Journal of the Society for Gynecologic Investigation

 

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Journal of the Society for Gynecologic Investigation, Vol. 7, No. 1 suppl, S53-S54 (2000)
DOI: 10.1177/107155760000700114

New Progestins and Potential Actions

Andrés Negro-Vilar, MD, PhD

Ligand 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


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