The inhibition of human farnesyl pyrophosphate synthase by nitrogen-containing bisphosphonates. Elucidating the role of active site threonine 201 and tyrosine 204 residues using enzyme mutants.

Farnesyl pyrophosphate synthase (FPPS) is the major molecular target of nitrogen-containing bisphosphonates (N-BPs), used clinically as bone resorption inhibitors. We investigated the role of threonine 201 (Thr201) and tyrosine 204 (Tyr204) residues in substrate binding, catalysis and inhibition by...

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Bibliographic Details
Main Authors: Tsoumpra, M, Muniz, JR, Barnett, B, Kwaasi, A, Pilka, E, Kavanagh, K, Evdokimov, A, Walter, R, Von Delft, F, Ebetino, F, Oppermann, U, Russell, G, Dunford, J
Format: Journal article
Language:English
Published: 2015