SAR and x-ray. A new approach combining fragment-based screening and rational drug design: Application to the discovery of nanomolar inhibitors of Src SH2

Journal of Medicinal Chemistry

Volumn 45, Issue 12, 2002, Pages 2379-2387

  Lesuisse, Dominique ^a   Lange, Gudrun ^b   Deprez, Pierre ^a   Bénard, Didier ^a   Schoot, Bernard ^a   Delettre, Georges ^a   Marquette, Jean Pierre ^a   Broto, Pierre ^a   Jean Baptiste, Véronique ^a   Bichet, Paulette ^a   Sarubbi, Edoardo ^a   Mandine, Eliane ^a  

^a SANOFI   (France)

^b SANOFI AVENTIS DEUTSCHLAND GMBH   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

AROMATIC COMPOUND; CAPROLACTAM; ENZYME INHIBITOR; PHENYL PHOSPHATE DERIVATIVE; PHOSPHATE; PHOSPHOTYROSINE; PROTEIN KINASE P60; PROTEIN SH2; PROTEIN TYROSINE KINASE; TETRAPEPTIDE; UNCLASSIFIED DRUG;

AMINO ACID SEQUENCE; ARTICLE; CRYSTAL STRUCTURE; CRYSTALLOGRAPHY; DRUG BINDING; DRUG DESIGN; DRUG IDENTIFICATION; DRUG PROTEIN BINDING; DRUG SCREENING; HUMAN; HYDROLYSIS; MULTIGENE FAMILY; NERVE CELL; OSTEOCLAST; PROTEIN DOMAIN; PROTEIN EXPRESSION; PROTEIN STRUCTURE; SIGNAL TRANSDUCTION; STRUCTURE ACTIVITY RELATION; THROMBOCYTE; X RAY;

CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME INHIBITORS; MODELS, MOLECULAR; PHOSPHORIC ACID ESTERS; PROTEIN BINDING; PROTO-ONCOGENE PROTEINS PP60(C-SRC); SRC HOMOLOGY DOMAINS; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0037030686     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm010927p     Document Type: Article

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