Structural analysis of the mechanism of inhibition and allosteric activation of the kinase domain of HER2 protein

Journal of Biological Chemistry

Volumn 286, Issue 21, 2011, Pages 18756-18765

  Aertgeerts, Kathleen ^a   Skene, Robert ^a   Yano, Jason ^a   Sang, Bi Ching ^a   Zou, Hua ^a   Snell, Gyorgy ^a   Jennings, Andy ^a   Iwamoto, Keiji ^b   Habuka, Noriyuki ^b   Hirokawa, Aki ^b   Ishikawa, Tomoyasu ^b   Tanaka, Toshimasa ^b   Miki, Hiroshi ^b   Ohta, Yoshikazu ^b   Sogabe, Satoshi ^b  

^a Takeda San Diego Inc   (United States)

^b TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ACTIVATION MECHANISMS; ACTIVE SITE; ALLOSTERIC ACTIVATION; ALLOSTERIC MECHANISMS; CANCER DRUG; CATALYTIC ACTIVITY; CONFORMATIONAL FLEXIBILITY; DESIGN AND DEVELOPMENT; EPIDERMAL GROWTH FACTOR RECEPTORS; HIGH RESOLUTION CRYSTAL STRUCTURE; HUMAN CANCER; HUMAN DISEASE; HUMAN EPIDERMAL GROWTH FACTOR; KINASE DOMAINS; MOLECULAR LEVELS; PROTEIN ACTIVATION; SELECTIVE INHIBITORS; SMALL MOLECULES;

ACTIVATION ANALYSIS; CATALYST ACTIVITY; CRYSTAL STRUCTURE; DIMERS; DISEASES; PEPTIDES; STRUCTURAL ANALYSIS;

ENZYMES;

EPIDERMAL GROWTH FACTOR RECEPTOR 2; EPIDERMAL GROWTH FACTOR RECEPTOR 4; GLYCINE; PHOSPHOTRANSFERASE;

ALLOSTERISM; ALPHA HELIX; ARTICLE; CATALYSIS; CONTROLLED STUDY; CRYSTAL STRUCTURE; ENZYME ACTIVATION; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME CONFORMATION; ENZYME INHIBITION; ENZYME STRUCTURE; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN DOMAIN; STRUCTURE ANALYSIS;

ALLOSTERIC REGULATION; ANTINEOPLASTIC AGENTS; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME ACTIVATION; HUMANS; NEOPLASMS; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, ERBB-2; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 79956310563     PISSN: 00219258     EISSN: 1083351X     Source Type: Journal    
DOI: 10.1074/jbc.M110.206193     Document Type: Article

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