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Molecules 2018, 23(6), 1479;

Targeting Transcription Factors for Cancer Treatment

INSERM UMR-S1172-JPARC (Jean-Pierre Aubert Research Center), Lille University and Hospital Center (CHU-Lille), Institut pour la Recherche sur le Cancer de Lille (IRCL), Place de Verdun, F-59045 Lille, France
These authors contributed equally to this work.
Author to whom correspondence should be addressed.
Academic Editor: Takaomi Sanda
Received: 15 May 2018 / Revised: 11 June 2018 / Accepted: 15 June 2018 / Published: 19 June 2018
(This article belongs to the Special Issue Transcription Factors as Therapeutic Targets)
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Transcription factors are involved in a large number of human diseases such as cancers for which they account for about 20% of all oncogenes identified so far. For long time, with the exception of ligand-inducible nuclear receptors, transcription factors were considered as “undruggable” targets. Advances knowledge of these transcription factors, in terms of structure, function (expression, degradation, interaction with co-factors and other proteins) and the dynamics of their mode of binding to DNA has changed this postulate and paved the way for new therapies targeted against transcription factors. Here, we discuss various ways to target transcription factors in cancer models: by modulating their expression or degradation, by blocking protein/protein interactions, by targeting the transcription factor itself to prevent its DNA binding either through a binding pocket or at the DNA-interacting site, some of these inhibitors being currently used or evaluated for cancer treatment. Such different targeting of transcription factors by small molecules is facilitated by modern chemistry developing a wide variety of original molecules designed to specifically abort transcription factor and by an increased knowledge of their pathological implication through the use of new technologies in order to make it possible to improve therapeutic control of transcription factor oncogenic functions. View Full-Text
Keywords: transcription factor; inhibitors; oncogenes; DNA binding; protein/DNA interaction; protein/protein interaction transcription factor; inhibitors; oncogenes; DNA binding; protein/DNA interaction; protein/protein interaction

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Lambert, M.; Jambon, S.; Depauw, S.; David-Cordonnier, M.-H. Targeting Transcription Factors for Cancer Treatment. Molecules 2018, 23, 1479.

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