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Literature summary for 3.4.17.23 extracted from

  • Rushworth, C.A.; Guy, J.L.; Turner, A.J.
    Residues affecting the chloride regulation and substrate selectivity of the angiotensin-converting enzymes (ACE and ACE2) identified by site-directed mutagenesis (2008), FEBS J., 275, 6033-6042.
    View publication on PubMed

Cloned(Commentary)

Cloned (Comment) Organism
expression in HEK-293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
K481Q angiotensin I cleavage activity is 21% of wild-type activity, angiotensin II cleavage activity is 71.8% of wild-type activity Homo sapiens
R169Q angiotensin I cleavage activity is 5.2% of wild-type activity, angiotensin II cleavage activity is 1.1% of wild-type activity. The mutant enzyme does not show any activity with angiotensin I in the absence of chloride ions Homo sapiens
R169QK481QR514Q angiotensin I cleavage activity is 53.2% of wild-type activity, angiotensin II cleavage activity is 203.4% of wild-type activity Homo sapiens
R514Q angiotensin I cleavage activity is 52% of wild-type activity, angiotensin II cleavage activity is 179.3% of wild-type activity, enhancement of angiotensin II cleavage is a result of a 2.5-fold increase in Vmax compared with the wild-type Homo sapiens
W271A angiotensin I cleavage activity is 5.3% of wild-type activity, angiotensin II cleavage activity is 0.9% of wild-type activity. Lacks any significant chloride sensitivity with the substrate angiotensin I Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
Cl- ACE2 activity is regulated by chloride ions. The presence of chloride increases the hydrolysis of angiotensin I by ACE2, but inhibits cleavage of the vasoconstrictor angiotensin II Homo sapiens
MLN-4760 ACE2-specific inhibitor. Inhibition of wild-type ACE2 was sensitive to chloride concentration Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.053
-
angiotensin II pH 7.4, 37°C, mutant enzyme R514Q Homo sapiens
0.0586
-
angiotensin II pH 7.4, 37°C, wild-type enzyme Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Cl- ACE2 activity is regulated by chloride ions. The presence of chloride increases the hydrolysis of angiotensin I by ACE2, but inhibits cleavage of the vasoconstrictor angiotensin II Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9BYF1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
angiotensin I + H2O
-
Homo sapiens angiotensin-(1-9) + Leu
-
?
angiotensin II + H2O
-
Homo sapiens angiotensin-(1-7) + Phe
-
?

Synonyms

Synonyms Comment Organism
ACE2
-
Homo sapiens