Mode of binding of E‐64‐c, a potent thiol protease inhibitor, to papain as determined by X‐ray crystal analysis of the complex
- 13 March 1989
- journal article
- Published by Wiley in FEBS Letters
- Vol. 245 (1-2) , 177-180
- https://doi.org/10.1016/0014-5793(89)80216-9
Abstract
The three-dimensional structure of the E-64-c-papain complex has been determined by X-ray crystal analysis at 2.5 Å resolution (conventional R = 26.9%). The structure determined indicates that: (i) the C2 atom of the oxirane ring of E-64-c is covalently bound by the Sγ atom of Cys-25 of papain; (ii) this covalent bond formation results in a configurational conversion of the oxirane C2 atom from the S- to the R-form; and (iii) extensive hydrogen bonding and hydrophobic interactions are responsible for the specific interaction of the E-64-c molecule with papainKeywords
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