Discovery of novel intracellular receptor modulating drugs

J Steroid Biochem Mol Biol. 1996 Jan;56(1-6 Spec No):61-6. doi: 10.1016/0960-0760(95)00224-3.

Abstract

Utilizing the co-transfection assay as a guide to determining structure activity relationships, we have been pursuing the discovery of non-steroidal hPR modulators. Small molecule, non-steroidal lead structures have been identified. Optimization of these structures has yielded more potent hPR modulators. Improved cross-reactivity profiles with other intracellular receptors are a feature of these compounds owing to their non-steroidal nature.

Publication types

  • Review

MeSH terms

  • Animals
  • Anisoles / chemistry
  • Anisoles / pharmacokinetics
  • Chlorocebus aethiops
  • Chlorophyta / chemistry
  • Cyclohexanes / chemistry
  • Cyclohexanes / pharmacokinetics
  • Drug Design*
  • Estrogen Replacement Therapy
  • Female
  • Gonanes / chemistry
  • Gonanes / pharmacokinetics
  • Hormone Antagonists / chemistry*
  • Hormone Antagonists / pharmacokinetics
  • Humans
  • Mifepristone / chemistry
  • Mifepristone / pharmacokinetics
  • Molecular Structure
  • Progesterone Congeners / adverse effects*
  • Progesterone Congeners / pharmacokinetics
  • Receptors, GABA / drug effects
  • Receptors, GABA / physiology
  • Receptors, Progesterone / drug effects*
  • Receptors, Progesterone / metabolism
  • Receptors, Steroid / drug effects
  • Receptors, Steroid / metabolism
  • Recombinant Proteins / drug effects
  • Sleep Stages / drug effects
  • Structure-Activity Relationship
  • Transfection

Substances

  • Anisoles
  • Cyclohexanes
  • Gonanes
  • Hormone Antagonists
  • LG 100127
  • Progesterone Congeners
  • Receptors, GABA
  • Receptors, Progesterone
  • Receptors, Steroid
  • Recombinant Proteins
  • Mifepristone
  • onapristone