Literature DB >> 20801032

Novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase.

Joris W De Schutter1, Serge Zaretsky, Sarah Welbourn, Arnim Pause, Youla S Tsantrizos.   

Abstract

A structure-based approach was pursued in designing novel bisphosphonate inhibitors of the human farnesyl pyrophosphate synthase (hFPPS). Preliminary SAR and structural evidence for the simultaneous binding of these inhibitors into the isopentenyl pyrophosphate (IPP) and the geranyl pyrophosphate (GPP) substrate sub-pockets of the enzyme are presented. Copyright (c) 2010 Elsevier Ltd. All rights reserved.

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Year:  2010        PMID: 20801032     DOI: 10.1016/j.bmcl.2010.07.133

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  2 in total

1.  1-(Fluoroalkylidene)-1,1-bisphosphonic acids are potent and selective inhibitors of the enzymatic activity of Toxoplasma gondii farnesyl pyrophosphate synthase.

Authors:  Sergio H Szajnman; Valeria S Rosso; Leena Malayil; Alyssa Smith; Silvia N J Moreno; Roberto Docampo; Juan B Rodriguez
Journal:  Org Biomol Chem       Date:  2012-01-03       Impact factor: 3.876

2.  An enzyme-coupled continuous fluorescence assay for farnesyl diphosphate synthases.

Authors:  Jonathan K Dozier; Mark D Distefano
Journal:  Anal Biochem       Date:  2011-10-28       Impact factor: 3.365

  2 in total

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