Literature summary for 3.4.17.23 extracted from

Dales, N.A.; Gould, A.E.; Brown, J.A.; Calderwood, E.F.; Guan, B.; Minor, C.A.; Gavin, J.M.; Hales, P.; Kaushik, V.K.; Stewart, M.; Tummino, P.J.; Vickers, C.S.; Ocain, T.D.; Patane, M.A.
Substrate-based design of the first class of angiotensin-converting enzyme-related carboxypeptidase (ACE2) inhibitors (2002), J. Am. Chem. Soc., 124, 11852-11853.

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Application

Application	Comment	Organism
pharmacology	design and synthesis of first potent and selective enzyme inhibitors may be useful as pharmacological tools to help understanding the biological relevance and potantial role of the enzyme in human disease	Homo sapiens

Inhibitors

Inhibitors	Comment	Organism	Structure
2-methylphenyl-benzylsuccinic acid	-	Homo sapiens
3,4-dimethylphenyl-benzylsuccinic acid	-	Homo sapiens
3,5-dichloro-benzylsuccinate	-	Homo sapiens
3,5-dimethylphenyl-benzylsuccinic acid	-	Homo sapiens
3-methylphenyl-benzylsuccinic acid	-	Homo sapiens
4-methylphenyl-benzylsuccinic acid	-	Homo sapiens
4-nitrophenyl-benzylsuccinic acid	-	Homo sapiens
angiotensin I	-	Homo sapiens
Benzylsuccinic acid	-	Homo sapiens
cyclohexyl-benzylsuccinic acid	-	Homo sapiens
dicyclohexyl-benzylsuccinic acid	-	Homo sapiens
additional information	no inhibition by lisinopril, no inhibition by captopril, no inhibition by enalaprilat	Homo sapiens
phenylbenzylsuccinic acid	-	Homo sapiens

KM Value [mM]

KM Value [mM]	KM Value Maximum [mM]	Substrate	Comment	Organism	Structure
0.0069	-	angiotensin I	-	Homo sapiens

Localization

Localization	Comment	Organism	GeneOntology No.	Textmining
additional information	transmembrane domain	Homo sapiens	-	-

Metals/Ions

Metals/Ions	Comment	Organism	Structure
Zn2+	contains zinc-binding consensus sequence HEXXH, amino acids 374-378, zinc-binding protease	Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
angiotensin I + H2O	Homo sapiens	-	angiotensin-(1-9) + Leu	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	Q9BYF1	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
colon	-	Homo sapiens	-
heart ventricle	-	Homo sapiens	-
kidney	-	Homo sapiens	-
small intestine	-	Homo sapiens	-
testis	-	Homo sapiens	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
angiotensin I + H2O	-	Homo sapiens	angiotensin-(1-9) + Leu	-	?
angiotensin I + H2O	C-terminal bond between His-Leu is cleaved	Homo sapiens	angiotensin-(1-9) + Leu	-	?

Synonyms

Synonyms	Comment	Organism
ACE2	-	Homo sapiens
angiotensin-converting enzyme homologue	-	Homo sapiens
angiotensin-converting enzyme-related carboxypeptidase	-	Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s]	Turnover Number Maximum [1/s]	Substrate	Comment	Organism	Structure
2	-	angiotensin I	pH 6.5, room temperature	Homo sapiens

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0022	-	angiotensin I	-	Homo sapiens

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Release 2023.1 (January 2023)