Definition of the binding mode of a new class of phosphoinositide 3-kinase α-selective inhibitors using in vitro mutagenesis of non-conserved amino acids and kinetic analysis

Biochemical Journal

Volumn 444, Issue 3, 2012, Pages 529-535

  Zheng, Zhaohua ^a   Amran, Syazwani I ^a   Zhu, Jiuxiang ^b   Schmidt Kittler, Oleg ^b   Kinzler, Kenneth W ^b   Vogelstein, Bert ^b   Shepherd, Peter R ^c   Thompson, Philip E ^a   Jennings, Ian G ^a  

^a MONASH UNIVERSITY   (Australia)

^b JOHNS HOPKINS UNIVERSITY   (United States)

^c UNIVERSITY OF AUCKLAND   (New Zealand)

Author keywords

Enzyme kinetics; In vitro mutagenesis; Mechanism of isoform selectivity; Phosphoinositide 3 kinase (PI3K); Small molecule inhibitor

Indexed keywords

AMINO ACID; GLUTAMINE; ISOLEUCINE; LYSINE; PHOSPHATIDYLINOSITOL 3 KINASE 75; PHOSPHATIDYLINOSITOL 3 KINASE A 66S; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3 KINASE J 32; PHOSPHATIDYLINOSITOL 3 KINASE P110 ALPHA; PHOSPHATIDYLINOSITOL 3 KINASE P110 BETA; SERINE; UNCLASSIFIED DRUG;

ARTICLE; CONTROLLED STUDY; ENZYME KINETICS; ENZYME MECHANISM; IN VITRO STUDY; MUTAGENESIS; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN INTERACTION; PROTEIN STRUCTURE;

AMINO ACIDS; CLASS II PHOSPHATIDYLINOSITOL 3-KINASES; CONSERVED SEQUENCE; DOSE-RESPONSE RELATIONSHIP, DRUG; HYDRAZONES; ISOENZYMES; KINETICS; MUTAGENESIS, SITE-DIRECTED; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN BINDING; SULFONAMIDES;

EID: 84862202084     PISSN: 02646021     EISSN: 14708728     Source Type: Journal    
DOI: 10.1042/BJ20120499     Document Type: Article

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