Monomeric B27 Lys destripeptide insulin: semisynthesis, characterization and biological activity.
In this paper, we report the semisynthesis of B27 Lys destripeptide insulin (B27 Lys DTrI), i.e. destetrapeptide insulin with an additional Lys residue at the C-terminus of B-chain. B27 Lys DTrI is also monomeric as shown by gel filtration. Its in vivo biological activity is 80% in comparison with that of native insulin. The addition of a Lys residue at the C-terminus of B-chain makes it possible to obtain monomeric B27 Lys DTrI from a precursor expressed in Saccharomyces cerevesiae by tryptic hydrolysis instead of the less efficient tryptic transpeptidation.
Ding
Jin-Guo
JG
Institute of Biochemistry and Cell Biology, Shanghai Institutes for Biological Sciences, the Chinese Academy of Sciences, Shanghai 200031, China.
Cui
Da-Fu
DF
Zhang
You-Shang
YS
D000595:Amino Acid Sequence; D000818:Animals; D001667:Binding, Competitive; D001786:Blood Glucose / Q000187:drug effects / Q000378:metabolism; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004591:Electrophoresis, Polyacrylamide Gel; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D007328:Insulin / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000302:isolation & purification / Q000494:pharmacology*; D051379:Mice; D010446:Peptide Fragments / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology; D011972:Receptor, Insulin / Q000378:metabolism; D013552:Swine
C477145:B27 Lys destripeptide insulin; D001786:Blood Glucose; D007004:Hypoglycemic Agents; D007328:Insulin; D010446:Peptide Fragments; D011972:Receptor, Insulin