Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR00267

Target Information
NamePeptide deformylase    
Type of targetClinical trial target    
SynonymsPDF    
Polypeptide deformylase    
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][2][3]
Malaria
[ICD9: 084   ICD10: B50-B54]
[4]
BioChemical ClassHydrolases acting on carbon-nitrogen bonds    
EC NumberEC 3.5.1.88
UniProt IDP27251
Q9HBH1
PDB Structure1BS4; 1BS5; 1BS6; 1BS7; 1BS8; 1BSJ; 3G5K; 3G5P.    
FunctionRemoves the formyl group from the n-terminal met of newly synthesized proteins. Requires at least a dipeptide for an efficient rate of reaction. N-terminal l-methionine is a prerequisite for activity but the enzyme has broad specificity at other positions.    
SequenceMSVLQVLHIPDERLRKVAKPVEEVNAEIQRIVDDMFETMYAEEGIGLAATQVDIHQRIIV IDVSENRDERLVLINPELLEKSGETGIEEGCLSIPEQRALVPRAEKVKIRALDRDGKPFE LEADGLLAICIQHEMDHLVGKLFMDYLSPLKQQRIRQKVEKLDRLKARA
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor2- (3-BENZOYLPHENOXY)ETHYL[5]
3-Sulfinoalanine[6]
Actinonin[7]
BB-3497[8]
Bb-3497[6]
Cysteinesulfonic Acid[6]
Double Oxidized Cysteine[6]
Formic Acid[6]
HYDROXY[3- (6-METHYLPYRIDIN-2-YL)PROPYL]FORMAMIDE[5]
N- (2-Acetamido)Iminodiacetic Acid[6]
N-alkyl urea hydroxamic acids[9]
NVP-PDF386 (VRC4887)[10]
VRC3375[3]
[HYDROXY (3-PHENYLPROPYL)AMINO]METHANOL[5]
BinderHydroxamates[11]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Characterization of a human peptide deformylase: implications for antibacterial drug design. Biochemistry. 2003 Aug 26;42(33):9952-8. To Reference
Ref 2Peptide deformylase as an antibacterial drug target: assays for detection of its inhibition in Escherichia coli cell homogenates and intact cells. Antimicrob Agents Chemother. 2001 Apr;45(4):1053-7. To Reference
Ref 3Peptide deformylase inhibitors as antibacterial agents: identification of VRC3375, a proline-3-alkylsuccinyl hydroxamate derivative, by using an integrated combinatorial and medicinal chemistry approach. Antimicrob Agents Chemother. 2004 Jan;48(1):250-61. To Reference
Ref 4Crystals of peptide deformylase from Plasmodium falciparum reveal critical characteristics of the active site for drug design. Structure. 2002 Mar;10(3):357-67. To Reference
Ref 5Berman 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 6Overington 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 7Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry. 2000 Feb 15;39(6):1256-62. To Reference
Ref 8Asymmetric synthesis of BB-3497--a potent peptide deformylase inhibitor. Bioorg Med Chem Lett. 2001 Oct 8;11(19):2585-8. To Reference
Ref 9N-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity. Antimicrob Agents Chemother. 2002 Sep;46(9):2752-64. To Reference
Ref 10Comparative spectrum and activity of NVP-PDF386 (VRC4887), a new peptide deformylase inhibitor. J Antimicrob Chemother. 2003 Jan;51(1):157-61. To Reference
Ref 11Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. To Reference



 

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