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Current Topics in Medicinal Chemistry


ISSN (Print): 1568-0266
ISSN (Online): 1873-4294

General Molecular Biology and Architecture of Nuclear Receptors

Author(s): Michal Pawlak, Philippe Lefebvre and Bart Staels

Volume 12, Issue 6, 2012

Page: [486 - 504] Pages: 19

DOI: 10.2174/156802612799436641


Nuclear receptors (NRs) regulate and coordinate multiple processes by integrating internal and external signals, thereby maintaining homeostasis in front of nutritional, behavioral and environmental challenges. NRs exhibit strong similarities in their structure and mode of action: by selective transcriptional activation or repression of cognate target genes, which can either be controlled through a direct, DNA binding-dependent mechanism or through crosstalk with other transcriptional regulators, NRs modulate the expression of gene clusters thus achieving coordinated tissue responses. Additionally, non genomic effects of NR ligands appear mediated by ill-defined mechanisms at the plasma membrane. These effects mediate potential therapeutic effects as small lipophilic molecule targets, and many efforts have been put in elucidating their precise mechanism of action and pathophysiological roles. Currently, numerous nuclear receptor ligand analogs are used in therapy or are tested in clinical trials against various diseases such as hypertriglyceridemia, atherosclerosis, diabetes, allergies and cancer and others.

Keywords: transcriptional regulation, nuclear receptors, coactivators, corepressors, structure, DNA binding-dependent mechanism, nuclear receptor ligand analogs, architecture and functional behavior, transactivation and transrepression activities, phylogenetic, DNA-binding domain (DBD), P-box, vicinity

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