Target Information
Target General Infomation | |||||
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Target ID |
T75596
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Former ID |
TTDR00721
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Target Name |
Methionine aminopeptidase 2
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Gene Name |
METAP2
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Synonyms |
(MetAP)-2; Initiation factor 2 associated 67 kDa glycoprotein; MetAP 2; P67; P67eIF2; Peptidase M 2; METAP2
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Target Type |
Clinical Trial
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Disease | Autoimmune diabetes [ICD10: E08-E13] | ||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48] | |||||
Function |
Cotranslationally removes the N-terminal methionine from nascent proteins. The N-terminal methionine is often cleaved when the second residue in the primary sequence is small and uncharged (Met-Ala-, Cys, Gly, Pro, Ser, Thr, or Val).
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BioChemical Class |
Peptidase
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Target Validation |
T75596
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UniProt ID | |||||
EC Number |
EC 3.4.11.18
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Sequence |
MAGVEEVAASGSHLNGDLDPDDREEGAASTAEEAAKKKRRKKKKSKGPSAAGEQEPDKES
GASVDEVARQLERSALEDKERDEDDEDGDGDGDGATGKKKKKKKKKRGPKVQTDPPSVPI CDLYPNGVFPKGQECEYPPTQDGRTAAWRTTSEEKKALDQASEEIWNDFREAAEAHRQVR KYVMSWIKPGMTMIEICEKLEDCSRKLIKENGLNAGLAFPTGCSLNNCAAHYTPNAGDTT VLQYDDICKIDFGTHISGRIIDCAFTVTFNPKYDTLLKAVKDATNTGIKCAGIDVRLCDV GEAIQEVMESYEVEIDGKTYQVKPIRNLNGHSIGQYRIHAGKTVPIVKGGEATRMEEGEV YAIETFGSTGKGVVHDDMECSHYMKNFDVGHVPIRLPRTKHLLNVINENFGTLAFCRRWL DRLGESKYLMALKNLCDLGIVDPYPPLCDIKGSYTAQFEHTILLRPTCKEVVSRGDDY |
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Structure |
1B59; 1B6A; 1BN5; 1BOA; 1KQ0; 1KQ9; 1QZY; 1R58; 1R5G; 1R5H; 1YW7; 1YW8; 1YW9; 2ADU; 2EA2; 2EA4; 2GA2; 2OAZ; 3FM3; 3FMQ; 3FMR
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Drugs and Mode of Action | |||||
Inhibitor | 2-(4-fluorophenylsulfonamido)-1-naphthoic acid | Drug Info | [528149] | ||
2-(phenylsulfonamido)-1-naphthoic acid | Drug Info | [528149] | |||
2-(phenylsulfonamido)-5-propylbenzoic acid | Drug Info | [528149] | |||
2-(pyridin-2-yl)-1H-benzo[d]imidazol-5-amine | Drug Info | [551242] | |||
2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | [551242] | |||
2-(pyridin-2-yl)-1H-imidazo[4,5-c]pyridine | Drug Info | [551242] | |||
2-(thiazol-4-yl)-1H-benzo[d]imidazol-5-amine | Drug Info | [551242] | |||
2-Methyl-2-Propanol | Drug Info | [551393] | |||
3,5,6,8-Tetramethyl-N-Methyl Phenanthrolinium | Drug Info | [551393] | |||
3,5-dimethyl-2-(phenylsulfonamido)benzoic acid | Drug Info | [528149] | |||
3-anilino-5-benzylthio-1,2,4-triazole | Drug Info | [528951] | |||
5-bromo-2-(4-chlorophenylsulfonamido)benzoic acid | Drug Info | [528149] | |||
5-butyl-2-(phenylsulfonamido)benzoic acid | Drug Info | [528149] | |||
5-chloro-2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | [551242] | |||
5-ethyl-2-(phenylsulfonamido)benzoic acid | Drug Info | [528149] | |||
5-fluoro-2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | [551242] | |||
5-methyl-2-(phenylsulfonamido)benzoic acid | Drug Info | [528266] | |||
5-methyl-2-(pyridin-2-yl)-1H-benzo[d]imidazole | Drug Info | [551242] | |||
5-METHYL-2-[(PHENYLSULFONYL)AMINO]BENZOIC ACID | Drug Info | [551374] | |||
5-p-Tolyl-1H-[1,2,3]triazole | Drug Info | [527712] | |||
A-357300 | Drug Info | [535871] | |||
Beloranib | Drug Info | [532701] | |||
D-Methionine | Drug Info | [551393] | |||
Ovalicin | Drug Info | [551393] | |||
OXYQUINOLINE | Drug Info | [551242] | |||
PPI-2458 | Drug Info | [532203] | |||
TNP-470 | Drug Info | [535871] | |||
XMT-1191 | Drug Info | [543441] | |||
ZGN-433 | Drug Info | [551785] | |||
Binder | Fumagillin | Drug Info | [535781] | ||
Pathways | |||||
References | |||||
Ref 521623 | ClinicalTrials.gov (NCT00100347) Safety/Tolerance Study of PPI-2458 in Subjects With Non-Hodgkin's Lymphoma and Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 523457 | ClinicalTrials.gov (NCT01345474) Phase 3 Clinical Trial: D-Methionine to Reduce Noise-Induced Hearing Loss (NIHL). U.S. National Institutes of Health. | ||||
Ref 524814 | ClinicalTrials.gov (NCT02179151) Double-Blind, Placebo Controlled, Phase 3 Trial of ZGN-440 (Beloranib) in Obese Subjects With Prader-Willi Syndrome. U.S. National Institutes of Health. | ||||
Ref 543139 | (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: 8445). | ||||
Ref 527712 | J Med Chem. 2005 Sep 8;48(18):5644-7.4-Aryl-1,2,3-triazole: a novel template for a reversible methionine aminopeptidase 2 inhibitor, optimized to inhibit angiogenesis in vivo. | ||||
Ref 528149 | Bioorg Med Chem Lett. 2006 Jul 1;16(13):3574-7. Epub 2006 May 2.Development of sulfonamide compounds as potent methionine aminopeptidase type II inhibitors with antiproliferative properties. | ||||
Ref 528266 | J Med Chem. 2006 Jun 29;49(13):3832-49.Discovery and optimization of anthranilic acid sulfonamides as inhibitors of methionine aminopeptidase-2: a structural basis for the reduction of albumin binding. | ||||
Ref 528951 | J Med Chem. 2007 Aug 9;50(16):3777-85. Epub 2007 Jul 18.Highly potent inhibitors of methionine aminopeptidase-2 based on a 1,2,4-triazole pharmacophore. | ||||
Ref 532203 | Metabolites of PPI-2458, a selective, irreversible inhibitor of methionine aminopeptidase-2: structure determination and in vivo activity. Drug Metab Dispos. 2013 Apr;41(4):814-26. | ||||
Ref 532701 | Inhibition of the methionine aminopeptidase 2 enzyme for the treatment of obesity. Diabetes Metab Syndr Obes. 2014 Feb 28;7:73-84. | ||||
Ref 535781 | Homology modeling and calculation of the cobalt cluster charges of the Encephazlitozoon cuniculi methionine aminopeptidase, a potential target for drug design. Biophys Chem. 2003 Aug 1;105(1):29-43. | ||||
Ref 535871 | Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. Cancer Res. 2003 Nov 15;63(22):7861-9. | ||||
Ref 543441 | (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. (Target id: 1573). |
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