Target Information

Target General Infomation
Target ID
T58093
Former ID
TTDR00267
Target Name
Peptide deformylase
Gene Name
def
Synonyms
PDF; Polypeptide deformylase; def
Target Type
Clinical Trial
Disease Bacterial infections [ICD9: 001-009, 010-018, 020-027, 030-041, 080-088, 090-099, 100-104; ICD10: A00-B99]
Infection of P. falciparum [ICD9: 84; ICD10: B50-B54]
Function
Removes 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 (By similarity).
BioChemical Class
Carbon-nitrogen hydrolase
UniProt ID
P68826
EC Number
EC 3.5.1.88
Sequence
MLTMKDIIRDGHPTLRQKAAELELPLTKEEKETLIAMREFLVNSQDEEIAKRYGLRSGVG
LAAPQINISKRMIAVLIPDDGSGKSYDYMLVNPKIVSHSVQEAYLPTGEGCLSVDDNVAG
LVHRHNRITIKAKDIEGNDIQLRLKGYPAIVFQHEIDHLNGVMFYDHIDKNHPLQPHTDA
VEV
Drugs and Mode of Action
Drug(s) GSK1322322 Drug Info Phase 2 Bacterial infections [532938]
Actinonin Drug Info Terminated Discovery agent [546250]
Inhibitor 2-(3-BENZOYLPHENOXY)ETHYL(HYDROXY)FORMAMIDE Drug Info [551374]
3-Sulfinoalanine Drug Info [551393]
Actinonin Drug Info [534962]
Bb-3497 Drug Info [551393]
Cysteinesulfonic Acid Drug Info [551393]
Double Oxidized Cysteine Drug Info [551393]
Formic Acid Drug Info [551393]
HYDROXY[3-(6-METHYLPYRIDIN-2-YL)PROPYL]FORMAMIDE Drug Info [551374]
N-(2-Acetamido)Iminodiacetic Acid Drug Info [551393]
N-alkyl urea hydroxamic acids Drug Info [535535]
NVP-PDF386 (VRC4887) Drug Info [535642]
VRC3375 Drug Info [535885]
[HYDROXY(3-PHENYLPROPYL)AMINO]METHANOL Drug Info [551374]
Modulator GSK1322322 Drug Info [532261], [532938]
Binder Hydroxamates Drug Info [536135]
References
Ref 532938Peptide deformylase: a new target in antibacterial, antimalarial and anticancer drug discovery. Curr Med Chem. 2015;22(2):214-36.
Ref 546250Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007111)
Ref 532261Comparative analysis of the antibacterial activity of a novel peptide deformylase inhibitor, GSK1322322. Antimicrob Agents Chemother. 2013 May;57(5):2333-42.
Ref 532938Peptide deformylase: a new target in antibacterial, antimalarial and anticancer drug discovery. Curr Med Chem. 2015;22(2):214-36.
Ref 534962Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry. 2000 Feb 15;39(6):1256-62.
Ref 535535N-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity. Antimicrob Agents Chemother. 2002 Sep;46(9):2752-64.
Ref 535642Comparative spectrum and activity of NVP-PDF386 (VRC4887), a new peptide deformylase inhibitor. J Antimicrob Chemother. 2003 Jan;51(1):157-61.
Ref 535885Peptide 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.
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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