bHLHTranscription Factors Inhibitors For Cancer Therapy: General Features For InSilico Drug Design

ISSN: 1875-533X (Online)
ISSN: 0929-8673 (Print)


Volume 21, 38 Issues, 2014


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bHLHTranscription Factors Inhibitors For Cancer Therapy: General Features For InSilico Drug Design

Author(s): Igor F. Tsigelny, Valentina L. Kouznetsova, Sandeep C. Pingle and Santosh Kesari

Affiliation: UCSD San Diego Supercomputer Center, 9500 Gilman Drive, La Jolla, CA 92093-0505, USA

Abstract

Numerous basic-helix-loop-helix (bHLH) transcription factors(TF) have been found to play important roles in tumor growth and progression.Elucidation of the common features of these TFs can pave the road to possible therapeutic intervention. The existing studies of possible inhibition of these TFs are concentrated on the development of peptides or small molecules that inhibit the dimerization of these TFs or prevent their DNA binding. The bHLH TFs have striking similarity in many functionally important regions, such as the helical regions of TFs that interact with each other during dimerization and have complementary sets of residues on both sides of a dimer. These are hydrophobic residues along with anionic and cationic residues with complementary charges.Such complementarity also exists in other contact regions of the bHLH TFs. They also have a very specific set of positivelycharged residues on the surface,which would contact DNA. Such specificity defines a common concept foran in-silicodesign of bHLH TFs inhibitors for a number of existing and important cancer relatedTFs


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Article Details

Volume: 21
First Page: 1
Last Page: 1
Page Count: 1
DOI: 10.2174/0929867321666140414111333
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