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Volumn 21, Issue 18, 2011, Pages 5191-5196

Design and synthesis of novel amide AKT1 inhibitors with selectivity over CDK2

Author keywords

AKT; Cancer; CDK; PKB

Indexed keywords

CYCLIC AMP DEPENDENT PROTEIN KINASE; CYCLIN DEPENDENT KINASE 2; PROTEIN KINASE B; PROTEIN KINASE B INHIBITOR; THIADIAZOLE DERIVATIVE; THIAZOLE DERIVATIVE;

EID: 80051927351     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.07.056     Document Type: Article
Times cited : (8)

References (21)
  • 10
    • 0037855834 scopus 로고    scopus 로고
    • U87MG cells in 5% FBS media were incubated with inhibitors in threefold serial dilutions for 1h at 37 °C. The cells were lysed and PRAS40 phosphorylation was quantified by ELISA assay. Phospho-PRAS40 was normalized to total PRAS40.
    • U87MG cells in 5% FBS media were incubated with inhibitors in threefold serial dilutions for 1h at 37 °C. The cells were lysed and PRAS40 phosphorylation was quantified by ELISA assay. Phospho-PRAS40 was normalized to total PRAS40. K.S. Kovacina, G.Y. Park, S.S. Bae, A.W. Guzzetta, E. Schaefer, M.J. Birnbaum, and R.A. Roth J. Biol. Chem. 278 2003 10189
    • (2003) J. Biol. Chem. , vol.278 , pp. 10189
    • Kovacina, K.S.1    Park, G.Y.2    Bae, S.S.3    Guzzetta, A.W.4    Schaefer, E.5    Birnbaum, M.J.6    Roth, R.A.7
  • 13
    • 34247116441 scopus 로고    scopus 로고
    • AKT1 was the only AKT isoform routinely tested against as it is thought to be the major isoform contributing to oncogenic activity. Dummler, B.; Hemmings, B. A. Biochem. Soc. Trans. 2007, 35, 231. In addition all other isoforms of AKT potency tracked well with AKT1 upon testing.
    • (2007) Biochem. Soc. Trans. , vol.35 , pp. 231
    • Dummler, B.1    Hemmings, B.A.2
  • 17
    • 0038206479 scopus 로고    scopus 로고
    • Mutations: PKA Val123 was mutated to AKT Ala, and PKA Leu173 was mutated to AKT Met. Additionally, PKA Lys181 was mutated to AKT Gln, but this residue faces away from the ATP binding pocket.
    • Mutations: PKA Val123 was mutated to AKT Ala, and PKA Leu173 was mutated to AKT Met. Additionally, PKA Lys181 was mutated to AKT Gln, but this residue faces away from the ATP binding pocket. M. Gassell, C.B. Breitenlechner, P. Ruger, U. Jucknischke, T. Schnieder, R. Huber, D. Bossemeyer, and R.A. Engh J. Mol. Biol. 329 2003 1021
    • (2003) J. Mol. Biol. , vol.329 , pp. 1021
    • Gassell, M.1    Breitenlechner, C.B.2    Ruger, P.3    Jucknischke, U.4    Schnieder, T.5    Huber, R.6    Bossemeyer, D.7    Engh, R.A.8
  • 20
    • 80051950125 scopus 로고    scopus 로고
    • The absolute configuration of the azetidines was determined by Mosher ester analysis - see Supplementary data
    • The absolute configuration of the azetidines was determined by Mosher ester analysis - see Supplementary data.


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.