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Nucleic Acids Symposium Series 2007 51(1):63-64; doi:10.1093/nass/nrm032
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© 2007 Oxford University Press

Transition State Analogue Inhibitors of N-Ribosyltransferases: New Drugs by Targeting Nucleoside Processing Enzymes.

Gary B. Evans1, Richard H. Furneaux1, Peter M. Kelly1, Vern L. Schramm2 and Peter C. Tyler1,*

1Carbohydrate Chemistry, Industrial Research Ltd., Lower Hutt, New Zealand and
2Department of Biochemistry, Albert Einstein College of Medicine, Bronx, New York

*Corresponding Author. E-mail: p.tyler{at}irl.cri.nz

Abstract

The characterization of the transition state structure of a number of N-ribosyltransferases has enabled the design and synthesis of some extremely powerful inhibitors of these enzymes. We have three generations of inhibitors for some nucleoside processing enzymes which are therapeutic targets, and the potency of these compounds confers special advantages in their development as new drugs against cancer, autoimmune diseases, microbial infections and malaria.


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