Analysis of imatinib and sorafenib binding to p38α Compared with c-Abl and b-Raf provides structural insights for understanding the selectivity of inhibitors targeting the DFG-out form of protein kinases

Biochemistry

Volumn 49, Issue 17, 2010, Pages 3611-3618

  Namboodiri, Haridasan V ^a   Bukhtiyarova, Marina ^a   Ramcharan, Joseph ^a   Karpusas, Michael ^a,b   Lee, Younghee ^a   Springman, Eric B ^a,c  

^a Locus Pharmaceuticals   (United States)

^b AGRICULTURAL UNIVERSITY OF ATHENS   (Greece)

^c ATDC Biosciences Center   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BINDING INTERACTION; BINDING KINETICS; CLINICAL TRIAL; COCRYSTAL STRUCTURE; GLEEVEC; IMATINIB; KINASE INHIBITORS; KINASE TARGETS; LIGAND BINDING; PHASE II; PROTEIN KINASE; PROTEIN KINASES C; SOLVENT ACCESSIBLE SURFACE AREAS; SORAFENIB; STRUCTURAL DETERMINANTS; STRUCTURAL ELEMENTS; STRUCTURAL INSIGHTS; STRUCTURAL REQUIREMENTS; THERAPEUTIC INTERVENTION;

BINDING ENERGY; LIGANDS; STABILIZATION; TARGETS;

PROTEINS;

ABELSON KINASE; ASPARTYLPHENYLALANYLGLYCINE; B RAF KINASE; DORAMAPIMOD; GLYCINE DERIVATIVE; IMATINIB; LIGAND; MITOGEN ACTIVATED PROTEIN KINASE 14; PROTEIN; PROTEIN KINASE; PROTEIN KINASE INHIBITOR; SOLVENT; SORAFENIB; UNCLASSIFIED DRUG;

ARTICLE; BINDING KINETICS; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG PROTEIN BINDING; DRUG SELECTIVITY; DRUG TARGETING; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN STABILITY; PROTEIN STRUCTURE; STRUCTURE ACTIVITY RELATION;

BENZENESULFONATES; CRYSTALLOGRAPHY, X-RAY; HUMANS; MITOGEN-ACTIVATED PROTEIN KINASE 14; MODELS, MOLECULAR; MOLECULAR STRUCTURE; NAPHTHALENES; PIPERAZINES; PROTEIN BINDING; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; PROTO-ONCOGENE PROTEINS C-ABL; PYRAZOLES; PYRIDINES; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77951689893     PISSN: 00062960     EISSN: 15204995     Source Type: Journal    
DOI: 10.1021/bi100070r     Document Type: Article

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