The Center for Integrative Chemical Biology and Drug Discovery was created with the mission of bringing dedicated medicinal chemistry expertise to bear on biological targets of therapeutic relevance under investigation by UNC faculty. Synthetic chemists, assay development and compound profiling scientists will work in the Center and create dedicated, multidisciplinary project teams with other groups on campus in order to progress targets through the drug discovery and development process.  The Center provides leadership of the North Carolina Comprehensive Chemical Biology Center, a member of NCI's Chemical Biology Consortium.

Conference News

Stephen Frye to speak at Molecular Therapeutics of Cancer Research Conference, July 14-18, 2013, Boulder, CO.  More information/registration

Research & Funding News

Chemical probe for the L3MBTL3 methyllysine reader domain featured on cover of Nature Chemical Biology, January 2013. See paper by Lindsey James et al. in collaboration with the Structural Genomics Consortium and U. Toronto.    Article Cover See also ESOP feature.

Efficient Solution-Phase Synthesis of 4,5,7-Trisubstituted Pyrrolo[3,2-d]pyrimidines published by Weihe Zhang et al. in ACS Combinatorial Science, 2013, 15 (1), pp 10–19.

Structure–activity relationships of methyl-lysine reader antagonists published by J.M. Herold, Lindsey James, et al. published in Med. Chem. Commun., 2012, 3, 45-51.

Assessment of free energy predictors for ligand binding to a methyllysine histone code reader published by C. Gao, J.M. Herold & D. Kireev in J Comput Chem 2012, 33 (6), 659-665.

Inhibitors of Streptococcus pneumoniae Surface Endonuclease EndA Discovered by High-Throughput Screening Using a PicoGreen Fluorescence Assay published by in collaboration with Eliza Peterson and Scott Singleton in . J Biomol Screen 2012.

High-Throughput Screening for RecA Inhibitors Using a Transcreener Adenosine 5 '-O-Diphosphate Assay published in collaboration with Peterson & Singleton in Assay Drug Dev. Technol. 2012, 10 (3), 260-268.

Development of a High-Throughput Assay for Identifying Inhibitors of TBK1 and IKKepsilon published with collaborators J. Hutti and A. Baldwin in PLoS ONE 2012, 7 (7), e41494.

Structure-Functional Selectivity Relationship Studies of Beta-arrestin-biased Dopamine D₂Receptor Agonists published by Xin Chen, Jian Jin, et al. in J. Med Chem 55, 7141-7153.

Combined PI3K/mTOR and MEK Inhibition Provides Broad Anti-Tumor Activity in Faithful Murine Cancer Models published with collaborators Zamboni, Johnson, Perou and Sharpless in Clinical Cancer Research 2012 (DOI: 10:1158/1078-0432.CCR-12-0563).

Orally Active Adenosine A1 Receptor Agonists with Antinociceptive Effects in Mice published with collaborator Mark Zylka in J. Med Chem 2012, vol. 55 (in press), DOI:10.1021/jm3004834.

An Allosteric Inhibitor of Protein Arginine Methyltransferase 3 published with collaborators from SGC in Structure 2012, in press, DOI: 10.1016/ j.str.2012.1006.1001.

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer published in Cell, vol. 149 (2), 307-321, April 13, 2012 by collaborator Gary Johnson et al.