Peptide versus Saccharide

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Science  12 Jul 2002:
Vol. 297, Issue 5579, pp. 161
DOI: 10.1126/science.297.5579.161b

Designing enzyme inhibitors on the basis of crystal structures of substrate complexes remains a challenging task. Taking advantage of naturally occurring inhibitors has been fruitful, especially because microorganisms have, in some cases, used synthetically-accessible building blocks. Chitinases, which hydrolyze linkages in insect and fungal polysaccharides, are an attractive target given the potential for selective inhibition of enzymatic function in pathogens such as Plasmodium. Houston et al. describe the structure of the complexes between chitinase and two cyclic pentapeptide inhibitors derived from fungi. The differences in how argifin and argadin fit within the active site help to explain their relative affinities and may provide clues for the development of drugs. — GJC

Proc. Natl. Acad. Sci. U.S.A.99, 9127 (2002).

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