Targeting the contact-kinin system: A cyclopeptide with anti-thromboinflammatory properties against stroke.

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Tác giả: Mingqian Fang, Yuqing Fang, Jinai Gao, Qiumin Lu, Chen Na, Rebecca Caroline Thuku, Wanting Wang, Juan Yang, Yan Zhang

Ngôn ngữ: eng

Ký hiệu phân loại:

Thông tin xuất bản: Netherlands : European journal of pharmacology , 2025

Mô tả vật lý:

Bộ sưu tập: NCBI

ID: 710973

 The contact-kinin system plays a central role in the thromboinflammatory pathology of ischemic stroke. Modulating this pathway represents a promising strategy for the prevention and treatment of ischemic stroke. Based on our recent findings demonstrating that the short peptide SD6 (SLGASD), derived from a specific influenza-related immunoglobulin heavy chain junction region sequence, exhibits anti-coagulant properties, we designed a cyclized version, cycloSD6, and evaluated its anti-ischemic stroke potential. Notably, cycloSD6 showed enhanced inhibition of activated coagulation factor XII (FXIIa
  with an inhibition constant (Ki) of 41.27 μM) and plasma kallikrein (PKa
  Ki: 28.54 μM), two key enzymes in the contact-kinin system, surpassing the inhibitory effects of its linear form. In vitro, 4-100 μM of CycloSD6 inhibited LPS-induced inflammation. And CycloSD6 at doses of 1 and 4 mg/kg displayed significant anti-thrombotic functions in several mouse models, including carrageenan-induced tail thrombosis, FeCl
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