Conformational analysis of the DFG-out kinase motif and biochemical profiling of structurally validated type II inhibitors

Journal of Medicinal Chemistry

Volumn 58, Issue 1, 2015, Pages 466-479

  Vijayan, R S K ^a   He, Peng ^a   Modi, Vivek ^b   Duong Ly, Krisna C ^b   Ma, Haiching ^c   Peterson, Jeffrey R ^b   Dunbrack, Roland L ^b   Levy, Ronald M ^a  

^a Temple University   (United States)

^b FOX CHASE CANCER CENTER   (United States)

^c REACTION BIOLOGY CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ASPARTIC ACID; AZ 628; B RAF KINASE INHIBITOR; B RAF KINASE INHIBITOR 1; BAFETINIB; BARASERTIB; DASATINIB; DORAMAPIMOD; DORSOMORPHIN; E 804; FORETINIB; IMATINIB; INDIRUBIN; MOTESANIB; N [3 (5 CHLORO 1H PYRROLO[2,3 B]PYRIDINE 3 CARBONYL) 2,4 DIFLUOROPHENYL]PROPANESULFONAMIDE; N [4 [(2 AMINO 3 CHLORO 4 PYRIDINYL)OXY] 3 FLUOROPHENYL] 4 ETHOXY 1 (4 FLUOROPHENYL) 2(1H) OXONICOTINAMIDE; NILOTINIB; PHOSPHOTRANSFERASE; PROTEIN KINASE INHIBITOR; PROTEIN KINASE TYPE 2 INHIBITOR; PROTEIN TYROSINE KINASE; REBASTINIB; SORAFENIB; SUNITINIB; TIVOZANIB; UNCLASSIFIED DRUG; MOLECULAR LIBRARY; PROTEIN BINDING; PROTEIN KINASE; PROTEOME;

ARTICLE; BIOCHEMICAL ANALYSIS; CARBOXY TERMINAL SEQUENCE; COMPARATIVE STUDY; CONFORMATIONAL TRANSITION; CROSS REACTION; CRYSTAL STRUCTURE; DRUG STRUCTURE; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME CONFORMATION; ENZYME STRUCTURE; HUMAN; HYDROGEN BOND; MOLECULAR DYNAMICS; PHYLOGENETIC TREE; ALLOSTERISM; AMINO ACID SEQUENCE; ANTAGONISTS AND INHIBITORS; BINDING SITE; BIOCATALYSIS; CHEMICAL STRUCTURE; CHEMISTRY; DRUG EFFECTS; METABOLISM; MOLECULAR LIBRARY; PHARMACOLOGY; PROTEIN CONFORMATION; PROTEIN DATABASE; PROTEIN MOTIF; PROTEIN TERTIARY STRUCTURE;

ALLOSTERIC REGULATION; ALLOSTERIC SITE; AMINO ACID MOTIFS; AMINO ACID SEQUENCE; BIOCATALYSIS; DATABASES, PROTEIN; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN BINDING; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PROTEIN KINASES; PROTEIN STRUCTURE, TERTIARY; PROTEOME; SMALL MOLECULE LIBRARIES;

EID: 84937110866     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm501603h     Document Type: Article

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