AnatomyOrganismsDiseasesChemicals and DrugsAnalytical, Diagnostic and Therapeutic Techniques and EquipmentPhenomena and ProcessesInformation Science
Receptors, GonadotropinHormone AntagonistsReceptors, LHChorionic GonadotropinGonadotropinsReceptors, FSHGonadotropin-Releasing HormoneLuteinizing HormoneFollicle Stimulating HormoneHormones, Hormone Substitutes, and Hormone AntagonistsChorionic Gonadotropin, beta Subunit, HumanGonadotropins, PituitaryOvaryThecomaTestosteroneGonadotropins, EquineSermorelinLeydig CellsProgesteroneEstradiolTestisOvarian FollicleReceptors, ThyrotropinPituitary GlandOvulation InductionGranulosa CellsLeydig Cell TumorFollicular PhaseReceptors, LHRHHormonesGrowth Hormone-Releasing HormoneFertilization in VitroReceptors, Cell SurfaceGlycoprotein Hormones, alpha SubunitCorpus LuteumOligopeptidesOvulationPregnancyCyclic AMPFollicle Stimulating Hormone, beta SubunitRNA, MessengerOrgan SizeGrowth HormoneSwineLuteinizing Hormone, beta SubunitCattleRats, Inbred StrainsPituitary Hormone-Releasing HormonesRats, Sprague-DawleyThyroid HormonesMolecular Sequence DataGonadal Steroid HormonesHypogonadismChoriocarcinomaInjections, SubcutaneousKineticsPituitary Gland, AnteriorGene ExpressionAmino Acid SequenceSexual MaturationProlactinInhibinsGonadotrophsCell LineEstrusDose-Response Relationship, DrugParathyroid HormonePituitary HormonesFertility Agents, FemaleLeuprolideMenotropinsProestrusSuperovulationOvariectomyAdrenocorticotropic HormoneRadioimmunoassayHypothalamusCastrationHuman Growth HormoneSteroidsHypothalamic HormonesTrophoblastic NeoplasmsReceptors, Thyroid HormoneCells, CulturedHypophysectomyTime FactorsThyrotropinDopamine AntagonistsRats, WistarTheca Cells
GnRHProstate cancerProgesteroneTestosteroneAgonists and antagonistsBindsAgonistRelugolixInhibitorLHRHEstradiolElagolixOvarianSelectiveUterine fibroidsPregnylCetrorelixProtein-coupledEstrogen receptor2017MetastaticEstrogensSuperagonistsMolecularCompoundsFollicleLeuprolideGPCRMedicationTreatmentClinicalGeneTreatmentsTherapySynergisticFertilityConcentrationsEndogenousCellsHumanLevels
GnRH28
  • Elagolix, sold under the brand name Orilissa, is a gonadotropin-releasing hormone antagonist (GnRH antagonist) medication which is used in the treatment of pain associated with endometriosis in women. (wikipedia.org)
  • Elagolix is a GnRH antagonist, or an antagonist of the gonadotropin-releasing hormone receptor (GnRHR), the biological target of the hypothalamic hormone gonadotropin-releasing hormone (GnRH). (wikipedia.org)
  • Elagolix is a short-acting GnRH antagonist, and can be used to achieve either partial or more substantial suppression of sex hormone levels. (wikipedia.org)
  • Unlike GnRH agonists and older GnRH antagonists, which are peptides and first-generation GnRH modulators, elagolix is not a GnRH analogue as it is not structurally related to GnRH. (wikipedia.org)
  • The introduction of elagolix in the United States and Canada was followed by that of relugolix (brand name Relumina), the next second-generation GnRH antagonist, in Japan in January 2019. (wikipedia.org)
  • Other approved and off-label uses of GnRH antagonists in general are the same as those of GnRHR desensitization therapy with GnRH agonists such as leuprorelin, and include uterine fibroids and breast cancer in premenopausal women, prostate cancer in men, precocious puberty in children, and hormone therapy in transgender adolescents and adults, among others. (wikipedia.org)
  • Degarelix injection is in a class of medications called gonadotropin-releasing hormone (GnRH) receptor antagonists. (medlineplus.gov)
  • The active substance in Yselty, linzagolix choline, is a gonadotropin-releasing hormone (GnRH) receptor antagonist. (europa.eu)
  • By attaching to GnRH receptors (targets) in the pituitary gland, it blocks the action of GnRH, leading to decreased blood concentrations of estrogen and progesterone, two hormones that promote the growth of uterine fibroids. (europa.eu)
  • Relugolix is a non-peptide GnRH receptor antagonist that competitively binds to pituitary GnRH receptors, thereby reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), leading to decreased serum concentrations of the ovarian sex hormones estradiol and progesterone and reduced bleeding associated with uterine fibroids. (centerwatch.com)
  • BASEL, Switzerland and NEW YORK, Dec. 28, 2020 (GLOBE NEWSWIRE) -- Myovant Sciences (NYSE: MYOV) and Pfizer Inc. (NYSE: PFE) today announced a collaboration to develop and commercialize relugolix - a once-daily, oral gonadotropin-releasing hormone (GnRH) receptor antagonist - in oncology and women's health in the U.S. and Canada. (pfizer.com)
  • Cetrorelix (GnRH antagonist) inhibited the preovulatory LH surge induced by OIF in llamas suggesting that LH secretion is modulated by a direct or indirect effect of OIF on GnRH neurons in the hypothalamus. (biomedcentral.com)
  • In mammals, ovulation implies pulsatile secretion of gonadotropin-releasing hormone (GnRH) from the medio-basal nuclei of the hypothalamus into the hypophyseal portal system, followed by the release of LH from the anterior pituitary into systemic circulation [ 1 ]. (biomedcentral.com)
  • Relugolix is a gonadotropin releasing hormone (GnRH) receptor antagonist that decreases serum estradiol and progesterone concentrations to postmenopausal levels. (figshare.com)
  • Degarelix, a gonadotropin-releasing hormone (GnRH) antagonist, binds to GnRH receptors on the pituitary gland thus suppressing testosterone release from the testes. (druglib.com)
  • Receptor for gonadotropin releasing hormone (GnRH) that mediates the action of GnRH to stimulate the secretion of the gonadotropic hormones luteinizing hormone (LH) and follicle-stimulating hormone (FSH). (drugbank.com)
  • Kakar SS, Grizzle WE, Neill JD: The nucleotide sequences of human GnRH receptors in breast and ovarian tumors are identical with that found in pituitary. (drugbank.com)
  • On Dec. 18, the FDA approved Myovant Sciences GmbH's Orgovyx (relugolix), a gonadotropin-releasing hormone (GnRH) receptor antagonist, to treat adults with advanced prostate cancer (RSP 1/21, p. 8) . (mmitnetwork.com)
  • LH stimulates receptors on Leydig cells in the testes to induce production of T. Suppression of this hypothalamic−pituitary−gonadal axis is the mechanism by which LHRH agonists (additionally referred to as gonadotropin-releasing hormone (GnRH)) and antagonists cut back circulating T ranges sixteen (Fig. (squareblogs.net)
  • Cetrorelix is a synthetic decapeptide with gonadotropin-releasing hormone (GnRH) antagonistic activity. (pharmacycode.com)
  • GnRH induces the production and release of luteinizing hormone (LH) and follicle stimulating hormone (FSH) from the gonadotrophic cells of the anterior pituitary. (pharmacycode.com)
  • Cetrorelix competes with natural GnRH for binding to membrane receptors on pituitary cells and thus controls the release of LH and FSH in a dose-dependent manner. (pharmacycode.com)
  • The purpose of this study was, therefore, to evaluate the effects of a long term treatment with orntide, a GnRH antagonist, on testosterone levels and fertility in male rats. (biomedcentral.com)
  • These results suggest that lack of fertility due to testosterone suppression is reversible after cessation of treatment with this GnRH antagonist. (biomedcentral.com)
  • Analogues of gonadotrophin releasing hormone (GnRH) are being used for a variety of hormone-dependent human disease states. (biomedcentral.com)
  • They act by hyper-stimulation of GnRH receptors on the gonadotroph cells of the pituitary, resulting in an initial phase of elevated levels of testosterone and androgens, followed by down-regulation of the receptors. (biomedcentral.com)
  • These are GnRH antagonists, which immediately block the GnRH receptors to access by native GnRH peptides. (biomedcentral.com)
  • This report is an evaluation of the effect of a long term treatment with a GnRH antagonist, orntide acetate, on the fertility of male rats. (biomedcentral.com)
Prostate cancer4
  • This article will summarize the available literature concerning the recent development of hormone therapy in reference to locally advanced prostate cancer. (touchoncology.com)
  • Since the discovery of hormone dependence of prostate cancer by Dr Huggins in 1941, hormone therapy has become the mainstay of treatment in metastatic prostate cancer. (touchoncology.com)
  • Xtandi (enzalutamide) is FDA-approved for use in patients with castration-resistant prostate cancer, metastatic hormone-sensitive prostate cancer, and non-metastatic castration-sensitive prostate cancer with biochemical recurrence at high risk for metastasis (FDA.gov). (jax.org)
  • bicalutamide reviews 2020 of alternative for progressive androgen-dependent prostate cancer is the nonsteroidal antiandrogen, bicalutamide, either as monotherapy or with adjuvant castration or luteinizing hormone-releasing hormone superagonists to block the synthesis of endogenous testosterone. (squareblogs.net)
Progesterone4
  • By blocking the GnRHR, it dose-dependently suppresses the gonadal production and hence circulating levels of sex hormones such as estradiol, progesterone, and testosterone. (wikipedia.org)
  • Progestins such as norethindrone act by binding to nuclear receptors that are expressed in progesterone responsive tissues. (centerwatch.com)
  • During the forecast period, launches of novel selective progesterone receptor regulators (SPRMs) and gonadotropin-releasing hormone (Gn-RH) antagonists will provide more efficacious medical alternatives over procedures such as hysterectomy and myomectomy in the long-term management of uterine fibroids. (clarivate.com)
  • Progesterone is the main female sex hormone that occurs naturally and is also manufactured into a drug that is used in menopausal hormone therapy. (wikizero.com)
Testosterone6
Agonists and antagonists1
  • While the net result of the treatments by agonists and antagonists appears to be the same, two characteristic of the antagonists make it essential to determine whether return to fertility may be a problem and of regulatory interest. (biomedcentral.com)
Binds1
Agonist3
  • Agonist activity of the KiSS1 receptor results in the release of gonadotropin-releasing hormones. (multispaninc.com)
  • Myovant Sciences completed a successful dose-finding pharmacokinetic/pharmacodynamic Phase 2a study of MVT-602, a kisspeptin-1 receptor agonist, in healthy women undergoing a minimal controlled ovarian stimulation protocol. (sumitovant.com)
  • Injecting proestrus, but not hormone primed, rats with a CB 1 (cannabinoid receptor 1) antagonist/inverse agonist and GPR18 antagonist, AM251 facilitated sexual motivation [ 4 ]. (hindawi.com)
Relugolix1
Inhibitor1
  • Xtandi (enzalutamide) is a second-generation small molecule inhibitor of androgen receptor, thereby resulting in decreased tumor growth ( PMID: 24009414 , PMID: 25945058 ). (jax.org)
LHRH4
  • The advent of safe and reversible forms of androgen deprivation, such as luteinizing hormone-releasing hormone (LHRH) analogues and antiandrogens (AAs), has also contributed to enthusiasm for NADT. (medscape.com)
  • The aim of the present study was to evaluate the expression of receptors for luteinizing hormone-releasing hormone (LHRH) in human specimens of triple-negative breast cancers (TNBC). (uni-luebeck.de)
  • In addition, we used in vitro and in vivo models of TNBC to investigate if these receptors are suitable targets for the treatment with the LHRH antagonist Cetrorelix. (uni-luebeck.de)
  • Receptors for LHRH were expressed in all tumor samples and in the TNBC cell lines HCC1806 and HCC1937. (uni-luebeck.de)
Estradiol1
  • Estradiol acts by binding to nuclear receptors that are expressed in estrogen-responsive tissues. (centerwatch.com)
Elagolix1
Ovarian1
  • The study demonstrated that MVT-602 was generally well-tolerated and produced the desired luteinizing hormone surge associated with high and dose-dependent rates of ovulation in healthy women following a minimal controlled ovarian stimulation protocol. (sumitovant.com)
Selective3
  • The invention relates to selective oestrogen receptor modulators (SERMs) and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception. (justia.com)
  • Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? (justia.com)
  • 7. Olaf Panknin, Andrea Wagenfeld, Wilhelm Bone, Eckhard Bender, Katrin Nowak-Reppel, Amaury E. Fernández-Montalván, Reinhard Nubbemeyer, Discovery and Characterization of BAY 1214784, an Orally Available Spiroindoline Derivative Acting as a Potent and Selective Antagonist of the Human Gonadotropin-Releasing Hormone Receptor as Proven in a First-In-Human Study in Postmenopausal Women. (rjptonline.org)
Uterine fibroids3
  • It is developing Linzagolix, an oral gonadotropin releasing hormone receptor antagonist that is in Phase III clinical trial for the treatment of pain associated with endometriosis and heavy menstrual bleeding associated with uterine fibroids in pre-menopausal women. (finabase.io)
  • What clinical role will second-generation, oral Gn-RH antagonist therapies play in the management of uterine fibroids? (clarivate.com)
  • What are clinical advantages of Gn-RH antagonists compared with Gn-RH agonists, in the long-term and preoperative management of symptomatic uterine fibroids? (clarivate.com)
Pregnyl2
Cetrorelix2
  • Tumors of mice treated with Cetrorelix expressed less mRNA for EGFR and HER3 receptors than untreated tumors. (uni-luebeck.de)
  • Given the low toxicity and clinical availability of Cetrorelix, this peptide antagonist should be considered for phase II studies in patients with advanced TNBC. (uni-luebeck.de)
Protein-coupled3
  • The KiSS1-derived peptide receptor is a G protein-coupled receptor (GPCR) involved in the regulation of puberty, fertility, and endocrine function. (multispaninc.com)
  • Follicle-stimulating hormone receptor (FSHR) is a G protein-coupled receptor (GPCR) with pivotal roles in reproduction. (frontiersin.org)
  • Membrane trafficking of G protein-coupled receptors (GPCRs) tightly orchestrates the signaling from this superfamily of signaling receptors. (frontiersin.org)
Estrogen receptor2
  • The concomitant inclusion of the "pure" estrogen antagonist, ICI 182, 780, did not alter the inhibitive effects of HPTE, suggesting that the effects of HPTE are not mediated through the estrogen receptor (ER) pathway. (cdc.gov)
  • Synergistic activation of estrogen receptor with combinations of environmental chemicals. (cdc.gov)
20173
  • Sarah Jane Baker, the storied British transgender rights activist who spent 30 years in prison and castrated herself there in 2017 in her effort to transition, has been denied hormone treatments as she endures another stretch behind bars after a charge of incitement to violence, according to advocates. (hjw.tv)
  • She was denied hormone replacement therapy until she cut off her own testicles with a razor blade in 2017. (hjw.tv)
  • [11] Bioidentical hormone replacement has inadequate clinical research to determine its safety and efficacy as of 2017. (wikizero.com)
Metastatic1
  • MIAMI BEACH -- Emerging data have helped optimize the use of CDK4/6 inhibitors in metastatic hormone receptor (HR)-positive breast cancer, and the focus has turned to overcoming resistance, a breast cancer specialist said here. (medpagetoday.com)
Estrogens1
  • Estrogens and progestogens are the main hormone drugs used in HRT. (wikizero.com)
Superagonists1
  • Clinically the antagonists differ from the superagonists in that the initial hyper-stimulation and release of LH and FSH do not occur [ 6 ]. (biomedcentral.com)
Molecular2
  • Kakar SS: Molecular structure of the human gonadotropin-releasing hormone receptor gene. (drugbank.com)
  • Bioidentical" hormone replacement is a development in the 21st century and uses manufactured compounds with "exactly the same chemical and molecular structure as hormones that are produced in the human body. (wikizero.com)
Compounds2
  • Given the critical nature of receptor internalization and endosomal signaling for FSHR activity, we assessed whether these compounds exhibit differential abilities to alter receptor endosomal trafficking and signaling within the VEE. (frontiersin.org)
  • All compounds exhibited a similar requirement for receptor internalization to increase cAMP and proportion of FSHR endosomes with active Gαs, suggesting regulation of cAMP signaling induced by T1 may be altered. (frontiersin.org)
Follicle1
Leuprolide1
  • Within the July difficulty of the Journal of Clinical Oncology, researchers from the Massachusetts Basic Hospital (MGH) describe how sufferers taking bicalutamide, which inhibits androgen exercise by binding to the hormones' receptors, had improved bone density and reported fewer unpleasant uncomfortable side effects than did those taking leuprolide, a standard type of hormone therapy that markedly lowers androgen ranges. (squareblogs.net)
GPCR1
  • In turn, receptor signaling is known to drive or regulate GPCR trafficking. (frontiersin.org)
Medication1
Treatment2
  • Within the landscape of treatment for early-stage, hormone receptor-positive [breast cancer], the appropriate therapy for patients who will develop disease recurrence while on adjuvant CDK4/6 inhibitors remains to be determined. (medpagetoday.com)
  • The concern is heightened by the likelihood that antagonists will be used for treatment of benign prostatic hypertrophy, a condition in men who might wish at some future time to sire offspring. (biomedcentral.com)
Clinical1
  • and Nolasiban, an oral oxytocin receptor antagonist that is in Phase I clinical trial to enhance clinical pregnancy and live birth rates in women undergoing in vitro fertilization. (finabase.io)
Gene2
  • Kottler ML, Bergametti F, Carre MC, Morice S, Decoret E, Lagarde JP, Starzec A, Counis R: Tissue-specific pattern of variant transcripts of the human gonadotropin-releasing hormone receptor gene. (drugbank.com)
  • Small Indels in the Androgen Receptor Gene: Phenotype Implications and Mechanisms of Mutagenesis. (medscape.com)
Treatments1
  • If your cancer cells are positive for hormone receptor sensitivity, they can give you hormone therapy treatments to trick the cancer cells into dying. (breastcancertalk.net)
Therapy7
  • Angiotensin II Receptor Antagonist for Post Cycle Therapy. (bodypharm.biz)
  • If you have already got heart problems or diabetes, speak to your physician earlier than you start hormone therapy. (squareblogs.net)
  • This article is about hormone replacement therapy in menopause. (wikizero.com)
  • For transgender applications, see Transgender hormone therapy . (wikizero.com)
  • For other forms, see Hormone therapy . (wikizero.com)
  • Hormone replacement therapy ( HRT ), also known as menopausal hormone therapy or postmenopausal hormone therapy , is a form of hormone therapy used to treat symptoms associated with female menopause . (wikizero.com)
  • These proteins may be pregnancy-specific (present only during pregnancy) or pregnancy-associated (present during pregnancy or under other conditions such as hormone therapy or certain malignancies. (bvsalud.org)
Synergistic1
  • Synergistic effects of Obatoclax with androgen receptor inactivation can be observed. (oncotarget.com)
Fertility1
  • There is concern that, whatever the mechanism might be, protracted administration of effective antagonist doses might make a return to fertility more difficult. (biomedcentral.com)
Concentrations1
  • Increasing concentrations of M or HPTE (100-1000 nM) caused a progressive decline in both basal and 10 mIU/ml human chorionic gonadotropin (hCG)- or 1 mM 8 Br-cAMP-stimulated T following exposure for 4 or 24 h, although the declines with HPTE were greater. (cdc.gov)
Endogenous2
  • Endocannabinoids are endogenous lipid neurotransmitters that activate cannabinoid receptors and play a role in regulating motivated behaviors, such as feeding, anxiety, drug seeking, pain, and reproduction [ 4 , 5 ]. (hindawi.com)
  • AEA), 2-arachidonoyl glycerol (2-AG) [ 6 ], and more recently the endogenous metabolite of AEA N -arachidonoyl glycine (NAGly) was shown to activate the GPR18, which is a putative cannabinoid receptor [ 7 - 9 ]. (hindawi.com)
Cells1
  • Altogether, our results suggest that MCL1 is a key molecule deciding over the fate of PCa cells upon inactivation of androgen receptor signaling. (oncotarget.com)
Human1
Levels2