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Type: Journal article
Title: BHLH-PAS proteins in cancer
Author: Bersten, D.
Sullivan, A.
Peet, D.
Whitelaw, M.
Citation: Nature Reviews. Cancer, 2013; 13(12):827-841
Publisher: Nature Publishing Group
Issue Date: 2013
ISSN: 1474-175X
Statement of
David C. Bersten, Adrienne E. Sullivan, Daniel J. Peet & Murray L. Whitelaw
Abstract: Mammalian basic HLH (helix–loop–helix)–PER–ARNT–SIM (bHLH–PAS) proteins are heterodimeric transcription factors that sense and respond to environmental signals (such as pollutants) or to physiological signals (for example, hypoxia and circadian rhythms) through their two PAS domains. PAS domains form a generic three-dimensional fold, which commonly contains an internal cavity capable of small-molecule binding and outer surfaces adept at protein–protein interactions. These proteins are important in several pro-tumour and antitumour pathways and their activities can be modulated by both natural metabolites and oncometabolites. Recently determined structures and successful small-moleculescreening programmes are now providing new opportunities to discover selective agonists and antagonists directed against this multitasking family of transcription factors.
Keywords: Animals; Humans; Neoplasms; Cell Hypoxia; Gene Expression Regulation, Neoplastic; Circadian Rhythm; Basic Helix-Loop-Helix Transcription Factors; CLOCK Proteins; Circadian Clocks
Rights: © 2013 Macmillan Publishers Limited. All rights reserved
RMID: 0020133467
DOI: 10.1038/nrc3621
Appears in Collections:Molecular and Biomedical Science publications

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