The human progesterone receptor A-form functions as a transcriptional modulator of mineralocorticoid receptor transcriptional acitivity

作者: Donald P. McDonnell , Mauoucher M. Shahbaz , Elisabetta Vegeto , Mark E. Goldman

DOI: 10.1016/0960-0760(94)90190-2

关键词:

摘要: The human progesterone receptor (hPR) exists as two distinct molecular forms in most cells, hPR-A and -B. These isoforms display biological functions demonstrate a cell promoter specific ability to regulate gene transcription. In cellular contexts where is transcriptionally inactive it can function ligand dependent inhibitor of mineralocorticoid (MR) transcriptional activity. Inhibition occurs by non-competitive mechanism direct binding MR not required. Interestingly, PR agonists differ their facilitate the inhibitory hPR-A, suggesting that conformation may be preferred for this Those compounds derived from 19-nor-testosterone are effective. antiprogestins RU486, ZK98299 ZK112993 effective antagonists presence coexpressed hPR-A. mediated inhibition activity unknown. We propose results competition with common transcription factor association productive.

参考文章(25)
M. E. Meyer, A. Pornon, J. W. Ji, M. T. Bocquel, P. Chambon, H. Gronemeyer, Agonistic and antagonistic activities of RU486 on the functions of the human progesterone receptor. The EMBO Journal. ,vol. 9, pp. 3923- 3932 ,(1990) , 10.1002/J.1460-2075.1990.TB07613.X
P. Kastner, A. Krust, B. Turcotte, U. Stropp, L. Tora, H. Gronemeyer, P. Chambon, Two distinct estrogen‐regulated promoters generate transcripts encoding the two functionally different human progesterone receptor forms A and B. The EMBO Journal. ,vol. 9, pp. 1603- 1614 ,(1990) , 10.1002/J.1460-2075.1990.TB08280.X
William T. Schrader, Bert W. O'Malley, Progesterone-binding components of chick oviduct. IV. Characterization of purified subunits. Journal of Biological Chemistry. ,vol. 247, pp. 51- 59 ,(1972) , 10.1016/S0021-9258(19)45757-8
Ronald J. Koenig, Mitchell A. Lazar, Richard A. Hodin, Gregory A. Brent, P. Reed Larsen, William W. Chin, David D. Moore, Inhibition of thyroid hormone action by a non-hormone binding c-erbA protein generated by alternative mRNA splicing. Nature. ,vol. 337, pp. 659- 661 ,(1989) , 10.1038/337659A0
M T Tzukerman, A Esty, D Santiso-Mere, P Danielian, M G Parker, R B Stein, J W Pike, D P McDonnell, Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions. Molecular Endocrinology. ,vol. 8, pp. 21- 30 ,(1994) , 10.1210/MEND.8.1.8152428
Tina S. Berger, Zahra Parandoosh, Bruce W. Perry, Robert B. Stein, Interaction of glucocorticoid analogues with the human glucocorticoid receptor. The Journal of Steroid Biochemistry and Molecular Biology. ,vol. 41, pp. 733- 738 ,(1992) , 10.1016/0960-0760(92)90414-E
PETER D. FEIL, CHRISTINE L. CLARKE, PONDICHERY G. SATYASWAROOP, Progestin-mediated changes in progesterone receptor forms in the normal human endometrium. Endocrinology. ,vol. 123, pp. 2506- 2513 ,(1988) , 10.1210/ENDO-123-5-2506