Small-molecule and mutational analysis of allosteric Eg5 inhibition by monastrol |
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| Authors: | Zoltan Maliga Timothy J Mitchison |
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| Institution: | (1) MPI-CBG, Pfotenhauer Strasse 108, 01307 Dresden, Germany;(2) Department of Systems Biology, Harvard Medical School, Boston, Massachusetts, USA |
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| Abstract: | Background A recent crystal structure of monastrol in a ternary complex with the kinesin Eg5 motor domain highlights a novel, induced-fit
drug binding site at atomic resolution. Mutational obliteration of the monastrol binding site results in a monastrol-resistant,
but otherwise catalytically active Eg5 motor domain. However, considering the conformational changes at this site, it is unclear
what specific interactions stabilize the interaction between monastrol and the Eg5 motor domain. |
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