Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors - Test2 - elhamkhani - TriplyDB

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

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Delineation of Polypharmacology across the Human Structural Kinome Using a Functional Site Interaction Fingerprint Approach Implications of the small number of distinct ligand binding pockets in proteins for drug discovery, evolution and biochemical function Electrophilic Fragment-Based Design of Reversible Covalent Kinase Inhibitors Substrate and Inhibitor Specificity of the Type II p21-Activated Kinase, PAK6 Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation Emergence of polyclonal FLT3 tyrosine kinase domain mutations during sequential therapy with sorafenib and sunitinib in FLT3-ITD-positive acute myeloid leukemia.Disruption of Angiogenesis by Anthocyanin-Rich Extracts of Hibiscus sabdariffa.Potent anti-angiogenesis and anti-tumor activity of a novel human anti-VEGF antibody, MIL60.In silico discovery of potential VEGFR-2 inhibitors from natural derivatives for anti-angiogenesis therapy.FLT3 kinase inhibitor TTT-3002 overcomes both activating and drug resistance mutations in FLT3 in acute myeloid leukemia.Retrospective review using targeted deep sequencing reveals mutational differences between gastroesophageal junction and gastric carcinomas.Crystal structure of the FLT3 kinase domain bound to the inhibitor Quizartinib (AC220).Tyrosine kinase inhibitors directed against the vascular endothelial growth factor receptor (VEGFR) have distinct cutaneous toxicity profiles: a meta-analysis and review of the literature.Computer-guided design, synthesis, and biological evaluation of quinoxalinebisarylureas as FLT3 inhibitors.Studies on [5,6]-Fused Bicyclic Scaffolds Derivatives as Potent Dual B-RafV600E/KDR Inhibitors Using Docking and 3D-QSAR Approaches.Targeting kinases with anilinopyrimidines: discovery of N-phenyl-N'-[4-(pyrimidin-4-ylamino)phenyl]urea derivatives as selective inhibitors of class III receptor tyrosine kinase subfamily.Motif mimetic of epsin perturbs tumor growth and metastasis Pharmacological targeting of VEGFR signaling with axitinib inhibits Tsc2-null lesion growth in the mouse model of lymphangioleiomyomatosis Single agent efficacy of the VEGFR kinase inhibitor axitinib in preclinical models of glioblastoma Discovery of Potent VEGFR-2 Inhibitors based on Furopyrimidine and Thienopyrimidne Scaffolds as Cancer Targeting Agents.Platelet-derived growth factor/vascular endothelial growth factor receptor inactivation by sunitinib results in Tsc1/Tsc2-dependent inhibition of TORC1 Electrochemical monitoring of an important biomarker and target protein: VEGFR2 in cell lysates.Structural characterization of nonactive site, TrkA-selective kinase inhibitors.Ruthenium(ii) p-cymene complexes of a benzimidazole-based ligand capable of VEGFR2 inhibition: hydrolysis, reactivity and cytotoxicity studies.Development of anti-angiogenic tyrosine kinases inhibitors: molecular structures and binding modes.Discovery and preclinical evaluation of 7-benzyl-N-(substituted)-pyrrolo[3,2-d]pyrimidin-4-amines as single agents with microtubule targeting effects along with triple-acting angiokinase inhibition as antitumor agents.Synthesis and Evaluation of Novel 2-Pyrrolidone-Fused (2-Oxoindolin-3-ylidene)methylpyrrole Derivatives as Potential Multi-Target Tyrosine Kinase Receptor Inhibitors.Discovery of new 4-alkoxyquinazoline-based derivatives as potent VEGFR2 inhibitors.The contribution of VEGF signalling to fostamatinib-induced blood pressure elevation.Kinase inhibitor pharmacokinetics: comprehensive summary and roadmap for addressing inter-individual variability in exposure.Characterization of interactions and pharmacophore development for DFG-out inhibitors to RET tyrosine kinase.Design, synthesis, biological evaluation, and molecular modeling study of 4-alkoxyquinazoline derivatives as potential VEGFR2 kinase inhibitors.Evolution of a New Class of VEGFR-2 Inhibitors from Scaffold Morphing and Redesign.NDEL1-PDGFRB fusion gene in a myeloid malignancy with eosinophilia associated with resistance to tyrosine kinase inhibitors.In vitro pharmacological profiling of R406 identifies molecular targets underlying the clinical effects of fostamatinib.Distinct binding mode of multikinase inhibitor lenvatinib revealed by biochemical characterization.Global connectivity of hub residues in Oncoprotein structures encodes genetic factors dictating personalized drug response to targeted Cancer therapy.An Alignment-Independent 3D-QSAR Study of FGFR2 Tyrosine Kinase Inhibitors.Structural optimization and evaluation of novel 2-pyrrolidone-fused (2-oxoindolin-3-ylidene)methylpyrrole derivatives as potential VEGFR-2/PDGFRβ inhibitors.MicroRNAs Associated with Von Hippel-Lindau Pathway in Renal Cell Carcinoma: A Comprehensive Review.

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P2860

Molecular conformations, interactions, and properties associated with drug efficiency and clinical performance among VEGFR TK inhibitors

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Proceedings of the National Academy of Sciences of the United States of America

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Molecular conformations, inter ...... ance among VEGFR TK inhibitors

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Brion William Murray

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James Solowiej

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Jeffrey H Chen

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Michele McTigue

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Robert S Kania

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Ya-Li Deng

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P2860

Crystallography & NMR System: A New Software Suite for Macromolecular Structure Determination

Crystal structure of the kinase domain of human vascular endothelial growth factor receptor 2: a key enzyme in angiogenesis

The structural basis for autoinhibition of FLT3 by the juxtamembrane domain

The 2.7 A crystal structure of the autoinhibited human c-Fms kinase domain

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation

KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patients

Refinement of macromolecular structures by the maximum-likelihood method

Features and development of Coot

A quantitative analysis of kinase inhibitor selectivity

Data processing and analysis with the autoPROC toolbox

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