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PXD010277

PXD010277 is an original dataset announced via ProteomeXchange.

Dataset Summary
TitleDesign and synthesis of tailored human caseinolytic protease P inhibitors
DescriptionHuman caseinolytic protease P (hClpP) is important for degradation of misfolded proteins in the mitochondrial unfolded protein response. We here introduce tailored hClpP inhibitors that utilize a steric discrimination in their core naphthofuran scaffold to selectively address the human enzyme. This novel inhibitor generation exhibited superior activity compared to previously introduced beta-lactones, optimized for bacterial ClpP. Further insights into the bioactivity and binding to cellular targets were obtained via chemical proteomics as well as proliferation- and migration studies in cancer cells.
HostingRepositoryPRIDE
AnnounceDate2019-03-05
AnnouncementXMLSubmission_2019-03-05_00:47:57.xml
DigitalObjectIdentifier
ReviewLevelPeer-reviewed dataset
DatasetOriginOriginal dataset
RepositorySupportUnsupported dataset by repository
PrimarySubmitterThomas Gronauer
SpeciesList scientific name: Homo sapiens (Human); NCBI TaxID: 9606;
ModificationListmonohydroxylated residue; iodoacetamide derivatized residue
InstrumentQ Exactive
Dataset History
RevisionDatetimeStatusChangeLog Entry
02018-06-29 08:59:59ID requested
12019-03-05 00:47:58announced
Publication List
Gronauer TF, Mandl MM, Lakemeyer M, Hackl MW, Me, ß, ner M, Korotkov VS, Pachmayr J, Sieber SA, Design and synthesis of tailored human caseinolytic protease P inhibitors. Chem Commun (Camb), 54(70):9833-9836(2018) [pubmed]
Keyword List
curator keyword: Biomedical
submitter keyword: ClpP, Huh7, Jurkat, Mitochondria, phenyl esters
Contact List
Stephan Axel Sieber
contact affiliationTU Munich, Department of Chemistry Lichtenbergstr. 4 Garching, DE 85747
contact emailstephan.sieber@tum.de
lab head
Thomas Gronauer
contact affiliationTU Munich Department of Chemistry Chair of Organic Chemistry 2 Lichtenbergstraße 4 85748 Garching Germany
contact emailthomas.gronauer@tum.de
dataset submitter
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Dataset FTP location
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PRIDE project URI
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