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Abstract

Abstract: DESCRIPTION (provided by applicant): Chemical probes will be developed to profile toxicities resulting from drug interactions. We have developed fluorescent probes that exclusively identify active members of the serine hydrolase super-family of enzymes. Using our technique, we can elucidate activity profiles of diseases, and broadly investigate interactions between the proteome and potential therapeutics. This technology could be used to determine molecular toxicological profiles, rapidly and inexpensively, early in the drug development process. To expand the range of detectable toxicologies, we will design, synthesize, and characterize probes for the following pharmacologically interesting families: kinases, phosphatases, and cytochromes P450. Phase I will demonstrate the use of our current probes in investigating the protein interactions of various inhibitors of enzymes implicated in the etiology of diabetes, obesity, and Alzheimers disease. In phase II we will design and synthesize probes for kinases, phosphatases, cytochromes P450, and cysteine proteases. Phase II will include profiling various compounds and tissue sources, identifying toxicological markers, and creating a database of tissue-specific protein-compound interactions. PROPOSED COMMERCIAL APPLICATIONS: A service for accurately screening potential drugs for toxicity before animal trials will be commercialized. The database component will also be marketed for interrogation with proteomas, targets, or compounds.

Thesaurus Terms:
chemical synthesis, drug adverse effect, drug interaction, fluorescent dye /probe, protein engineering, protein structure function, proteomics, serine proteinase, toxicology
peptidyl dipeptidase, protein protein interaction
biotechnology

Institution:	ACTIVX BIOSCIENCES
	11025 N TORREY PINES RD, STE 120
	SAN DIEGO, CA 92037
Fiscal Year:	2002
Department:
Project Start:	08-AUG-2002
Project End:	07-FEB-2003
ICD:	NATIONAL CANCER INSTITUTE
IRG:	ZCA1