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DrugBank target: P12821

DrugBank target: P12821 (ACE_HUMAN)     

Example drug-target structure: 1o86

( There are 28 structures corresponding to this UniProt sequence in the PDB. Click the orange, plus icon above for a list. )

Angiotensin-converting enzyme

Dipeptidyl carboxypeptidase I, Kininase II, Angiotensin-converting enzyme, soluble form, ACE.

Function

Converts angiotensin I to angiotensin II by release of the terminal His-Leu, this results in an increase of the vasoconstrictor activity of angiotensin. Also able to inactivate bradykinin, a potent vasodilator. Has also a glycosidase activity which releases GPI-anchored proteins from the membrane by cleaving the mannose linkage in the GPI moiety..

Enzyme

3.2.1.-   [EC->PDB]   [IntEnz]   [ExPASy]   [KEGG]  
3.4.15.1   [EC->PDB]   [IntEnz]   [ExPASy]   [KEGG]  

Catalytic activity

Release of a C-terminal dipeptide, oligopeptide-|-Xaa-Yaa, when Xaa is not Pro, and Yaa is neither Asp nor Glu. Thus, conversion of angiotensin I to angiotensin II, with increase in vasoconstrictor activity, but no action on angiotensin II.

Disease(s)

Ischemic stroke (ISCHSTR) [MIM:601367]: A stroke is an acute neurologic event leading to death of neural tissue of the brain and resulting in loss of motor, sensory and/or cognitive function. Ischemic strokes, resulting from vascular occlusion, is considered to be a highly complex disease consisting of a group of heterogeneous disorders with multiple genetic and environmental risk factors. Note=Disease susceptibility is associated with variations affecting the gene represented in this entry.
Renal tubular dysgenesis (RTD) [MIM:267430]: Autosomal recessive severe disorder of renal tubular development characterized by persistent fetal anuria and perinatal death, probably due to pulmonary hypoplasia from early-onset oligohydramnios (the Potter phenotype). Note=The disease is caused by mutations affecting the gene represented in this entry.
Microvascular complications of diabetes 3 (MVCD3) [MIM:612624]: Pathological conditions that develop in numerous tissues and organs as a consequence of diabetes mellitus. They include diabetic retinopathy, diabetic nephropathy leading to end- stage renal disease, and diabetic neuropathy. Diabetic retinopathy remains the major cause of new-onset blindness among diabetic adults. It is characterized by vascular permeability and increased tissue ischemia and angiogenesis. Note=Disease susceptibility is associated with variations affecting the gene represented in this entry.
Intracerebral hemorrhage (ICH) [MIM:614519]: A pathological condition characterized by bleeding into one or both cerebral hemispheres including the basal ganglia and the cerebral cortex. It is often associated with hypertension and craniocerebral trauma. Intracerebral bleeding is a common cause of stroke. Note=Disease susceptibility is associated with variations affecting the gene represented in this entry.

Schematic diagram of Pfam domains in target sequence plus wiring diagram of PDB structure containing drug molecule

1o86

Key:    PfamA domain  Secondary structure  Bound drug molecule

Sequence length: 1305 a.a.

Approved drugs targeting this protein

The DrugBank database identifies 14 drugs for this target protein:

 

 
Generic name: DB00790 perindopril
Formula: C19H32N2O5
Structure: There are no structures of this molecule in the PDB.
Generic name: DB00722 lisinopril
LPR
Formula: C21H31N3O5
Structure: There are 4 PDB structures containing this molecule of which 2 are bound to the above target protein.
 
Generic name: DB00519 trandolapril
Formula: C24H34N2O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00178 ramipril
Formula: C23H32N2O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01348 spirapril
Formula: C22H30N2O5S2
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00881 quinapril
Formula: C25H30N2O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00492 fosinopril
Formula: C30H46No7P
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00616 candoxatril
Formula: C29H41No7
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01340 cilazapril
Formula: C22H31N3O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00542 benazepril
Formula: C24H28N2O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01180 rescinnamine
Formula: C35H42N2O9
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00584 enalapril
Formula: C20H28N2O5
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB01197 captopril
Formula: C9H15No3S
Structure: There are no structures of this molecule in the PDB.
 
Generic name: DB00691 moexipril
Formula: C27H34N2O7
Structure: There are no structures of this molecule in the PDB.

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