MEDI 73-Modeling, synthetic, crystallographic, and activity studies of novel bisphosphonates as inhibitors of farnesyl pyrophosphate synthase

Detalles Bibliográficos
Main Authors:	Hogan, J, Deprele, S, Kashemirov, B, Barnett, B, Evdokimov, A, Dunford, J, Russell, R, Ebetino, F, McKenna, C
Formato:	Journal article
Publicado:	2007

A mirror image pair of bisphosphonate analogs further demonstrates the mode of binding of the bisphosphonates in farnesyl pyrophosphate synthase
por: Ebetino, F, et al.
Publicado: (2008)

The mode of binding of nitrogen containing bisphosphonates in farnesyl pyrophosphate synthase
por: Ebetino, F, et al.
Publicado: (2007)

The Role of Active Site Threonine 201 in the Inhibition of Farnesyl Pyrophosphate Synthase by Nitrogen Containing Bisphosphonates
por: Dunford, J, et al.
Publicado: (2008)

Evidence for the involvement of the threonine 201 side-chain in the interaction of nitrogen-containing bisphosphonates with farnesyl pyrophosphate synthase
por: Kwassi, A, et al.
Publicado: (2009)

Analysis of the kinetic mechanism of inhibition of Farnesyl Pyrophosphate Synthase by nitrogen containing bisphosphonates.
por: Dunford, J, et al.
Publicado: (2006)

Kinetic analysis of conformational changes in farnesyl pyrophosphate synthase induced by nitrogen containing bisphosphonates
por: Dunford, J, et al.
Publicado: (2007)

The interaction of sidechain nitrogen with active site threonine is not essential for inhibition of farnesyl pyrophosphate synthase by nitrogen containing bisphosphonates
por: Dunford, J, et al.
Publicado: (2008)

Molecular interactions of nitrogen-containing bisphosphonates within farnesyl diphosphate synthase
por: Ebetino, F, et al.
Publicado: (2005)

Molecular modeling comparison of nitrogen-containing bisphosphonates of varying potency co-crystalized in farnesyl diphosphate synthase
por: Ebetino, F, et al.
Publicado: (2006)

Human farnesyl diphosphate synthase crystal structures with active and inactive bisphosphonates
por: Evdokimov, A, et al.
Publicado: (2006)

Structure activity relationships of nitrogen containing bisphosphonates which induce conformational changes in farnesyl pyrophosphate synthase
por: Dunford, J, et al.
Publicado: (2008)

Interaction of the active site threonine 201 sidechain with the nitrogen of nttrogen-containing bisphosphonates is not essential for slow tight inhibition to farnesyl pyrophosphate synthase
por: Dunford, J, et al.
Publicado: (2008)

Modeling of bisphosphonate binding to farnesyl diphosphate synthase
por: Ebetino, F, et al.
Publicado: (2002)

Refining structure activity relationships among nitrogen containing bisphosphonates: Dissociation of mineral binding affinity and inhibitory potency on farnesyl diphosphate synthase.
por: Xia, Z, et al.
Publicado: (2006)

Kinetic analysis of conformational changes in farnesyl pyrophosphate synthase induced by nitrogen containing bisphosphonates
por: Dunford, J, et al.
Publicado: (2007)

Stereochemical evidence of the mode of binding of nitrogen containing bisphosphonates in farnesyl diphosphate synthase
por: Ebetino, F, et al.
Publicado: (2007)

Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
por: Dunford, J, et al.
Publicado: (2008)

Molecular modeling comparison of nitrogen-containing bisphosphonates of varying potency co-crystalized in farnesyl diphosphate synthase
por: Ebetino, F, et al.
Publicado: (2006)

Nitrogen-containing bisphosphonates of varying antiresorptive potency have been co-crystallized in farnesyl diphosphate synthase and modelled to understand the key structural features involved in enzyme inhibition.
por: Ebetino, F, et al.
Publicado: (2006)

Predicting the clinical potencies of bisphosphonates: Divergence of hydroxyapatite and farnesyl diphosphate synthase binding affinities
por: Xia, Z, et al.
Publicado: (2007)

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
por: Tsoumpra, M, et al.
Publicado: (2010)

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.
por: Tsoumpra, M, et al.
Publicado: (2015)

Bisphosphonate affinity to hydroxyapatite and farnesyl pyrophosphate inhibitory potency, together, drive in vivo efficacy
por: Lundy, M, et al.
Publicado: (2007)

Investigations into the kinetic mechanism of inhibition of farnesyl diphosphate synthase by nitrogen containing bisphosphonates
por: Dunford, J, et al.
Publicado: (2006)

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
por: Tsoumpra, MK, et al.
Publicado: (2015)

Molecular modeling of the bisphosphonates (BPs) in farnesyl diphosphate (FPP) synthase. Proposed new mechanism of inhibition by potent nitrogen containing bisphosphonates (NBPs).
por: Ebetino, F, et al.
Publicado: (2002)

Molecular modeling of the bisphosphonates in farnesyl diphosphate synthase. potential new details of the precise biochemical mechanism of action of potent nitrogen containing bisphosphonates
por: Ebetino, F, et al.
Publicado: (2002)

Human farnesyl diphosphate synthase (FDFS): Crystal structure and molecular interactions with Nnitrogen-containing bisphosphonates.
por: Kavanagh, K, et al.
Publicado: (2005)

New anti-candida active nitrogen-containing bisphosphonates as inhibitors of farnesyl pyrophosphate synthase Candida albicans
por: L. O. Metelytsia, et al.
Publicado: (2019-05-01)

Correlation between time-dependent inhibition of human farnesyl pyrophosphate synthase and blockade of mevalonate pathway by nitrogen-containing bisphosphonates in cultured cells
por: Räikkönen, J, et al.
Publicado: (2011)

Correlation between time-dependent inhibition of human farnesyl pyrophosphate synthase and blockade of mevalonate pathway by nitrogen-containing bisphosphonates in cultured cells.
por: Räikkönen, J, et al.
Publicado: (2011)

Inhibition of human mevalonate kinase by allosteric inhibitors of farnesyl pyrophosphate synthase
por: Saman Salari, et al.
Publicado: (2024-08-01)

Molecular Cloning and Characterisation of Farnesyl Pyrophosphate Synthase from Tripterygium wilfordii.
por: Yu-Jun Zhao, et al.
Publicado: (2015-01-01)

Functional characterization of the Xanthophyllomyces dendrorhous farnesyl pyrophosphate synthase and geranylgeranyl pyrophosphate synthase encoding genes that are involved in the synthesis of isoprenoid precursors.
por: Jennifer Alcaíno, et al.
Publicado: (2014-01-01)

The relationship between the chemistry and biological activity of the bisphosphonates.
por: Ebetino, F, et al.
Publicado: (2011)

Crystal structures and molecular interactions of risedronate and zoledronate with human farnesyl diphosphate synthase
por: Kavanagh, K, et al.
Publicado: (2006)

Role of the geminal hydroxyl group in target enzyme inhibition by bisphosphonates and phosphonocarboxylates
por: Stewart, C, et al.
Publicado: (2007)

Differential effects of alpha-halogenation on the potency of bisphosphonates and phosphonocarboxylates for inhibition of their target enzymes
por: Stewart, C, et al.
Publicado: (2007)

Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
por: Marma, MS, et al.
Publicado: (2007)

Nitrogen-containing bisphosphonate induces enhancement of OPG expression and inhibition of RANKL expression via inhibition of farnesyl pyrophosphate synthase to inhibit the osteogenic differentiation and calcification in vascular smooth muscle cells
por: Wei Xu, et al.
Publicado: (2024-09-01)

MEDI 73-Modeling, synthetic, crystallographic, and activity studies of novel bisphosphonates as inhibitors of farnesyl pyrophosphate synthase

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