Synthesis and thrombolytic activity of fibrinogen fragment related cyclopeptides.

Abstract:

:In the modification of the fibrinogen fragment related sequences ARPAK, QRPAK GRPAK and KRPAK, the corresponding cyclo-ARPAK, cyclo-QRPAK, cyclo-GRPAK, and cyclo-KRPAK were prepared in the diluted solution. The bioassay in vivo indicated that the thrombolytic potencies of cyclo-ARPAK, cyclo-GRPAK, cyclo-QRPAK, and cyclo-KRPAK were significantly higher than that of ARPAK, QRPAK, GRPAK, and KRPAK. In water, the cyclopeptides were incubated with pepsin or trypsin at 37 degrees C for 64 h. There was no degradation product observed, on the other hand, with the same condition, the peptides were completely hydrolyzed in 8 h. The relationships among the rigidity or the conformation and the thrombolytic activity in vivo and the stability to enzyme-induced hydrolysis in vitro of the cyclopeptides were discussed.

journal_name

Bioorg Med Chem Lett

authors

Zhao M,Lin N,Wang C,Peng S

doi

10.1016/s0960-894x(02)01072-7

subject

Has Abstract

pub_date

2003-03-10 00:00:00

pages

961-4

issue

5

eissn

0960-894X

issn

1464-3405

pii

S0960894X02010727

journal_volume

13

pub_type

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