Structural biology structural basis for activation and inhibition of class I phosphoinositide 3-kinases

Science Signaling

Volumn 4, Issue 195, 2011, Pages

  Vadas, Oscar ^a   Burke, John E ^a   Zhang, Xuxiao ^a,b   Berndt, Alex ^a   Williams, Roger L ^a  

^a MRC LABORATORY OF MOLECULAR BIOLOGY   (United Kingdom)

^b NANYANG TECHNOLOGICAL UNIVERSITY   (Singapore)

Author keywords

[No Author keywords available]

Indexed keywords

2 (1H INDAZOL 4 YL) 6 (4 METHANESULFONYL 1 PIPERAZINYLMETHYL) 4 MORPHOLINOTHIENO[3,2 D]PYRIMIDINE; CAL 101; CYCLIC AMP; CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIC AMP DEPENDENT PROTEIN KINASE ANCHORING PROTEIN; G PROTEIN COUPLED RECEPTOR; GS 1101; MAMMALIAN TARGET OF RAPAMYCIN COMPLEX 1; NONSTRUCTURAL PROTEIN 1; PHOSPHATIDYLINOSITOL 3 KINASE; PHOSPHATIDYLINOSITOL 3 KINASE INHIBITOR; PHOSPHATIDYLINOSITOL 3,4,5 TRISPHOSPHATE 3 PHOSPHATASE; PICTRELISIB; PROTEIN KINASE C; PROTEIN P85; PROTEIN TYROSINE KINASE; RAS PROTEIN; UNCLASSIFIED DRUG; 2 (1H INDAZOL 4 YL) 6 (4 METHANESULFONYLPIPERAZIN 1 YLMETHYL) 4 MORPHOLIN 4 YLTHIENO(3,2 D)PYRIMIDINE; 2-(1H-INDAZOL-4-YL)-6-(4-METHANESULFONYLPIPERAZIN-1-YLMETHYL)-4-MORPHOLIN-4-YLTHIENO(3,2-D)PYRIMIDINE; INDAZOLE DERIVATIVE; SULFONAMIDE;

ADVANCED CANCER; BINDING AFFINITY; BREAST CANCER; CARBOXY TERMINAL SEQUENCE; CARCINOGENESIS; CELL DIFFERENTIATION; CELL GROWTH; CELL METABOLISM; CELL MIGRATION; CELL PROLIFERATION; CRYSTAL STRUCTURE; DNA REPAIR; DNA REPLICATION; DRUG BIOAVAILABILITY; DRUG TARGETING; DRUG TOLERABILITY; ENDOMETRIUM CANCER; ENZYME ACTIVATION; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME MECHANISM; ENZYME STRUCTURE; ENZYME SUBSTRATE COMPLEX; GENE MUTATION; GENE OVEREXPRESSION; GLIOBLASTOMA; HUMAN; LEUKEMIA; LYMPHOMA; MELANOMA; MOLECULAR INTERACTION; POINT MUTATION; PRIORITY JOURNAL; PROTEIN DOMAIN; PROTEIN PROTEIN INTERACTION; REVIEW; SIGNAL TRANSDUCTION; SOLID TUMOR; SOMATIC MUTATION; CHEMICAL STRUCTURE; CHEMISTRY; DRUG ANTAGONISM; DRUG EFFECT; ENZYMOLOGY; GENETICS; METABOLISM; NEOPLASM; PATHOLOGY; PROTEIN MULTIMERIZATION; PROTEIN SUBUNIT; PROTEIN TERTIARY STRUCTURE;

ENZYME ACTIVATION; HUMANS; INDAZOLES; MODELS, MOLECULAR; NEOPLASMS; PHOSPHATIDYLINOSITOL 3-KINASES; PROTEIN MULTIMERIZATION; PROTEIN STRUCTURE, TERTIARY; PROTEIN SUBUNITS; SIGNAL TRANSDUCTION; SULFONAMIDES;

EID: 80054736907     PISSN: 19450877     EISSN: 19379145     Source Type: Journal    
DOI: 10.1126/scisignal.2002165     Document Type: Review

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105. Acknowledgments: We are grateful to members of R.W.'s group for fruitful discussions. Funding: O.V. was supported by a Swiss National Science foundation fellowship (grant number PA00P3-134202) and an European Molecular Biology Organization (EMBO) fellowship (ALTF 690-2010), J.E.B. by an EMBO fellowship (ALTF 268-2009), and X.Z. by a Medical Research Council-LMB Cambridge Scholarship and Cambridge Overseas Trust. Work in Williams lab was funded by the Medical Research Council.