Hormonal receptor antagonists

Schapira M, Raaka BM, Samuels HH, Abagyan R. Rational discovery of novel nuclear hormone receptor antagonists. Proc Natl Acad Sci USA 2000 97 1008-13. 

R, Samuels HH. Discovery of diverse thyroid hormone receptor antagonists by high-throughput docking. Proc Natl Acad Sci USA 2003 100 7354-9. 

The use of structure-based virtual screening toward novel nuclear hormone receptor antagonists was described by Schapira et al. [263]. As only X-ray structures of ligand binding domains of agonist-bound nuclear receptors with exception of the antagonist-bound estrogen receptor-a are available, the authors constructed an inactive ... 

Thyroid hormone receptor antagonists, IC50 20 PM (upper), 0.75 fiM (lower) from structure-based virtual screening... 

Pegvisomant is a growth hormone receptor antagonist registered for the treatment of patients with acromegaly who had insufficient benefit from surgery or radiation. 

Habib, K.E., Weld, K.P., Rice, K.C., Pushkas, J., Champoux, M., Listwak, S., et al. (2000) Oral administration of a corticotropinreleasing hormone receptor antagonist significantly attenuates behavioral, neuroendocrine, and autonomic responses to stress in primates. Proc Natl Acad Sci USA 97 6079-6084. 

A variety of hydrolysable tannins have been shown to act as hormone receptor antagonists or inhibitors of particular enzymes. The inhibition of protein kinases by various hydrolysable tannins becomes more potent as the number of phenolic groups increases. 

Rational Discovery of Novel Nuclear Hormone Receptor Antagonists. 

Huime JAP, Lambalk C B 2001 Gonadotrophin-releasing-hormone-receptor antagonists. Lancet 358 1793-1802... 

Hormone receptor antagonist The hepatocytes possess oestrogen receptors and react to oestrogen with proliferation. Therefore, it seemed advisable to apply anti-oestrogens as part of the therapy. However, the efficacy of these substances, e.g. tamoxifen at 10(-20) mg twice daily, could not be confirmed. Toremifen appeared to be more successful. Cyproterone acetate proved inefficacious as an anti-androgenic agent. Flutamide likewise showed no effect. 

Docking routines in the program packages DOCK and ICM [81] have heen used in two published studies to identify novel nuclear hormone receptor antagonists... 

Trainer PJ, Drake WM, Katznelson L, et al. Treatment of acromegaly with the growth hormone-receptor antagonist Pegvisomant. N Engl J Med 2000 342 1171-1177. 

Van Der Lely AJ, Hutson R, Trainer PJ, et al. Long-term treatment of acromegaly with pegvisomant, a growth hormone receptor antagonist. Lancet 2001 358 1754-1759. 

Marimuthu, A. et al. (2002) Design of thyroid hormone receptor antagonists from first principles. Journal of Steroid Biochemistry and Molecular Biology, 83, 59-73. 

Kopchick, J.J., Parkinson, C., Stevens, E.C., Trainer, P.J. Growth hormone receptor antagonists discovery, development, and use in patients with acromegaly, Endocr. Rev. 23, 623-646, 2002. 

N. Doyle, M.J. Waters et al. (2001). Binding and functional studies with the growth hormone receptor antagonist, B2036-PEG (pegvisomant), reveal effects of pegylation and evidence that it binds to a receptor dimer. J. Clin. Endocrinol. Metab. 86, 1716-1723. 

---