Proteinase-activated receptors (PARs), ubiquitous surface molecules participating on many biological processes have been recently discovered. Specific receptors for thrombin (PAR-1 and PAR-3) and trypsin (PAR-2) are described in this review. They belong to a family of G protein-coupled receptors activated by amino acid sequence of N-terminal part of bound ligand revealed by site-specific proteolysis. PARs participate in tissue growth and differentiation, regeneration and reparation, inflammatory response regulation, malignant transformation, but even in vascular tonus and blood pressure regulation. (Fig. 5, Ref. 35.)
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Replacement of a single residue changes the primary specificity of thrombin.
Fertil Steril
January 2025
Edward A. Doisy Department of Biochemistry and Molecular Biology, Saint Louis University School of Medicine, St. Louis, MO 63104 USA. Electronic address:
Background: Thrombin prefers substrates carrying Arg at the site of cleavage (P1) because of the presence of D189 in the primary specificity (S1) pocket but can also cleave substrates carrying Phe at P1. The structural basis of this property is unknown.
Objective: Solve the X-ray structure of thrombin bound to a ligand carrying Phe at P1 and investigate the effects of replacing D189.
Replacement of a single residue changes the primary specificity of thrombin.
J Thromb Haemost
January 2025
Edward A. Doisy Department of Biochemistry and Molecular Biology, Saint Louis University School of Medicine, St. Louis, MO 63104 USA. Electronic address:
Background: Thrombin prefers substrates carrying Arg at the site of cleavage (P1) because of the presence of D189 in the primary specificity (S1) pocket but can also cleave substrates carrying Phe at P1. The structural basis of this property is unknown.
Objective: Solve the X-ray structure of thrombin bound to a ligand carrying Phe at P1 and investigate the effects of replacing D189.
Ex vivo evaluation of the effect of plasma-derived factor VIII/von Willebrand factor in patients with severe hemophilia A on emicizumab prophylaxis.
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Discovery Research, Scientific Innovation Office, Grifols, Palou 3, 08150, Parets del Vallès, Barcelona, Spain.
Hemophilia A (HA) patients under emicizumab prophylaxis may require the concomitant use of procoagulant factors for breakthrough bleedings or immune tolerance induction (ITI). The aim of this study is to evaluate the ex vivo procoagulant effect of plasma-derived FVIII concentrates containing von Willebrand factor (pdFVIII/VWF) in samples from patients with severe HA without inhibitors on emicizumab prophylaxis. Samples from healthy controls (HC) and HA patients were drawn in sodium citrate plus corn trypsin inhibitor tubes and spiked with increasing concentrations of pdFVIII/VWF concentrates (10-400 IU/dL) (Fanhdi/Alphanate, Grifols), activated prothrombin complex concentrate (aPCC, 0.
View Article and Find Full Text PDFAeruginosin 525 (AER525) from Cyanobacterium Sp. (KUCC C2): A New Serine Proteases Inhibitor.
Mar Drugs
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Department of Marine Biology and Biotechnology, University of Gdańsk, M. J. Piłsudskiego 46, PL-81378 Gdynia, Poland.
Aeruginosins (AERs) are one of the most common classes of cyanobacterial peptides synthesised through a hybrid non-ribosomal peptide synthase/polyketide synthase pathway. They have been found in , , /, and The presence of AER in isolated from the Curonian Lagoon was reported for the first time in our previous work. Here, the structure of aeruginosin 525 (AER525), isolated from sp.
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November 2024
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Article Synopsis
- Cyanobacteria produce various secondary metabolites, including bioactive oligopeptides with unclear functions, particularly from the under-studied species Woronichinia naegeliana.
- * The oligopeptides cyanopeptolin 1081 and anabaenopeptin 899 are known to negatively impact zooplankton and show structural similarities to related compounds.
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