LP99: Discovery and Synthesis of the First Selective BRD7/9 Bromodomain Inhibitor

Is there a link between selectivity and binding thermodynamics profiles?

(2015) Ákos Tarcsay et al.   DRUG DISCOVERY TODAY

BRD7, a Tumor Suppressor, Interacts with p85α and Regulates PI3K Activity

(2014) Yu-Hsin Chiu et al.   MOLECULAR CELL

Structure-based approaches towards identification of fragments for the low-druggability ATAD2 bromodomain

(2014) Apirat Chaikuad et al.   MedChemComm

Machine-assisted synthesis of modulators of the histone reader BRD9 using flow methods of chemistry and frontal affinity chromatography

(2014) Lucie Guetzoyan et al.   MedChemComm

Assessing cellular efficacy of bromodomain inhibitors using fluorescence recovery after photobleaching

(2014) Martin Philpott et al.   Epigenetics & Chromatin

TET2 and TET3 regulate GlcNAcylation and H3K4 methylation through OGT and SET1/COMPASS

(2013) Rachel Deplus et al.   EMBO JOURNAL

[1,2,4]Triazolo[4,3-a]phthalazines: Inhibitors of Diverse Bromodomains

(2013) Oleg Fedorov et al.   JOURNAL OF MEDICINAL CHEMISTRY

Stereoselective, nitro-Mannich/lactamisation cascades for the direct synthesis of heavily decorated 5-nitropiperidin-2-ones and related heterocycles

(2012) Pavol Jakubec et al.   Beilstein Journal of Organic Chemistry

Prognostic relevance of BRD7 expression in colorectal carcinoma

(2012) Wen-Jing Wu et al.   EUROPEAN JOURNAL OF CLINICAL INVESTIGATION

A New Family of Cinchona-Derived Bifunctional Asymmetric Phase-Transfer Catalysts: Application to the Enantio- and Diastereoselective Nitro-Mannich Reaction of Amidosulfones

(2012) Kayli M. Johnson et al.   ORGANIC LETTERS

BRD7, a Subunit of SWI/SNF Complexes, Binds Directly to BRCA1 and Regulates BRCA1-Dependent Transcription

(2010) M. T. Harte et al.   CANCER RESEARCH

Thermodynamics guided lead discovery and optimization

(2010) György G. Ferenczy et al.   DRUG DISCOVERY TODAY

BRD7 is a candidate tumour suppressor gene required for p53 function

(2010) Jarno Drost et al.   NATURE CELL BIOLOGY

The art of total synthesis through cascade reactions

(2009) K. C. Nicolaou et al.   CHEMICAL SOCIETY REVIEWS

Escape from Flatland: Increasing Saturation as an Approach to Improving Clinical Success

(2009) Frank Lovering et al.   JOURNAL OF MEDICINAL CHEMISTRY

Catalytic activity of the proteasome fine-tunes Brg1-mediated chromatin remodeling to regulate the expression of inflammatory genes

(2009) Sarah J. Cullen et al.   MOLECULAR IMMUNOLOGY

Tocilizumab

(2009) Clemens Scheinecker et al.   NATURE REVIEWS DRUG DISCOVERY

Integrative genomics analysis of chromosome 5p gain in cervical cancer reveals target over-expressed genes, including Drosha

(2008) Luigi Scotto et al.   Molecular Cancer