Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
about
Developing irreversible inhibitors of the protein kinase cysteinomeDiscovery of Potent and Selective Covalent Inhibitors of JNKElectrophilic Fragment-Based Design of Reversible Covalent Kinase InhibitorsReversible targeting of noncatalytic cysteines with chemically tuned electrophilesPseudokinases: update on their functions and evaluation as new drug targets.Design, Synthesis, and Biological Evaluation of Novel Conformationally Constrained Inhibitors Targeting EGFR.Ibrutinib, a Bruton's tyrosine kinase inhibitor, exhibits antitumoral activity and induces autophagy in glioblastoma.A road map to evaluate the proteome-wide selectivity of covalent kinase inhibitors.Development of covalent inhibitors that can overcome resistance to first-generation FGFR kinase inhibitors.DFG-out mode of inhibition by an irreversible type-1 inhibitor capable of overcoming gate-keeper mutations in FGF receptors.Bruton's TK inhibitors: structural insights and evolution of clinical candidates.Identification of Covalent Bromodomain Binders through DNA Display of Small Molecules.Prolonged and tunable residence time using reversible covalent kinase inhibitors.Identification and Characterization of an Irreversible Inhibitor of CDK2.An NMR-Guided Screening Method for Selective Fragment Docking and Synthesis of a Warhead Inhibitor.Irreversible inhibitors of c-Src kinase that target a nonconserved cysteine.Hypothemycin, a fungal natural product, identifies therapeutic targets in Trypanosoma brucei [corrected].Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance.Targeting protein kinases with selective and semipromiscuous covalent inhibitors.New drug design with covalent modifiers.Targeted Covalent Inhibitors for Drug Design.A general approach for the development of fluorogenic probes suitable for no-wash imaging of kinases in live cells.Ibrutinib (ImbruvicaTM) potently inhibits ErbB receptor phosphorylation and cell viability of ErbB2-positive breast cancer cells.Recent Development of the Second and Third Generation Irreversible Epidermal Growth Factor Receptor Inhibitors.Rational design of resorcylic acid lactone analogues as covalent MNK1/2 kinase inhibitors by tuning the reactivity of an enamide Michael acceptor.Molecular insights into cancer therapeutic effects of the dietary medicinal phytochemical withaferin A.Advances of small molecule targeting of kinases.Irreversible Nek2 kinase inhibitors with cellular activity.Data driven polypharmacological drug design for lung cancer: analyses for targeting ALK, MET, and EGFR.Reversible covalent inhibition of eEF-2K by carbonitriles.Design, synthesis, and in vitro evaluation of a fluorescently labeled irreversible inhibitor of the catalytic subunit of cAMP-dependent protein kinase (PKACα).Proteome-wide Map of Targets of T790M-EGFR-Directed Covalent Inhibitors.Synthesis of deoxyelephantopin analogues.Kinase-targeted cancer therapies: progress, challenges and future directions.Protein-ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling
P2860
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P2860
Cysteine mapping in conformationally distinct kinase nucleotide binding sites: application to the design of selective covalent inhibitors.
description
2011 nî lūn-bûn
@nan
2011年の論文
@ja
2011年論文
@yue
2011年論文
@zh-hant
2011年論文
@zh-hk
2011年論文
@zh-mo
2011年論文
@zh-tw
2011年论文
@wuu
2011年论文
@zh
2011年论文
@zh-cn
name
Cysteine mapping in conformati ...... selective covalent inhibitors.
@en
Cysteine mapping in conformati ...... selective covalent inhibitors.
@nl
type
label
Cysteine mapping in conformati ...... selective covalent inhibitors.
@en
Cysteine mapping in conformati ...... selective covalent inhibitors.
@nl
prefLabel
Cysteine mapping in conformati ...... selective covalent inhibitors.
@en
Cysteine mapping in conformati ...... selective covalent inhibitors.
@nl
P2093
P356
P1476
Cysteine mapping in conformati ...... selective covalent inhibitors
@en
P2093
Dino Moras
Emeline Leproult
Sofia Barluenga
P304
P356
10.1021/JM101396Q
P407
P577
2011-02-15T00:00:00Z