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  • GnRH
  • One particularly effective peptide, a decapeptide analog of the GnRH antagonist Acyline, has the formula: Ac-D-2Nal-D-4Cpa-D-Dpr(methylcarbamoyl)-Ser-4Aph(acetyl)-D-4Aph(acetyl)-Leu-Lys(isopropyl)-Pro-D-Ala-NH 2 . (google.com.au)
  • 2. A GnRH antagonist according to claim 1 wherein Xaa 3 is D-Dpr(Q). (google.com.au)
  • 3. A GnRH antagonist according to claim 2 wherein R is methyl. (google.com.au)
  • 4. A GnRH antagonist according to claim 2 wherein R is ethyl or H. (google.com.au)
  • 5. A GnRH antagonist according to claim 1 wherein X is Ac, Xaa 8 is Lys(ipr) and Xaa 10 is D-Ala-NH 2 . (google.com.au)
  • 8. A GnRH antagonist according to claim 1 wherein Xaa 5 is 4Aph(Ac) and Xaa 6 is D-4Aph(Ac) or wherein Xaa 5 is 4Aph (3-amino-1,2,4-triazole) and Xaa 6 is D-4Aph(3-amino-1,2,4-triazole). (google.com.au)
  • 10. A GnRH antagonist according to claim 1 having the formula: Ac-D-2Nal-D-4ClPhe-D-Dpr(methylCbm)-Ser-4Aph(Ac)-D-4Aph(Ac)-Leu-Lys(ipr)-Pro-D-Ala-NH 2 . (google.com.au)
  • Gonadotropin-releasing hormone antagonists ( GnRH antagonists ) are a class of medications that antagonize the gonadotropin-releasing hormone receptor (GnRH receptor) and thus the action of gonadotropin-releasing hormone (GnRH). (wikipedia.org)
  • Cetrorelix , one of the most widely used GnRH antagonists. (wikipedia.org)
  • Some GnRH antagonists, such as cetrorelix , are similar in structure to natural GnRH (a hormone made by neurons in the hypothalamus) but that have an antagonistic effect, while other GnRH antagonists, such as elagolix and relugolix , are non-peptide and small-molecule compounds. (wikipedia.org)
  • GnRH antagonists are used to provide fast suppression of testosterone without the surge in testosterone levels that is seen when treating patients with GnRH agonists. (wikipedia.org)
  • As testosterone surge does not occur with GnRH antagonists, there is no need for patients to receive an antiandrogen as flare protection during prostate cancer treatment. (wikipedia.org)
  • GnRH agonists also induce an increase in testosterone levels after each reinjection of the drug - a phenomenon that does not occur with GnRH antagonists. (wikipedia.org)
  • The reduction in testosterone levels that occurs during GnRH antagonist therapy subsequently reduces the size of the prostate cancer. (wikipedia.org)
  • GnRH antagonists have an immediate onset of action leading to a fast and profound suppression of testosterone and are therefore especially valuable in the treatment of patients with prostate cancer, where fast control of disease is needed. (wikipedia.org)
  • The GnRH antagonist abarelix was withdrawn from the United States market in 2005 and is now only marketed in Germany for use in patients with symptomatic prostate cancer. (wikipedia.org)
  • Degarelix is a GnRH antagonist that is approved for use in patients with advanced hormone-sensitive prostate cancer throughout Europe and also in the United States. (wikipedia.org)
  • GnRH antagonists are also used for short periods in the prevention of premature LH surge and endogenous ovulation in patients undergoing ovarian hyperstimulation with FSH in preparation for in-vitro fertilization (IVF). (wikipedia.org)
  • The GnRH antagonists that are currently licensed for use in fertility treatment are cetrorelix and ganirelix. (wikipedia.org)
  • GnRH antagonists are being investigated in the treatment of women with hormone-sensitive breast cancer . (wikipedia.org)
  • GnRH antagonists are also used as puberty blockers in transgender youth and to suppress sex hormone levels in transgender adolescents and adults. (wikipedia.org)
  • downstream
  • 1999 ) subsequently cloned the gene encoding for the DRE-binding protein, which they named downstream regulatory element antagonist modulator (DREAM). (springer.com)
  • Craig TA, Ramachandran PL, Bergen 3rd HR, Podratz JL, Windebank AJ, Kumar R. The regulation of apoptosis by the downstream regulatory element antagonist modulator/potassium channel interacting protein 3 (DREAM/KChIP3) through interactions with hexokinase I. Biochem Biophys Res Commun. (springer.com)
  • drugs
  • As they induce opioid withdrawal effects in people who are taking, or have recently used, opioid full agonists, these drugs are generally considered to be antagonists for practical purposes. (wikipedia.org)
  • differ
  • In the short-term clinical trials, adverse effects did not differ between the leukotriene antagonists, placebo or inhaled glucocorticoids. (ubc.ca)
  • compounds
  • These antagonists may be used in the same manner as the compounds of which they are analogs to regulate fertility and to treat steroid-dependent tumors and for other short-term. (google.com.au)
  • trials
  • BL-8040 is a CXCR4 antagonist that has undergone clinical trials (e.g. in various leukemias), with one planned for pancreatic cancer (in combination with pembrolizumab). (wikipedia.org)