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dc.contributor.author이근용-
dc.date.accessioned2019-11-25T06:10:40Z-
dc.date.available2019-11-25T06:10:40Z-
dc.date.issued2017-05-
dc.identifier.citationMOLECULAR PHARMACEUTICS, v. 14, no. 5, page. 1558-1570en_US
dc.identifier.issn1543-8384-
dc.identifier.urihttps://pubs.acs.org/doi/10.1021/acs.molpharmaceut.6b01083-
dc.identifier.urihttps://repository.hanyang.ac.kr/handle/20.500.11754/114153-
dc.description.abstractBiological ligands such as aptamer, antibody, glucose, and peptide have been widely used to bind specific surface molecules or receptors in tumor cells or subcellular structures to improve tumor-targeting efficiency of nanoparticles. However, this active-targeting strategy has limitations for tumor targeting due to inter- and intraheterogeneity of tumors. In this study, we demonstrated an alternative active-targeting strategy using metabolic engineering and bioorthogonal click reaction to improve tumor-targeting efficiency of nanoparticles. We observed that azide-containing chemical reporters were successfully generated onto surface glycans of various tumor cells such as lung cancer (A549), brain cancer (U87), and breast cancer (BT-474, MDA-MB231, MCF-7) via metabolic engineering in vitro. In addition, we compared tumor targeting-of artificial azide reporter with bicyclononyne (BCN)-conjugated glycol chitosan nanoparticles (BCN-CNPs) and integrin alpha(v)beta(3) with cyclic RGD-conjugated CNPs (cRGD-CNPs) in vitro and in vivo. Fluorescence intensity of azide-reporter-targeted BCN-CNPs in tumor tissues was 1.6-fold higher and with a more uniform distribution compared to that of cRGD-CNPs. Moreover, even in the isolated heterogeneous U87 cells, BCN-CNPs could bind artificial azide reporters on tumor cells more unifornaly (similar to 92.9%) compared to cRGD-CNPs. Therefore, the artificial azide-reporter-targeting strategy can be utilized for targeting heterogeneous tumor cells via bioorthogonal click reaction and may provide an alternative method of tumor targeting for further investigation in cancer therapy.en_US
dc.description.sponsorshipThis work was supported by the GiRC (NRF-2012K1A1A2A01 055811), the GRL project (NRF-2013K1A1A2A02050115), and the Intramural Research Program (CATS) of KIST.en_US
dc.language.isoen_USen_US
dc.publisherAMER CHEMICAL SOCen_US
dc.subjectmetabolic glycoengineeringen_US
dc.subjectbioorthogonal click reactionen_US
dc.subjectactive tumor targetingen_US
dc.subjectheterogeneityen_US
dc.titleArtificial Chemical Reporter Targeting Strategy Using Bioorthogonal Click Reaction for Improving Active-Targeting Efficiency of Tumoren_US
dc.typeArticleen_US
dc.relation.no5-
dc.relation.volume14-
dc.identifier.doi10.1021/acs.molpharmaceut.6b01083-
dc.relation.page1558-1570-
dc.relation.journalMOLECULAR PHARMACEUTICS-
dc.contributor.googleauthorYoon, Hong Yeol-
dc.contributor.googleauthorShin, Mm Lee-
dc.contributor.googleauthorShim, Man Kyu-
dc.contributor.googleauthorLee, Sangmin-
dc.contributor.googleauthorNa, Jin Hee-
dc.contributor.googleauthorKoo, Heebeom-
dc.contributor.googleauthorLee, Hyukjin-
dc.contributor.googleauthorKim, Jong-Ho-
dc.contributor.googleauthorLee, Kuen Yong-
dc.contributor.googleauthorKim, Kwangmeyung-
dc.relation.code2017007779-
dc.sector.campusS-
dc.sector.daehakCOLLEGE OF ENGINEERING[S]-
dc.sector.departmentDEPARTMENT OF BIOENGINEERING-
dc.identifier.pidleeky-
dc.identifier.orcidhttp://orcid.org/0000-0002-5759-5952-
Appears in Collections:
COLLEGE OF ENGINEERING[S](공과대학) > BIOENGINEERING(생명공학과) > Articles
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