Immobilized small-molecule inhibitors are suited for enrichment of biomolecules by affinity chromatography, as it is shown for metalloproteinases and an immobilizable derivative of the hydroxamate-type inhibitor marimastat. A new asymmetric synthesis of marimastat is presented that allows for site-specific attachment to a solid surface, e.g., a ...
Jenssen, K, Sewald, K, Sewald, Norbert
openaire +3 more sources
Broad-spectrum matrix metalloproteinase inhibition curbs inflammation and liver injury but aggravates experimental liver fibrosis in mice. [PDF]
Liver fibrosis is characterized by excessive synthesis of extracellular matrix proteins, which prevails over their enzymatic degradation, primarily by matrix metalloproteinases (MMPs). The effect of pharmacological MMP inhibition on fibrogenesis, however,
Vincent E de Meijer +7 more
doaj +3 more sources
Tumor necrosis factor α-converting enzyme inhibition reverses hepatic steatosis and improves insulin sensitivity markers and surgical outcome in mice. [PDF]
Hepatic steatosis is an established risk factor for complications following major hepatic resection. Pharmacological options to reverse steatosis prior to surgery, however, are lacking. We hypothesized that treatment with the pharmacologic tumor necrosis
Vincent E de Meijer +5 more
doaj +3 more sources
Demonstration of the Anthelmintic Potency of Marimastat in the Heligmosomoides polygyrus Rodent Model [PDF]
In the course of a structure based drug discovery program the known anticancer candidate marimastat was uncovered as a potent inhibitor of an enzyme in nematode cuticle biogenesis. It was shown to kill Caenorhabditis elegans, and the sheep parasites Haemonchus contortus and Teladorsagia circumcinta via an entirely novel nematode-specific pathway ...
Robertson, Elaine +6 more
openaire +4 more sources
Repurposing Cancer Drugs Batimastat and Marimastat to Inhibit the Activity of a Group I Metalloprotease from the Venom of the Western Diamondback Rattlesnake, Crotalus atrox [PDF]
Snakebite envenomation causes over 140,000 deaths every year, predominantly in developing countries. As a result, it is one of the most lethal neglected tropical diseases. It is associated with incredibly complex pathophysiology due to the vast number of
Harry J. Layfield +12 more
doaj +2 more sources
Marimastat as maintenance therapy for patients with advanced gastric cancer: a randomised trial
This randomised, double-blind, placebo-controlled study was designed to evaluate the ability of the orally administered matrix metalloproteinase inhibitor, marimastat, to prolong survival in patients with non-resectable gastric and gastro-oesophageal adenocarcinoma.
Bramhall, SR +11 more
openaire +3 more sources
Marimastat Inhibits Neointimal Thickening in aModel of Human Arterial Intimal Hyperplasia [PDF]
matrix metalloproteases (MMPs) produced by vascular smooth-muscle cells (VSMCs) degrade extracellular matrix and facilitate the migration of these cells. This is a fundamental process in arterial intimal hyperplasia. This study investigated whether Marimastat (a selective but non-specific MMP inhibitor) can prevent intimal hyperplasia in cultured human
Peterson, M +4 more
openaire +4 more sources
Investigating the role of MMP9 in anti‐Abeta immunotherapy‐associated ARIA [PDF]
Abstract Background Amyloid related imaging abnormalities (ARIA) remain a major obstacle to the widespread use of anti‐amyloid immunotherapy. Data has indicated an association of neuroinflammation and subsequent MMP activation as being associated with anti‐amyloid immunotherapy.
Foley K +4 more
europepmc +3 more sources
PURPOSE: The prognosis for unresectable pancreatic cancer remains dismal (1-year survival rate, < 10%; 5-year survival rate, < 5%). Recent advances in conventional chemotherapy and novel molecular treatment strategies warrant investigation. This, the largest randomized study in pancreatic cancer performed to date, compares marimastat, the first ...
S R, Bramhall +4 more
openaire +3 more sources
Snake Venom Protease Detection and Inhibition in Serum. [PDF]
A fluorescence assay enables sensitive detection of the activities of snake venom metalloproteases (SVMP) and serine proteases (SVSP) from viper venoms in buffer and serum. In combination with effective low‐molecular‐weight inhibitors such as ilomastat and nafamostat, this approach offers new prospects for the rapid diagnosis and adjunctive therapy of ...
Riedel M, Kersten C.
europepmc +2 more sources

