Optimization and validation of a fluorogenic dipeptidyl peptidase 4 enzymatic assay in human plasma
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Yoon, Hyunyee | - |
dc.contributor.author | Cho, Su Hee | - |
dc.contributor.author | Seo, Yu Rim | - |
dc.contributor.author | Yu, Kyung-Sang | - |
dc.contributor.author | Park, Sung Sup | - |
dc.contributor.author | Song, Moon Jung | - |
dc.date.accessioned | 2021-08-30T04:28:13Z | - |
dc.date.available | 2021-08-30T04:28:13Z | - |
dc.date.created | 2021-06-19 | - |
dc.date.issued | 2021-01-01 | - |
dc.identifier.issn | 0003-2697 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/50167 | - |
dc.description.abstract | During the development of a specific dipeptidyl peptidase 4 (DPP4) inhibitor to treat type 2 diabetes, a fluorogenic kinetic analysis for DPP4 enzymatic activity using Gly-Pro-Aminomethylcoumarin (AMC) as a substrate was optimized and validated for recombinant DPP4 and human plasma samples. The sensitivity, calibration curve, detection range, accuracy, precision, recovery efficiency, Km constant, short/long-term stability, and stability after freezing-thawing cycles were analyzed. DPP4 enzymatic activity (mU/min) was measured as the initial velocity (Vo) of the enzymatic reaction over time. The sensitivity of the Vo value was 14,488 mU/min for recombinant DPP4 and 17,995 mU/min for human plasma samples. The dynamic ranges of the calibration curve were linear and reliable between 1.11 x 10(4)-1.86 x 10(6) mU/min of the mean Vo value and in the DPP4 concentration range of 23.4-3,000 ng/mL. The assay's accuracy and precision met acceptance criteria for all samples. Plasma DPP4 was stable under various storage temperatures, even after three freeze-thaw cycles. Our optimized, validated bioanalytic method for measuring DPP4 activity in plasma samples was successfully employed to evaluate the effect of evogliptin (DA-1229) tartrate, which irreversibly and dose-dependently inhibits DPP4 enzymatic activity, without the dilution effect of human plasma samples and irrespective of the co-treated metformin. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | ACADEMIC PRESS INC ELSEVIER SCIENCE | - |
dc.subject | IV INHIBITOR | - |
dc.subject | DPP4 INHIBITOR | - |
dc.subject | DOUBLE-BLIND | - |
dc.subject | EVOGLIPTIN | - |
dc.subject | DA-1229 | - |
dc.subject | SITAGLIPTIN | - |
dc.subject | EFFICACY | - |
dc.subject | METFORMIN | - |
dc.subject | SAFETY | - |
dc.subject | PHARMACOKINETICS | - |
dc.title | Optimization and validation of a fluorogenic dipeptidyl peptidase 4 enzymatic assay in human plasma | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Song, Moon Jung | - |
dc.identifier.doi | 10.1016/j.ab.2020.113952 | - |
dc.identifier.scopusid | 2-s2.0-85092146744 | - |
dc.identifier.wosid | 000597177800002 | - |
dc.identifier.bibliographicCitation | ANALYTICAL BIOCHEMISTRY, v.612 | - |
dc.relation.isPartOf | ANALYTICAL BIOCHEMISTRY | - |
dc.citation.title | ANALYTICAL BIOCHEMISTRY | - |
dc.citation.volume | 612 | - |
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 | Biochemical Research Methods | - |
dc.relation.journalWebOfScienceCategory | Biochemistry & Molecular Biology | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Analytical | - |
dc.subject.keywordPlus | IV INHIBITOR | - |
dc.subject.keywordPlus | DPP4 INHIBITOR | - |
dc.subject.keywordPlus | DOUBLE-BLIND | - |
dc.subject.keywordPlus | EVOGLIPTIN | - |
dc.subject.keywordPlus | DA-1229 | - |
dc.subject.keywordPlus | SITAGLIPTIN | - |
dc.subject.keywordPlus | EFFICACY | - |
dc.subject.keywordPlus | METFORMIN | - |
dc.subject.keywordPlus | SAFETY | - |
dc.subject.keywordPlus | PHARMACOKINETICS | - |
dc.subject.keywordAuthor | Dipeptidyl peptidase 4 (DPP4) | - |
dc.subject.keywordAuthor | Enzymatic assay | - |
dc.subject.keywordAuthor | Evogliptin (DA-1229) tartrate | - |
dc.subject.keywordAuthor | Human plasma | - |
dc.subject.keywordAuthor | Type 2 diabetes mellitus (T2DM) | - |
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.