2-Aminothiadiazole inhibitors of AKT1 as potential cancer therapeutics

Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 5, 2010, Pages 1652-1656

  Zeng, Qingping ^a   Bourbeau, Matthew P ^a   Wohlhieter, G Erich ^a   Yao, Guomin ^a   Monenschein, Holger ^a   Rider, James T ^a   Lee, Matthew R ^a   Zhang, Shiwen ^a   Lofgren, Julie ^a   Freeman, Daniel ^a   Li, Chun ^a   Tominey, Elizabeth ^a   Huang, Xin ^a   Hoffman, Douglas ^a   Yamane, Harvey ^a   Tasker, Andrew S ^a   Dominguez, Celia ^a   Viswanadhan, Vellarkad N ^a   Hungate, Randall ^a   Zhang, Xiaoling ^a  

^a AMGEN INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 AMINOTHIAZOLE DERIVATIVE; ANTINEOPLASTIC AGENT; CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIN DEPENDENT KINASE 2; PROTEIN SERINE THREONINE KINASE; TRANSCRIPTION FACTOR FKHRL1;

ANIMAL EXPERIMENT; ARTICLE; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG HALF LIFE; DRUG STRUCTURE; MOUSE; NONHUMAN; PROTEIN PHOSPHORYLATION; RAT; STRUCTURE ACTIVITY RELATION; X RAY CRYSTALLOGRAPHY;

ANIMALS; ANTINEOPLASTIC AGENTS; CATALYTIC DOMAIN; CRYSTALLOGRAPHY, X-RAY; CYCLIC AMP-DEPENDENT PROTEIN KINASES; CYCLIN-DEPENDENT KINASE 2; ISOQUINOLINES; MICE; NEOPLASMS; PHOSPHORYLATION; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS C-AKT; RATS; STRUCTURE-ACTIVITY RELATIONSHIP; THIADIAZOLES; THIAZOLES;

EID: 76649118093     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2010.01.046     Document Type: Article

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26. 2O). 1, 3, 6, or 16 h post-dose, AKT signaling was stimulated in mouse liver by hepatocyte growth factor (HGF) via tail vein injection (5 μg). Five minutes post HGF stimulation, the mice were sacrificed and livers were harvested for protein lysate preparation and quantitation by Western blot analysis of phospho-FKHRL1 (Thr32), normalized to total FKHRL1 levels