Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
about
Human isoprenoid synthase enzymes as therapeutic targetsFine-tuning multiprotein complexes using small moleculesExploring the role of receptor flexibility in structure-based drug discoveryExpanding the number of 'druggable' targets: non-enzymes and protein-protein interactionsTernary complex structures of human farnesyl pyrophosphate synthase bound with a novel inhibitor and secondary ligands provide insights into the molecular details of the enzyme’s active site closureHIV-1 Integrase Inhibitor-Inspired Antibacterials Targeting Isoprenoid BiosynthesisStructure of human farnesyl pyrophosphate synthase in complex with an aminopyridine bisphosphonate and two molecules of inorganic phosphateCrystal Structure of Human Soluble Adenylate Cyclase Reveals a Distinct, Highly Flexible Allosteric Bicarbonate Binding PocketSubstrate Deconstruction and the Nonadditivity of Enzyme RecognitionTaxodione and arenarone inhibit farnesyl diphosphate synthase by binding to the isopentenyl diphosphate siteDiscovery of Novel Allosteric Non-Bisphosphonate Inhibitors of Farnesyl Pyrophosphate Synthase by Integrated Lead FindingA General Strategy for Targeting Drugs to BoneDynamic Structure and Inhibition of a Malaria Drug Target: Geranylgeranyl Diphosphate SynthaseDetection of secondary binding sites in proteins using fragment screeningRecent trends and observations in the design of high-quality screening collections.Non-bisphosphonate inhibitors of isoprenoid biosynthesis identified via computer-aided drug design.Farnesyl diphosphate synthase inhibitors with unique ligand-binding geometriesSmall-molecule modulation of Ras signaling.Structural characterization of substrate and inhibitor binding to farnesyl pyrophosphate synthase from Pseudomonas aeruginosa.Isoprenoids and related pharmacological interventions: potential application in Alzheimer's disease.An enzyme-coupled continuous fluorescence assay for farnesyl diphosphate synthasesComputational Advances for the Development of Allosteric Modulators and Bitopic Ligands in G Protein-Coupled ReceptorsAntagonism screen for inhibitors of bacterial cell wall biogenesis uncovers an inhibitor of undecaprenyl diphosphate synthase.Formation of a Novel Macrocyclic Alkaloid from the Unnatural Farnesyl Diphosphate Analogue Anilinogeranyl Diphosphate by 5-Epi-Aristolochene Synthase.Fragment library screening identifies hits that bind to the non-catalytic surface of Pseudomonas aeruginosa DsbA1ASD v3.0: unraveling allosteric regulation with structural mechanisms and biological networks.Farnesyl diphosphate synthase inhibitors from in silico screening.Terpene biosynthesis: modularity rulesFarnesyl pyrophosphate synthase modulators: a patent review (2006 - 2010).Harnessing allostery: a novel approach to drug discovery.Approaches for Designing new Potent Inhibitors of Farnesyl Pyrophosphate Synthase.Targeting Cancer Cells with a Bisphosphonate Prodrug.The isoprenoid derivative N6 -benzyladenosine CM223 exerts antitumor effects in glioma patient-derived primary cells through the mevalonate pathway.Bisphosphonate inhibitors reveal a large elasticity of plastidic isoprenoid synthesis pathway in isoprene-emitting hybrid aspen.Structural propensities of human ubiquitination sites: accessibility, centrality and local conformation.Human farnesyl pyrophosphate synthase is allosterically inhibited by its own product.Bacterial Cell Growth Inhibitors Targeting Undecaprenyl Diphosphate Synthase and Undecaprenyl Diphosphate Phosphatase.A comparison of the dynamics of pantothenate synthetase from M. tuberculosis and E. coli: computational studies.Allosteric sites can be identified based on the residue-residue interaction energy difference.SEC-TID: A Label-Free Method for Small-Molecule Target Identification.
P2860
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P2860
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
description
2010 nî lūn-bûn
@nan
2010 թուականի Սեպտեմբերին հրատարակուած գիտական յօդուած
@hyw
2010 թվականի սեպտեմբերին հրատարակված գիտական հոդված
@hy
2010年の論文
@ja
2010年論文
@yue
2010年論文
@zh-hant
2010年論文
@zh-hk
2010年論文
@zh-mo
2010年論文
@zh-tw
2010年论文
@wuu
name
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@ast
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@en
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@nl
type
label
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@ast
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@en
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@nl
prefLabel
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@ast
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@en
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@nl
P2093
P356
P1476
Allosteric non-bisphosphonate FPPS inhibitors identified by fragment-based discovery
@en
P2093
Andreas Marzinzik
André Strauss
Chrystèle Henry
Francis Bitsch
J Fraser Glickman
Jean-Michel Rondeau
Jonathan R Green
Marjo Götte
Martin Geiser
René Hemmig
P2888
P356
10.1038/NCHEMBIO.421
P577
2010-09-01T00:00:00Z
P5875
P6179
1024680678