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
<p>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 inhib...
Main Authors: | Tsoumpra, MK, Muniz, JR, Barnett, BL, Kwaasi, AA, Pilka, ES, Kavanagh, KL, Evdokimov, A, Walter, RL, Von Delft, F, Ebetino, FH, Oppermann, U, Russell, RGG, Dunford, JE |
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Format: | Journal article |
Language: | English |
Published: |
Elsevier
2015
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