Strategies for the isoform-selective regulation of protein function with small molecules

ORGN 737

Peter J. Belshaw1, Brock F. Binkowski2, Russel A. Miller2, Konstantin Levitsky2, Christopher J. Ciolli2, and Melissa D. Boersma2. (1) Department of Chemistry and Biochemistry, University of Wisconsin-Madison, 1101 University Ave, Madison, WI 53706, (2) Departments of Chemistry and Biochemistry, University of Wisconsin-Madison, 1101 University Ave, Madison, WI 53706
Methods for the isoform-specific regulation of protein function are of great importance as tools to determine the functions of proteins in cells, validate targets and develop therapeutics. We will describe our progress in developing approaches that utilize engineered receptors to obtain specificity in small molecule regulation. One approach utilizes proximity accelerated alkylation to impart specificity of small molecule targeting. Another approach utilizes allosteric regulation by small molecules of receptor binding to cellular targets.
 

Proteins, Peptides, and Amino Acids
8:00 AM-12:00 PM, Thursday, August 26, 2004 Pennsylvania Convention Center -- 201A, Oral

Division of Organic Chemistry

The 228th ACS National Meeting, in Philadelphia, PA, August 22-26, 2004