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Volumn 18, Issue 11, 2008, Pages 3359-3363

Synthesis and structure based optimization of novel Akt inhibitors

Author keywords

Akt; Imidazopiperidine; Pyrrolopyrimidine; Spiroindoline

Indexed keywords

PROTEIN KINASE B INHIBITOR;

EID: 44149113025     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2008.04.034     Document Type: Article
Times cited : (74)

References (28)
  • 20
    • 44149099190 scopus 로고    scopus 로고
    • note
    • 50 of 223 ± 110 nM. As expected, no compounds tested have shown Akt isozyme selectivity (Akt1, 2 or 3).
  • 23
    • 44149101101 scopus 로고    scopus 로고
    • note
    • Pandit, J. WO 2005113762A1, 2005; Atomic coordinates and structure factors of the protein structures in this paper have been deposited in the RCSB Protein Data Bank, with accession numbers 3CQU and 3CQW.
  • 26
    • 44149128778 scopus 로고    scopus 로고
    • note
    • Akt cell assay: The phosphorylation status of an Akt substrate, GSK-3α, in the U87 glioblastoma line is measured. Cells were incubated with compound (7 concentrations plus vehicle) for 2 h in DMEM medium lacking fetal calf serum (FCS). After cell lysis, p-GSK-3α was captured on 96-well plates coated with a phosphospecific antibody to GSK-3α/β (#9331, Cell Signaling Technology). The reporter antibody bound total GSK-3α (#SC-5264, Santa Cruz), and was measured in an ELISA format.
  • 27
    • 44149120827 scopus 로고    scopus 로고
    • note
    • Unfortunately, it was not possible to obtain high-quality crystal structures on any member of the spiroindoline lead series (13).


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.