Title : Thermodynamic evaluation of the binding of bisphosphonates to human farnesyl pyrophosphate synthase.

Pub. Date : 2014

PMID : 24172032






9 Functional Relationships(s)
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1 Thermodynamic evaluation of the binding of bisphosphonates to human farnesyl pyrophosphate synthase. Diphosphonates farnesyl diphosphate synthase Homo sapiens
2 BPs with nitrogen-containing side chains (N-BPs) are known to act as inhibitors for farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Diphosphonates farnesyl diphosphate synthase Homo sapiens
3 BPs with nitrogen-containing side chains (N-BPs) are known to act as inhibitors for farnesyl pyrophosphate synthase (FPPS), a key enzyme in the mevalonate pathway. Diphosphonates farnesyl diphosphate synthase Homo sapiens
4 In this study, we evaluated the effect of different side chains on the binding affinity of BPs to human FPPS using calorimetric techniques. Diphosphonates farnesyl diphosphate synthase Homo sapiens
5 Differential scanning calorimetry (DSC) was used to determine the thermal unfolding of FPPS in the presence of BPs. Diphosphonates farnesyl diphosphate synthase Homo sapiens
6 The addition of a series of clinically available BPs increased the structural stability of human FPPS by preferential binding, as indicated by an increase in the FPPS unfolding temperature. Diphosphonates farnesyl diphosphate synthase Homo sapiens
7 The addition of a series of clinically available BPs increased the structural stability of human FPPS by preferential binding, as indicated by an increase in the FPPS unfolding temperature. Diphosphonates farnesyl diphosphate synthase Homo sapiens
8 The magnitude of the increase was correlated with in vivo antiresorptive efficacy, suggesting that the stabilization of FPPS underlies the inhibitory effect of the BPs. Diphosphonates farnesyl diphosphate synthase Homo sapiens
9 Isothermal titration calorimetry (ITC) experiments were performed to evaluate the binding thermodynamics of BPs against human FPPS. Diphosphonates farnesyl diphosphate synthase Homo sapiens