Target Information

Target General Infomation
Target ID
T67272
Former ID
TTDR00784
Target Name
Aminopeptidase N
Gene Name
ANPEP
Synonyms
Alanyl aminopeptidase; Aminopeptidase M; Gp150; HAPN; Microsomal aminopeptidase; Myeloid plasma membrane glycoprotein CD13; ANPEP
Target Type
Clinical Trial
Disease Psoriasis [ICD9: 696; ICD10: L40]
Function
Broad specificity aminopeptidase. Plays a role in the final digestion of peptides generated from hydrolysis of proteins by gastric and pancreatic proteases. May play a critical role in the pathogenesis of cholesterol gallstone disease. May be involved in the metabolism of regulatory peptides of diverse cell types, responsible for the processing of peptide hormones, such as angiotensin III and IV, neuropeptides, and chemokines. Found to cleave antigen peptides bound to major histocompatibility complex class II molecules of presenting cells and to degrade neurotransmitters at synaptic junctions. Is also implicated as a regulator of IL-8 bioavailability in the endometrium, and therefore may contribute to the regulation of angiogenesis. Is used as a marker for acute myeloid leukemia and plays a role in tumor invasion. In case of human coronavirus 229E (HCoV-229E) infection, serves as receptor for HCoV-229E spike glycoprotein. Mediates as well human cytomegalovirus (HCMV) infection.
BioChemical Class
Peptidase
Target Validation
T67272
UniProt ID
P15144
EC Number
EC 3.4.11.2
Sequence
MAKGFYISKSLGILGILLGVAAVCTIIALSVVYSQEKNKNANSSPVASTTPSASATTNPA
SATTLDQSKAWNRYRLPNTLKPDSYRVTLRPYLTPNDRGLYVFKGSSTVRFTCKEATDVI
IIHSKKLNYTLSQGHRVVLRGVGGSQPPDIDKTELVEPTEYLVVHLKGSLVKDSQYEMDS
EFEGELADDLAGFYRSEYMEGNVRKVVATTQMQAADARKSFPCFDEPAMKAEFNITLIHP
KDLTALSNMLPKGPSTPLPEDPNWNVTEFHTTPKMSTYLLAFIVSEFDYVEKQASNGVLI
RIWARPSAIAAGHGDYALNVTGPILNFFAGHYDTPYPLPKSDQIGLPDFNAGAMENWGLV
TYRENSLLFDPLSSSSSNKERVVTVIAHELAHQWFGNLVTIEWWNDLWLNEGFASYVEYL
GADYAEPTWNLKDLMVLNDVYRVMAVDALASSHPLSTPASEINTPAQISELFDAISYSKG
ASVLRMLSSFLSEDVFKQGLASYLHTFAYQNTIYLNLWDHLQEAVNNRSIQLPTTVRDIM
NRWTLQMGFPVITVDTSTGTLSQEHFLLDPDSNVTRPSEFNYVWIVPITSIRDGRQQQDY
WLIDVRAQNDLFSTSGNEWVLLNLNVTGYYRVNYDEENWRKIQTQLQRDHSAIPVINRAQ
IINDAFNLASAHKVPVTLALNNTLFLIEERQYMPWEAALSSLSYFKLMFDRSEVYGPMKN
YLKKQVTPLFIHFRNNTNNWREIPENLMDQYSEVNAISTACSNGVPECEEMVSGLFKQWM
ENPNNNPIHPNLRSTVYCNAIAQGGEEEWDFAWEQFRNATLVNEADKLRAALACSKELWI
LNRYLSYTLNPDLIRKQDATSTIISITNNVIGQGLVWDFVQSNWKKLFNDYGGGSFSFSN
LIQAVTRRFSTEYELQQLEQFKKDNEETGFGSGTRALEQALEKTKANIKWVKENKEVVLQ
WFTENSK
Drugs and Mode of Action
Drug(s) IP10 C8 Drug Info Phase 2 Psoriasis [530043]
IP10.C8-1 Drug Info Phase 2 Psoriasis [530043]
Inhibitor (1-Amino-2-phenyl-ethyl)-phosphinic acid Drug Info [525524]
(1-Amino-3-methyl-butyl)-phosphinic acid Drug Info [525524]
(1-Amino-3-methylsulfanyl-propyl)-phosphinic acid Drug Info [525524]
(1-Amino-3-phenyl-propyl)-phosphinic acid Drug Info [525524]
(1-Amino-ethyl)-phosphinic acid Drug Info [525524]
(Amino-phenyl-methyl)-phosphinic acid Drug Info [525524]
(S)-2-Amino-2-phenyl-ethanethiol Drug Info [525524]
(S)-2-Amino-3-phenyl-propane-1-thiol Drug Info [525524]
(S)-2-Amino-4-methyl-pentane-1-thiol Drug Info [525524]
(S)-2-Amino-4-methylsulfanyl-butane-1-thiol Drug Info [525524]
(S)-2-Amino-4-phenyl-butane-1-thiol Drug Info [525524]
(S)-2-Amino-propane-1-thiol Drug Info [525524]
1-aminobutylphosphonic acid Drug Info [530815]
1-aminohexylphosphonic acid Drug Info [530815]
1-aminohexylphosphonic acid monophenyl ester Drug Info [530815]
1-aminopentylphosphonic acid monophenyl ester Drug Info [530815]
2-amino-N1-benzyl-N3-hydroxymalonamide Drug Info [528703]
2-benzyl-N1-hydroxy-N3-(3-phenylpropyl)malonamide Drug Info [528703]
2-benzyl-N1-hydroxy-N3-(4-phenylbutyl)malonamide Drug Info [528703]
2-benzyl-N1-hydroxy-N3-phenethylmalonamide Drug Info [528703]
2-Cinnamamido-N1-hydroxy-N4-octylsuccinamide Drug Info [530409]
2-Cinnamamido-N1-hydroxy-N4-pentylsuccinamide Drug Info [530409]
2-Cinnamamido-N4-hexyl-N1-hydroxysuccinamide Drug Info [530409]
Angiotensin IV Drug Info [529535]
compound I3 Drug Info [532241]
IP10.C8-1 Drug Info [522549], [530043]
KELATORPHAN Drug Info [533380]
N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide Drug Info [528703]
N-Hydroxy-2-(naphthalen-2-ylsulfanyl)-acetamide Drug Info [527322]
N1,2-dibenzyl-N3-hydroxy-N1-phenethylmalonamide Drug Info [528703]
N1,2-dibenzyl-N3-hydroxymalonamide Drug Info [528703]
N1-(3,3-diphenylpropyl)-N3-hydroxymalonamide Drug Info [528703]
N1-(3-phenoxybenzyl)-N3-hydroxymalonamide Drug Info [528703]
N1-(4-chlorobenzyl)-2-amino-N3-hydroxymalonamide Drug Info [528703]
N1-(4-chlorobenzyl)-2-benzyl-N3-hydroxymalonamide Drug Info [528703]
N1-(4-fluorobenzyl)-2-benzyl-N3-hydroxymalonamide Drug Info [528703]
N1-benzyl-N3-hydroxy-2-isobutylmalonamide Drug Info [528501]
N1-hydroxy-2-isobutyl-N3-phenethylmalonamide Drug Info [528501]
N4-Butyl-2-cinnamamido-N1-hydroxysuccinamide Drug Info [530409]
[(125)I] RB129 Drug Info [535925]
Modulator IP10 C8 Drug Info [530043]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Glutathione-mediated detoxification
KEGG Pathway Glutathione metabolism
Metabolic pathways
Renin-angiotensin system
Hematopoietic cell lineage
Pathway Interaction Database C-MYB transcription factor network
PathWhiz Pathway Glutathione Metabolism
Reactome Metabolism of Angiotensinogen to Angiotensins
WikiPathways Metabolism of Angiotensinogen to Angiotensins
Cardiac Progenitor Differentiation
miR-targeted genes in squamous cell - TarBase
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in leukocytes - TarBase
Glutathione metabolism
References
Ref 530043Recent insights into the role of dipeptidyl aminopeptidase IV (DPIV) and aminopeptidase N (APN) families in immune functions. Clin Chem Lab Med. 2009;47(3):253-61.
Ref 522549ClinicalTrials.gov (NCT00824980) Combined Inhibition of Dipeptidyl Peptidase IV (DPIV/CD26) and Aminopeptidase N (APN/CD13) in the Treatment of Psoriasis. U.S. National Institutes of Health.
Ref 525524Bioorg Med Chem Lett. 1999 Jun 7;9(11):1511-6.Design of the first highly potent and selective aminopeptidase N (EC 3.4.11.2) inhibitor.
Ref 527322Bioorg Med Chem Lett. 2005 Jan 3;15(1):181-3.N-hydroxy-2-(naphthalene-2-ylsulfanyl)-acetamide, a novel hydroxamic acid-based inhibitor of aminopeptidase N and its anti-angiogenic activity.
Ref 528501Bioorg Med Chem. 2007 Jan 1;15(1):63-76. Epub 2006 Oct 12.A library of novel hydroxamic acids targeting the metallo-protease family: design, parallel synthesis and screening.
Ref 528703J Med Chem. 2007 Mar 22;50(6):1322-34. Epub 2007 Feb 28.Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents.
Ref 529535Bioorg Med Chem. 2008 Jul 15;16(14):6924-35. Epub 2008 May 27.Ligands to the (IRAP)/AT4 receptor encompassing a 4-hydroxydiphenylmethane scaffold replacing Tyr2.
Ref 530043Recent insights into the role of dipeptidyl aminopeptidase IV (DPIV) and aminopeptidase N (APN) families in immune functions. Clin Chem Lab Med. 2009;47(3):253-61.
Ref 530409Bioorg Med Chem. 2009 Oct 15;17(20):7398-404. Epub 2009 Sep 24.Design, synthesis, and preliminary studies of the activity of novel derivatives of N-cinnamoyl-L-aspartic acid as inhibitors of aminopeptidase N/CD13.
Ref 530815Bioorg Med Chem. 2010 Apr 15;18(8):2930-6. Epub 2010 Mar 1.New aromatic monoesters of alpha-aminoaralkylphosphonic acids as inhibitors of aminopeptidase N/CD13.
Ref 532241Selective aminopeptidase-N (CD13) inhibitors with relevance to cancer chemotherapy. Bioorg Med Chem. 2013 Apr 1;21(7):2135-44.
Ref 533380J Med Chem. 1988 Sep;31(9):1825-31.Retro-inverso concept applied to the complete inhibitors of enkephalin-degrading enzymes.
Ref 535925Ontogenic and adult whole body distribution of aminopeptidase N in rat investigated by in vitro autoradiography. Biochimie. 2004 Feb;86(2):105-13.

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