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Bioorganic and Medicinal Chemistry Letters

Volumn 20, Issue 13, 2010, Pages 3897-3902

Design and synthesis of benzoazepin-2-one analogs as allosteric binders targeting the PIF pocket of PDK1

(8) Wei, Linyi a Gao, Xiaoqi a Warne, Robert b Hao, Xueshi a Bussiere, Dirksen b Gu, Xiang Ju a Uno, Tetsuo a Liu, Yi a

a GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION (United States)

b NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH (United States)

Author keywords

3 Phosphoinositide dependent kinase 1; AGC protein kinases; Allosteric activators; PDK1; PIF pocket

Indexed keywords

AGC PROTEIN KINASE; AZEPINE DERIVATIVE; BENZOAZEPIN 2 ONE; PHOSPHOINOSITIDE DEPENDENT PROTEIN KINASE 1; PROTEIN KINASE; SULFIDE; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; DRUG BINDING SITE; DRUG DESIGN; DRUG SYNTHESIS; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME SUBSTRATE; IN VITRO STUDY; STRUCTURE ACTIVITY RELATION;

AZEPINES; BINDING SITES; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; ENZYME ACTIVATION; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PROTEIN KINASE INHIBITORS; PROTEIN-SERINE-THREONINE KINASES; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 77954316554 PISSN: 0960894X EISSN: None Source Type: Journal
DOI: 10.1016/j.bmcl.2010.05.019 Document Type: Article

Times cited : (26)

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- note
- Labeled PIF tide: Biotin-KTFCGTPEYLAPEVRREPRILSEEEQEMFRDFDYIADWK-CONH2, was obtained from SynPep Corp. (Dublin, CA, USA). Unlabeled PIF peptide: QEMFRDFDYIADW, was synthesized by us and the purity verified by HPLC.

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