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New Progestins and Potential ActionsLigand Pharmaceuticals Inc., 10275 Science Center Drive, San Diego, CA 92121 Newer, nonsteroidal, orally active, tissue-selective progestins are being developed through a molecular approach to compound selection with human progesterone receptor (hPR) serving as the molecular target. The co-transfection and binding assays are used to test receptor selectivity and cross reactivity with a panel of receptors. Transcriptional products are used to further profile new progestin compounds. Desirable new progestins will suppress estrogen-induced endometrial stimulation, show no or minimal proliferative activity, maintain pregnancy, inhibit ovulation, contain no androgenic, mineralocorticoid or glucocorticoid activity, and possess minimal adverse physiologic effects. Newer progestins that possess many of these desirable properties are in development.
Key Words: Progestins human progesterone receptor transcriptional products co-transfection binding assay
Journal of the Society for Gynecologic Investigation, Vol. 7, No. 1 suppl,
S53-S54 (2000) |
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