The hexapeptide inhibitor of Galβ1,3GalNAc-specific α2,3-Sialyltransferase as a generic inhibitor of sialyltransferases

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dc.contributor.authorKi-Young Lee-
dc.contributor.authorH G Kim-
dc.contributor.authorMi Ran Hwang-
dc.contributor.authorJung Il Chae-
dc.contributor.authorJ M Yang-
dc.contributor.authorY C Lee-
dc.contributor.authorY K Choo-
dc.contributor.authorYoung Ik Lee-
dc.contributor.authorS S Lee-
dc.contributor.authorSu Il Do-
dc.date.accessioned2017-04-19T08:59:27Z-
dc.date.available2017-04-19T08:59:27Z-
dc.date.issued2002-
dc.identifier.issn0021-9258-
dc.identifier.uri10.1074/jbc.M209618200ko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/5986-
dc.description.abstractThe mammalian Galβ1,3GalNAc-specific α2,3-sialyltransferase (ST3Gal I) was expressed as a secreted glycoprotein in High Five™ (Trichoplusia ni) cells. Using this recombinant ST3Gal I, we screened the synthetic hexapeptide combinatorial library to explore a sialyltransferase inhibitor. We found that the hexapeptide, NH2-GNWWWW, exhibited the most strong inhibition of ST3Gal I among five different hexapeptides that were finally selected. The kinetic analysis of ST3Gal I inhibition demonstrated that this hexapeptide could act as a competitive inhibitor (Ki = 1.1 μm) on CMP-NeuAc binding to the enzyme. Moreover, the hexapeptide was shown to strongly inhibit both N-glycan-specific α2,3and α2,6-sialyltranferase in vitro, suggesting that this peptide may inhibit the broad range of sialyltransferases regardless of their linkage specificity. The inhibitory activity in vivo was investigated by RCA-I lectin blot analyses and by metabolic D-[6-3H]GlcNH2 radiolabeling analyses of N- and O-linked oligosaccharides in Chines hamster ovary cells. Our results demonstrate that the hexapeptide can act as a generic inhibitor of the N- and O-glycan-specific sialyltransferases in mammalian cells, which results in the significantly reduced NeuAc expression on cellular glycoproteins in vivo.-
dc.publisherElsevier-
dc.titleThe hexapeptide inhibitor of Galβ1,3GalNAc-specific α2,3-Sialyltransferase as a generic inhibitor of sialyltransferases-
dc.title.alternativeThe hexapeptide inhibitor of Galβ1,3GalNAc-specific α2,3-Sialyltransferase as a generic inhibitor of sialyltransferases-
dc.typeArticle-
dc.citation.titleJournal of Biological Chemistry-
dc.citation.number51-
dc.citation.endPage49351-
dc.citation.startPage49341-
dc.citation.volume277-
dc.contributor.affiliatedAuthorKi-Young Lee-
dc.contributor.affiliatedAuthorMi Ran Hwang-
dc.contributor.affiliatedAuthorJung Il Chae-
dc.contributor.affiliatedAuthorYoung Ik Lee-
dc.contributor.affiliatedAuthorSu Il Do-
dc.contributor.alternativeName이기영-
dc.contributor.alternativeName김형구-
dc.contributor.alternativeName황미란-
dc.contributor.alternativeName채정일-
dc.contributor.alternativeName양재명-
dc.contributor.alternativeName이영춘-
dc.contributor.alternativeName추영국-
dc.contributor.alternativeName이영익-
dc.contributor.alternativeName이상수-
dc.contributor.alternativeName도수일-
dc.identifier.bibliographicCitationJournal of Biological Chemistry, vol. 277, no. 51, pp. 49341-49351-
dc.identifier.doi10.1074/jbc.M209618200-
dc.description.journalClassY-
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