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Ki : 2 nM for RARα

Three retinoic acid receptors (RARα, RARβ and RARγ and three retinoid X receptors, members of the nuclear receptor (NR) superfamily, mediate the biological effects of retinoic acids (all-tratis and 9-cis retinoic acids; t-RA and 9c-RA) upon development, cell differentiation and proliferation, and homeostasis. BMS 753 is identified as a RARα-selective agonist.

In vitro: Increasing concentrations of BMS 753 resulted in low levels of RARβ2 transcripts in WT cells, even at the highest concentration, while 100 nM BMS 753 efficiently induced RARβ2 transcripts in RARγ-/- cells. In contrast, no activation was seen in RARα-/- cells up to 100 nM BMS 753, demonstrating that it is specific for RARα [1].

In vivo: To investigate whether similar RARα-dependent events in Sertoli cells (SC) also operate in the reinitiation of spermatogenesis in a vitamin A-deficient (VAD) testis, Rbp4-null adult males fed a VAD diet for 14 wk were treated with BMS 753 or with its vehicle only. Interestingly, spermatogenesis did not initiate upon administration of BMS 753 to VAD Rbp4-null mutants; only SC and spermatogonia were present in their seminiferous epithelium, as in the vehicle-treated situation [2].

Clinical trial: Up to now, BMS 753 is still in the preclinical development stage.

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