DC Field | Value | Language |
---|---|---|
dc.contributor.author | Lee, Joong-Jae | ko |
dc.contributor.author | Choi, Hyo-Jung | ko |
dc.contributor.author | Yun, Misun | ko |
dc.contributor.author | Kang, YingJin | ko |
dc.contributor.author | Jung, Ji-Eun | ko |
dc.contributor.author | Ryu, Yi Seul | ko |
dc.contributor.author | Kim, Tae Yoon | ko |
dc.contributor.author | Cha, Young-je | ko |
dc.contributor.author | Cho, Hyun-Soo | ko |
dc.contributor.author | Min, Jung-Joon | ko |
dc.contributor.author | Chung, Chul-Woong | ko |
dc.contributor.author | Kim, Hak-Sung | ko |
dc.date.accessioned | 2016-04-20T06:54:46Z | - |
dc.date.available | 2016-04-20T06:54:46Z | - |
dc.date.created | 2015-11-30 | - |
dc.date.created | 2015-11-30 | - |
dc.date.created | 2015-11-30 | - |
dc.date.created | 2015-11-30 | - |
dc.date.created | 2015-11-30 | - |
dc.date.created | 2015-11-30 | - |
dc.date.issued | 2015-10 | - |
dc.identifier.citation | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION, v.54, no.41, pp.11020 - 11024 | - |
dc.identifier.issn | 1433-7851 | - |
dc.identifier.uri | http://hdl.handle.net/10203/205570 | - |
dc.description.abstract | Targeted therapy based on protein-drug conjugates has attracted significant attention owing to its high efficacy and low side effects. However, efficient and stable drug conjugation to a protein binder remains a challenge. Herein, a chemo-enzymatic method to generate highly stable and homogenous drug conjugates with high efficiency is presented. The approach comprises the insertion of the CaaX sequence at the C-terminal end of the protein binder, prenylation using farnesyltransferase, and drug conjugation through an oxime ligation reaction. MMAF and an EGFR-specific repebody are used as the antitumor agent and protein binder, respectively. The method enables the precisely controlled synthesis of repebody-drug conjugates with high yield and homogeneity. The utility of this approach is illustrated by the notable stability of the repebody-drug conjugates in human plasma, negligible off-target effects, and a remarkable antitumor activity in vivo. The present method can be widely used for generating highly homogeneous and stable PDCs for targeted therapy. | - |
dc.language | English | - |
dc.publisher | WILEY-V C H VERLAG GMBH | - |
dc.title | Enzymatic Prenylation and Oxime Ligation for the Synthesis of Stable and Homogeneous Protein-Drug Conjugates for Targeted Therapy | - |
dc.type | Article | - |
dc.identifier.wosid | 000363396000021 | - |
dc.identifier.scopusid | 2-s2.0-84942816757 | - |
dc.type.rims | ART | - |
dc.citation.volume | 54 | - |
dc.citation.issue | 41 | - |
dc.citation.beginningpage | 11020 | - |
dc.citation.endingpage | 11024 | - |
dc.citation.publicationname | ANGEWANDTE CHEMIE-INTERNATIONAL EDITION | - |
dc.identifier.doi | 10.1002/anie.201505964 | - |
dc.contributor.localauthor | Kim, Hak-Sung | - |
dc.contributor.nonIdAuthor | Choi, Hyo-Jung | - |
dc.contributor.nonIdAuthor | Yun, Misun | - |
dc.contributor.nonIdAuthor | Kang, YingJin | - |
dc.contributor.nonIdAuthor | Jung, Ji-Eun | - |
dc.contributor.nonIdAuthor | Cha, Young-je | - |
dc.contributor.nonIdAuthor | Cho, Hyun-Soo | - |
dc.contributor.nonIdAuthor | Min, Jung-Joon | - |
dc.contributor.nonIdAuthor | Chung, Chul-Woong | - |
dc.description.isOpenAccess | N | - |
dc.type.journalArticle | Article | - |
dc.subject.keywordAuthor | cancer | - |
dc.subject.keywordAuthor | drug delivery | - |
dc.subject.keywordAuthor | oxime ligation | - |
dc.subject.keywordAuthor | prenylation | - |
dc.subject.keywordAuthor | protein-drug conjugates | - |
dc.subject.keywordPlus | CANCER-THERAPY | - |
dc.subject.keywordPlus | ANTIBODY THERAPEUTICS | - |
dc.subject.keywordPlus | DELIVERY | - |
dc.subject.keywordPlus | MODULE | - |
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