Effect of O-glycosylation and tyrosine sulfation of leech-derived peptides on binding and inhibitory activity against thrombin.

نویسندگان

  • Yves S Y Hsieh
  • Deni Taleski
  • Brendan L Wilkinson
  • Lakshmi C Wijeyewickrema
  • Ty E Adams
  • Robert N Pike
  • Richard J Payne
چکیده

Synthesis of sulfated and unsulfated (glyco)peptide fragments of Hirudin P6 (a potent anticoagulant from the leech Hirudinaria manillensis) is described. The effect of O-glycosylation and tyrosine sulfation on thrombin binding and peptidolytic activity was investigated, together with the inhibition of fibrinogen cleavage.

برای دانلود رایگان متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید

ثبت نام

اگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید

منابع مشابه

Cloning and Expression of Two New Recombinant Antimicrobial Dermaseptin B1 Peptides in Tobacco to Control the Growth of Human Bacterial Pathogens

Background and purpose: Rapid emergence of traditional antibiotic-resistant pathogens is one of the most important global challenges in medical sciences. To this end, substitution of current antibiotics with strong antimicrobial peptides could be of great benefit. Materials and methods: In this study, the DNA sequence encoding dermaseptin B1 (DrsB1) antimicrobial peptide derived from Phyllomed...

متن کامل

Discovery of Novel Peptidomimetics for Brain-Derived Neurotrophic Factor using Phage Display Technology

Brain-Derived Neurotrophic Factor (BDNF) is a neuroprotectant candidate for neurodegenerative diseases. However, there are several clinical concerns about its therapeutic applications. In the current study, we selected BDNF-mimicking small peptides from phage-displayed peptide library as alternative molecules to the clinical challenges. The peptide library was screened against BDNF receptor (Ne...

متن کامل

Anticoagulant activity of synthetic hirudin peptides.

Synthetic peptides based on the COOH-terminal 21 residues of hirudin were prepared in order to 1) evaluate the role of this segment in hirudin action toward thrombin, 2) define the shortest peptide derivative with anticoagulant activity, and 3) investigate the role of tyrosine sulfation in the peptides' inhibitory activities. A hirudin derivative of 20 amino acids, Hir45-64 (derived from residu...

متن کامل

Expression and antimicrobial activity analysis of dermaseptin B1 recombinant peptides in tobacco transgenic plants

Recently, new molecular breeding and genetic engineering approaches have emerged to overcome the limitations of conventional breeding methods in generating disease-resistance transgenic plants. The use of antimicrobial peptides (AMPs) to produce transgenic plants resistant to a wide range of plant pathogens has achieved great success. Among huge number of AMPs, Dermaseptin B1 (DrsB1), an antimi...

متن کامل

Receptor Tyrosine Kinase Inhibitory Activities and Molecular Docking Studies of Some Pyrrolo[2,3-d]pyrimidine Derivatives

In this study, we aimed to determine VEGFR-2, EGFR and PDGFR-β tyrosine kinase inhibitory activities of some pyrrolo[2,3-d]pyrimidine derivatives previously synthesized and showed potent cytotoxic and apoptotic effects against several cancer cell lines by our group and to evaluate the relationships between inhibitory activities and binding properties of the active compounds by molecular docking...

متن کامل

ذخیره در منابع من


  با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید

عنوان ژورنال:
  • Chemical communications

دوره 48 10  شماره 

صفحات  -

تاریخ انتشار 2012