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The term Proteases or Sulfatases refers to two distinct and expansive classes of enzymes rather than a single therapeutic target. Proteases, also known as peptidases, are enzymes that catalyze the hydrolysis of peptide bonds in proteins, playing vital roles in digestion, immune response, and cell signaling [1]. Sulfatases are enzymes that catalyze the hydrolysis of sulfate esters from various molecules, including steroids and carbohydrates, and are essential for the degradation of complex macromolecules within lysosomes [2]. Both classes are highly significant in drug discovery; for instance, protease inhibitors are widely used in treating HIV, hepatitis C, and various cancers, while sulfatase inhibitors are investigated for the treatment of hormone-dependent cancers [3, 4]. However, because this designation groups hundreds of different enzymes with diverse structures, substrates, and biological functions, it is considered too broad for specific target annotation and does not represent a single pharmacological entity. [1] Rawlings ND, et al. (2018). MEROPS: the peptidases database. Nucleic Acids Research. [2] Diez-Roux G, Ballabio A. (2005). Sulfatases and human disease. Annual Review of Genomics and Human Genetics. [3] Drag M, Salvesen GS. (2010). Emerging principles in protease-based drug discovery. Nature Reviews Drug Discovery. [4] Thomas CF, Potter BV. (2015). The structural biology of sulfatases and their mechanism of inhibition. ChemBioChem.
Inhibition of proteolytic cleavage of peptide bonds or the hydrolysis of sulfate esters from various biological substrates.
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