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Chemical Compound Review:

SureCN1649697 (11R)-11-(4- dimethylaminophenyl)-17...

Synonyms: AC1L1M7Y

Okuda, K. et al., Snyder, B.W. et al., Delabre, K. et al., Truss, M. et al., Shanker, Y.G. et al., et al.

Okuda, Korzekwa, Shibaya, Murakami, Nishimura, Tsubouchi, Woclawek-Potocka, Skarzynski,

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High impact information on ZK 98299

The antiprogestins RU 486 and ZK 98299 do not promote binding of the progesterone receptor to this natural HRE in vivo, even at concentrations that completely inhibit the agonistic effects of potent synthetic progestins [1].
We show here that RU 486 and ZK 98299 have the same effects on receptor activation, dimerization, and binding to hormone responsive elements; differences in their action are explained by the 10-fold difference in their affinity for the receptor (ZK 98299 having the lower affinity) [2].
The inhibition of P4 action by OP increased the expression of Fas mRNA (P <0.01); however, it did not affect bax or bcl-2 mRNA expression (P >0.05) [3].
Moreover, OP stimulated expression of caspase-3 mRNA (P <0.01) [3].
Luteal cells obtained from the cows in the midluteal phase of the estrous cycle (Days 8-12 of the cycle) were exposed to a specific P4 antagonist (onapristone [OP], 10(-4) M) with or without 100 ng/ml Fas L [3].

Biological context of ZK 98299

DNA fragmentation was observed in the cells treated with Fas L in the presence of OP [3].
RU 486 and ZK 98299, which are antagonists of progesterone receptor, significantly modulated progesterone synthesis in the human placenta but exhibited paradoxical effects on the first trimester and term placenta [4].

Anatomical context of ZK 98299

ZK 98734 bound to the rat thymus glucocorticoid receptor and to the rat ventral prostate androgen receptor with a greater affinity than ZK 98299 [5].
These effects could be counteracted by the anti-progestin onapristone or ZK 98299 (ZK) suggesting that MPA interacted with progesterone (PRG) receptors to increase B-cell response [6].

Associations of ZK 98299 with other chemical compounds

These compounds were tested for their binding affinity to various steroid receptors and for their bio-activity in various animal models and the results were compared with those of RU38486 and ZK 98299 [7].

Gene context of ZK 98299

The affinity of ZK 98299 for the rat uterine estrogen receptor was weak while the binding of ZK 98734 was not detectable [5].
In vitro binding studies showed that ZK 98299 and ZK 98734 bound to the rat uterine progesterone receptor in vitro with approximately equal affinity [5].

References

Antiprogestins prevent progesterone receptor binding to hormone responsive elements in vivo. Truss, M., Bartsch, J., Beato, M. Proc. Natl. Acad. Sci. U.S.A. (1994) [Pubmed]
In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Delabre, K., Guiochon-Mantel, A., Milgrom, E. Proc. Natl. Acad. Sci. U.S.A. (1993) [Pubmed]
Progesterone is a suppressor of apoptosis in bovine luteal cells. Okuda, K., Korzekwa, A., Shibaya, M., Murakami, S., Nishimura, R., Tsubouchi, M., Woclawek-Potocka, I., Skarzynski, D.J. Biol. Reprod. (2004) [Pubmed]
Regulation of progesterone biosynthesis in the human placenta by estradiol 17 beta and progesterone. Shanker, Y.G., Rao, A.J. Biochem. Mol. Biol. Int. (1997) [Pubmed]
Effect of epostane, ZK 98299, and ZK 98734 on the interruption of pregnancy in the rat. Snyder, B.W., Reel, J.R., Winneker, R.C., Batzold, F.H., Potts, G.O. Biol. Reprod. (1989) [Pubmed]
Medroxyprogesterone acetate enhances in vivo and in vitro antibody production. Vermeulen, M., Pazos, P., Lanari, C., Molinolo, A., Gamberale, R., Geffner, J.R., Giordano, M. Immunology (2001) [Pubmed]
Pharmacology of two new very selective antiprogestagens: Org 31710 and Org 31806. Kloosterboer, H.J., Deckers, G.H., Schoonen, W.G. Hum. Reprod. (1994) [Pubmed]

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