Suppression of inflammation by a synthetic histone mimic
- E. Nicodème, K. Jeffrey, A. Tarakhovsky
- BiologyNature
- 23 December 2010
A synthetic compound (I-BET) is described that by ‘mimicking’ acetylated histones disrupts chromatin complexes responsible for the expression of key inflammatory genes in activated macrophages, and confers protection against lipopolysaccharide-induced endotoxic shock and bacteria-induced sepsis.
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
- O. Mirguet, R. Gosmini, E. Nicodème
- BiologyJournal of Medicinal Chemistry
- 25 September 2013
This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
- C. Chung, H. Coste, E. Nicodème
- Biology, ChemistryJournal of Medicinal Chemistry
- 13 May 2011
X-ray crystal structures of compounds bound into bromodomains of Brd2 and Brd4 elucidate the molecular interactions of binding and explain the precisely defined stereochemistry required for activity.
Identification of liver receptor homolog-1 as a novel regulator of apolipoprotein AI gene transcription.
- P. Delerive, C. Galardi, J. Bisi, E. Nicodème, B. Goodwin
- BiologyMolecular Endocrinology
- 1 October 2004
It is demonstrated that LRH-1 is a novel regulator of APOAI transcription and underscore the role of this receptor in cholesterol homeostasis.
Using advanced intercross lines for high-resolution mapping of HDL cholesterol quantitative trait loci.
- Xiaosong Wang, I. Le Roy, B. Paigen
- BiologyGenome Research
- 1 July 2003
All the major HDL QTLs in this study had homologous counterparts in humans, implying that their underlying genes regulate HDL in humans.
Tapinarof Is a Natural AhR Agonist that Resolves Skin Inflammation in Mice and Humans.
- S. Smith, C. Jayawickreme, J. Cote-Sierra
- Biology, MedicineJournal of Investigative Dermatology
- 1 October 2017
Development of a Topical Treatment for Psoriasis Targeting RORγ: From Bench to Skin
- S. Smith, C. Peredo, J. Cote-Sierra
- Biology, MedicinePLoS ONE
- 12 February 2016
A progressive series of assays are described to demonstrate the potential clinical value of a novel RORγ inverse agonist small molecule with high potency and selectivity, which will enter clinical trials in late 2015 for psoriasis patients.
Substituted 2-[(4-aminomethyl)phenoxy]-2-methylpropionic acid PPARalpha agonists. 1. Discovery of a novel series of potent HDLc raising agents.
- M. L. Sierra, Véronique Bénéton, P. Pianetti
- Biology, ChemistryJournal of Medicinal Chemistry
- 23 January 2007
Optimization of the series gave 25a, which shows EC50 = 4 nM on PPARalpha and at least 500-fold selectivity versus PPARdelta and PPARgamma, has been progressed to clinical trials for the treatment of diseases of lipid imbalance.
Co-activation of AMPK and mTORC1 Induces Cytotoxicity in Acute Myeloid Leukemia.
- P. Sujobert, L. Poulain, J. Tamburini
- Biology, ChemistryCell Reports
- 9 June 2015
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
- Jonathan T. Seal, Yann Lamotte, R. Prinjha
- ChemistryBioorganic & Medicinal Chemistry Letters
- 15 April 2012
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