Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation
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Using a Fragment-Based Approach To Target Protein-Protein InteractionsStructural characterization of the apo form and NADH binary complex of human lactate dehydrogenasePyridomycin bridges the NADH- and substrate-binding pockets of the enoyl reductase InhAStructures of lactate dehydrogenase A (LDHA) in apo, ternary and inhibitor-bound formsMetabolic plasticity underpins innate and acquired resistance to LDHA inhibitionRegulation of pyruvate metabolism and human diseaseTargeting lactate dehydrogenase--a inhibits tumorigenesis and tumor progression in mouse models of lung cancer and impacts tumor-initiating cells.Mapping the protein interaction landscape for fully functionalized small-molecule probes in human cells.Quinoline 3-sulfonamides inhibit lactate dehydrogenase A and reverse aerobic glycolysis in cancer cells.Fragment-based screening by protein crystallography: successes and pitfalls.Protein crystallography and fragment-based drug design.Lactate dehydrogenase-B is silenced by promoter methylation in a high frequency of human breast cancers.Synergistic inhibitor binding to the papain-like protease of human SARS coronavirus: mechanistic and inhibitor design implications.Inhibition of lactate dehydrogenase activity as an approach to cancer therapy.Relationships between VEGF protein expression and pathological characteristics of diffuse large B cell lymphoma: a meta-analysis.Search for Human Lactate Dehydrogenase A Inhibitors Using Structure-Based Modeling.A Streamlined, Automated Protocol for the Production of Milligram Quantities of Untagged Recombinant Rat Lactate Dehydrogenase A Using ÄKTAxpressTM.Twenty years on: the impact of fragments on drug discovery.Anticancer agents that counteract tumor glycolysis.Assessing the differential action on cancer cells of LDH-A inhibitors based on the N-hydroxyindole-2-carboxylate (NHI) and malonic (Mal) scaffoldsDual targeting of the Warburg effect with a glucose-conjugated lactate dehydrogenase inhibitor.Small-molecule inhibitors of human LDH5.Targeting Metabolic Remodeling in Triple Negative Breast Cancer in a Murine Model.Cell Active Hydroxylactam Inhibitors of Human Lactate Dehydrogenase with Oral Bioavailability in MiceIdentification of New Structural Fragments for the Design of Lactate Dehydrogenase A InhibitorsIntercepting the Breslow intermediate via Claisen rearrangement: synthesis of complex tertiary alcohols without organometallic reagents.Human lactate dehydrogenase a inhibitors: a molecular dynamics investigation.Phenylethynyl-butyltellurium inhibits the sulfhydryl enzyme Na+, K+ -ATPase: an effect dependent on the tellurium atom.Cell death and cell lysis are separable events during pyroptosis.Symmetric molecules with 1,4-triazole moieties as potent inhibitors of tumour-associated lactate dehydrogenase-A.Three-Dimensional Analysis of the Interactions between hLDH5 and Its Inhibitors.Discovery and Optimization of Potent, Cell-Active Pyrazole-Based Inhibitors of Lactate Dehydrogenase (LDH).Exploiting Metabolic Vulnerabilities of Cancer with Precision and Accuracy.Development and validation of a docking-based virtual screening platform for the identification of new lactate dehydrogenase inhibitors.A Virtual Screening Study for Lactate Dehydrogenase 5 Inhibitors by Using a Pharmacophore-based Approach.A widely-applicable high-throughput cellular thermal shift assay (CETSA) using split Nano Luciferase.
P2860
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P2860
Design and synthesis of novel lactate dehydrogenase A inhibitors by fragment-based lead generation
description
2012 nî lūn-bûn
@nan
2012 թուականի Ապրիլին հրատարակուած գիտական յօդուած
@hyw
2012 թվականի ապրիլին հրատարակված գիտական հոդված
@hy
2012年の論文
@ja
2012年論文
@yue
2012年論文
@zh-hant
2012年論文
@zh-hk
2012年論文
@zh-mo
2012年論文
@zh-tw
2012年论文
@wuu
name
Design and synthesis of novel ...... fragment-based lead generation
@ast
Design and synthesis of novel ...... fragment-based lead generation
@en
Design and synthesis of novel ...... fragment-based lead generation
@nl
type
label
Design and synthesis of novel ...... fragment-based lead generation
@ast
Design and synthesis of novel ...... fragment-based lead generation
@en
Design and synthesis of novel ...... fragment-based lead generation
@nl
prefLabel
Design and synthesis of novel ...... fragment-based lead generation
@ast
Design and synthesis of novel ...... fragment-based lead generation
@en
Design and synthesis of novel ...... fragment-based lead generation
@nl
P2093
P356
P1476
Design and synthesis of novel ...... fragment-based lead generation
@en
P2093
Claire Brassington
David Whittaker
Gareth Davies
Geoffrey A Holdgate
Giles Hassall
Jon Winter
Jonathan Tart
Jonathan Wingfield
Julie A Tucker
Kevin Hudson
P304
P356
10.1021/JM201734R
P407
P577
2012-03-26T00:00:00Z