Browse result page of AntiTbPdb
The total number entries retrieved from this search are 22
| ID | Name | Sequence | N-Terminal Modification | C-Terminal Modification | Chemical Modification | Linear/Cyclic | Length | Chirality | Nature | Source | Origin | Species | Strain | Inhibition Concentration | In vitro/ In vivo | Cell Line | Intracellular Inhibition | Cytotoxicity | Animal Model | Effective Dose in model organism | Immune Responce | Mechanism of Action | Target | Combination Therapy | Other Activities | Year of Publication | Pubmed ID/ Patent No. |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| antitb_1195 | Boropentapeptide | AVKAA-B(OH)2 | Free | Conjugated with Boronic acid | Conjugated with Boronic acid | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium thermoresistible | Mycobacterium thermoresistible | Poorer inhibition than Pinanediol PD-protected Boropentapeptide | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1196 | Boropentapeptide | AVKAA-B(OH)2 | Free | Conjugated with Boronic acid | Conjugated with Boronic acid | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium smegmatis | Mycobacterium smegmatis | Poorer inhibition than Pinanediol PD-protected Boropentapeptide | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1197 | Boropentapeptide | AVKAA-B(OH)2 | Free | Conjugated with Boronic acid | Conjugated with Boronic acid | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium tuberculosis | Mycobacterium tuberculosis | Poorer inhibition than Pinanediol PD-protected Boropentapeptide | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1198 | Pinanediol PD-protected Boropentapeptide | AVKAA-BO2(PD) | Free | Conjugated with Boronic acid and pinanediol PD | Conjugated with Boronic acid and pinanediol PD | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium thermoresistible | Mycobacterium thermoresistible | IC50 = 121.6 ± 25.3 μM for MycP1 | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1199 | Pinanediol PD-protected Boropentapeptide | AVKAA-BO2(PD) | Free | Conjugated with Boronic acid and pinanediol PD | Conjugated with Boronic acid and pinanediol PD | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium smegmatis | Mycobacterium smegmatis | IC50 = 93.2±33.7 μM for MycP2 | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1200 | Pinanediol PD-protected Boropentapeptide | AVKAA-BO2(PD) | Free | Conjugated with Boronic acid and pinanediol PD | Conjugated with Boronic acid and pinanediol PD | Linear | 5 | L | NA | Synthetic | NA | Mycobacterium tuberculosis | Mycobacterium tuberculosis | IC50 = 37.9±5.2 μM for MycP3 | In vitro | None | NA | NA | None | NA | NA | Inhibit enzyme (MycP1) reponsible for cleavage of virulence factor (ESX secretion-associated protein B (EspB)) | Mycosin protease-1 (MycP1) | None | None | 2014 | 24915878 |
| antitb_1271 | Inhibitor 1 | PK-(boroMet) | Acetylation | Free | boroMet = methionine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 12 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1272 | Inhibitor 2 | HK-(boroMet) | Acetylation | Free | boroMet = methionine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 6 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1273 | Inhibitor 3 | AK-(boroMet) | Acetylation | Free | boroMet = methionine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 3 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1274 | Inhibitor 4 | Ala(1-naphtyl)-K-boroLeu | Free | Free | Ala(1-naphtyl) = 1-napthylalanine, boroLeu = leucine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 12 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1275 | Inhibitor 4 | Ala(1-naphtyl)-K-boroLeu | Free | Free | Ala(1-naphtyl) = 1-napthylalanine, boroLeu = leucine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium smegmatis | Mycobacterium smegmatis strain constitutively expressing GFP-ssrA | MIC50 = 1.5 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1276 | Inhibitor 5 | WK-(boroMet) | Addition of N-picolinoyl | Free | boroLeu = leucine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 3 μM | In vitro | Myeloma cells (MM1.S) | NA | Slight toxic (25%) at 10 μM | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1277 | Inhibitor 6 | AK-(boroMet) | Addition of N-picolinoyl | Free | boroMet = methionine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 3 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1278 | Inhibitor 7 | PK-(boroMet) | Addition of N-picolinoyl | Free | boroMet = methionine boronic acid | Linear | 3 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 24 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1279 | Inhibitor 8 | K-(boroMet) | Addition of N-picolinoyl | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 6 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1280 | Inhibitor 9 | K-(boroMet) | Addition of N-(3-Phenyl)propanoyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 3 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1281 | Inhibitor 10 | K-(boroMet) | Addition of N-(Benzyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 6 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1282 | Inhibitor 11 | K-(boroMet) | Addition of N-(2-(3,5-Difluorophenyl)acetyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 6 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1283 | Inhibitor 12 | W-(boroMet) | Addition of N-(2-(3,5-Difluorophenyl)acetyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 12 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1284 | Inhibitor 12 | W-(boroMet) | Addition of N-(2-(3,5-Difluorophenyl)acetyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium smegmatis | Mycobacterium smegmatis strain constitutively expressing GFP-ssrA | MIC50 = 12 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1285 | Inhibitor 13 | K-(boroMet) | Addition of N-(1H-benzo(b)thiophene-7-carbonyl | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 12 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |
| antitb_1286 | Inhibitor 14 | K-(boroMet) | Addition of N-(Phenylmetanesulfonyl) | Free | boroMet = methionine boronic acid | Linear | 2 | L | NA | Synthetic | substrate-based boronate inhibitors | Mycobacterium tuberculosis | Mycobacterium tuberculosis H37Rv | MIC50 = 200 μM | In vitro | Myeloma cells (MM1.S) | NA | No cytotoxicty | None | NA | NA | Inhibit ClpP1P2 peptidase activity and protein degradation in the presence of ClpC1 and ClpX ATPases. | ClpP1P2 peptidase | None | None | 2015 | 25759383 |