Article
Enzyme adaptation to inhibitor binding: a cryptic binding site in phenylethanolamine N-methyltransferase.
Journal of medicinal chemistry - 4 Oct 2007
Gee Christine L, Drinkwater Nyssa, Tyndall Joel D A, Grunewald Gary L, Wu Qian, McLeish Michael J, Martin Jennifer L
Abstract excerpt
Shape complementarity is a fundamental principle of inhibitor design. Here we show that an enzyme for which the crystal structure has been determined (phenylethanolamine N-methyltransferase, PNMT) conceals a cryptic binding site. This site is revealed upon binding of inhibitors that are double th...
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