Proteomics

Dataset Information

0

HDX-MS analysis of the mechanism of AKT1 inhibitor binding


ABSTRACT: Analysis of AKT1 inhibitor binding using HDX-MS .

INSTRUMENT(S): impact HD

ORGANISM(S): Homo Sapiens (human)

SUBMITTER: John Burke  

LAB HEAD: Dr. John E. Burke

PROVIDER: PXD032929 | Pride | 2023-02-22

REPOSITORIES: Pride

Dataset's files

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Publications

ATP-competitive and allosteric inhibitors induce differential conformational changes at the autoinhibitory interface of Akt1.

Shaw Alexandria L AL   Parson Matthew A H MAH   Truebestein Linda L   Jenkins Meredith L ML   Leonard Thomas A TA   Burke John E JE  

Structure (London, England : 1993) 20230208 3


Akt is a master regulator of pro-growth signaling in the cell. Akt is activated by phosphoinositides that disrupt the autoinhibitory interface between the kinase and pleckstrin homology (PH) domains and then is phosphorylated at T308 and S473. Akt hyperactivation is oncogenic, which has spurred development of potent and selective inhibitors as therapeutics. Using hydrogen deuterium exchange mass spectrometry (HDX-MS), we interrogated the conformational changes upon binding Akt ATP-competitive an  ...[more]

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