Selectively targeting an inactive conformation of interleukin-2-inducible T-cell kinase by allosteric inhibitors

Biochemical Journal

Volumn 460, Issue 2, 2014, Pages 211-222

  Han, Seungil ^a   Czerwinski, Robert M ^a   Caspers, Nicole L ^a   Limburg, David C ^a   Ding, Wei Dong ^a   Wang, Hong ^a   Ohren, Jeffrey F ^a   Rajamohan, Francis ^a   McLellan, Thomas J ^a   Unwalla, Ray ^a   Choi, Chulho ^a   Parikh, Mihir D ^a   Seth, Nilufer ^a   Edmonds, Jason ^a   Phillips, Chris ^a   Shakya, Subarna ^a   Li, Xin ^a   Spaulding, Vikki ^a   Hughes, Samantha ^a   Cook, Andrew ^a   Robinson, Colin ^a   Mathias, John P ^a   Navratilova, Iva ^a   Medley, Quintus G ^a   Anderson, David R ^a   Kurumbail, Ravi G ^a   Aulabaugh, Ann ^a   more..

^a PFIZER INC   (United States)

Author keywords

Allosteric; Drug discovery; Inhibition mechanism; Interleukin 2 inducible T cell kinase (ITK); Kinase inhibitor; Structure based drug design

Indexed keywords

ADENOSINE TRIPHOSPHATE; INTERLEUKIN 2 INDUCIBLE T CELL KINASE; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN TYROSINE KINASE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; BINDING SITE; CRYSTAL STRUCTURE; ENZYME ACTIVATION; ENZYME ACTIVITY; ENZYME CONFORMATION; ENZYME INHIBITION; ENZYME KINETICS; ENZYME PHOSPHORYLATION; ENZYME REGULATION; ENZYMOLOGY; ISOTHERMAL TITRATION CALORIMETRY; NUCLEAR MAGNETIC RESONANCE; PRIORITY JOURNAL; PROTEIN DOMAIN; STEADY STATE; STRUCTURE ACTIVITY RELATION; SURFACE PLASMON RESONANCE; X RAY CRYSTALLOGRAPHY;

ADENOSINE TRIPHOSPHATE; ALLOSTERIC REGULATION; ALLOSTERIC SITE; CRYSTALLIZATION; CRYSTALLOGRAPHY, X-RAY; HUMANS; MODELS, MOLECULAR; PROTEIN CONFORMATION; PROTEIN KINASE INHIBITORS; PROTEIN STRUCTURE, TERTIARY; PROTEIN-TYROSINE KINASES; SURFACE PLASMON RESONANCE;

EID: 84900491469     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20131139     Document Type: Article

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