General Information of the Protein
Protein ID
PT01575
Protein Name
Neprilysin
Secondarily
Protein Name
Atriopeptidase
Common acute lymphocytic leukemia antigen
Enkephalinase
Neutral endopeptidase 24.11
Skin fibroblast elastase
Gene Name
MME
Secondarily
Gene Name
EPN
Sequence
MGKSESQMDITDINTPKPKKKQRWTPLEISLSVLVLLLTIIAVTMIALYATYDDGICKSSDCIKSAARLIQNMDATTEPCTDFFKYACGGWLKRNVIPETSSRYGNFDILRDELEVVLKDVLQEPKTEDIVAVQKAKALYRSCINESAIDSRGGEPLLKLLPDIYGWPVATENWEQKYGASWTAEKAIAQLNSKYGKKVLINLFVGTDDKNSVNHVIHIDQPRLGLPSRDYYECTGIYKEACTAYVDFMISVARLIRQEERLPIDENQLALEMNKVMELEKEIANATAKPEDRNDPMLLYNKMTLAQIQNNFSLEINGKPFSWLNFTNEIMSTVNISITNEEDVVVYAPEYLTKLKPILTKYSARDLQNLMSWRFIMDLVSSLSRTYKESRNAFRKALYGTTSETATWRRCANYVNGNMENAVGRLYVEAAFAGESKHVVEDLIAQIREVFIQTLDDLTWMDAETKKRAEEKALAIKERIGYPDDIVSNDNKLNNEYLELNYKEDEYFENIIQNLKFSQSKQLKKLREKVDKDEWISGAAVVNAFYSSGRNQIVFPAGILQPPFFSAQQSNSLNYGGIGMVIGHEITHGFDDNGRNFNKDGDLVDWWTQQSASNFKEQSQCMVYQYGNFSWDLAGGQHLNGINTLGENIADNGGLGQAYRAYQNYIKKNGEEKLLPGLDLNHKQLFFLNFAQVWCGTYRPEYAVNSIKTDVHSPGNFRIIGTLQNSAEFSEAFHCRKNSYMNPEKKCRVW
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Organism
Homo sapiens, Human
Protein Classification
Enzyme
>
Protease
>
Metallo protease
>
Metallo protease MAE clan
>
Metallo protease M13 family
Function
Thermolysin-like specificity, but is almost confined on acting on polypeptides of up to 30 amino acids (PubMed:6349683, PubMed:6208535, PubMed:15283675, PubMed:8168535). Biologically important in the destruction of opioid peptides such as Met- and Leu-enkephalins by cleavage of a Gly-Phe bond (PubMed:6349683, PubMed:17101991). Catalyzes cleavage of bradykinin, substance P and neurotensin peptides (PubMed:6208535). Able to cleave angiotensin-1, angiotensin-2 and angiotensin 1-9 (PubMed:6349683, PubMed:15283675). Involved in the degradation of atrial natriuretic factor (ANF) and brain natriuretic factor (BNP(1-32)) (PubMed:2531377, PubMed:2972276, PubMed:16254193). Displays UV-inducible elastase activity toward skin preelastic and elastic fibers (PubMed:20876573).
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Uniprot ID
Primary ID:
P08473

Secondarily ID:
A8K6U6
D3DNJ9
Q3MIX4
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Ensembl ID
ENSG00000196549
HGNC ID
HGNC:7154
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000011 , CHO
Compound ID Compound Name Compound Formula
CP0534817
(2S)-2-[[(2S)-1-[[(1S)-1-carboxy-2-(4-hydroxyphenyl)ethyl]amino]-1-oxohexan-2-yl]amino]-4-phenylbutanoic acid
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C25H32N2O6
 1
1
Ki = 600 nM
   TI
   LI
   LO
   TS
CP0950358
(S)-2-((S)-1-((S)-1-carboxy-2-(1H-indol-3-yl)ethylamino)-1-oxohexan-2-ylamino)-4-phenylbutanoic acid
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C27H33N3O5
 1
1
Ki = 19000 nM
   TI
   LI
   LO
   TS
CP0578057
(2S,5R)-1-[2-[[(1S)-1-carboxy-3-phenylpropyl]amino]acetyl]-5-(4-methylphenyl)pyrrolidine-2-carboxylic acid
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C24H28N2O5
 1
1
Ki > 50000 nM
   TI
   LI
   LO
   TS
Clinical Information about the Protein
Target 1 ( Neutral endopeptidase (MME) )
Target Type Clinical trial Target
Disease 5 Target-related Diseases  5
1 Hypotension [ICD-11: BA20-BA21]
2 Pain [ICD-11: MG30-MG3Z]
3 Asthma [ICD-11: CA23]
4 Cardiovascular disease [ICD-11: BA00-BE2Z]
5 Hypertension [ICD-11: BA00-BA04]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 Sampatrilat Phase 2
Hypotension
2 Gallopamil Phase 2
Asthma
Discontinued Drug(s) 6 Discontinued Drugs  6
1 Fasidotril Discontinued in Phase 2
Hypotension
2 Gemopatrilat Discontinued in Phase 2
Hypotension
3 SCH-32615 Discontinued in Phase 2
Pain
4 BMS-182657 Terminated
Cardiovascular disease
5 Omapatrilat Terminated
Hypertension
6 SQ-28603 Terminated
Hypertension