Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T27889
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| Former ID |
TTDNC00602
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| Target Name |
Recombinant human angiotensin converting enzyme 2
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| Gene Name |
ACE2
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| Synonyms |
ACEH; ACErelated carboxypeptidase; Angiotensinconverting enzyme 2; Angiotensinconverting enzyme homolog; Metalloprotease MPROT15; Processed angiotensinconverting enzyme 2; ACE2
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| Target Type |
Clinical Trial
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| 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.
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| BioChemical Class |
Peptidase
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| UniProt ID | |||||
| EC Number |
EC 3.4.17.23
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| Sequence |
MSSSSWLLLSLVAVTAAQSTIEEQAKTFLDKFNHEAEDLFYQSSLASWNYNTNITEENVQ
NMNNAGDKWSAFLKEQSTLAQMYPLQEIQNLTVKLQLQALQQNGSSVLSEDKSKRLNTIL NTMSTIYSTGKVCNPDNPQECLLLEPGLNEIMANSLDYNERLWAWESWRSEVGKQLRPLY EEYVVLKNEMARANHYEDYGDYWRGDYEVNGVDGYDYSRGQLIEDVEHTFEEIKPLYEHL HAYVRAKLMNAYPSYISPIGCLPAHLLGDMWGRFWTNLYSLTVPFGQKPNIDVTDAMVDQ AWDAQRIFKEAEKFFVSVGLPNMTQGFWENSMLTDPGNVQKAVCHPTAWDLGKGDFRILM CTKVTMDDFLTAHHEMGHIQYDMAYAAQPFLLRNGANEGFHEAVGEIMSLSAATPKHLKS IGLLSPDFQEDNETEINFLLKQALTIVGTLPFTYMLEKWRWMVFKGEIPKDQWMKKWWEM KREIVGVVEPVPHDETYCDPASLFHVSNDYSFIRYYTRTLYQFQFQEALCQAAKHEGPLH KCDISNSTEAGQKLFNMLRLGKSEPWTLALENVVGAKNMNVRPLLNYFEPLFTWLKDQNK NSFVGWSTDWSPYADQSIKVRISLKSALGDKAYEWNDNEMYLFRSSVAYAMRQYFLKVKN QMILFGEEDVRVANLKPRISFNFFVTAPKNVSDIIPRTEVEKAIRMSRSRINDAFRLNDN SLEFLGIQPTLGPPNQPPVSIWLIVFGVVMGVIVVGIVILIFTGIRDRKKKNKARSGENP YASIDISKGENNPGFQNTDDVQTSF |
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| Drugs and Mode of Action | |||||
| Drug(s) | GSK2586881 | Drug Info | Phase 2 | Acute lung injury | [1] |
| ORE-1001 | Drug Info | Phase 1/2 | Diabetes | [2] | |
| MLN4760 | Drug Info | Discontinued in Phase 1 | Type 2 diabetes | [3], [4] | |
| Inhibitor | compound 28 | Drug Info | [5] | ||
| MLN4760 | Drug Info | [6] | |||
| ORE-1001 | Drug Info | [7] | |||
| Modulator | GSK2586881 | Drug Info | [8] | ||
| Activator | XNT | Drug Info | [9] | ||
| 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 1 | ClinicalTrials.gov (NCT01597635) The Safety, Tolerability, PK and PD of GSK2586881 in Patients With Acute Lung Injury. U.S. National Institutes of Health. | ||||
| REF 2 | ClinicalTrials.gov (NCT01039597) Safety and Activity of ORE1001 in Subjects With Ulcerative Colitis. U.S. National Institutes of Health. | ||||
| REF 3 | (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 4 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800016663) | ||||
| REF 5 | Development of potent and selective phosphinic peptide inhibitors of angiotensin-converting enzyme 2. J Med Chem. 2008 Apr 10;51(7):2216-26. | ||||
| REF 6 | Species-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 7 | Effects of the ACE2 inhibitor GL1001 on acute dextran sodium sulfate-induced colitis in mice. Inflamm Res. 2009 Nov;58(11):819-27. | ||||
| REF 8 | New Developments in the Pharmacological Treatment of Hypertension: Dead-End or a Glimmer at the Horizon?. Curr Hypertens Rep. 2015; 17(6): 42. | ||||
| REF 9 | Structure-based identification of small-molecule angiotensin-converting enzyme 2 activators as novel antihypertensive agents. Hypertension. 2008 May;51(5):1312-7. | ||||
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