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

Author:

Tsoumpra Maria K.,Muniz Joao R.,Barnett Bobby L.,Kwaasi Aaron A.,Pilka Ewa S.,Kavanagh Kathryn L.,Evdokimov Artem,Walter Richard L.,Von Delft Frank,Ebetino Frank H.,Oppermann Udo,Russell R. Graham G.,Dunford James E.

Funder

Oxford NIHR Biomedical Research Unit, Arthritis Research UK

Structural Genomics Consortium

Publisher

Elsevier BV

Subject

Histology,Physiology,Endocrinology, Diabetes and Metabolism

Reference38 articles.

1. Mevalonate pathway: a review of clinical and therapeutical implications;Buhaescu;Clin. Biochem.,2007

2. Structure–activity relationships for inhibition of farnesyl diphosphate synthase in vitro and inhibition of bone resorption in vivo by nitrogen-containing bisphosphonates;Dunford;J. Pharmacol. Exp. Ther.,2001

3. Cellular and molecular mechanisms of action of bisphosphonates;Rogers;Cancer,2000

4. Heterocycle-containing bisphosphonates cause apoptosis and inhibit bone resorption by preventing protein prenylation: evidence from structure–activity relationships in J774 macrophages;Luckman;J. Bone Miner. Res.,1998

5. Protein geranylgeranylation is required for osteoclast formation, function, and survival: inhibition by bisphosphonates and GGTI-298;Coxon;J. Bone Miner. Res.,2000

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