DC Field | Value | Language |
---|---|---|
dc.contributor.author | Park, Mingu Gordon | ko |
dc.contributor.author | Han, Ah-reum | ko |
dc.contributor.author | Kim, Su Yeon | ko |
dc.contributor.author | Kim, Tai Young | ko |
dc.contributor.author | Kim, Ho Min | ko |
dc.contributor.author | Lee, C. Justin | ko |
dc.date.accessioned | 2021-09-26T00:50:38Z | - |
dc.date.available | 2021-09-26T00:50:38Z | - |
dc.date.created | 2021-09-24 | - |
dc.date.created | 2021-09-24 | - |
dc.date.created | 2021-09-24 | - |
dc.date.created | 2021-09-24 | - |
dc.date.issued | 2021-12 | - |
dc.identifier.citation | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, v.36, no.1, pp.2016 - 2024 | - |
dc.identifier.issn | 1475-6366 | - |
dc.identifier.uri | http://hdl.handle.net/10203/287848 | - |
dc.description.abstract | Many studies have focussed on modulating the activity of gamma-aminobutyric acid transaminase (GABA-T), a GABA-catabolizing enzyme, for treating neurological diseases, such as epilepsy and drug addiction. Nevertheless, human GABA-T synthesis and purification have not been established. Thus, biochemical and drug design studies on GABA-T have been performed by using porcine GABA-T mostly and even bacterial GABA-T. Here we report an optimised protocol for overexpression of 6xHis-tagged human GABA-T in human cells followed by a two-step protein purification. Then, we established an optimised human GABA-T (0.5 U/mg) activity assay. Finally, we compared the difference between human and bacterial GABA-T in sensitivity to two irreversible GABA-T inhibitors, gabaculine and vigabatrin. Human GABA-T in homodimeric form showed 70-fold higher sensitivity to vigabatrin than bacterial GABA-T in multimeric form, indicating the importance of using human GABA-T. In summary, our newly developed protocol can be an important first step in developing more effective human GABA-T modulators. | - |
dc.language | English | - |
dc.publisher | TAYLOR & FRANCIS LTD | - |
dc.title | High-yield synthesis and purification of recombinant human GABA transaminase for high-throughput screening assays | - |
dc.type | Article | - |
dc.identifier.wosid | 000695129200001 | - |
dc.identifier.scopusid | 2-s2.0-85114812910 | - |
dc.type.rims | ART | - |
dc.citation.volume | 36 | - |
dc.citation.issue | 1 | - |
dc.citation.beginningpage | 2016 | - |
dc.citation.endingpage | 2024 | - |
dc.citation.publicationname | JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY | - |
dc.identifier.doi | 10.1080/14756366.2021.1975697 | - |
dc.contributor.localauthor | Kim, Ho Min | - |
dc.contributor.nonIdAuthor | Park, Mingu Gordon | - |
dc.contributor.nonIdAuthor | Han, Ah-reum | - |
dc.contributor.nonIdAuthor | Kim, Su Yeon | - |
dc.contributor.nonIdAuthor | Kim, Tai Young | - |
dc.contributor.nonIdAuthor | Lee, C. Justin | - |
dc.description.isOpenAccess | Y | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | 4-Aminobutyrate transaminase | - |
dc.subject.keywordAuthor | isolation and purification | - |
dc.subject.keywordAuthor | high-throughput screening assays | - |
dc.subject.keywordAuthor | gabaculine | - |
dc.subject.keywordAuthor | vigabatrin | - |
dc.subject.keywordPlus | AMINOBUTYRIC-ACID AMINOTRANSFERASE | - |
dc.subject.keywordPlus | GAMMA-VINYL GABA | - |
dc.subject.keywordPlus | HUMAN-BRAIN | - |
dc.subject.keywordPlus | 4-AMINOBUTYRATE AMINOTRANSFERASE | - |
dc.subject.keywordPlus | TISSUE DISTRIBUTION | - |
dc.subject.keywordPlus | ASTROCYTES | - |
dc.subject.keywordPlus | INACTIVATION | - |
dc.subject.keywordPlus | INHIBITION | - |
dc.subject.keywordPlus | MECHANISM | - |
dc.subject.keywordPlus | OVEREXPRESSION | - |
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