The ins and outs of selective kinase inhibitor development.
about
Delineation of Polypharmacology across the Human Structural Kinome Using a Functional Site Interaction Fingerprint ApproachStructural and Biochemical Basis for Intracellular Kinase Inhibition by Src-specific Peptidic MacrocyclesImatinib binding to human c-Src is coupled to inter-domain allostery and suggests a novel kinase inhibition strategyTargeting kinase signaling pathways with constrained peptide scaffolds.Data on evolution of intrinsically disordered regions of the human kinome and contribution of FAK1 IDRs to cytoskeletal remodeling.Regulation of Ste20-like kinase, SLK, activity: Dimerization and activation segment phosphorylation.Insights into the binding mode of MEK type-III inhibitors. A step towards discovering and designing allosteric kinase inhibitors across the human kinomeDetermining Cysteines Available for Covalent Inhibition Across the Human Kinome.Discovery of a novel allosteric inhibitor-binding site in ERK5: comparison with the canonical kinase hinge ATP-binding site.Dichotomy of cellular inhibition by small-molecule inhibitors revealed by single-cell analysis.Selective Phosphorylation Inhibitor of Delta Protein Kinase C-Pyruvate Dehydrogenase Kinase Protein-Protein Interactions: Application for Myocardial Injury in Vivo.Privileged Electrophile Sensors: A Resource for Covalent Drug Development.High-throughput screening of a GlaxoSmithKline protein kinase inhibitor set identifies an inhibitor of human cytomegalovirus replication that prevents CREB and histone H3 post-translational modification.From Type I to Type II: Design, Synthesis, and Characterization of Potent Pyrazin-2-ones as DFG-Out Inhibitors of PDGFRβ.Combating mutations in genetic disease and drug resistance: understanding molecular mechanisms to guide drug design.Selective JAK3 Inhibitors with a Covalent Reversible Binding Mode Targeting a New Induced Fit Binding Pocket.Allosteric inhibition of Aurora-A kinase by a synthetic vNAR domain.Mapping of inhibitors and activity data to the human kinome and exploring promiscuity from a ligand and target perspective.Structure-Guided Strategy for the Development of Potent Bivalent ERK Inhibitors.Defined, serum/feeder-free conditions for expansion and drug screening of primary B-acute lymphoblastic leukemia.Pockets as structural descriptors of EGFR kinase conformations.A Comprehensive Structural Overview of p38α Mitogen-Activated Protein Kinase in Complex with ATP-Site and Non-ATP-Site Binders.PAK4 crystal structures suggest unusual kinase conformational movements.A continuous luminescence assay for monitoring kinase activity: signalling the ADP/ATP ratio using a discrete europium complex.Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature.A Chemical Probe Strategy for Interrogating Inhibitor Selectivity Across the MEK Kinase Family.Enhancing the selectivity of kinase inhibitors in oncology: a chemical biology perspective.Structural characterization of the heme-based oxygen sensor, AfGcHK, its interactions with the cognate response regulator, and their combined mechanism of action in a bacterial two-component signaling system.Effects of rigidity on the selectivity of protein kinase inhibitors.RIPK1-dependent cell death: a novel target of the Aurora kinase inhibitor Tozasertib (VX-680).Target class drug discovery.Slowly on, Slowly off: Bisubstrate-Analogue Conjugates of 5-Iodotubercidin and Histone H3 Peptide Targeting Protein Kinase Haspin.Structural pliability adjacent to the kinase domain highlights contribution of FAK1 IDRs to cytoskeletal remodeling.Src signaling in a low-complexity unicellular kinome.High yield bacterial expression, purification and characterisation of bioactive Human Tousled-like Kinase 1B involved in cancer.Casein kinase 1ε and 1α as novel players in polycystic kidney disease and mechanistic targets for (R)-roscovitine and (S)-CR8.
P2860
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P2860
The ins and outs of selective kinase inhibitor development.
description
2015 nî lūn-bûn
@nan
2015年の論文
@ja
2015年論文
@yue
2015年論文
@zh-hant
2015年論文
@zh-hk
2015年論文
@zh-mo
2015年論文
@zh-tw
2015年论文
@wuu
2015年论文
@zh
2015年论文
@zh-cn
name
The ins and outs of selective kinase inhibitor development.
@ast
The ins and outs of selective kinase inhibitor development.
@en
type
label
The ins and outs of selective kinase inhibitor development.
@ast
The ins and outs of selective kinase inhibitor development.
@en
prefLabel
The ins and outs of selective kinase inhibitor development.
@ast
The ins and outs of selective kinase inhibitor development.
@en
P2860
P356
P1476
The ins and outs of selective kinase inhibitor development.
@en
P2093
Nathanael S Gray
Susanne Müller
P2860
P2888
P304
P356
10.1038/NCHEMBIO.1938
P577
2015-10-01T00:00:00Z
P6179
1014924974