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Fluorescent nitrile-based inhibitors of cysteine cathepsins
Bioorganic & Medicinal Chemistry Letters, 2012Cysteine cathepsins play an important role in many (patho)physiological conditions. Among them, cathepsins L, S, K and B are subjects of several drug discovery programs. Besides their role as drug targets, cysteine cathepsins are additionally considered to be possible biomarkers for inflammation and cancer.
Maxim, Frizler +2 more
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Lysosomal cysteine cathepsins: signaling pathways in apoptosis
bchm, 2007Abstract Apoptosis is the major mechanism by which eukaryotic organisms eliminate potentially dangerous, superfluous and damaged cells. Initially, nuclei and mitochondria were found to be the key organelles involved in the process. However, recent data suggest that lysosomes and the endoplasmic reticulum also play important roles in the ...
Veronika, Stoka, Vito, Turk, Boris, Turk
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Lysosomal cysteine proteases (cathepsins): promising drug targets
Acta Crystallographica Section D Biological Crystallography, 2003Papain-like lysosomal cysteine proteases are processive and digestive enzymes expressed in organisms from bacteria to humans. Their ubiquity alone makes them potential drug targets, with the assumption that appropriate specificities may be achieved.
Dusan, Turk, Gregor, Guncar
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Cysteine Cathepsins and the Skeleton
Clinical Reviews in Bone and Mineral Metabolism, 2011Cysteine cathepsins are lysosomal proteases with housekeeping as well as tissue-specific functions. One of their specialized functions includes the degradation of extracellular matrix proteins and the regulation of the immune response. In recent years, this protease family received increasing attention as drug targets for bone and cartilage-related ...
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Cathepsin K: a unique collagenolytic cysteine peptidase
bchm, 2013Abstract Cathepsin K has emerged as a promising target for the treatment of osteoporosis in recent years. Initially identified as a papain-like cysteine peptidase expressed in high levels in osteoclasts, the important role of this enzyme in bone metabolism was highlighted by the finding that mutations in the CTSK gene cause the rare ...
Marko, Novinec, Brigita, Lenarčič
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Prodrug-Inspired Probes Selective to Cathepsin B over Other Cysteine Cathepsins
Journal of Medicinal Chemistry, 2014Cathepsin B (CTB) is a cysteine protease believed to be an important therapeutic target or biomarker for several diseases including aggressive cancer, arthritis, and parasitic infections. The development of probes capable of assessing CTB activity in cell lysates, living cells, and animal models of disease are needed to understand its role in disease ...
Morshed A, Chowdhury +6 more
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Cysteine cathepsin proteases as pharmacological targets in cancer
Trends in Pharmacological Sciences, 2008Proteolytic activity is required for several key pro-tumorigenic processes: angiogenesis, invasion and metastasis. Consequently, increases in protease expression and activity are frequently reported in human cancers, and correlate with malignant progression and poor patient prognosis.
Carmela, Palermo, Johanna A, Joyce
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Cathepsin B-like cysteine proteases of Leishmania mexicana
Molecular and Biochemical Parasitology, 1993A group of Leishmania mexicana cysteine proteases that differ from those previously found in this protozoon are described. The enzymes characteristically have a preference for peptidyl substrates with a phenylalanyl-valyl-arginyl moiety, do not hydrolyse gelatin in substrate-sodium dodecyl sulphate polyacrylamide gels, are stimulated by thiol-reducing ...
C D, Robertson, G H, Coombs
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Prognostic Impact of Cysteine Proteases Cathepsin B and Cathepsin L in Pancreatic Adenocarcinoma
Pancreas, 2004The cysteine proteases cathepsin B (CTSB) and L (CTSL) have been implicated in tumor spread and metastatic formation. In pancreatic adenocarcinoma, the role of these proteases is not very well defined. To find out which cell types produce CTSB and CTSL and to evaluate the prognostic impact of these proteases, 70 specimens from curatively resected ...
Marco, Niedergethmann +5 more
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