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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
| Research |
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.
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| Collaborations |
Professor David P. Fairlie
Centre for Drug Design and Development
Institute for Molecular Bioscience
University of Queensland
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| Publications |
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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