Premium
Cover Picture: Studies of Glutathione Transferase P1‐1 Bound to a Platinum(IV)‐Based Anticancer Compound Reveal the Molecular Basis of Its Activation (Chem. Eur. J. 28/2011)
Author(s) -
Parker Lorien J.,
Italiano Louis C.,
Morton Craig J.,
Hancock Nancy C.,
Ascher David B.,
Aitken Jade B.,
Harris Hugh H.,
Campomanes Pablo,
Rothlisberger Ursula,
De Luca Anastasia,
Lo Bello Mario,
Ang Wee Han,
Dyson Paul J.,
Parker Michael W.
Publication year - 2011
Publication title -
chemistry – a european journal
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.687
H-Index - 242
eISSN - 1521-3765
pISSN - 0947-6539
DOI - 10.1002/chem.201190140
Subject(s) - chemistry , stereochemistry , conjugate , catenane , platinum , piperidine , covalent bond , molecule , biochemistry , catalysis , organic chemistry , mathematical analysis , mathematics
The effectiveness… of platinum‐based cancer drugs are limited by drug resistance and pi class glutathione S‐transferase, a major detoxifying enzyme, plays a role in this resistance. X‐ray crystallography and molecular modeling have been used to visualize how a platinum cancer drug (shown in ball‐and‐stick) is recognized by the dimeric enzyme (protein backbone shown as pink ribbons). The ethacrynate ligands (orange spheres), potent inhibitors of the enzyme, dissociate from the metal‐bound enzyme complex, where they likely diffuse through a surface cavity (grey surface) a short distance to the active sites of each monomer leading to enzymatic inhibition. For more details see the Full Paper by M. W. Parker et al. on page 7806 ff.