The mosquito-borne West Nile virus (WNV) causes a wide range of symptoms ranging from fever to the often fatal viral encephalitis. To date, no vaccine or drug therapy is available. The trypsin-like WNV NS2B-NS3 protease is deemed a plausible drug target and was shown to be inhibited by bovine pancreatic trypsin inhibitor (BPTI), a 58-residue protein isolated from bovine lung. Herein, we report a protein truncation study that resulted in a novel 14-residue cyclic peptide with equipotent inhibitory activity to native BPTI. We believe our truncation strategy can be further applied in the development of peptide-based inhibitors targeting trypsin-like proteases.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1080/14756366.2016.1190713 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Molecular Docking Studies and In Vitro Activity of Pancreatic Lipase Inhibitors from Yak Milk Cheese.
Int J Mol Sci
January 2025
Functional Dairy Products Engineering Laboratory of Gansu Province, College of Food Science and Engineering, Gansu Agricultural University, Lanzhou 730070, China.
Pancreatic lipase serves as a primary trigger for hyperlipidemia and is also a crucial target in the inhibition of hypercholesterolemia. By synthesizing anti-hypercholesterolemic drugs such as atorvastatin, which are used to treat hypercholesterolemia, there were some side effects associated with the long-term use of statins. Based on this idea, in the present study, we identified peptides that inhibited PL by virtual screening and in vitro activity assays.
View Article and Find Full Text PDFFDA-Approved Hydrogel-Mediated In Situ Sonodynamic and Chemotherapeutic Therapy for Pancreatic Cancer.
Pharmaceuticals (Basel)
December 2024
Department of Radiology, Sixth People's Hospital, Shanghai Jiaotong University School of Medicine, Shanghai 200025, China.
Albumin-bound paclitaxel (nab-PTX) nanoparticles have been proven effective in treating advanced pancreatic cancer. However, the clinical application of nab-PTX nanoparticles is often associated with suboptimal outcomes and severe side effects due to its non-specific distribution and rapid clearance. This study aims to develop a novel nanoplatform that integrates sonodynamic therapy (SDT) and chemotherapy to enhance treatment efficacy and reduce systemic side effects.
View Article and Find Full Text PDFIvermectin Combined With Recombinant Methioninase (rMETase) Synergistically Eradicates MiaPaCa-2 Pancreatic Cancer Cells.
Anticancer Res
January 2025
AntiCancer Inc., San Diego, CA, U.S.A.;
Background/aim: Ivermectin was initially utilized as a veterinary medication, demonstrating efficacy against various parasites. Pancreatic cancer is currently one of the most recalcitrant diseases. The aim of the present study was to demonstrate the synergy of the combination of recombinant methioninase (rMETase) and ivermectin to eradicate human pancreatic cancer cells in vitro.
View Article and Find Full Text PDFTechniques of Oncovascular Reconstruction of Portal and Mesenteric Veins during Pancreatic and Hepatobiliary Surgery.
Vasc Specialist Int
December 2024
Division of Vascular Surgery, Department of Surgery, Seoul National University College of Medicine, Seoul, Korea.
Major vessel invasion, particularly involving the portal and superior mesenteric veins, poses significant challenges during the radical resection of hepatobiliary and pancreatic cancers. Oncovascular surgery is essential for curative outcomes, and often requires portomesenteric vein reconstruction. Techniques, such as lateral venorrhaphy, patch repair, end-to-end anastomosis, and interposition grafting, have been employed.
View Article and Find Full Text PDFDeciphering the role of neutral diruthenium complexes in protein binding.
Int J Biol Macromol
December 2024
Department of Chemical Sciences, University of Naples Federico II, Complesso Univ. di Monte Sant'Angelo, via Cinthia, 26, 80126 Naples, Italy. Electronic address:
The charge of paddlewheel diruthenium complexes has a major role in defining their interaction with proteins: negatively charged complexes bind proteins non-covalently, while cationic complexes form adducts where the Ru core binds to Asp side chains at the equatorial sites, or to the main chain carbonyl groups or the side chains of His, Arg or Lys residues at the axial sites. Here we study the interactions of the neutral compound [Ru(D-p-FPhF)(OCCH)(OCO)]·3HO (D-p-FPhF = N,N'-bis(4-fluorophenyl)formamidinate), a very rare example of a paddlewheel diruthenium compound with three different equatorial ligands, with the model protein bovine pancreatic ribonuclease (RNase A) by means of UV-visible absorption spectroscopy, circular dichroism (CD), electrospray ionization mass spectrometry (ESI-MS) and X-ray crystallography. It is the first attempt to investigate the binding of a neutral diruthenium compound to a protein.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!