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Abstract
Grant Number: 1R21NS057066-01 Project Title: Development of cell-based assays for discovery of GIcNAc-TV inhibitors.
PI Information: Name Title CRAWFORD, BRETT E. bcrawford@zacharon.com Abstract: DESCRIPTION (provided by applicant): Malignant transformation induces changes in the structures of many glycans. One of the most consistent alterations observed in a wide range of cancers is the increased expression of beta 1,6 branched N-linked glycans. Genetic experiments and human clinical data have shown that beta 1,6 branched N-linked glycans directly promote cancer progression. The goal of this proposal is to develop a cell-based screening system to identify inhibitors of the biosynthesis of complex beta 1,6 branched N-linked glycans. Small molecule inhibitors of the biosynthesis of beta 1,6 branched N-linked glycans will be useful as tools to study the biological roles of these glycans and as starting points to develop novel anti-cancer agents. Relevant structural changes in N-linked glycans have been shown to be associated with malignant transformation and metastasis. Specifically, an increase in beta 1,6 branched N-linked glycans in tumors has been found to promote aggressive cancer progression. The goal of this proposal is to develop a system to identify small molecule inhibitors of the biosynthesis of complex beta 1,6 branched N-linked glycans for the development as a novel anti-cancer drugs.
Public Health Relevance:
This Public Health Relevance is not available.Thesaurus Terms:
chemical synthesis, hexosan, inhibitor /antagonist, pentosan, small molecule, technology /technique development
NIH Roadmap Initiative tag, bioassay, cell line, high throughput technology
Institution: ZACHARON PHARMACEUTICALS, INC. 505 COAST BLVD SOUTH, SUITE 106 LA JOLLA, CA 92037 Fiscal Year: 2006 Department: Project Start: 01-JUL-2006 Project End: 30-DEC-2007 ICD: NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE IRG: ZNS1