A Short Half-Life α_IIbβ₃ Antagonist ANTP266 Reduces Thrombus Formation.

ABSTRACT: Integrin α_IIbβ₃ plays a pivotal role in platelet aggregation. Three α_IIbβ₃ antagonists have been approved by the Food and Drug Administration (FDA) for the treatment of cardiovascular diseases. Unfortunately, all of these three drugs can cause the side effect of severe bleeding. Therefore, developing a new α_IIbβ₃ antagonist with low bleeding was needed. In the present study, we screened compounds by using a fibrinogen/integrin α_IIbβ₃ enzyme-linked immunosorbent assay (ELISA), and a novel α_IIbβ₃ antagonist ANTP266 was attained. The antithrombotic effects of ANTP266 were estimated by using two animal models, the bleeding risk was estimated by using a mice tail cutting assay, and the plasma half-life time was tested by LC-MS/MS. The resul

SUBMITTER: Liu TD 

PROVIDER: S-EPMC6121621 | biostudies-literature | 2018 Aug

REPOSITORIES: biostudies-literature