Details of the Target

General Information of Target

Target ID LDTP02766
Target Name Aminopeptidase N (ANPEP)
Gene Name ANPEP
Gene ID 290
Synonyms
APN; CD13; PEPN; Aminopeptidase N; AP-N; hAPN; EC 3.4.11.2; Alanyl aminopeptidase; Aminopeptidase M; AP-M; Microsomal aminopeptidase; Myeloid plasma membrane glycoprotein CD13; gp150; CD antigen CD13
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAKGFYISKSLGILGILLGVAAVCTIIALSVVYSQEKNKNANSSPVASTTPSASATTNPA
SATTLDQSKAWNRYRLPNTLKPDSYRVTLRPYLTPNDRGLYVFKGSSTVRFTCKEATDVI
IIHSKKLNYTLSQGHRVVLRGVGGSQPPDIDKTELVEPTEYLVVHLKGSLVKDSQYEMDS
EFEGELADDLAGFYRSEYMEGNVRKVVATTQMQAADARKSFPCFDEPAMKAEFNITLIHP
KDLTALSNMLPKGPSTPLPEDPNWNVTEFHTTPKMSTYLLAFIVSEFDYVEKQASNGVLI
RIWARPSAIAAGHGDYALNVTGPILNFFAGHYDTPYPLPKSDQIGLPDFNAGAMENWGLV
TYRENSLLFDPLSSSSSNKERVVTVIAHELAHQWFGNLVTIEWWNDLWLNEGFASYVEYL
GADYAEPTWNLKDLMVLNDVYRVMAVDALASSHPLSTPASEINTPAQISELFDAISYSKG
ASVLRMLSSFLSEDVFKQGLASYLHTFAYQNTIYLNLWDHLQEAVNNRSIQLPTTVRDIM
NRWTLQMGFPVITVDTSTGTLSQEHFLLDPDSNVTRPSEFNYVWIVPITSIRDGRQQQDY
WLIDVRAQNDLFSTSGNEWVLLNLNVTGYYRVNYDEENWRKIQTQLQRDHSAIPVINRAQ
IINDAFNLASAHKVPVTLALNNTLFLIEERQYMPWEAALSSLSYFKLMFDRSEVYGPMKN
YLKKQVTPLFIHFRNNTNNWREIPENLMDQYSEVNAISTACSNGVPECEEMVSGLFKQWM
ENPNNNPIHPNLRSTVYCNAIAQGGEEEWDFAWEQFRNATLVNEADKLRAALACSKELWI
LNRYLSYTLNPDLIRKQDATSTIISITNNVIGQGLVWDFVQSNWKKLFNDYGGGSFSFSN
LIQAVTRRFSTEYELQQLEQFKKDNEETGFGSGTRALEQALEKTKANIKWVKENKEVVLQ
WFTENSK
Target Type
Clinical trial
Target Bioclass
Enzyme
Family
Peptidase M1 family
Subcellular location
Cell membrane
Function
Broad specificity aminopeptidase which plays a role in the final digestion of peptides generated from hydrolysis of proteins by gastric and pancreatic proteases. Also involved in the processing of various peptides including peptide hormones, such as angiotensin III and IV, neuropeptides, and chemokines. May also be involved the cleavage of peptides bound to major histocompatibility complex class II molecules of antigen presenting cells. May have a role in angiogenesis and promote cholesterol crystallization. May have a role in amino acid transport by acting as binding partner of amino acid transporter SLC6A19 and regulating its activity.; (Microbial infection) Acts as a receptor for human coronavirus 229E/HCoV-229E. In case of human coronavirus 229E (HCoV-229E) infection, serves as receptor for HCoV-229E spike glycoprotein.; (Microbial infection) Mediates as well Human cytomegalovirus (HCMV) infection.
TTD ID
T67272
Uniprot ID
P15144
DrugMap ID
TTPHMWB
Ensemble ID
ENST00000300060.7
HGNC ID
HGNC:500
ChEMBL ID
CHEMBL1907

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
YN-1
 Probe Info  		100.00  LDD0444  [1]
OPA-S-S-alkyne
 Probe Info  		K379(0.50); K836(0.79); K104(1.17); K923(2.33)  LDD3494  [2]
m-APA
 Probe Info  		11.69  LDD0403  [3]
DBIA
 Probe Info  		C223(2.48)  LDD3310  [4]
CY-1
 Probe Info  		N.A.  LDD0246  [5]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 11.69  LDD0403  [3]
 LDCM0022  KB02 42-MG-BA C223(4.01)  LDD2244  [4]
 LDCM0023  KB03 42-MG-BA C223(4.31)  LDD2661  [4]
 LDCM0024  KB05 COLO792 C223(2.48)  LDD3310  [4]

The Interaction Atlas With This Target

The Drug(s) Related To This Target

Approved
Click To Hide/Show 3 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ezetimibe Small molecular drug DB00973
Icatibant Small molecular drug DB06196
Human Calcitonin . DB06773
Phase 2
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ip10 C8 . D0E3HY
Investigative
Click To Hide/Show 39 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(1-amino-2-phenyl-ethyl)-phosphinic Acid Small molecular drug D0P9YU
(1-amino-3-methyl-butyl)-phosphinic Acid Small molecular drug D0N3UO
(1-amino-3-methylsulfanyl-propyl)-phosphinic Acid Small molecular drug D0EG8X
(1-amino-3-phenyl-propyl)-phosphinic Acid Small molecular drug D00KIV
(1-amino-ethyl)-phosphinic Acid Small molecular drug D06RLF
(Amino-phenyl-methyl)-phosphinic Acid Small molecular drug D04MKQ
(S)-2-amino-2-phenyl-ethanethiol Small molecular drug D06VON
(S)-2-amino-3-phenyl-propane-1-thiol Small molecular drug D04KOZ
(S)-2-amino-4-methyl-pentane-1-thiol Small molecular drug D0Q0EY
(S)-2-amino-4-methylsulfanyl-butane-1-thiol Small molecular drug D0GI9S
(S)-2-amino-4-phenyl-butane-1-thiol Small molecular drug D0DS7F
(S)-2-amino-propane-1-thiol Small molecular drug D0R9AA
1-aminobutylphosphonic Acid Small molecular drug D05EPO
1-aminohexylphosphonic Acid Small molecular drug D03JAL
1-aminohexylphosphonic Acid Monophenyl Ester Small molecular drug D04XBZ
1-aminopentylphosphonic Acid Monophenyl Ester Small molecular drug D0RH4S
2-amino-n1-benzyl-n3-hydroxymalonamide Small molecular drug D0Z4AC
2-benzyl-n1-hydroxy-n3-(3-phenylpropyl)Malonamide Small molecular drug D0YA8C
2-benzyl-n1-hydroxy-n3-(4-phenylbutyl)Malonamide Small molecular drug D0YO0R
2-benzyl-n1-hydroxy-n3-phenethylmalonamide Small molecular drug D0D8FZ
2-cinnamamido-n1-hydroxy-n4-octylsuccinamide Small molecular drug D0Z4NU
2-cinnamamido-n1-hydroxy-n4-pentylsuccinamide Small molecular drug D0F2HJ
2-cinnamamido-n4-hexyl-n1-hydroxysuccinamide Small molecular drug D0UI1P
Angiotensin Iv Small molecular drug D0L3PY
Kelatorphan Small molecular drug D04QJY
N-biphenyl-3-ylmethyl-n'-hydroxy-malonamide Small molecular drug D0J9TD
N-hydroxy-2-(Naphthalen-2-ylsulfanyl)-acetamide Small molecular drug D06AFP
N1,2-dibenzyl-n3-hydroxy-n1-phenethylmalonamide Small molecular drug D02EFK
N1,2-dibenzyl-n3-hydroxymalonamide Small molecular drug D0Z2JN
N1-(3,3-diphenylpropyl)-n3-hydroxymalonamide Small molecular drug D00SLJ
N1-(3-phenoxybenzyl)-n3-hydroxymalonamide Small molecular drug D0UT7Y
N1-(4-chlorobenzyl)-2-amino-n3-hydroxymalonamide Small molecular drug D0NL7J
N1-(4-chlorobenzyl)-2-benzyl-n3-hydroxymalonamide Small molecular drug D01LFP
N1-(4-fluorobenzyl)-2-benzyl-n3-hydroxymalonamide Small molecular drug D0K9XV
N1-benzyl-n3-hydroxy-2-isobutylmalonamide Small molecular drug D06TVS
N1-hydroxy-2-isobutyl-n3-phenethylmalonamide Small molecular drug D0GB8I
N4-butyl-2-cinnamamido-n1-hydroxysuccinamide Small molecular drug D0J0WJ
Pmid23428964ci3 Small molecular drug D0H5BG
[(125)I] Rb129 Small molecular drug D0U8IF

References

1 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
2 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
3 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
4 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
5 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.