Literature DB >> 22386529

From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.

Olivier Mirguet1, Yann Lamotte, Frédéric Donche, Jérôme Toum, Françoise Gellibert, Anne Bouillot, Romain Gosmini, Van-Loc Nguyen, Delphine Delannée, Jonathan Seal, Florence Blandel, Anne-Bénédicte Boullay, Eric Boursier, Sandrine Martin, Jean-Marie Brusq, Gael Krysa, Alizon Riou, Rémi Tellier, Agnès Costaz, Pascal Huet, Yann Dudit, Lionel Trottet, Jorge Kirilovsky, Edwige Nicodeme.   

Abstract

The discovery, synthesis and biological evaluation of a novel series of 7-isoxazoloquinolines is described. Several analogs are shown to increase ApoA1 expression within the nanomolar range in the human hepatic cell line HepG2.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 22386529     DOI： 10.1016/j.bmcl.2012.01.125

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  32 in total

Review 1.  The bromodomain: from epigenome reader to druggable target.

Authors:  Roberto Sanchez; Jamel Meslamani; Ming-Ming Zhou
Journal:  Biochim Biophys Acta       Date:  2014-03-28

2.  RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain.

Authors:  Sarah Picaud; Christopher Wells; Ildiko Felletar; Deborah Brotherton; Sarah Martin; Pavel Savitsky; Beatriz Diez-Dacal; Martin Philpott; Chas Bountra; Hannah Lingard; Oleg Fedorov; Susanne Müller; Paul E Brennan; Stefan Knapp; Panagis Filippakopoulos
Journal:  Proc Natl Acad Sci U S A       Date:  2013-11-18       Impact factor: 11.205

3.  I-BET151 selectively regulates IL-6 production.

Authors:  Elyse Barrett; Shaun Brothers; Claes Wahlestedt; Eléonore Beurel
Journal:  Biochim Biophys Acta       Date:  2014-05-22

Review 4.  Targeting bromodomains: epigenetic readers of lysine acetylation.

Authors:  Panagis Filippakopoulos; Stefan Knapp
Journal:  Nat Rev Drug Discov       Date:  2014-04-22       Impact factor: 84.694

Review 5.  Protein lysine acetylation by p300/CBP.

Authors:  Beverley M Dancy; Philip A Cole
Journal:  Chem Rev       Date:  2015-01-16       Impact factor: 60.622

6.  Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor.

Authors:  Wylie S Palmer; Guillaume Poncet-Montange; Gang Liu; Alessia Petrocchi; Naphtali Reyna; Govindan Subramanian; Jay Theroff; Anne Yau; Maria Kost-Alimova; Jennifer P Bardenhagen; Elisabetta Leo; Hannah E Shepard; Trang N Tieu; Xi Shi; Yanai Zhan; Shuping Zhao; Michelle C Barton; Giulio Draetta; Carlo Toniatti; Philip Jones; Mary Geck Do; Jannik N Andersen
Journal:  J Med Chem       Date:  2015-07-06       Impact factor: 7.446

Review 7.  BET bromodomain proteins and epigenetic regulation of inflammation: implications for type 2 diabetes and breast cancer.

Authors:  Dequina A Nicholas; Guillaume Andrieu; Katherine J Strissel; Barbara S Nikolajczyk; Gerald V Denis
Journal:  Cell Mol Life Sci       Date:  2016-08-04       Impact factor: 9.261

8.  Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition.

Authors:  Natalie H Theodoulou; Paul Bamborough; Andrew J Bannister; Isabelle Becher; Rino A Bit; Ka Hing Che; Chun-wa Chung; Antje Dittmann; Gerard Drewes; David H Drewry; Laurie Gordon; Paola Grandi; Melanie Leveridge; Matthew Lindon; Anne-Marie Michon; Judit Molnar; Samuel C Robson; Nicholas C O Tomkinson; Tony Kouzarides; Rab K Prinjha; Philip G Humphreys
Journal:  J Med Chem       Date:  2015-04-30       Impact factor: 7.446

9.  Discovery, Design, and Optimization of Isoxazole Azepine BET Inhibitors.

Authors:  Victor S Gehling; Michael C Hewitt; Rishi G Vaswani; Yves Leblanc; Alexandre Côté; Christopher G Nasveschuk; Alexander M Taylor; Jean-Christophe Harmange; James E Audia; Eneida Pardo; Shivangi Joshi; Peter Sandy; Jennifer A Mertz; Robert J Sims; Louise Bergeron; Barbara M Bryant; Steve Bellon; Florence Poy; Hariharan Jayaram; Ravichandran Sankaranarayanan; Sreegouri Yellapantula; Nandana Bangalore Srinivasamurthy; Swarnakumari Birudukota; Brian K Albrecht
Journal:  ACS Med Chem Lett       Date:  2013-07-16       Impact factor: 4.345

Review 10.  Privileged diazepine compounds and their emergence as bromodomain inhibitors.

Authors:  Steven G Smith; Roberto Sanchez; Ming-Ming Zhou
Journal:  Chem Biol       Date:  2014-04-17
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