Revisiting antithrombotic therapeutics; sculptin, a novel specific, competitive, reversible, scissile and tight binding inhibitor of thrombin.

ABSTRACT: Thrombin is a multifunctional enzyme with a key role in the coagulation cascade. Its functional modulation can culminate into normal blood coagulation or thrombosis. Thus, the identification of novel potent inhibitors of thrombin are of immense importance. Sculptin is the first specific thrombin inhibitor identified in the transcriptomics analysis of tick's salivary glands. It consists of 168 residues having four similar repeats and evolutionary diverged from hirudin. Sculptin is a competitive, specific and reversible inhibitor of thrombin with a K_i of 18.3 ± 1.9 pM (k _on 4.04 ± 0.03 × 10⁷ M^-1 s^-1 and k _off 0.65 ± 0.04 × 10^-3 s^-1). It is slowly consumed by thrombin eventually losing its activity. Contra

SUBMITTER: Iqbal A 

PROVIDER: S-EPMC5431157 | biostudies-literature | 2017 May

REPOSITORIES: biostudies-literature