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Dr Michael J Kelso
Department of Chemistry, BCC480
The Scripps Research Institute
10550 North Torrey Pines Road, La Jolla, CA 92037, USA
Email: mkelso@scripps edu
Tel: +1 (858)784-7529
Fax: +1 (858)784-7550
Homepage: http://www.scripps.edu/chem/boger/group.html

I have been involved with the design and synthesis of macrocyclic peptidomimetic inhibitors of HIV Protease. These potent inhibitors contained conformationally constrained macrocycles which mimic the b-strand substrate conformation known to be preferentially recognized by most, if not all, proteases. I have also worked on related molecules which comprehensive NMR studies showed to be conformationally locked into the b-strand conformation. Appropriate functionalization of these compounds offers a generic strategy for producing inhibitors of proteases with known substrate specificities.

Although not currently working with proteases I continue to have a standing interest in the field, and I am particularly interested in novel strategies for producing inhibitors of HIV Protease (and other viral proteases) which are able to circumvent the problems of viral resistance.
Professor David P. Fairlie
Centre for Drug Design and Development
Institute for Molecular Bioscience
University of Queensland
1) Kelso, M. J.; Fairlie, D. P. Current Approaches To Peptidomimetics in Molecular Pathomechanisms And New Trends In Drug Research, Chapter 44, pp. 579-598 (Eds Toth I & Keri G) Taylor & Francis London and New York (2003) ISBN 0-415-27725-6.

2)Reid, R. C.; Kelso, M. J.; Scanlon, M. J.; Fairlie, D. P. Conformationally Constrained Macrocycles That Mimic Tripeptide b-Strands In Water and Aprotic Solvents,
J. Am. Chem. Soc. 2002, 124, 5673-5683.

3) Kelso, M. J.; Hoang, H. N.; Oliver, W. N.; Sokolenko, N.; March, D. R.; Appleton, T. G.; Fairlie, D. P. A Cyclic Metallopeptide That Induces Alpha Helicity In Short Peptide Fragments of Thermolysin. Angew Chem, Int. Edit. 2003, 42, 421-424.

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