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.

RESEARCH & FUNDING NEWS

Targeting protein lysine methylation and demethylation in cancers published in Acta Biochim Biophsy Sin, 2012.

Jian Jin and Xin Chen contribute to Nature publication with collaborators Ben Philpot*, Bryan Roth and Mark Zylka:  Topoisomerase inhibitors unsilence the dormant allele of Ube3a in neurons.  Nature 2011, DOI:10.1036/nature10726 published online 12/21/11.

Jin and Roth PNAS publication highlighted in SciBX Cover Story:  Targets and Mechanisms.

MBT Domain Antagonist UNC669 now available from EMD Chemicals.  See online publication by Herold et al. 

Structure-activity relationships of methyl-lysine reader antagonists. Concise article published online Oct. 10, 2011 in  Med. Chem. Commun.

Discovery by Jian Jin and Bryan Roth could lead to improvements in schizophrenia drugs.   View article in PNAS Early Edition

Jian Jin & molecular probe UNC0638 for G9a & GLP featured in UNC Endeavors post on Oct. 4, 2011.

Published in International Drug Discovery  Aug/Sep - Janzen & Hull-Ryde.  Kinases as Targets for Drug Discovery in an Academic Setting

Published Online July 22, 2011 in J. Medicinal Chemistry.  Optimization of Cellular Activity of G9a Inhibitors 7-Aminoalkoxy-quinazolines

Published Online July 10, 2011 in Nature Chemical Biology. A Chemical Probe Selectively Inhibits G9a and GLP Methyltransferase Activity in Cells 

Published online June 1, 2011 - Frye, Crosby, Edwards, & Juliano. US academic drug discovery

Published online May 13, 2011 - Liu and Wang. Microwave-Assisted, Divergent Solution-Phase Synthesis of 1,3,6-Trisubstituted Pyrazolo[3,4-d]pyrimidines

Third Drug Discovery Contract awarded for Cancer Target

In August 2011 SAIC-Frederick, Inc., a prime contractor to the National Cancer Institute, extended UNC's contract for discovery of drugs to treat childhood leukemia based on milestones achieved during the first 12 months.  The second contract, focused on brain tumors, is ongoing.  In October SAIC awarded a third contract to UNC for a cancer target from NCI's NeXT program. 

Stephen Frye, PhD, professor in the division of chemical biology and medicinal chemistry, and director of the UNC Center for Integrative Chemical Biology and Drug Discovery in the UNC Eshelman School of Pharmacy, is the lead principal investigator for the contracts. Frye is also a member of UNC Lineberger Comprehensive Cancer Center. The two centers are collaborating on all three projects.