Target Information

Target General Infomation
Target ID
T27889
Former ID
TTDNC00602
Target Name
Recombinant human angiotensin converting enzyme 2
Gene Name
ACE2
Synonyms
ACEH; ACErelated carboxypeptidase; Angiotensinconverting enzyme 2; Angiotensinconverting enzyme homolog; Metalloprotease MPROT15; Processed angiotensinconverting enzyme 2; ACE2
Target Type
Clinical Trial
Disease Acute lung injury [ICD9: 518; ICD10: J80]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Carboxypeptidase which converts angiotensin I to angiotensin 1-9, a peptide of unknown function, and angiotensin II to angiotensin 1-7, a vasodilator. Also able to hydrolyze apelin- 13 and dynorphin-13 with high efficiency. May be an important regulator of heart function. In case of human coronaviruses SARS and HCoV-NL63 infections, serve as functional receptor for the spike glycoprotein of both coronaviruses.
BioChemical Class
Peptidase
UniProt ID
Q9BYF1
EC Number
EC 3.4.17.23
Sequence
MSSSSWLLLSLVAVTAAQSTIEEQAKTFLDKFNHEAEDLFYQSSLASWNYNTNITEENVQ
NMNNAGDKWSAFLKEQSTLAQMYPLQEIQNLTVKLQLQALQQNGSSVLSEDKSKRLNTIL
NTMSTIYSTGKVCNPDNPQECLLLEPGLNEIMANSLDYNERLWAWESWRSEVGKQLRPLY
EEYVVLKNEMARANHYEDYGDYWRGDYEVNGVDGYDYSRGQLIEDVEHTFEEIKPLYEHL
HAYVRAKLMNAYPSYISPIGCLPAHLLGDMWGRFWTNLYSLTVPFGQKPNIDVTDAMVDQ
AWDAQRIFKEAEKFFVSVGLPNMTQGFWENSMLTDPGNVQKAVCHPTAWDLGKGDFRILM
CTKVTMDDFLTAHHEMGHIQYDMAYAAQPFLLRNGANEGFHEAVGEIMSLSAATPKHLKS
IGLLSPDFQEDNETEINFLLKQALTIVGTLPFTYMLEKWRWMVFKGEIPKDQWMKKWWEM
KREIVGVVEPVPHDETYCDPASLFHVSNDYSFIRYYTRTLYQFQFQEALCQAAKHEGPLH
KCDISNSTEAGQKLFNMLRLGKSEPWTLALENVVGAKNMNVRPLLNYFEPLFTWLKDQNK
NSFVGWSTDWSPYADQSIKVRISLKSALGDKAYEWNDNEMYLFRSSVAYAMRQYFLKVKN
QMILFGEEDVRVANLKPRISFNFFVTAPKNVSDIIPRTEVEKAIRMSRSRINDAFRLNDN
SLEFLGIQPTLGPPNQPPVSIWLIVFGVVMGVIVVGIVILIFTGIRDRKKKNKARSGENP
YASIDISKGENNPGFQNTDDVQTSF
Drugs and Mode of Action
Drug(s) GSK2586881 Drug Info Phase 2 Acute lung injury [523900]
ORE-1001 Drug Info Phase 1/2 Diabetes [522906]
MLN4760 Drug Info Discontinued in Phase 1 Type 2 diabetes [542794], [547469]
Inhibitor compound 28 Drug Info [529358]
MLN4760 Drug Info [544202]
ORE-1001 Drug Info [530201]
Modulator GSK2586881 Drug Info [544476]
Activator XNT Drug Info [529403]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Renin-angiotensin system
Protein digestion and absorption
Reactome Metabolism of Angiotensinogen to Angiotensins
WikiPathways ACE Inhibitor Pathway
Metabolism of Angiotensinogen to Angiotensins
References
Ref 522906ClinicalTrials.gov (NCT01039597) Safety and Activity of ORE1001 in Subjects With Ulcerative Colitis. U.S. National Institutes of Health.
Ref 523900ClinicalTrials.gov (NCT01597635) The Safety, Tolerability, PK and PD of GSK2586881 in Patients With Acute Lung Injury. U.S. National Institutes of Health.
Ref 542794(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7866).
Ref 547469Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016663)
Ref 529358Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2. J Med Chem. 2008 Apr 10;51(7):2216-26.
Ref 529403Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents. Hypertension. 2008 May;51(5):1312-7.
Ref 530201Effects of the ACE2 inhibitor GL1001 on acute dextran sodium sulfate-induced colitis in mice. Inflamm Res. 2009 Nov;58(11):819-27.
Ref 544202Species-specific inhibitor sensitivity of angiotensin-converting enzyme 2 (ACE2) and its implication for ACE2 activity assays. Am J Physiol Regul Integr Comp Physiol. 2011 November; 301(5): R1293-R1299.
Ref 544476New Developments in the Pharmacological Treatment of Hypertension: Dead-End or a Glimmer at the Horizon?. Curr Hypertens Rep. 2015; 17(6): 42.

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