Constellation Pharmaceuticals | Date: 2016-09-27
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
Constellation Pharmaceuticals | Date: 2016-09-06
Constellation Pharmaceuticals | Date: 2015-04-02
Described herein are novel methods for treating subjects with a cancer which is not overexpressing at least one of BCL-xL, BCL-w, and BAD, and optionally further overexpressing BCL-2. Also provided herein are tools for determining and/or assessing, and for the administration of, cancer treatments involving BET bromodomain inhibitors, BCL-xL inhibitors, or combinations thereof.
Genentech and Constellation Pharmaceuticals | Date: 2015-11-25
The present invention relates to compounds of formula (I) or formula (II): and to salts thereof, wherein R^(1)-R^(4 )of formula (I) and R^(1)-R^(3 )of formula (II) have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) of formula (II) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders.
Genentech and Constellation Pharmaceuticals | Date: 2016-04-11
The present invention relates to use of CBP/EP300 bromodomain inhibitors for the treatment of cancer.
McGrath J.,Constellation Pharmaceuticals |
Trojer P.,Constellation Pharmaceuticals
Pharmacology and Therapeutics | Year: 2015
Within the vast landscape of histone modifications lysine methylation has gained increasing attention because of its profound regulatory potential. The methylation of lysine residues on histone proteins modulates chromatin structure and thereby contributes to the regulation of DNA-based nuclear processes such as transcription, replication and repair. Protein families with opposing catalytic activities, lysine methyltransferases (KMTs) and demethylases (KDMs), dynamically control levels of histone lysine methylation and individual enzymes within these families have become candidate oncology targets in recent years. A number of high quality small molecule inhibitors of these enzymes have been identified. Several of these compounds elicit selective cancer cell killing in vitro and robust efficacy in vivo, suggesting that targeting 'histone lysine methylation pathways' may be a relevant, emerging cancer therapeutic strategy. Here, we discuss individual histone lysine methylation pathway targets, the properties of currently available small molecule inhibitors and their application in the context of cancer. © 2015 Elsevier Inc. All rights reserved.
Constellation Pharmaceuticals | Date: 2015-08-28
Constellation Pharmaceuticals | Date: 2015-05-08
Constellation Pharmaceuticals | Date: 2015-03-18
Constellation Pharmaceuticals | Date: 2016-05-16
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.