Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors
DC Field | Value | Language |
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dc.contributor.author | Kwon, Hongmok | - |
dc.contributor.author | Kim, YunHye | - |
dc.contributor.author | Park, Kieung | - |
dc.contributor.author | Choi, Soo An | - |
dc.contributor.author | Son, Sang-Hyun | - |
dc.contributor.author | Byun, Youngjoo | - |
dc.date.accessioned | 2021-09-04T03:50:07Z | - |
dc.date.available | 2021-09-04T03:50:07Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2016-01-15 | - |
dc.identifier.issn | 0960-894X | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/89789 | - |
dc.description.abstract | Hepsin, a type II transmembrane serine protease, is an attractive protein as a potential therapeutic and diagnostic biomarker for prostate cancer because it is highly up-regulated in prostate cancer and promotes both progression and metastasis. Starting from the reported tetrapeptide hepsin inhibitor Ac-KQLR-ketothiazole (kt) (1), we investigated the minimal structural requirements for hepsin inhibitory activity by truncating amino acids at the N-terminus. The kt and ketobenzothiazole (kbt) dipeptide analogs Ac-LR-kt (3) and Ac-LR-kbt (15) were found to be potent hepsin inhibitors, exhibiting K-i values of 22 nM and 3 nM, respectively. The present work suggests that LR-containing dipeptide molecules could be useful as lead compounds for the development of novel hepsin inhibitors. (C) 2015 Elsevier Ltd. All rights reserved. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | PERGAMON-ELSEVIER SCIENCE LTD | - |
dc.subject | PROSTATE-CANCER | - |
dc.subject | SERINE PROTEASES | - |
dc.subject | EXPRESSION | - |
dc.subject | STATISTICS | - |
dc.subject | BIOMARKERS | - |
dc.subject | CELLS | - |
dc.title | Structure-based design, synthesis, and biological evaluation of Leu-Arg dipeptide analogs as novel hepsin inhibitors | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Choi, Soo An | - |
dc.contributor.affiliatedAuthor | Son, Sang-Hyun | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.identifier.doi | 10.1016/j.bmcl.2015.12.023 | - |
dc.identifier.scopusid | 2-s2.0-84952802076 | - |
dc.identifier.wosid | 000367329700013 | - |
dc.identifier.bibliographicCitation | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, v.26, no.2, pp.310 - 314 | - |
dc.relation.isPartOf | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.title | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | - |
dc.citation.volume | 26 | - |
dc.citation.number | 2 | - |
dc.citation.startPage | 310 | - |
dc.citation.endPage | 314 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | PROSTATE-CANCER | - |
dc.subject.keywordPlus | SERINE PROTEASES | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | STATISTICS | - |
dc.subject.keywordPlus | BIOMARKERS | - |
dc.subject.keywordPlus | CELLS | - |
dc.subject.keywordAuthor | Hepsin | - |
dc.subject.keywordAuthor | Prostate cancer | - |
dc.subject.keywordAuthor | Dipeptides | - |
dc.subject.keywordAuthor | Serine protease | - |
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