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Noncanonical mechanisms to regulate nuclear receptor signaling

Sadana, P.

Future Medicinal Chemistry 4(10): 1307-1333

2012


ISSN/ISBN: 1756-8927
PMID: 22800372
DOI: 10.4155/fmc.12.72
Accession: 054645085

Nuclear receptor (NR)-targeted therapies comprise a large class of clinically employed drugs. A number of drugs currently being used against this protein class were designed as structural analogs of the endogenous ligand of these receptors. In recent years, there has been significant interest in developing newer strategies to target NRs, especially those that rely on mechanistic pathways of NR function. Prominent among these are noncanonical means of targeting NRs, which include selective NR modulation, NR coactivator interaction inhibition, inhibition of NR DNA binding, modulation of NR cellular localization, modulation of NR ligand biosynthesis and downregulation of NR levels in target tissues. This article reviews each of these promising emerging strategies for NR drug development and highlights some of most significant successes achieved in using them.

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