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antitb_1006 details
Primary information
IDantitb_1006
Peptide NameEcumicin
Sequence(N,N-Me2-Val)-(Val)-(N-Me-allo-Ilu)-(Thr)-(N-Me-Thr)-(Val)-(N-Me-Leu)-(Val)-(N-Me-Val)-(N-Me-4-OMe-Trp)-(Val)-(Ph-threo-Ser)-(Val)
N-terminal ModificationFree
C-terminal ModificationFree
Chemical ModificationN-methylation pattern, N-Me-Val = N-methyl-valine, N,N-Me2-Val = N,N-dimethyl-valine, N-Me-Thr = N-methyl-threonine, N-Me-Leu = N-methyl-leucine, N-Me-allo-Ilu = N-methyl-isoleucine, N-Me-4-OMe-Trp = N-methyl-4-methoxy-tryptophan, Ph-threo-Ser = Phe
Linear/ CyclicMacrocyclic
Length13
ChiralityL
NatureNA
SourceNatural
OriginProduced by a genetically distinct Nonomuraea species, strain MJM5123.
SpeciesMycobacterium tuberculosis
StrainMycobacterium tuberculosis Erdman (ATCC 35801)
Inhibition ConcentartionMIC = 0.16 μM
In vitro/In vivoBoth
Cell LineJ774.1 macrophage cell line
Inhibition Concentartion0.12 μM, ecumicin reduced M. tuberculosis viabilities in J774 macrophages by 2 x log10
Cytotoxicity>63 μM for J774.1 cells
In vivo ModelFemale BALB/c mice, male CD-1 mice
Lethal Dose32 mg/kg reductions in M. tuberculosis lung CFU 1.
Immune ResponseNA
Mechanism of ActionEcumicin markedly enhanced the ATPase activity of wild-type (WT) ClpC1 but prevented activation of proteolysis by ClpC1. so toxic proteins which are normally degraded by the ClpC1P1P2 complex, accumulate in the presence of ecumicin
TargetClpC1 ATPase complex
Combination TherapyEcumicin encapsulated in micelles distributes to mouse lung tissue
Other ActivitiesNA
Pubmed ID25421483
Year of Publication2015
3-D StructureNA