Endometiral effects of selective progesterone receptor modulators

The Endometrium: Molecular, Cellular and Clinical Perspectives, Second Edition

Volumn , Issue , 2008, Pages 613-622

  Chwalisz, Kristof ^a   Williams, Alistair ^b   Brenner, Robert ^c  

^a TAP PHARMACEUTICAL PRODUCTS INC   (United States)

^b UNIVERSITY OF EDINBURGH   (United Kingdom)

^c INDIANA UNIVERSITY SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 67449167198     PISSN: None     EISSN: None     Source Type: Book    
DOI: None     Document Type: Chapter

References (53)

1. Allen WM, Wintersteiner O. Crystalline progesterone. Science 1934; 80: 190-1.
2. Butenandt A, Westphal U, Hohlweg W. [Uber das Hormon des corpus luteum]. Hopper-Seyler’s Z Physiol Chem 1934; 227: 84-98. [in German]
3. Elger W, Bartley J, Schneider et al. Endocrine pharmacological characterization of progesterone antagonists and progesterone receptor modulators with respect to PR-agonistic and antagonistic activity. Steroids 2000; 65: 713-23.
4. Schubert G, Elger W, Kaufmann G et al. Discovery, chemistry, and reproductive pharmacology of asoprisnil and related 11beta-benzaldoxime substituted selective progesterone receptor modulators (SPRMs). Semin Reprod Med 2005; 23: 58-73.
5. Dong Y, Roberge JY, Wang Z et al. Characterization of a new class of selective nonsteroidal progesterone receptor agonists. Steroids 2004; 69: 201-17.
6. Zhi L, Tegley CM, Pio B et al. 5-benzylidene-1,2-dihydrochromeno[3,4-f]quinolines as selective progesterone receptor modulators. J Med Chem 2003; 46: 4104-12.
7. Giannoukos G, Szapary D, Smith CL, et al. New antiprogestins with partial agonist activity: potential selective progesterone receptor modulators (SPRMs) and probes for receptor- and coregulator-induced changes in progesterone receptor induction properties. Mol Endocrinol 2001; 15: 255-70.
8. Chwalisz K, Elger W, Stickler T et al. The effects of 1-month administration of asoprisnil (J867), a selective progesterone receptor modulator, in healthy premenopausal women. Hum Reprod 2005; 20: 1090-9.
9. Ishwad PC, Katkam RR, Hinduja IN et al. Treatment with a progesterone antagonist ZK 98.299 delays endometrial development without blocking ovulation in bonnet monkeys. Contraception 1993; 48: 57-70.
10. Katkam RR, Gopalkrishnan K, Chwalisz K et al. Onapristone (ZK 98.299): a potential antiprogestin for endometrial contraception. Am J Obstet Gynecol 1995; 173: 779-87.
11. Slayden OD, Zelinski-Wooten MB, Chwalisz K et al. Chronic treatment of cycling rhesus monkeys with low doses of the antiprogestin ZK 137 316: morphometric assessment of the uterus and oviduct. Hum Reprod 1998; 13: 269-77.
12. Chwalisz K, Perez MC, DeManno D et al. Selective progesterone receptor modulator development and use in the treatment of leiomyomata and endometriosis [published erratum appears in Endocr Rev 2005; 26: 703]. Endocr Rev 2005; 26: 423-38.
13. Smith CL, O’Malley BW. Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr Rev 2004; 25: 45-71.
14. Horwitz KB, Jackson TA, Bain DL et al. Nuclear receptor coactivators and corepressors. Mol Endocrinol 1996; 10: 1167-77.
15. Hull ML, Prentice A, Wang DY et al. Nimesulide, a COX-2 inhibitor, does not reduce lesion size or number in a nude mouse model of endometriosis. Hum Reprod 2004; 20: 665.
16. Chen JD, Evans RM. A transcriptional co-repressor that interacts with nuclear hormone receptors. Nature. 1995; 377: 454-47.
17. Onate SA, Tsai SY, Tsai MJ, O’Malley BW. Sequence and characterization of a coactivator for the steroid hormone receptor superfamily. Science 1995; 270: 1354-7.
18. McDonnell DP. The molecular pharmacology of SERMs. Trends Endocrinol Metab 1999; 10: 301-11.
19. Jackson TA, Richer JK, Bain DL et al. The partial agonist activity of antagonist-occupied steroid receptors is controlled by a novel hinge domain-binding coactivator L7/SPA and the corepressors N-CoR or SMRT. Mol Endocrinol 1997; 11: 693-705.
20. Wagner BL, Norris JD, Knotts TA et al. The nuclear corepressors NCoR and SMRT are key regulators of both ligand- and 8-bromo-cyclic AMP-dependent transcriptional activity of the human progesterone receptor. Mol Cell Biol 1998; 18: 1369-78.
21. Wagner BL, Pollio G, Leonhardt S et al. 16 alpha-substituted analogs of the antiprogestin RU486 induce a unique conformation in the human progesterone receptor resulting in mixed agonist activity. Proc Natl Acad Sci USA 1996; 93: 8739-44.
22. Melvin V, Perez M, Chwalisz K, Edwards D. Mechanism of action of the selective progesterone receptor modulator asoprisnil. Endocrine Society’s 87th Annual Meeting, 2005: 613.
23. Brenner RM, Nayak NR, Slayden OD et al. Premenstrual and menstrual changes in the macaque and human endometrium: relevance to endometriosis. Ann NY Acad Sci 2002; 955: 60-74; discussion 86-68, 396-406.
24. Chwalisz K, Brenner RM, Fuhrmann UU et al. Antiproliferative effects of progesterone antagonists and progesterone receptor modulators on the endometrium. Steroids 2000; 65: 741-51.
25. Wolf JP, Hsiu JG, Anderson TL et al. Noncompetitive antiestrogenic effect of RU 486 in blocking the estrogen-stimulated luteinizing hormone surge and the proliferative action of estradiol on endometrium in castrate monkeys. Fertil Steril 1989; 52: 1055-60.
26. Brenner RM, Slayden OD, Critchley HO. Anti-proliferative effects of progesterone antagonists in the primate endometrium: a potential role for the androgen receptor. Reproduction 2002; 124: 167-72.
27. Slayden OD, Hirst JJ, Brenner RM. Estrogen action in the reproductive tract of rhesus monkeys during antiprogestin treatment. Endocrinology 1993; 132: 1845-56.
28. Slayden OD, Brenner RM. RU 486 action after estrogen priming in the endometrium and oviducts of rhesus monkeys (Macaca mulatta). J Clin Endocrinol Metab 1994; 78: 440-8.
29. Chwalisz K, Stockemann K, Fritzemeier KH, Fuhrmann U. Modulation of oestrogenic effects by progesterone antagonists in the rat uterus. Hum Reprod Update 1998; 4: 570-83.
30. DeManno D, Elger W, Garg R et al. Asoprisnil (J867): a selective progesterone receptor modulator for gynecological therapy. Steroids 2003; 68: 1019-32.
31. Brenner RM, Slayden OD, Garg R, Chwalisz K. Asoprisnil suppresses endometrial proliferation in cynomolgus macaques. J Soc Gynecol Invest 2005; 12(Suppl): 208A.
32. Chwalisz K, Garg R, Brener R et al. Role of nonhuman primate models in the discovery and clinical development of selective progesterone receptor modulators (SPRMs). Reprod Biol Endocrinol 2006; 4(Suppl 1): S8.
33. Brenner RM, Slayden OD, Rodgers WH et al. Immunocytochemical assessment of mitotic activity with an antibody to phosphorylated histone H3 in the macaque and human endometrium. Hum Reprod 2003; 18: 1185-93.
34. Chwalisz K, Parker RL, Williamson S et al. Treatment of uterine leiomyomas with the novel selective progesterone receptor modulator (SPRM) J867. J Soc Gynecol Investig 2003; 10(Suppl 2): 636.
35. Chwalisz K, Larsen L, McCrary K, Edmonds A. Effects of the novel selective progesterone receptor modulator (SPRM) asoprisnil on bleeding patterns in subjects with leiomyomata. J Soc Gynecol Invest 2004; 11(Suppl 2): 320-1A.
36. Williams AR, Critchley HO, Osei J, et al. The selective progesterone receptor modulator asoprisnil inhibits glandular proliferation and induces consistent morphological effects in human endometrium. J Soc Gynecol Investig 2006; 13(Suppl 2): 261-2A.
37. Fraser IS, Weisberg E, Minehan E, Johansson ED. A detailed analysis of menstrual blood loss in women using Norplant and Nestorone progestogen-only contraceptive implants or vaginal rings. Contraception 2000; 61: 241-51.
38. Lobo RA, Stanczyk FZ. New knowledge in the physiology of hormonal contraceptives. Am J Obstet Gynecol 1994; 170: 1499-507.
39. Conn PM, Crowley WF Jr. Gonadotropin-releasing hormone and its analogues. N Engl J Med 1991; 324: 93-103.
40. Brown A, Cheng L, Lin S, Baird DT. Daily low-dose mifepristone has contraceptive potential by suppressing ovulation and menstruation: a double-blind randomized control trial of 2 and 5 mg per day for 120 days. J Clin Endocrinol Metab 2002; 87: 63-70.
41. Kettel LM, Murphy AA, Morales AJ, Yen SS. Clinical efficacy of the antiprogesterone RU486 in the treatment of endometriosis and uterine fibroids. Hum Reprod 1994; 9(Suppl 1): 116-20.
42. Croxatto HB, Kovacs L, Massai R et al. Effects of long-term low-dose mifepristone on reproductive function in women. Hum Reprod 1998; 13: 793-8.
43. Chwalisz K, Mattia-Goldberg C, Lee M et al. Treatment of endometriosis with the novel selective progesterone receptor modulator (SPRM) asoprisnil. Fertil Steril 2004; 82(Suppl 2): S83-4.
44. Noyes R, Hertig AT, Rock J. Dating the endometrial biopsy. Fertil Steril 1950; 1: 3-25.
45. Mutter G, Ferenczy A. Anatomy and histology of the uterine corpus. In: Kurman R, ed. Blaustein’s Pathology of the Female Genital Tract. New York: Springer-Verlag, 2002: 383-419.
46. Baird DT, Brown A, Critchley HO et al. Effect of long-term treatment with low-dose mifepristone on the endometrium. Hum Reprod 2003; 18: 61-8.
47. Narvekar N, Cameron S, Critchley HO et al. Low-dose mifepristone inhibits endometrial proliferation and up-regulates androgen receptor. J Clin Endocrinol Metab 2004; 89: 2491-7.
48. Hickey M, Dwarte D, Fraser IS. Superficial endometrial vascular fragility in Norplant users and in women with ovulatory dysfunctional uterine bleeding. Hum Reprod 2000; 15: 1509-14.
49. Hickey M, Fraser IS. The structure of endometrial microvessels. Hum Reprod 2000; 15 (Suppl 3): 57-66.
50. Simbar M, Manconi F, Markham R et al. A three-dimensional study of endometrial microvessels in women using the contraceptive subdermal levonorgestrel implant system, Norplant. Micron 2004; 35: 589-95.
51. Slayden OD, Nayak NR, Burton KA et al. Progesterone antagonists increase androgen receptor expression in the rhesus macaque and human endometrium. J Clin Endocrinol Metab 2001; 86: 2668-79.
52. Brenner RM, Slayden OD, Nayak NR et al. A role for the androgen receptor in the endometrial antiproliferative effects of progesterone antagonists. Steroids 2003; 68: 1033-9.
53. Brenner RM, Slayden OD. Progesterone receptor antagonists and the endometrial antiproliferative effect. Semin Reprod Med 2005; 23: 74-81.