NDLI: Convergent chemoenzymatic synthesis of a library of glycosylated analogues of pramlintide: structure-activity relationships for amylin receptor agonism.

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Convergent chemoenzymatic synthesis of a library of glycosylated analogues of pramlintide: structure-activity relationships for amylin receptor agonism.

Content Provider	Semantic Scholar
Author	Kowalczyk, Renata Brimble, Margaret A. Tomabechi, Yusuke Fairbanks, Antony John Fletcher, Madeleine De Gogorza Hay, Debbie L.
Copyright Year	2014
Abstract	Pramlintide (Symlin®), a synthetic analogue of the naturally occurring pancreatic hormone amylin, is currently used with insulin in adjunctive therapy for type 1 and type 2 diabetes mellitus. Herein we report a systematic study into the effect that N-glycosylation of pramlintide has on activation of amylin receptors. A highly efficient convergent synthetic route, involving a combination of solid phase peptide synthesis and enzymatic glycosylation, delivered a library of N-glycosylated variants of pramlintide bearing either GlcNAc, the core N-glycan pentasaccharide [Man3(GlcNAc)2] or a complex biantennary glycan [(NeuAcGalGlcNAcMan)2Man(GlcNAc)2] at each of its six asparagine residues. The majority of glycosylated versions of pramlintide were potent receptor agonists, suggesting that N-glycosylation may be used as a tool to optimise the pharmacokinetic properties of pramlintide and so deliver improved therapeutic agents for the treatment of diabetes and obesity.
Starting Page	54
Ending Page	59
Page Count	6
File Format	PDF HTM / HTML
Alternate Webpage(s)	http://www.rsc.org/suppdata/ob/c4/c4ob01208a/c4ob01208a1.pdf
Alternate Webpage(s)	http://pubs.rsc.org/en/content/getauthorversionpdf/C4OB01208A
PubMed reference number	25030939v1
Alternate Webpage(s)	https://doi.org/10.1039/c4ob01208a
DOI	10.1039/c4ob01208a
Journal	Organic & biomolecular chemistry
Volume Number	12
Issue Number	41
Language	English
Access Restriction	Open
Subject Keyword	2.7 ML pramlintide acetate 1 MG/ML Pen Injector [Symlin] Amylin Analog Asparagine Diabetes Mellitus Diabetes Mellitus, Non-Insulin-Dependent Glycosylphosphatidylinositol Diacylglycerol-Lyase IAPP gene Obesity Polysaccharides Receptors, Islet Amyloid Polypeptide Stiff-Person Syndrome Version
Content Type	Text
Resource Type	Article

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Convergent chemoenzymatic synthesis of a library of glycosylated analogues of pramlintide: structure-activity relationships for amylin receptor agonism.

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