonist/antagonist activity than the parent drug. (sigmaaldrich.com)
- BPA has estrogen and anti-androgen effects, thereby destroying the development and function of Leydig cells and causing related reproductive diseases such as testicular dysgenesis syndrome, delayed puberty, and subfertility/infertility. (frontiersin.org)
- It is recommended that MTFs take both an anti-androgen and a source of estrogen before having an orchiectomy, and discontinue using anti-androgens after an orchiectomy (Asscheman & Gooren). (trans-health.com)
- Although EDCs affect a broad range of endocrine functions in different tissues and organs, many studies have focused on the estrogen signaling pathway [ 6 ] and fewer on the androgen or other hormonal signaling pathways. (pubmedcentralcanada.ca)
Agonist10
- Elevated AR expression in tumor cells correlates with a change in the functional activity of bicalutamide from antagonist to agonist, suggesting that prostate tumors may adapt to survive on any residual agonism. (aacrjournals.org)
- We first show that the agonist activities of weak androgens and an AR antagonist (cyproterone acetate) are still dependent on the AR NH 2 /COOH-terminal interaction and are enhanced by steroid receptor coactivator (SRC)-1, whereas the bicalutamide-liganded AR did not undergo a detectable NH 2 /COOH-terminal interaction and was not coactivated by SRC-1. (aacrjournals.org)
- Taken together, these results indicate that bicalutamide lacks agonist activity and functions as an AR antagonist due to ineffective recruitment of coactivator proteins and that enhanced coactivator recruitment, rather than loss of corepressors, may be a mechanism contributing to bicalutamide resistance. (aacrjournals.org)
- One mechanism that may contribute to AR reactivation is increased accumulation or synthesis of androgens by prostate cancer cells, and a subset of patients who relapse after castration or luteinizing hormone-releasing hormone agonist treatment will respond to secondary hormonal therapies with AR antagonists such as bicalutamide or to treatments that suppress residual adrenal androgen production such as ketoconozole. (aacrjournals.org)
- Increased AR expression can enhance the growth of prostate cancer xenografts in castrated mice and has been reported to enhance the agonist activity of the AR antagonist bicalutamide ( 10 ). (aacrjournals.org)
- Molecular mechanism of R-bicalutamide switching from androgen receptor antagonist to agonist induced by amino acid mutations using molecular dynamics simulations and free energy calculation. (medchemexpress.com)
- Antihormone therapy, such as flutamide, bicalutamide, and luteinizing hormone-releasing hormone agonist, may lessen the amount of androgens made by the body. (clinicaltrials.gov)
- Surprisingly, ABT263 lacks senolytic effect in both AR agonist- and antagonist-pretreated cells. (biomedcentral.com)
- These data indicate a difference in the agonist- or antagonist-induced cellular senescence and suggest a novel role of MK2206 as a senolytic agent preferentially for AR antagonist-treated cells. (biomedcentral.com)
- Taken together, our data suggest that both AR agonist and antagonist induce cellular senescence but differentially upregulate a pro-survival signaling which preferentially sensitize androgen-sensitive PCa LNCaP cells to a specific senolytic compound. (biomedcentral.com)
Inhibitors3
- [5] These include AR antagonists , androgen synthesis inhibitors , and antigonadotropins . (wikipedia.org)
- [5] AR antagonists work by directly blocking the effects of androgens, while androgen synthesis inhibitors and antigonadotropins work by lowering androgen levels. (wikipedia.org)
- Nonsteroidal androgen synthesis inhibitors like ketoconazole can also be described as "NSAAs", although the term is usually reserved to describe AR antagonists. (wikipedia.org)
Agonists5
- and d) select standard reference doses of TP and FLU for future studies with weakly potent agonists, antagonists, and nonandrogenic test substances. (thefreedictionary.com)
- Interestingly, cellular senescence in prostate cancer (PCa) cells can be induced by either androgen receptor (AR) agonists at supraphysiological androgen level (SAL) used in bipolar androgen therapy or by AR antagonists. (biomedcentral.com)
- Cardiovascular Risk Profile in Prostate Cancer Patients Treated with GnRH Agonists versus Antagonists: An Italian Real-World Analysis. (urotoday.com)
- To evaluate and compare the incidence of cardiovascular (CV) events in a large contemporary cohort of patients diagnosed with prostate cancer (PCa) and in treatment with GnRH agonists or GnRH antagonists. (urotoday.com)
- As seen in African green monkey kidney CV1 cells, the present study confirmed that BPA and BPAF act as ERα agonists (half maximal effective concentration EC 50 of 10-100 nM) and as AR antagonists (half maximal inhibitory concentration IC 50 of 1-2 μM). (pubmedcentralcanada.ca)
Antiandrogens10
- Antiandrogens are one of three types of sex hormone antagonists , the others being antiestrogens and antiprogestogens . (wikipedia.org)
- Antiandrogens are used to treat an assortment of androgen-dependent conditions . (wikipedia.org)
- [4] In women, antiandrogens are used to treat acne , seborrhea , excessive hair growth , scalp hair loss, and high androgen levels , such as those that occur in polycystic ovary syndrome (PCOS). (wikipedia.org)
- In women, antiandrogens are much better tolerated , and antiandrogens that work only by directly blocking androgens are associated with minimal side effects. (wikipedia.org)
- Antiandrogens are used in the treatment of an assortment of androgen-dependent conditions in both males and females. (wikipedia.org)
- The representatives of the family of non-steroidal antiandrogens are potent antagonists at the androgen receptor. (altmeyers.org)
- Antiandrogens are used in the treatment of an assortment of androgen-dependent conditions in both men and women. (wikipedia.org)
- Both conditions represent abnormal growth patterns that often exhibit a significant degree of androgen dependence, which could be antagonized by antiandrogens. (springer.com)
- Antiandrogens are molecules that compete with androgens to bind in the ligand binding site of the AR. (news-medical.net)
- For these reasons, they have improved efficacy and selectivity as antiandrogens and do not lower androgen levels, instead acting solely by directly blocking the actions of androgens at the level of their biological target, the AR. (wikipedia.org)
Therapy11
- Other forms of therapy include androgen antagonist drugs such as ketoconazole, finasteride and insulin-sensitizing drugs such as metformin. (thefreedictionary.com)
- Oral androgens have provided the most successful preventive therapy. (medscape.com)
- Mutant ARs that are strongly stimulated by the AR antagonist flutamide have been found in approximately one third of patients who relapse after combination therapy with flutamide, and a distinct mutant AR that is strongly stimulated by bicalutamide has been found in long-term bicalutamide-treated patients, but such mutations are uncommon in patients treated with surgical or medical castration monotherapy ( 9 , 11 ). (aacrjournals.org)
- Inhibition of human AR by androgen ablation therapy and by applying synthetic anti- androgens is therefore the primary goal in treatment of patients. (curehunter.com)
- Hormone therapy is best used in combination with other treatments such as radiotherapy, chemotherapy, and androgen receptor-targeted agents. (globalrph.com)
- By selectively occupying the strongest binding sites, AR signaling remains active even when androgen levels are low, as is characteristic of first-line androgen ablation therapy. (biomedcentral.com)
- While androgen ablation therapy is a standard first-line treatment, the vast majority of prostate tumors eventually become hormone refractory and continue to proliferate even with very low levels of androgen. (biomedcentral.com)
- The finding that somatostatin analog RC-160 and bombesin/GRP antagonist RC-3095 inhibit the growth of androgen-independent prostate tumors in mice might be of practical importance for human prostate cancer therapy. (elsevier.com)
- GH-RH antagonists could be considered for further development for the therapy of prostate cancer, especially after the relapse. (elsevier.com)
- The principal clinical uses of the androgens include replacement therapy in hypogonadism and anabolic stimulation in states of negative nitrogen balance. (springer.com)
- Not as effective for MTF hormone therapy, because it can potentially stimulate androgen production. (trans-health.com)
Therapeutic8
- However, the AR and AR-regulated genes are still expressed at high levels in androgen-independent prostate cancer, indicating that AR transcriptional activity is reactivated in these tumors and that AR remains as a potential therapeutic target ( 1 - 4 ). (aacrjournals.org)
- UT-34 is a selective androgen receptor degrader (SARD) ligand.Orally Bioavailable Androgen Receptor Degrader, Potential Next-Generation Therapeutic for Enzalutamide-Resistant Prostate Cancer. (raystarbio.cn)
- The postchemotherapy study of abiraterone acetate was recently reported and confirmed that targeting of the androgen receptor (AR) is a valid therapeutic strategy in CRPC, imparting overall survival (OS) benefit in advanced prostate cancer. (aacrjournals.org)
- What are some therapeutic uses of androgens? (flashcardmachine.com)
- Therapeutic used of anti-androgens? (flashcardmachine.com)
- Therapeutic uses for androgen receptor antagonists? (flashcardmachine.com)
- The androgen receptor is a transcription factor and validated therapeutic target for prostate cancer. (bcgsc.ca)
- This review presents an overview of androgen receptor-related mechanisms of resistance as well as novel therapeutic agents to overcome resistance that is linked to the expression of androgen receptor splice variants in castration-resistant prostate cancer. (bcgsc.ca)
Steroidal androgen receptor antagonists1
- The non-steroidal androgen receptor antagonists have common structural elements with the exception of darolutamide. (altmeyers.org)
Bicalutamide11
- All test systems showed that bicalutamide and hydroxyflutamide act as potent androgen antagonists (Ma et al. (thefreedictionary.com)
- MDV3100, a more potent AR antagonist (∼5x vs bicalutamide) without residual agonism, has demonstrated excellent efficacy in CRPC patients and has been approved by FDA for treating CRPC in clinic. (aacrjournals.org)
- However, these responses are usually partial and transient, with AR activity becoming resistant to even high doses of the AR antagonist bicalutamide through unclear mechanisms ( 5 ). (aacrjournals.org)
- R)-Bicalutamide is an androgen receptor (AR) antagonist, with antineoplastic activity. (medchemexpress.com)
- The effects of the 17beta-estradiol, dihydrotestosterone and hormone antagonists tamoxifen and bicalutamide on telomerase activity and expression of cell cycle related proteins in the androgen-sensitive prostatic cancer cell line LNCaP were studied. (uni-regensburg.de)
- 17beta-estradiol stimulated cell growth more effectively than dihydrotestosterone whereas hormone antagonists tamoxifen and bicalutamide caused a significant decrease in cell viability. (uni-regensburg.de)
- 50 microM of bicalutamide down-regulated the levels of the androgen receptor, the proliferating cell nuclear antigen and telomerase activity, and up-regulated the expression of p27(Kip1). (uni-regensburg.de)
- Bicalutamide , a nonsteroidal antiandrogen and the most widely used androgen receptor antagonist in the treatment of prostate cancer . (wikipedia.org)
- Currently approved drugs aimed at androgen signaling axis include the AR antagonist bicalutamide and the CYP17 inhibitor abiraterone[ 7 ]. (biomedcentral.com)
- [13] [15] When castration is combined with a nonsteroidal antiandrogen like bicalutamide , this strategy is referred to as combined androgen blockade (also known as complete or maximal androgen blockade). (wikipedia.org)
- MDV3100 also binds to the androgen receptor with a greater relative affinity than the clinically used antiandrogen bicalutamide (Casodex), Dr. Sawyers and colleagues said. (medpagetoday.com)
GnRH3
- Androgen receptor antagonists lead to an increase in the release of gonadotropin and must therefore be used together with GnrH analogues. (altmeyers.org)
- What are the two GnRH antagonists to know? (flashcardmachine.com)
- MOA of the GnRH antagonists? (flashcardmachine.com)
Synthesis7
- Synthesis and pharmacological evaluation of novel arylpiperazine derivatives as nonsteroidal androgen receptor antagonists. (sigmaaldrich.com)
- Synthesis and biological activity of a novel series of nonsteroidal, peripherally selective androgen receptor antagonists derived from 1,2-dihydrop. (nih.gov)
- 1993). The endocrine and reproductive effects of xenobiotics are believed to be due to their 1) mimicking the effects of endogenous hormones such as estrogens and androgens, 2) antagonizing the effects of normal, endogenous hormones, 3) altering the pattern of synthesis and metabolism of natural hormones, and 4) modifying the hormone receptor levels. (springer.com)
- We report here the design and synthesis of novel androgen antagonists bearing carborane. (semanticscholar.org)
- Design and synthesis of nonsteroidal progesterone receptor antagonists based on C,C'-diphenylcarborane scaffold as a hydrophobic pharmacophore. (semanticscholar.org)
- Design and synthesis of androgen receptor full antagonists bearing a p-carborane cage: promising ligands for anti-androgen withdrawal syndrome. (semanticscholar.org)
- These hormones also play an important role in facilitating protein synthesis in androgen-sensitive tissues such as skeletal muscle, bone, and the kidneys. (springer.com)
MDV31004
- Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. (selleckchem.com)
- Amajor metabolite of Enzalutamide (MDV3100) which is an androgen-receptor (AR) antagonist for treatment of prostate cancer. (raystarbio.cn)
- MDV3100 is a novel antagonist of AR that is also in phase III clinical trials. (aacrjournals.org)
- Despite encouraging clinical results with next generation drugs (MDV3100 and abiraterone) that inhibit androgen receptor (AR) signaling in patients with castration-resistant prostate cancer (CRPC), responses are variable and short-lived. (biomedsearch.com)
Flutamide5
- Flutamide (molecular formula: C11H11F3N2O3) is an oral, non-steroidal anti-androgen agent (androgen recepto. (altmeyers.org)
- This is a prospective, single-center, two-phase study to assess the efficacy of single pulsed-dose flutamide in creating double strand breaks (DSBs) in prostate cancer within patients receiving central androgen suppression and brachytherapy. (clinicaltrials.gov)
- To confirm DNA double strand breaks occur in prostate cancer tissue following pulse-dose flutamide administration in patients who are androgen suppressed, as compared to control patients receiving placebo. (clinicaltrials.gov)
- It is used along with long-acting gonadotropin antagonists such as leuprolide as an effective and less toxic alternative to flutamide, and has now become the most commonly used, with a single daily dose protocol. (news-medical.net)
- To evaluate whether, by blocking androgen action, flutamide can decrease and normalize vascular resistance in the uterine artery in patients with polycystic ovary syndrome (PCOS). (curehunter.com)
Dihydrotestosterone1
- It inhibited 5α-dihydrotestosterone stimulated AR reporter gene activity with an IC(50)=4.7 μM and produced a concentration dependent reduction in androgen receptor levels in prostate cancer cells. (rcsb.org)
Selective5
- Collectively, our results suggested a selective mechanism of action of degarelix against androgen steroidogenesis and AR-variants. (aacrjournals.org)
- Cortexolone 17 alpha-propionate (CB-03-01, Clascoterone) is a topical and peripherally selective androgen antagonist, displays a strong local antiandrogenic activity in hamster's flank organ test, does not exhibit antiandrogenic activity after subcutaneous injection in vivo. (raystarbio.cn)
- The selective androgen receptor. (tylerweitzman.tk)
- Compound 2 retained nanomolar potency and selective inhibition of AKR1C3 but also acted as an AR antagonist. (rcsb.org)
- It acts as a selective antagonist of the androgen receptor. (news-medical.net)
Potent androgen receptor2
- Abstract 2460: Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. (aacrjournals.org)
- Discovery of potent androgen receptor antagonists for treating CRPC and AR+ breast cancer. (aacrjournals.org)
Antiandrogen3
- It was investigated as a topical antiandrogen for the treatment of androgen-dependent skin conditions in the early 1950s, and was found to produce some benefit. (wikipedia.org)
- Likewise, it is significantly more efficacious as an antiandrogen than other AR antagonists such as enzalutamide and spironolactone in scalp dermal papilla cells and sebocytes in vitro. (wikipedia.org)
- Prostate cancer becomes resistant to antiandrogen drugs when cancer cells begin to increase production of the androgen receptor, Dr. Sawyers noted in a statement. (medpagetoday.com)
Metabolism1
- Coupled cistrome and transcriptome profiling upon small molecule antagonism led to the identification of a core set of AR direct effector genes that are most likely to mediate the activities of targeted agents: unbiased pathway mapping revealed that AR is a key modulator of steroid metabolism by forming a tightly controlled feedback loop with other nuclear receptor family members and this oncogenic effect can be relieved by antagonist treatment. (biomedcentral.com)
Actions of androgens1
- A compound which inhibits or antagonises the biosynthesis or actions of androgens. (ebi.ac.uk)
Treatment of androgen-dependent skin1
- be useful for the topical treatment of androgen-dependent skin disorders such as acne, androgenetic alopecia and hirsutism. (raystarbio.cn)
Steroid3
- Clascoterone, also known as cortexolone 17α-propionate or 11-deoxycortisol 17α-propionate, as well as 17α,21-dihydroxyprogesterone 17α-propionate or 17α,21-dihydroxypregn-4-en-3,20-dione 17α-propionate, is a synthetic pregnane steroid and a derivative of progesterone and 11-deoxycortisol (cortexolone). (wikipedia.org)
- Androgens are steroid hormones that possess virilizing actions and, consequently, serve to stimulate differentiation and maintenance of the androgen-dependent tissues of the male reproductive system. (springer.com)
- Glucocorticoids such as prednisone, exert a negative feedback mechanism on central stimulation of steroid production, thus preventing adrenal androgen production. (news-medical.net)
Small molecule2
- Kintor Pharmaceuticals is developing and commercializing a robust pipeline of small molecule and biological drugs for androgen-receptor-related disease areas with unmet medical needs, including COVID-19, prostate, breast and liver cancer, alopecia and acne. (biospace.com)
- Here we investigated EPI-001, a small-molecule antagonist of AR NTD that inhibits protein-protein interactions necessary for AR transcriptional activity. (bcgsc.ca)
Endogenous1
- The normal development and function of the male reproductive system is dependent on the action of endogenous androgens (review and references therein, [ 10 ]) and the biological functions of androgens are primarily mediated by the AR [ 13 , 14 ], which is expressed in many organs including the hypothalamus, pituitary, liver, prostate, and testes. (pubmedcentralcanada.ca)
Abstract1
- abstract = "Nude mice bearing xenografts of the androgen-independent human prostate cancer DU-145 were treated for 4-5 weeks with somatostatin analog RC-160 or the bombesin/gastrin-releasing peptide (GRP) antagonist RC-3095. (elsevier.com)
Inhibition6
- Although these phenotypic alterations are thought to be mediated by the oestrogen receptor, they are also consistent with inhibition of androgen receptor-mediated events. (nih.gov)
- Anti-androgenic activity of various phthalimide analogs was evaluated based on inhibition of androgen-induced activation of nuclear androgen receptor (CAT assay) and on growth inhibition of the androgen-dependent clonal cell line SC-3. (elsevier.com)
- Our results indicate that GH-RH antagonist MZ-4-71 suppresses growth of PC-3, DU-145 and Dunning AT-I androgen-independent prostate cancers, through diminution of GH release and the resulting decrease in the secretion of hepatic IGF-I, or through mechanisms involving a lowering of tumour IGF-I levels and possibly an inhibition of tumour IGF-I and IGF-II production. (elsevier.com)
- Inhibition of androgen biosynthesis and/or AR antagonism should be efficacious in the treatment of CRPC. (rcsb.org)
- Relative to enzalutamide and apalutamide, shows greater efficacy as an AR antagonist, improved activity against mutated AR variants in prostate cancer, little or no inhibition or induction of cytochrome P450 enzymes, and little or no central nervous system distribution. (wikipedia.org)
- Both BPA and BPAF antagonized AR function via competitive inhibition of the action of synthetic androgen R1881. (pubmedcentralcanada.ca)
Inhibit androgen receptor1
- Oral curcumin intake could inhibit androgen receptor expression and probably PSA activity. (greenmedinfo.com)
Suppresses2
- We herein show that orchiectomy synergizes with immunotherapy, whereas the more widely used treatment of medical ADT involving androgen receptor (AR) antagonists suppresses immunotherapy. (sciencemag.org)
- to androgen suppresses sexual.Guyton and Hall Textbook of Medical Physiology, 12th edition pdf and chm free download.Transcriptional profiling identifies gene expression changes induced in HCV-subgenomic. (tylerweitzman.tk)
Pathway5
- Various relevant study results support the importance of the androgen receptor signaling pathway in the treatment of prostate cancer. (altmeyers.org)
- This stage, often referred to as castration-resistant prostate cancer (CRPC), is associated with an active androgen receptor (AR)-signaling pathway. (biomedcentral.com)
- Treatment of human prostate carcinoma‐derived LNCaP cells with androgen or oestradiol triggers simultaneous association of androgen receptor and oestradiol receptor β with Src, activates the Src/Raf‐1/Erk‐2 pathway and stimulates cell proliferation. (embopress.org)
- The influence of androgen and its receptor signaling pathway on sebaceous glands and sebum secretion is one of the important factors causing acne vulgaris. (biospace.com)
- It competitively inhibits the binding of androgen in the skin tissue to the androgen receptor and can locally control the activation of the receptor signaling pathway caused by androgen hyperactivity without changing the activity of the androgen receptor signaling pathway in the human body. (biospace.com)
LNCaP2
- Importantly, AA is able to efficiently repress the growth of both the androgen-dependent LNCaP and also the androgen-independent C4-2 Pca cells but not that of PC3 or CV1 cells lacking AR. (curehunter.com)
- Here, we first induced cellular senescence by treating androgen-sensitive PCa LNCaP cells with either SAL or the AR antagonist Enzalutamide (ENZ). (biomedcentral.com)
Castration-resistant prostate3
- Purpose: Enzalutamide, a second-generation androgen antagonist, was approved by the U.S. Food and Drug Administration (FDA) for castration-resistant prostate cancer (CRPC) treatment. (elsevier.com)
- Androgen receptor targeted therapies in castration-resistant prostate cancer: Bench to clinic. (bcgsc.ca)
- Hormone therapies for advanced prostate cancer target the androgen receptor (AR) ligand-binding domain (LBD), but these ultimately fail and the disease progresses to lethal castration-resistant prostate cancer (CRPC). (bcgsc.ca)
Anti-androgen effect1
- Peppermint tea has an anti-androgen effect in rats. (greenmedinfo.com)
Inhibits androgen receptor1
- The compound, being developed by Medivation, of San Francisco, blocks the androgen receptor and also inhibits androgen receptor function by preventing nuclear translocation of the receptor and DNA binding. (medpagetoday.com)
Prostate cancer cell2
- Here, we examined the biological effects of Frzb/sFRP3 on an androgen-independent prostate cancer cell model. (elsevier.com)
- Tumour-inhibitory effects of a new antagonist of growth hormone-releasing hormone (GH-RH), MZ-4-71, were evaluated in nude mice bearing androgen-independent human prostate cancer cell lines DU-145 and PC-3 and in Copenhagen rats implanted with Dunning R-3327 AT-1 prostatic adenocarcinoma. (elsevier.com)
MeSH1
- Androgen Antagonists" is a descriptor in the National Library of Medicine's controlled vocabulary thesaurus, MeSH (Medical Subject Headings) . (harvard.edu)
Growth of prostate cancer3
- Androgen antagonists prevent the growth of prostate cancer cells and induce a G1 cell cycle arrest. (mskcc.org)
- Androgens can cause the growth of prostate cancer cells. (clinicaltrials.gov)
- All current androgen receptor-targeting therapies inhibit the growth of prostate cancer by blocking the ligand-binding domain, where androgen binds to activate the receptor. (bcgsc.ca)
Active androgen receptor1
- Persuasive evidence supports the concept that constitutively active androgen receptor splice variants lacking the ligand-binding domain are one of the resistant mechanisms underlying advanced disease. (bcgsc.ca)
Enzalutamide and apalutamide1
- Similar to enzalutamide and apalutamide, but with increased efficacy as an AR antagonist, little or no central nervous system distribution, and no induction of seizures in animals. (wikipedia.org)
Receptor expression1
- Androgen Receptor Expression. (tylerweitzman.tk)
Adrenal3
- Consequently, Nilutamide blocks the action of androgens of adrenal and testicular origin which stimulate the growth of normal and malignant prostatic tissue. (pharmacycode.com)
- Castration, therefore, does not suppress adrenal androgens and achieves a "hormone-reduced" rather than a "hormone-free" state, hence, the recent renaming of this stage of the disease as castration-resistant in preference to hormone-refractory. (aacrjournals.org)
- These are used along with chemical or surgical castration to remove all chances of exposure of prostate cancer cells to androgens from the adrenal gland, rather than removing the adrenal gland which could result in fatal or debilitating outcomes, such as hypoadrenalism. (news-medical.net)
Synthetic4
- Synthetic attenuated androgens (eg, danazol, oxandrolone) taken prophylactically increase the serum concentration of C1 inhibitor (C1INH), presumably by enhancing the function of the C1INH gene ( SERPING1 ). (medscape.com)
- It is a synthetic attenuated androgen with relatively few adverse effects. (medscape.com)
- Adverse effects of synthetic androgen treatment? (flashcardmachine.com)
- Adverse effects of synthetic androgen treatment in women and children? (flashcardmachine.com)
Transcriptional activity2
- Here we report that the major and persistent DDT metabolite, p,p'-DDE (1,1-dichloro-2,2-bis(p-chlorophenyl)ethylene), has little ability to bind the oestrogen receptor, but inhibits androgen binding to the androgen receptor, androgen-induced transcriptional activity, and androgen action in developing, pubertal and adult male rats. (nih.gov)
- Transcriptional activity of the androgen receptor requires a functional AF-1 region in its N-terminal domain. (bcgsc.ca)
Levels of androgens2
- This belief has persisted despite the fact that there is no scientific evidence to date that shows that increased levels of androgens down regulates the androgen receptor in muscle tissue. (anabolicminds.com)
- This increased activity is independent of androgens and explains the poor correlation between systemic levels of androgens and the severity of acne lesions. (thefreedictionary.com)
Tumor1
- Recently, AR antagonists demonstrated anti-tumor activities in preclinical AR+ breast cancer models. (aacrjournals.org)
Rats1
- Androgen Optimization Simple.A receptor antagonist is a. in skeletal muscle encoded by a. rats and which increases muscle mass. (tylerweitzman.tk)
Metastatic2
- The mainstay of first-line treatment for patients with metastatic prostate cancer is suppression of gonadal androgens by medical or surgical castration, a strategy that was described 7 decades ago by Charles Huggins and colleagues ( 1 ). (aacrjournals.org)
- What is used with androgen receptor antagonists to treat metastatic prostate cancers? (flashcardmachine.com)