Abstract:
:A method for the preparation of insulin derivatives having protected sulfhydryl group(s) on definite site(s) on the molecule which uses anion-exchange high performance liquid chromatography on a TSKgel DEAE-2SW column for separation is described. Porcine insulin reacts with N-succinimidyl S-acetylthioacetate to afford four species of insulin derivatives that have S-acetylthioglycoloyl group(s) at: i) Gly(A1), ii) Gly(A1) and Phe(B1), iii) Gly(A1) and Lys(B29), and iv) Gly(A1), Phe(B1) and Lys(B29) positions. An insulin derivative which has a group at the Lys(B29)-position is prepared by the S-acetylthioglycoloylation of Gly(A1), Phe(B1)-dicitraconyl insulin followed by decitraconylation. The five derivatives are readily deacetylated with hydroxylamine to yield the corresponding sulfhydryl insulin derivatives.
journal_name
Chem Pharm Bull (Tokyo)journal_title
Chemical & pharmaceutical bulletinauthors
Nanami M,Zaitsu K,Ohkura Ydoi
10.1248/cpb.40.957subject
Has Abstractpub_date
1992-04-01 00:00:00pages
957-60issue
4eissn
0009-2363issn
1347-5223journal_volume
40pub_type
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