Therapeutic Targets Database
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TTD Target ID: TTDR00721

Target Information
NameMethionine aminopeptidase 2    
Type of targetClinical trial target    
Synonyms(MetAP)-2    
Initiation factor 2 associated 67 kDa glycoprotein    
MetAP 2    
P67    
P67eIF2    
Peptidase M 2    
DiseaseBacterial infections
[ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104   ICD10: A00-A09, A15-A19, A20-A28, A30-A49, A65-A69, A70-A74, A75-A79]
[1]
Cancer, unspecific
[ICD9: 140-229   ICD10: C00-C96]
[2]
Mesothelioma
[ICD9: 163   ICD10: C45]
[3]
Drug(s)ZGN-433Phase IObesity[4]
BioChemical ClassHydrolases acting on peptide bonds (Peptidases)    
EC NumberEC 3.4.11.18
UniProt IDP50579
Q8SR45
PDB Structure3FM3; 3FMQ; 3FMR.    
FunctionRemoves the amino-terminal methionine from nascent proteins.    
SequenceMAGVEEVAASGSHLNGDLDPDDREEGAASTAEEAAKKKRRKKKKSKGPSAAGEQEPDKES GASVDEVARQLERSALEDKERDEDDEDGDGDGDGATGKKKKKKKKKRGPKVQTDPPSVPI CDLYPNGVFPKGQECEYPPTQDGRTAAWRTTSEEKKALDQASEEIWNDFREAAEAHRQVR KYVMSWIKPGMTMIEICEKLEDCSRKLIKENGLNAGLAFPTGCSLNNCAAHYTPNAGDTT VLQYDDICKIDFGTHISGRIIDCAFTVTFNPKYDTLLKAVKDATNTGIKCAGIDVRLCDV GEAIQEVMESYEVEIDGKTYQVKPIRNLNGHSIGQYRIHAGKTVPIVKGGEATRMEEGEV YAIETFGSTGKGVVHDDMECSHYMKNFDVGHVPIRLPRTKHLLNVINENFGTLAFCRRWL DRLGESKYLMALKNLCDLGIVDPYPPLCDIKGSYTAQFEHTILLRPTCKEVVSRGDDY
Related US Patent6,566,541
Target ValidationClick to Find Target Validation Information.    
Inhibitor2- (4-fluorophenylsulfonamido)-1-naphthoic acid[5]
2- (phenylsulfonamido)-1-naphthoic acid[5]
2- (phenylsulfonamido)-5-propylbenzoic acid[5]
2- (pyridin-2-yl)-1H-benzo[d]imidazol-5-amine[6]
2- (pyridin-2-yl)-1H-benzo[d]imidazole[6]
2- (pyridin-2-yl)-1H-imidazo[4,5-c]pyridine[6]
2- (thiazol-4-yl)-1H-benzo[d]imidazol-5-amine[6]
2-Methyl-2-Propanol[7]
3,5,6,8-Tetramethyl-N-Methyl Phenanthrolinium[7]
3,5-dimethyl-2- (phenylsulfonamido)benzoic acid[5]
3-anilino-5-benzylthio-1,2,4-triazole[8]
5-METHYL-2-[ (PHENYLSULFONYL)AMINO]BENZOIC ACID[9]
5-bromo-2- (4-chlorophenylsulfonamido)benzoic acid[5]
5-butyl-2- (phenylsulfonamido)benzoic acid[5]
5-chloro-2- (pyridin-2-yl)-1H-benzo[d]imidazole[6]
5-ethyl-2- (phenylsulfonamido)benzoic acid[5]
5-fluoro-2- (pyridin-2-yl)-1H-benzo[d]imidazole[6]
5-methyl-2- (phenylsulfonamido)benzoic acid[10]
5-methyl-2- (pyridin-2-yl)-1H-benzo[d]imidazole[6]
5-p-Tolyl-1H-[1,2,3]triazole[11]
A-357300[2]
D-Methionine[7]
OXYQUINOLINE[6]
Ovalicin[7]
TNP-470[2]
ZGN-433[4]
LigandFumagillin[1]
Fumagillin[12]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Homology 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. To Reference
Ref 2Tumor suppression by a rationally designed reversible inhibitor of methionine aminopeptidase-2. Cancer Res. 2003 Nov 15;63(22):7861-9. To Reference
Ref 3Methionine aminopeptidase-2 regulates human mesothelioma cell survival: role of Bcl-2 expression and telomerase activity. Am J Pathol. 2001 Aug;159(2):721-31. To Reference
Ref 42011 Pipeline of Zafgen. To Reference
Ref 5Bioorg 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. To Reference
Ref 6Bioorg. Med. Chem. Lett. 20(14):4038-4044 (2010) To Reference
Ref 7Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 8J 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. To Reference
Ref 9Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 10J 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. To Reference
Ref 11J 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. To Reference
Ref 12Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference



 

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