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Browse result page of AntiTbPdb

The total number entries retrieved from this search are 550
IDNameSequenceN-Terminal ModificationC-Terminal ModificationChemical ModificationLinear/CyclicLengthChiralityNatureSourceOriginSpeciesStrainInhibition ConcentrationIn vitro/ In vivoCell LineIntracellular InhibitionCytotoxicityAnimal ModelEffective Dose in model organismImmune ResponceMechanism of ActionTargetCombination TherapyOther ActivitiesYear of PublicationPubmed ID/ Patent No.
antitb_1205Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF (85)MIC = 1.56-3.1 μg/ml or 0.83 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1206Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF (7)MIC = 1.56 μg/ml or 0.83 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1207Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR (86)MIC = 1.56 μg/ml or 0.83 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1208Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR, FQ (136)MIC = 0.78 μg/ml or 0.41 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1209Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR, FQ (133)MIC = 0.78 μg/ml or 0.41 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1210Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR, FQ (189)MIC = 3.1 μg/ml or 1.65 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1211Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, EMB, FQ (3)MIC = 3.1 μg/ml or 1.65 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1212Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, EMB, PZA, FQ (30)MIC = 0.78 μg/ml or 0.41 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1213Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, EMB, PZA, FQ (181)MIC = 0.78 μg/ml or 0.41 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1214Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR, EMB, PZA, FQ (183)MIC = 3.1 μg/ml or 1.65 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1215Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis resistant to INH, RIF, STR, EMB, PZA, FQ (188)MIC = 3.1 μg/ml or 1.65 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1216Lassomycin GLRRLFADQLVGRRNI-CO2CH3Involved in Cyclic formationAddition of Methyl esterFormation of an amide bond between N-terminal amine and the side chain carboxyl group of Asp8.Cyclic16LHighly BasicNaturalExtracts from soil actinomycetesMycobacterium tuberculosis Mycobacterium tuberculosis mc26020MIC = 0.39-0.78 μg/ml or 0.21-0.41 μMIn vitroHuman NIH 3T3 and HepG2, erythrocytes NALow cytotoxicty (IC50, 350 μg/ml) against human NIH 3T3 and HepG2 cellsNone NANAUncoupling ATPase from proteolytic activityClpC1 ATPase complex NoneAntibacterial (other actinobacteria, gram positive and gram negative bacteria)201424684906
antitb_1221PK34 PRVIETKVHGREVTGLARNVSEENVDRLAKRWIKFreeFreeNoneLinear34LCationicSyntheticSearched and selected from mycobacteriophage genome sequencesMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv strain (ATCC 27294 MIC = 50 μg/mlBothMurine macrophage-like J774A.1 NANAFour-week-old female BALB/c mice Dose of 20 mg (5×10−6 mol)/kg BW/d, PK34 had coInhibits the proinflammatory factor (IFN-γ, TNF-α, MCP-1, IL-6, IL-10, IL-12) production of macrophage cells induced by TDM.Cell wall disruptiontrehalose-6,6=-dimycolate (TDM) NoneNone201323603838
antitb_1223Human neutrophil peptide 1 (HNP-1)ACYCRIPACIAGERRYGTCIYQGRLWAFCCFreeFreeDisulfide bridge: 2-30, 4-19, 9-29Cyclic30LNAProtein DerivedHuman neutrophilMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv 96.5 % inhibition at 10 μg/mlIn vitroTHP-1 cells Significant reduction in CFUNANone NANANANANoneNone201323827033
antitb_1224Human neutrophil peptide 1 (HNP-1)ACYCRIPACIAGERRYGTCIYQGRLWAFCCFreeFreeDisulfide bridge: 2-30, 4-19, 9-30Cyclic30LNAProtein DerivedHuman neutrophilMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv 98.3 % inhibition at 15 μg/mlIn vitroTHP-1 cells Significant reduction in CFUNANone NANANANANoneNone201323827033
antitb_1225Human neutrophil peptide 1 (HNP-1)ACYCRIPACIAGERRYGTCIYQGRLWAFCCFreeFreeDisulfide bridge: 2-30, 4-19, 9-31Cyclic30LNAProtein DerivedHuman neutrophilMycobacterium tuberculosis 36 Clinical isolates of Mycobacterium tuberculosis11 isolates (31%) showed greater sensitivity to HNP-1 than H37Rv strains. At 15 μg/ml, they wer completely inhibited.In vitroTHP-1 cells Sixteen clinical isolates had lower intracellular growth ability than the H37Rv strain. NANone NANANANANoneNone201323827033
antitb_1228High Activity Binding Peptides (HABPs) TGMAALEQYLGSGHAVIVSIFreeFreeNoneLinear20LNAProtein DerivedFrom Rv1268c protein Mycobacterium tuberculosis Mycobacterium tuberculosis H37Rv NAIn vitroalveolar epithelial cells A549 (ATCC No. CCL-185) Inhibited mycobacterial entry by up to 65%. NANone NANAInhibit mycobacterial entry into cellsNANoneNone201323993672
antitb_1229High Activity Binding Peptides (HABPs) AVALGLASPADAAAGTMYGDFreeFreeNoneLinear20LNAProtein DerivedFrom Rv1268c protein Mycobacterium tuberculosis Mycobacterium tuberculosis H37Rv NAIn vitroU937 monocyte derived macrophages (ATCC No. CRL-1593.2) Inhibited mycobacterial entry by up to 65%. NANone NANAInhibit mycobacterial entry into cellsNANoneNone201323993672
antitb_1232(LLKK)2LLKKLLKKFreeFreeNoneLinear8LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv MIC > 500 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1233(LLKK)2LLKKLLKKFreeFreeNoneLinear8LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis CSU87 reistant to rifampicin, isoniazid, ethambutol, streptomycin and kanamycinMIC > 500 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1237C(LLKK)2CLLKKLLKKFreeFreeNoneLinear9LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv MIC > 500 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1238C(LLKK)2CLLKKLLKKFreeFreeNoneLinear9LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis CSU87 reistant to rifampicin, isoniazid, ethambutol, streptomycin and kanamycinMIC > 500 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1245(LLKK)2M LLKKLLKKMFreeFreeNoneLinear9LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv MIC > 500 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1246(LLKK)2M LLKKLLKKMFreeFreeNoneLinear9LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis CSU87 reistant to rifampicin, isoniazid, ethambutol, streptomycin and kanamycinMIC = 125 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1253M(LLKK)2M MLLKKLLKKMFreeFreeNoneLinear10LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv MIC = 125 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1254M(LLKK)2M MLLKKLLKKMFreeFreeNoneLinear10LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis H37Rv MIC = 7.81 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeRifampicin, shows synergyAntibacterial201424314557
antitb_1255M(LLKK)2M MLLKKLLKKMFreeFreeNoneLinear10LCationicSyntheticNAMycobacterium tuberculosis Mycobacterium tuberculosis CSU87 reistant to rifampicin, isoniazid, ethambutol, streptomycin and kanamycinMIC = 62.5 mg/LIn vitroRat red blood cells (rRBCs) NAVery low, i.e. 50% hemolysis concentration (HC50) > 1000 mg/LNone NANAMembrane-lytic mechanism Cell envelopeNoneAntibacterial201424314557
antitb_1268VapB30 (52-59)ELAAIRHRFreeFreeNoneLinear8LNAProtein DerivedFrom VapB30 toxinMycobacterium tuberculosis Mycobacterium tuberculosis (strain H37Rv) NANANANANANone NANABy disrupting the toxin-antitoxin complex (VapBC)VapBCNoneNA201526150422
antitb_1269VapC30 (14-30)DEPDAERFEAAVEADHIFreeFreeNoneLinear17LNAProtein DerivedFrom VapC30 toxinMycobacterium tuberculosis Mycobacterium tuberculosis (strain H37Rv) NANANANANANone NANABy disrupting the toxin-antitoxin complex (VapBC)VapBCNoneNA201526150422
antitb_1270VapC30 (48-56)RFGEPGGREFreeFreeNoneLinear9LNAProtein DerivedFrom VapC30 toxinMycobacterium tuberculosis Mycobacterium tuberculosis (strain H37Rv) NANANANANANone NANABy disrupting the toxin-antitoxin complex (VapBC)VapBCNoneNA201526150422
antitb_1271Inhibitor 1PK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1272Inhibitor 2HK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1273Inhibitor 3AK-(boroMet)AcetylationFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1274Inhibitor 4Ala(1-naphtyl)-K-boroLeu FreeFreeAla(1-naphtyl) = 1-napthylalanine, boroLeu = leucine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1276Inhibitor 5WK-(boroMet) Addition of N-picolinoylFreeboroLeu = leucine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NASlight toxic (25%) at 10 μMNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1277Inhibitor 6AK-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1278Inhibitor 7PK-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear3LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 24 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1279Inhibitor 8K-(boroMet) Addition of N-picolinoylFreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1280Inhibitor 9K-(boroMet) Addition of N-(3-Phenyl)propanoyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 3 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1281Inhibitor 10K-(boroMet) Addition of N-(Benzyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1282Inhibitor 11K-(boroMet) Addition of N-(2-(3,5-Difluorophenyl)acetyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 6 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1283Inhibitor 12W-(boroMet) Addition of N-(2-(3,5-Difluorophenyl)acetyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1285Inhibitor 13K-(boroMet) Addition of N-(1H-benzo(b)thiophene-7-carbonylFreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 12 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1286Inhibitor 14K-(boroMet) Addition of N-(Phenylmetanesulfonyl)FreeboroMet = methionine boronic acidLinear2LNASyntheticsubstrate-based boronate inhibitors Mycobacterium tuberculosisMycobacterium tuberculosis H37Rv MIC50 = 200 μMIn vitroMyeloma cells (MM1.S) NANo cytotoxictyNone NANAInhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases.ClpP1P2 peptidase NoneNone201525759383
antitb_1287Bcn1  FVYGNGVTSILVQAQFLVNGQRRFFYTPDKFreeFreeNoneLinear30LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv MIC90 = 0.1 mg/LBothMouse macrophagesNo inhibitionNo cytotoxictyNone NANAFormation of pores in cell membranesCell envelopeNoneNone200717347179
antitb_1288Bcn2 ATYYGNGLYCNKQKHYTWVDWNKASREIGKITVNGWVQHFreeFreeNoneLinear39LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv MIC90 = 0.1 mg/LBothMouse macrophagesNo inhibitionNegligible at a concentration of 1 mg/L None NANAFormation of pores in cell membranesCell envelopeNoneNone200717347179
antitb_1289Bcn3KTYYGTNGVHCTKNSLWGKVRLKNMKYDQNTTYMGRLQDILLGWATGAFGKTHFreeFreeNoneLinear53LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv MIC90 = 0.1 mg/LBothMouse macrophagesNo inhibitionNegligible at a concentration of 1 mg/L None NANAFormation of pores in cell membranesCell envelopeNoneNone200717347179
antitb_1290Bcn4RWYYGNGVGGVGGAAVCGLAGYVGEAKENIAGEVRKGWGMAGGFTHNKACKSFPGSGWASGFreeFreeNoneLinear61LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv MIC90 = 0.1 mg/LBothMouse macrophagesNo inhibitionNo cytotoxictyNone NANAFormation of pores in cell membranesCell envelopeNoneNone200717347179
antitb_1291Bcn5TTKNYGNGVCNSVNWCQCGNVWASCNLATGCAAWLCKLAFreeFreeNoneLinear39LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv MIC90 = 0.1 mg/LBothMouse macrophagesNo inhibitionNo cytotoxictyC57BL/6JCit (B6) feamale mice of age 14 10 mg/mouse of Bcn5 NAFormation of pores in cell membranesCell envelopeNoneNone200717347179
antitb_1292Bcn5TTKNYGNGVCNSVNWCQCGNVWASCNLATGCAAWLCKLAFreeFreeNoneLinear39LNANaturalIsolated from diverse Gram-positive bacteria speciesMycobacterium tuberculosisMycobacterium tuberculosis strain H37Rv NABothMouse macrophagesNo inhibitionNo cytotoxictyC57BL/6JCit (B6) feamale mice of age 15 10 mg/mouse of Bcn5-PhC complexNAFormation of pores in cell membranesCell envelopeMixture of phosphatidylcholine (Ph) and cardiolipin (C) with Bcn5None200717347179