Synthesis and biological evaluation of substrate-based imaging agents for the prostate-specific membrane antigen
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Byun, Youngjoo | - |
dc.contributor.author | Pullambhatla, Mrudula | - |
dc.contributor.author | Wang, Haofan | - |
dc.contributor.author | Mease, Ronnie C. | - |
dc.contributor.author | Pomper, Martin G. | - |
dc.date.accessioned | 2021-09-06T01:46:52Z | - |
dc.date.available | 2021-09-06T01:46:52Z | - |
dc.date.created | 2021-06-18 | - |
dc.date.issued | 2013-05 | - |
dc.identifier.issn | 1598-5032 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/103291 | - |
dc.description.abstract | Prostate-specific membrane antigen (PSMA) is an attractive target for the imaging of prostate cancer (PCa) due to the elevated expression on the surface of prostate tumor cells. Most PSMA-targeted low molecular weight imaging agents are inhibitors of PSMA. We have synthesized a series of substrate-based PSMA-targeted imaging agents by mimicking poly-gamma-glutamyl folic acid, an endogenous substrate of PSMA. In vitro the gamma-linked polyglutamate conjugates proved to be better substrates than the corresponding alpha-linked glutamates. However, in vivo imaging studies of gamma-ray-emitting and gamma-linked glutamates did not demonstrate selective uptake in PSMA-positive over PSMA-negative tumors. Subsequent chromatographic studies and in silico molecular dynamics simulations indicated that hydrolysis of the substrates is slow and access to the enzymatic active site is limited. These results inform the design of future substrate-based imaging agents for PSMA. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | POLYMER SOC KOREA | - |
dc.subject | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject | INHIBITORS | - |
dc.subject | EXPRESSION | - |
dc.subject | INTERNALIZATION | - |
dc.subject | BINDING | - |
dc.subject | CANCER | - |
dc.subject | PSMA | - |
dc.title | Synthesis and biological evaluation of substrate-based imaging agents for the prostate-specific membrane antigen | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.identifier.doi | 10.1007/s13233-013-1050-5 | - |
dc.identifier.scopusid | 2-s2.0-84877743285 | - |
dc.identifier.wosid | 000318177900014 | - |
dc.identifier.bibliographicCitation | MACROMOLECULAR RESEARCH, v.21, no.5, pp.565 - 573 | - |
dc.relation.isPartOf | MACROMOLECULAR RESEARCH | - |
dc.citation.title | MACROMOLECULAR RESEARCH | - |
dc.citation.volume | 21 | - |
dc.citation.number | 5 | - |
dc.citation.startPage | 565 | - |
dc.citation.endPage | 573 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.identifier.kciid | ART001769631 | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.description.journalRegisteredClass | kci | - |
dc.relation.journalResearchArea | Polymer Science | - |
dc.relation.journalWebOfScienceCategory | Polymer Science | - |
dc.subject.keywordPlus | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject.keywordPlus | INHIBITORS | - |
dc.subject.keywordPlus | EXPRESSION | - |
dc.subject.keywordPlus | INTERNALIZATION | - |
dc.subject.keywordPlus | BINDING | - |
dc.subject.keywordPlus | CANCER | - |
dc.subject.keywordPlus | PSMA | - |
dc.subject.keywordAuthor | molecular imaging | - |
dc.subject.keywordAuthor | prodrug | - |
dc.subject.keywordAuthor | prostate cancer | - |
dc.subject.keywordAuthor | SPECT | - |
dc.subject.keywordAuthor | PSMA | - |
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.