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Aminopeptidases catalyze the cleavage of amino acids from the amino terminus of protein (N-terminus) or peptide substrates. They are widely distributed throughout the animal and plant kingdoms and are found in many subcellular organelles, in cytoplasm, and as membrane components. Aminopeptidases are used in essential cellular functions. Many, but not all, of these peptidases are zinc Metalloenzymes. Some aminopeptidases are monomeric, and others are assemblies of relatively high mass (50 kDa) subunits. CDNA sequences are available for several aminopeptidases and a crystal structure of the open state of human endoplasmic reticulum Aminopeptidase 1 ERAP1 is presented here. Amino acid sequences determined directly or deduced from cDNAs indicate some amino acid sequence homologies in organisms as diverse as Escherichia coli and mammals, particularly in catalytically important residues or in residues involved in metal ion binding. One important aminopeptidase is a zinc-dependent enzyme produced and secreted by glands of the small intestine. It helps the enzymatic digestion of proteins. Additional digestive enzymes produced by these glands include dipeptidases, maltase, sucrase, lactase, and enterokinase.

Cat. No. Product Name CAS No. Information

CHR 2863


CHR 2863 is a potent, orally available hydrophobic aminopeptidase inhibitor that structurally mimics the aminopeptidase inhibitor Tostedostat.




TNP-470 (AGM-1470) is a specific, rreversible MetAP-2 inhibitor and and annti-angiogenic compound, inhibits endothelial cell proliferation and angiogenesis; has anti-growth factor properties and inhibits the activation of Cdk 2 and phosphorylation of RB protein, inhibits potently PDGF- and bFGF-stimulated proliferation of rat mesangial cells in vitro (IC50 = 50 pg/ml); inhibits tumor growth and metastasis of rodent tumors; does not bind to or inhibit MetAP-1.




A potent, orally active, centrally acting aminopeptidase inhibitor, the prodrug of the specific and selective aminopeptidase A inhibitor EC33; blocks the brain renin-angiotensin system activity and normalises blood pressure,with no effect on the systemic renin-angiotensin-aldosterone parameters and on PCop concentrations.




Tosedostat (CHR-2797, CHR2797) is a potent, orally bioavailable aminopeptidases inhibitor with IC50 of 150, 220 and 100 nM for PuSA, aminopeptidase N and leucine aminopeptidase, respectively; exerts antiproliferative effects against a range of tumor cell lines in vitro and in vivo and shows selectivity for transformed over nontransformed cells; inhibits phosphorylation of mTOR substrates and reduces protein synthesis in HL-60 cells.

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