Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00153
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| PDC Name |
GA-TAT
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Bladder cancer
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| Structure |
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| Peptide Name |
TAT (trans-activator of transcription)
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Peptide Info | ||||
| Drug Name |
Gambogic acid
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Drug Info | ||||
| Linker Name |
Aminocaproic acid
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Linker Info | ||||
| Peptide Modified Type |
The modification of binding with chemical macromolecules
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| Modified Segment |
6-Aminocaproic acid
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| Ternimal Modification |
N-terminal modification
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| Formula |
C111H176N34O23S
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 2386.911 | ||||
| Lipid-water partition coefficient (xlogp) | -3.9119 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 32 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 31 | |||||
| Rotatable Bond Count (rotbonds) | 80 | |||||
Full List of Activity Data of This Peptide-drug Conjugate
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Bladder cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
1.24 µM
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| Administration Time | 24 h | ||||
| Evaluation Method | MTT assay | ||||
| MOA of PDC |
These findings suggest that GA-TAT-induced EJ cell apoptosis is mediated via ROS production. Our study demonstrated that GA-TAT enhanced the pro-apoptotic effect via increasing caspase-3 and caspase-9 processing and activities and decreasing the Bcl-2/Bax ratio, which were regulated by intracellular ROS.
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| Description |
The 50% inhibitory concentration (IC50) of GA-TAT at 24 h was 1.24 uM
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| In Vitro Model | Bladder cancer | Bladder cancer cell | Homo sapiens | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Bladder cancer | ||||
| Efficacy Data | Inhibition rate |
46.4% ± 4.86%
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| Administration Time | 24 h | ||||
| Administration Dosage | 1.0 µM | ||||
| MOA of PDC |
These findings suggest that GA-TAT-induced EJ cell apoptosis is mediated via ROS production. Our study demonstrated that GA-TAT enhanced the pro-apoptotic effect via increasing caspase-3 and caspase-9 processing and activities and decreasing the Bcl-2/Bax ratio, which were regulated by intracellular ROS.
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| Description |
However, after treatment with GA-TAT, the percentage of apoptotic cells was greatly increased to 46.4%±4.86%.
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| In Vitro Model | Bladder carcinoma | EJ-1 cell | CVCL_2893 | ||
References