DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kang, Deokhee | ko |
dc.contributor.author | Kim, Do-Wook | ko |
dc.contributor.author | Kim, Joo-Chan | ko |
dc.contributor.author | Park, Hee-Sung | ko |
dc.date.accessioned | 2023-02-10T02:00:15Z | - |
dc.date.available | 2023-02-10T02:00:15Z | - |
dc.date.created | 2023-01-30 | - |
dc.date.issued | 2023-02 | - |
dc.identifier.citation | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, v.62, no.7 | - |
dc.identifier.issn | 1433-7851 | - |
dc.identifier.uri | http://hdl.handle.net/10203/305121 | - |
dc.description.abstract | Demand for peptide-based pharmaceuticals has been steadily increasing, but only limited success has been achieved to date. To expedite peptide-based drug discovery, we developed a general scheme for cell-based screening of cyclic peptide inhibitors armed with a user-designed warhead. We combined unnatural amino acid incorporation and split intein-mediated peptide cyclization techniques and integrated a yeast-based colorimetric screening assay to generate a new scheme that we call the custom-designed warhead-armed cyclic peptide screening platform (CWCPS). This strategy successfully discovered a potent inhibitor, CY5-6Q, that targets human histone deacetylase 8 (HDAC8) with a K-D value of 15 nM. This approach can be a versatile and general platform for discovering cyclic peptide inhibitors. | - |
dc.language | English | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.title | A Versatile Strategy for Screening Custom-Designed Warhead-Armed Cyclic Peptide Inhibitors | - |
dc.type | Article | - |
dc.identifier.wosid | 000910554000001 | - |
dc.identifier.scopusid | 2-s2.0-85146079544 | - |
dc.type.rims | ART | - |
dc.citation.volume | 62 | - |
dc.citation.issue | 7 | - |
dc.citation.publicationname | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | - |
dc.identifier.doi | 10.1002/anie.202214815 | - |
dc.contributor.localauthor | Park, Hee-Sung | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | Cyclic Peptide Inhibitor | - |
dc.subject.keywordAuthor | Genetic Code Expansion | - |
dc.subject.keywordAuthor | Warhead-Bearing Unnatural Amino Acid | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | HDAC8 | - |
dc.subject.keywordPlus | MECHANISM | - |
dc.subject.keywordPlus | EVOLUTION | - |
dc.subject.keywordPlus | DISCOVERY | - |
dc.subject.keywordPlus | CORNELIA | - |
dc.subject.keywordPlus | SPECTRUM | - |
dc.subject.keywordPlus | VECTORS | - |
dc.subject.keywordPlus | DISPLAY | - |
dc.subject.keywordPlus | YEAST | - |
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