Enabling structure-based drug design of Tyk2 through co-crystallization with a stabilizing aminoindazole inhibitor

BMC Structural Biology

Volumn 12, Issue , 2012, Pages

  Argiriadi, Maria A ^a   Goedken, Eric R ^a   Banach, David ^a   Borhani, David W ^b   Burchat, Andrew ^a   Dixon, Richard W ^c   Marcotte, Doug ^d   Overmeyer, Gary ^a   Pivorunas, Valerie ^e   Sadhukhan, Ramkrishna ^a   Sousa, Silvino ^a   Moore, Nigel St John ^b   Tomlinson, Medha ^a   Voss, Jeffrey ^a   Wang, Lu ^a   Wishart, Neil ^a   Woller, Kevin ^a   Talanian, Robert V ^a  

^a ABBOTT LABORATORIES   (United States)

^b D E SHAW RESEARCH   (United States)

^c VERTEX PHARMACEUTICALS   (United States)

^d BIOGEN   (United States)

^e HARVARD UNIVERSITY   (United States)

Author keywords

Crystallization; Jak kinase; Proteolysis; Tyk2

Indexed keywords

ADENOSINE TRIPHOSPHATE; ENZYME INHIBITOR; FURAN 2 CARBOXYLIC ACID [5 [4 (3 CHLORO BENZENESULFONYLAMINO) PHENYL] 1 H INDAZOL 3 YL]AMIDE; GLYCINE; N [4 (3 AMINO 1H INDAZOL 5 YL) PHENYL] 3 CHLORO BENZENESULFONAMIDE; PHOSPHOTRANSFERASE; PROTEIN KINASE TYK2; THERMOLYSIN; UNCLASSIFIED DRUG;

AMINO TERMINAL SEQUENCE; ANIMAL TISSUE; ARTICLE; CARBOXY TERMINAL SEQUENCE; COMPLEX FORMATION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DRUG CONFORMATION; DRUG DESIGN; DRUG STRUCTURE; HIGH THROUGHPUT SCREENING; LIGAND BINDING; MOLECULAR CLONING; MOUSE; MUTATION; NONHUMAN; ORTHOLOGY; PROTEIN DEGRADATION; PROTEIN PURIFICATION; PROTEIN STABILITY;

AMINO ACID SEQUENCE; ANIMALS; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; DRUG DESIGN; ENZYME STABILITY; HUMANS; INDAZOLES; JANUS KINASES; MICE; MOLECULAR SEQUENCE DATA; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, SECONDARY; PROTEOLYSIS; STRUCTURE-ACTIVITY RELATIONSHIP; TYK2 KINASE;

MURINAE;

EID: 84866493922     PISSN: None     EISSN: 14726807     Source Type: Journal    
DOI: 10.1186/1472-6807-12-22     Document Type: Article

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