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

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

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<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...

Bibliografski detalji
Glavni autori:	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
Format:	Journal article
Jezik:	English
Izdano:	Elsevier 2015

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Designed mutants of human farnesyl pyrophosphate synthase (FPPS) help to characterise the interactions of nitrogen-containing bisphosphonates with Tyrosine 204 and Phenylalanine 239 side-chain residues
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