Semisynthesis and biological properties of the [B24-leucine]-, [B25-leucine]- and [B24-leucine,B25-leucine]-analogues of human insulin |
| |
Authors: | K Inouye K Watanabe Y Tochino T Kanaya M Kobayashi Y Shigeta |
| |
Institution: | (1) Shionogi Research Laboratories, Shionogi & Co., Ltd., Fukushima-ku, 553 Osaka, (Japan);(2) The Third Department of Internal Medicine, Shiga University of Medical Science, Ohtsu, 520-21 Shiga, (Japan) |
| |
Abstract: | Summary Trypsin-catalyzed coupling of porcine desoctapeptide-insulin with synthetic octapeptides produced the LeuB24]-(I), LeuB25]- (II) and LeuB24, LeuB25]- (III)analogues of human insulin. I, II and III displayed respectively 20–30%, 1–2% and 0.5% of the receptor binding activity of the normal hormone. Biological activities of these analogues seemed to be proportional to their binding potencies when assayed in vitro, while in an in vivo assay analogue I was fully active and II exhibited 10–20% of normal activity. III was less active than II in all assays tested. |
| |
Keywords: | |
本文献已被 SpringerLink 等数据库收录! |
|