The discovery of potent ribosomal S6 kinase inhibitors by highthroughput screening and structure-guided drug design

Oncotarget

Volumn 4, Issue 10, 2013, Pages 1647-1661

  Couty, Sylvain ^a   Westwood, Isaac M ^a   Kalusa, Andrew ^a   Cano, Celine ^b   Travers, Jon ^a   Boxall, Kathy ^a   Chow, Chiau Ling ^a   Burns, Sam ^a   Schmitt, Jessica ^a   Pickard, Lisa ^a   Barillari, Caterina ^a   McAndrew, P Craig ^a   Clarke, Paul A ^a   Linardopoulos, Spiros ^a   Griffin, Roger J ^b   Aherne, G Wynne ^a   Raynaud, Florence I ^a   Workman, Paul ^a   Jones, Keith ^a   Van Montfort, Rob L M ^a  

^a INSTITUTE OF CANCER RESEARCH   (United Kingdom)

^b NEWCASTLE UNIVERSITY   (United Kingdom)

Author keywords

Cancer; Inhibitor; P70S6K; S6 kinase; Structure based drug design

Indexed keywords

4 (1 BENZYL 1H BENZOIMIDAZOL 2 YL) 1,2,5 OXADIAZOL 3 YLAMINE; 4 (1 CYCLOPROPYL 1H BENZOIMIDAZOL 2 YL) 1,2,5 OXADIAZOL 3 YLAMINE; 4 (1 CYCLOPROPYLMETHYL 1H BENZOIMIDAZOL 2 YL) 1,2,5 OXADIAZOL 3 YLAMINE; 4 (1 ETHYL 1H BENZOIMIDAZOL 2 YL) 1,2,5 OXADIAZOL 3 YLAMINE; 4 (1 METHYL 1H BENZOIMIDAZOL 2 YL) 1,2,5 OXADIAZOL 3 YLAMINE; 4 [1 ETHYL 6 (3 METHANESULFONYL PHENOXY) 1H IMIDAZO[4,5 C]PYRIDIN 2 YL] 1,2,5 OXADIAZOL 3 YLAMINE; 4 [1 ETHYL 6 METHYL 1H IMIDAZO[4,5 C]PYRIDIN 2 YL] 1,2,5 OXADIAZOL 3 YLAMINE; 4 [1 ETHYL 6 MORPHOLIN 4 YL 1H IMIDAZO[4,5 C]PYRIDIN 2 YL] 1,2,5 OXADIAZOL 3 YLAMINE; 4 [1 ETHYL 6 PHENYL 1H IMIDAZO[4,5 C]PYRIDIN 2 YL] 1,2,5 OXADIAZOL 3 YLAMINE; ANTINEOPLASTIC AGENT; BROMOAZABENZIMIDAZOLE; CARBOXAMIDOBENZIMIDAZOLE DERIVATIVE; PHOSPHOTRANSFERASE INHIBITOR; PROTEIN KINASE INHIBITOR; PROTEIN SERINE THREONINE KINASE INHIBITOR; S6 KINASE; UNCLASSIFIED DRUG;

ANTINEOPLASTIC ACTIVITY; ARTICLE; BINDING AFFINITY; BINDING SITE; CANCER CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG DESIGN; DRUG MECHANISM; DRUG PROTEIN BINDING; DRUG STRUCTURE; ENZYME ACTIVITY; ENZYME INHIBITION; ENZYME PHOSPHORYLATION; HIGH THROUGHPUT SCREENING; HUMAN; HUMAN CELL;

CELL LINE, TUMOR; CYCLIC AMP-DEPENDENT PROTEIN KINASES; DRUG DESIGN; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; IMIDAZOLES; MODELS, MOLECULAR; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; RECOMBINANT FUSION PROTEINS; RIBOSOMAL PROTEIN S6 KINASES, 90-KDA; SIGNAL TRANSDUCTION; STRUCTURE-ACTIVITY RELATIONSHIP; URINARY BLADDER NEOPLASMS;

EID: 84886743114     PISSN: None     EISSN: 19492553     Source Type: Journal    
DOI: 10.18632/oncotarget.1255     Document Type: Article

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