A photoaffinity label for the thromboxane A2/prostaglandin H2 receptor in human blood platelets

FEBS Letters

Lim, C.T.³  Venton, D.L.¹  Le Breton, G.C.⁴  Arora, S.K.²  Kattelman, E.J.³ 

[1] College of Pharmacy, University of Illinois at Chicago, Chicago, IL 60612, USA;Department of Medicinal Chemistry, University of Illinois at Chicago, Chicago, IL 60612, USA;Department of Pharmacology, University of Illinois at Chicago, Chicago, IL 60612, USA;College of Medicine, University of Illinois at Chicago, Chicago, IL 60612, USA

关键词: Platelet;    Thromboxane receptor;    Photoaffinity label;    U46619;   

DOI  :  10.1016/0014-5793(87)81487-4

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

A photoactive iodoarylazide derivative (I-APA-PhN₃) of the competitive thromboxane A₂/prostaglandin H₂ (TXA₂/PGH₂) antagonist 13-azaprostanoic acid is evaluated. Upon photoactivation, the compound was found to inhibit specifically and irreversibly human platelet aggregation induced by the TXA₂/PGH₂ mimetic U46619. In receptor-binding studies using [³H]U46619, I-APA-PhN₃ exhibited an IC₅₀ of 300 nM for inhibition of U46619 binding. Photoactivation of I-APA-PhN₃ resulted in an irreversible 58% reduction in specific binding of U46619. This compound and its corresponding radio-iodinated form will prove to be useful tools for the isolation and purification of the TXA₂/PGH₂-binding protein in human platelets.

【 授权许可】

Unknown