Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTICO5G)

• DTT Name: Staphylococcus Peptide deformylase (Stap-coc def)
• Synonyms: def; Stap-coc Polypeptide deformylase
• Gene Name: Stap-coc def
• DTT Type: Clinical trial target; [1]
• BioChemical Class: Carbon-nitrogen hydrolase
• UniProt ID: DEF_STAAU
• TTD ID: T58093
• Sequence:
  MLTMKDIIRDGHPTLRQKAAELELPLTKEEKETLIAMREFLVNSQDEEIAKRYGLRSGVG
  LAAPQINISKRMIAVLIPDDGSGKSYDYMLVNPKIVSHSVQEAYLPTGEGCLSVDDNVAG
  LVHRHNRITIKAKDIEGNDIQLRLKGYPAIVFQHEIDHLNGVMFYDHIDKNHPLQPHTDA
  VEV
• 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.

Molecular Interaction Atlas (MIA) of This DTT

1 Clinical Trial Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
GSK1322322	DM1EPMF	Bacterial infection	1A00-1C4Z	Phase 2	[1]

1 Discontinued Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
Actinonin	DMT4P89	N. A.	N. A.	Terminated	[2]

12 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
2-(3-BENZOYLPHENOXY)ETHYL(HYDROXY)FORMAMIDE	DMWMFTJ	Discovery agent	N.A.	Investigative	[3]
3-Sulfinoalanine	DMILTRN	N. A.	N. A.	Investigative	[4]
Bb-3497	DM5SDV9	Discovery agent	N.A.	Investigative	[4]
Cysteinesulfonic Acid	DMXI8FP	Discovery agent	N.A.	Investigative	[4]
Double Oxidized Cysteine	DM6TU84	Discovery agent	N.A.	Investigative	[4]
Formic Acid	DMNFZC6	Discovery agent	N.A.	Investigative	[4]
HYDROXY[3-(6-METHYLPYRIDIN-2-YL)PROPYL]FORMAMIDE	DMA4SIN	Discovery agent	N.A.	Investigative	[3]
N-(2-Acetamido)Iminodiacetic Acid	DM7D3GL	Discovery agent	N.A.	Investigative	[4]
N-alkyl urea hydroxamic acids	DM9T0OK	Discovery agent	N.A.	Investigative	[5]
NVP-PDF386	DMOV0QT	Discovery agent	N.A.	Investigative	[6]
VRC3375	DM1QKVL	Discovery agent	N.A.	Investigative	[7]
[HYDROXY(3-PHENYLPROPYL)AMINO]METHANOL	DM7NXMB	Discovery agent	N.A.	Investigative	[3]

References

• [1] Peptide deformylase: a new target in antibacterial, antimalarial and anticancer drug discovery. Curr Med Chem. 2015;22(2):214-36.
• [2] Actinonin, a naturally occurring antibacterial agent, is a potent deformylase inhibitor. Biochemistry. 2000 Feb 15;39(6):1256-62.
• [3] The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
• [4] How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
• [5] N-alkyl urea hydroxamic acids as a new class of peptide deformylase inhibitors with antibacterial activity. Antimicrob Agents Chemother. 2002 Sep;46(9):2752-64.
• [6] Comparative spectrum and activity of NVP-PDF386 (VRC4887), a new peptide deformylase inhibitor. J Antimicrob Chemother. 2003 Jan;51(1):157-61.
• [7] Peptide 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.