RAR antagonists

Product Overview

Alternative Name: Retinoic acid receptor (RAR) antagonists

Development Status: Active Development

Target: Male

Mode: Non-hormonal

Duration Type: Short-acting

Description: Vitamin A (dietary retinol) is essential for normal spermatogenesis. Defects in spermatogenesis (as a result of RARa knock-out) include failure of spermatids to align and be released into the lumen, and presumably reflecting aberrant orientation to the Sertoli cells. However, the molecular mechanisms underlying retinol regulation of spermatogensis remains to be elucidated.

Updated date: May 30, 2018

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Status

Project Phase: Discovery

Project Stage: Target ID/Validation

Status Details:
  • Target has been validated in knock-out mice models. RARą knockout model exhibited male sterility and aberrant spermatogenesis. Potential lead compounds specific to the individual receptors have been identified and synthesized. Testing of a potential lead compound induced sterility in vivo in a time dependent manner.
  • BMS-189453 is a synthetic retinoid that acts as a panantagonist for all three RARs.

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