Structure-activity relationship studies of prostate-specific membrane antigen (PSMA) inhibitors derived from alpha-amino acid with (S)- or (R)-configuration at P1 ' region
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Kwon, Hongmok | - |
dc.contributor.author | Lim, Hyunwoong | - |
dc.contributor.author | Ha, Hyunsoo | - |
dc.contributor.author | Choi, Doyoung | - |
dc.contributor.author | Son, Sang-Hyun | - |
dc.contributor.author | Nam, Hwanhee | - |
dc.contributor.author | Minn, Il | - |
dc.contributor.author | Byun, Youngjoo | - |
dc.date.accessioned | 2021-08-30T09:43:53Z | - |
dc.date.available | 2021-08-30T09:43:53Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2020-11 | - |
dc.identifier.issn | 0045-2068 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/51993 | - |
dc.description.abstract | Prostate-specific membrane antigen (PSMA), a type II membrane glycoprotein, is considered an excellent target for the diagnosis or treatment of prostate cancer. We previously investigated the effect of beta and gamma-amino acids with (S)or (R)-configuration in the S1 pocket on the binding affinity for PSMA. However, comprehensive studies on the effect of alpha-amino acid with (R)-configuration in the S1 ' pocket has not been reported yet. We selected ZJ43 (1) and DCIBzL (5) as templates and synthesized their analogues with (S)or (R)-configuration in the P1 and P1 ' regions. The PSMA-inhibitory activities of compounds with altered chirality in the P1 ' region were dropped dramatically, with their IC50 values changing from nM to mu M ranges. The compounds with (S)-configuration at both P1 and P1 ' regions were more potent than the others. The findings of this study may provide insights regarding the structural modification of PSMA inhibitor in the S1 ' binding pocket. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | - |
dc.subject | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject | UREA-BASED INHIBITORS | - |
dc.subject | HYDROXAMATE-BASED INHIBITORS | - |
dc.subject | NAAG PEPTIDASE INHIBITORS | - |
dc.subject | N-ACETYLASPARTYLGLUTAMATE | - |
dc.subject | BIOLOGICAL EVALUATION | - |
dc.subject | GCPII INHIBITORS | - |
dc.subject | DESIGN | - |
dc.subject | NEUROPATHY | - |
dc.subject | NAALADASE | - |
dc.title | Structure-activity relationship studies of prostate-specific membrane antigen (PSMA) inhibitors derived from alpha-amino acid with (S)- or (R)-configuration at P1 ' region | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.identifier.doi | 10.1016/j.bioorg.2020.104304 | - |
dc.identifier.scopusid | 2-s2.0-85091903406 | - |
dc.identifier.wosid | 000592397400004 | - |
dc.identifier.bibliographicCitation | BIOORGANIC CHEMISTRY, v.104 | - |
dc.relation.isPartOf | BIOORGANIC CHEMISTRY | - |
dc.citation.title | BIOORGANIC CHEMISTRY | - |
dc.citation.volume | 104 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Biochemistry & Molecular Biology | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject.keywordPlus | UREA-BASED INHIBITORS | - |
dc.subject.keywordPlus | HYDROXAMATE-BASED INHIBITORS | - |
dc.subject.keywordPlus | NAAG PEPTIDASE INHIBITORS | - |
dc.subject.keywordPlus | N-ACETYLASPARTYLGLUTAMATE | - |
dc.subject.keywordPlus | BIOLOGICAL EVALUATION | - |
dc.subject.keywordPlus | GCPII INHIBITORS | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | NEUROPATHY | - |
dc.subject.keywordPlus | NAALADASE | - |
dc.subject.keywordAuthor | Absolute configuration | - |
dc.subject.keywordAuthor | PSMA | - |
dc.subject.keywordAuthor | SAR | - |
dc.subject.keywordAuthor | Prostate cancer | - |
Items in ScholarWorks are protected by copyright, with all rights reserved, unless otherwise indicated.
(02841) 서울특별시 성북구 안암로 14502-3290-1114
COPYRIGHT © 2021 Korea University. All Rights Reserved.
Certain data included herein are derived from the © Web of Science of Clarivate Analytics. All rights reserved.
You may not copy or re-distribute this material in whole or in part without the prior written consent of Clarivate Analytics.