Target intelligence / Profile preview

Aminopeptidase

Molecular classification
Enzyme, Peptidase, Metalloenzyme, Cysteine aminopeptidase, Serine peptidase, membrane-bound enzyme, cytosolic enzyme
01

Overview

Aminopeptidase is a generic term for enzymes that catalyze the hydrolysis of amino acids from the N-terminus of peptides or proteins. Most are metalloenzymes, requiring zinc, manganese, or similar ions for activity, though cysteine- and serine-dependent forms exist. Found throughout animal and plant tissues in cytosol, membranes, and organelles, aminopeptidases mediate key steps in protein digestion, maturation, cellular recycling of proteins, and participate in diverse processes from immunity to angiogenesis. Dysregulation or abnormal activity is linked to cancer, inflammation, hypertension, and infection. Aminopeptidase inhibitors have therapeutic potential, especially in oncology and cardiovascular medicine, but safety concerns arise due to the broad physiological roles of these enzymes.

Other names
Aminopeptidase N (APN)Aminopeptidase A (APA)Leucyl aminopeptidase (LAP)Aminopeptidase BAminopeptidase PMembrane aminopeptidaseCytosol aminopeptidaseMetalloaminopeptidaseCysteine aminopeptidase
02

Mechanism of action

Competitive inhibition of the active site by bestatin or similar small molecules; Chelation or replacement of essential metal ions inhibiting metalloaminopeptidase activity; Inhibition of substrate binding or turnover of peptides

03

Biological functions

Protein and peptide digestionProtein turnoverAntigen presentationNeuropeptide and hormone processingCell growth and proliferationImmune responseNutritional amino acid liberationBlood pressure regulationAngiogenesisMemory formationInflammatory responseReproductive processes
04

Disease associations

Cancer (tumor growth, metastasis)InflammationHypertension and cardiovascular diseasePregnancy-related conditionsNeurodegenerative diseasesInfectionMetabolic disorders
05

Safety considerations

Off-target effects due to enzyme ubiquity and involvement in multiple physiological pathwaysRisk of interfering with normal immune, digestive, or cardiovascular functionPotential toxicity due to inhibition of essential protein turnover
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Interacting drugs

Bestatin (ubenimex)

2 more in the full profile.

07

Biomarkers

Aminopeptidase N (APN) tissue expression or activity in cancer diagnosis/prognosisUrinary/circulating aminopeptidase levels in hypertension and renal disease monitoringExpression levels in tumor tissue or immune cell subsets

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