The Synthesis of N-Ribosyl Transferase Inhibitors Based on a Transition State Blueprint
Gary B. Evans AA Industrial Research Limited, P.O. Box 31-310, Lower Hutt, New Zealand (e-mail: g.evans@irl.cri.nz).
Gary Evans received his first class B.Sc.(Hons) from the University of Otago in 1988 and his Ph.D. from the same institution in 1991. The same year, he began an 18 month post-doctoral fellowship with S. G. Davies at Oxford University and then joined Oxford Asymmetry as head chemist in 1992. He returned to New Zealand in 1994 as a New Zealand Science and Technology postdoctoral fellow within the Carbohydrate Chemistry Team at Industrial Research, studying the antibacterial properties of totarol and its derivatives. Upon completion of this fellowship he was instrumental in establishing process development capabilities within the Carbohydrate Chemistry Team. His current research interests focus on the application of transition state analysis to the design and synthesis of enzyme inhibitors. |
Australian Journal of Chemistry 57(9) 837-854 https://doi.org/10.1071/CH04112
Submitted: 29 April 2004 Accepted: 1 July 2004 Published: 1 September 2004
Abstract
A quarter of a century ago transition state analysis and transition state analogue design promised the prospect of extraordinarily potent enzyme inhibitors. The present overview describes the transition state analysis of a variety of N-ribosyl transferases, the design and synthesis of extremely powerful transition state analogue inhibitors of these nucleoside processing enzymes, and their current therapeutic uses and potentials.
Acknowledgments
I thank Dr Richard Furneaux and Dr Peter Tyler for their assistance in the preparation of this review.
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