SINGLE CHAIN INSULIN AGONISTS EXHIBITING HIGH ACTIVITY AT THE INSULIN RECEPTOR
摘要
Single chain insulin analogs are provided having high potency and specificity for the insulin receptor. As disclosed herein optimally sized linking moieties can be used to link human insulin A and B chains, or analogs or derivatives thereof, wherein the carboxy terminus of the B25 amino acid of the B chain is linked to the amino terminus of the A1 amino acid of the A chain via the intervening linking moiety. In on embodiment the linking moiety comprises a polyethylene glycol of 6-16 monomer units and in an alternative embodiment the linking moiety comprises a non-native amino acid sequence derived form the IGF-1 C-peptide and comprising at least 8 amino acids and no more than 12 amino acid in length. Also disclosed are prodrug and conjugate derivatives of the single chain insulin analogs.
申请公布号
EP2582719(A2)
申请公布日期
2013.04.24
申请号
EP20110796430
申请日期
2011.06.16
申请人
INDIANA UNIVERSITY RESEARCH AND TECHNOLOGY CORPORATION
发明人
DIMARCHI, RICHARD, D.;AZRIEL, JULIA;KAUR, ZACH;MEYERS, JONATHAN;PARODY, TODD;ZHAO, YAN