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Effect of C-terminus Conjugation via Different Conjugation Chemistries on In Vivo Activity of Albumin-Conjugated Recombinant GLP-1

Pharmaceutics. 2021-02; 
Junyong Park, Mijeong Bak, Kiyoon Min, Hyun-Woo Kim, Jeong-Haeng Cho, Giyoong Tae, Inchan Kwon
Products/Services Used Details Operation
Peptide Synthesis … USA). The GLP-1_WT and GLP-1_8GWT peptides were synthesized by GenScript (Piscataway, NJ, USA). Vivaspin 6 concentrator and 10,000 MWCO were purchased from Sartorius (Weender Landstra?e, G?ttingen, Germany)?… Get A Quote

摘要

Glucagon-like peptide-1 (GLP-1) is a peptide hormone with tremendous therapeutic potential for treating type 2 diabetes mellitus. However, the short half-life of its native form is a significant drawback. We previously prolonged the plasma half-life of GLP-1 via site-specific conjugation of human serum albumin (HSA) at position 16 of recombinant GLP-1 using site-specific incorporation of p-azido-phenylalanine (AzF) and strain-promoted azide-alkyne cycloaddition (SPAAC). However, the resulting conjugate GLP1_8G16AzF-HSA showed only moderate in vivo glucose-lowering activity, probably due to perturbed interactions with GLP-1 receptor (GLP-1R) caused by the albumin-linker. To identify albumin-conjugated GLP-1 vari... More

關鍵詞

albumin conjugation, glucagon-like peptide-1, in vivo glucose-lowering activity, plasma half-life extension
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