A novel approach in potential anticoagulants from peptides epitope 558-565 of A2 subunit of factor VIII

C. Anastasopoulos, Y. Sarigiannis, G. Stavropoulos

Research output: Contribution to journalArticle

2 Citations (Scopus)

Abstract

Factor VIII, a human blood plasma protein, plays an important role during the intrinsic pathway of blood coagulation cascade after its activation by thrombin. The activated form of FVIII acts as cofactor to the serine protease Factor IXa, in the conversion of the zymogen Factor X to the active enzyme Factor Xa. The Ser558-Gln565 region of the A2 subunit of Factor VIII has been shown to be crucial for FVIIIa-FIXa interaction. Based on this, a series of linear peptides, analogs of the 558-565 loop of the A2 subunit of the heavy chain of Factor VIII were synthesized using the acid labile 2-chlorotrityl chloride resin and biologically evaluated in vitro by measuring the chronic delay of activated partial thromboplastin time and the inhibition of Factor VIII activity, as potential anticoagulants.

Original languageEnglish
Pages (from-to)1159-1165
Number of pages7
JournalAmino Acids
Volume44
Issue number4
DOIs
Publication statusPublished - Apr 2013

Keywords

  • Activated partial thromboplastin time
  • Anticoagulant activity
  • Blood coagulation cascade
  • Factor VIII
  • FVIII-FIX interaction
  • Synthetic peptides

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