Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00022
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| Peptide Name |
TAT (trans-activator of transcription)
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| Structure |
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| Sequence |
CYGRKKRRQRRR
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| Peptide Type |
Linear
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| PDC Transmembrane Types | Cell-penetrating peptides (CPPs) | |||||
| Formula |
C67H123N33O15S
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| Isosmiles |
[H]NCCCC[C@H](NC(=O)[C@H](CCC/N=C(/N)N[H])NC(=O)CNC(=O)[C@H](Cc1ccc(O[H])cc1)NC(=O)[C@H](CS[H])N[H])C(=O)N[C@@H](CCCCN[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](CCC(=O)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)N[C@@H](CCC/N=C(/N)N[H])C(=O)O
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| InChI |
InChI=1S/C67H123N33O15S/c68-25-3-1-11-40(92-53(106)39(13-5-27-84-62(72)73)91-50(103)34-90-52(105)48(100-51(104)38(70)35-116)33-36-19-21-37(101)22-20-36)54(107)93-41(12-2-4-26-69)55(108)94-42(14-6-28-85-63(74)75)56(109)95-44(16-8-30-87-65(78)79)58(111)98-46(23-24-49(71)102)60(113)97-43(15-7-29-86-64(76)77)57(110)96-45(17-9-31-88-66(80)81)59(112)99-47(61(114)115)18-10-32-89-67(82)83/h19-22,38-48,101,116H,1-18,23-35,68-70H2,(H2,71,102)(H,90,105)(H,91,103)(H,92,106)(H,93,107)(H,94,108)(H,95,109)(H,96,110)(H,97,113)(H,98,111)(H,99,112)(H,100,104)(H,114,115)(H4,72,73,84)(H4,74,75,85)(H4,76,77,86)(H4,78,79,87)(H4,80,81,88)(H4,82,83,89)/t38-,39-,40-,41-,42-,43-,44-,45-,46-,47-,48-/m0/s1
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| InChIKey |
CCNCSLMFWCFJFV-AIFXSXIMSA-N
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| Pharmaceutical Properties |
Molecule Weight
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1663.004
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Polar area
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885.18
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Complexity
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1661.959711
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xlogp Value
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-11.9143
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Heavy Count
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116
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Rot Bonds
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66
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Hbond acc
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24
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Hbond Donor
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30
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Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
GA-TAT [Investigative]
Revealed Based on the Cell Line Data
| Experiment 1 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 | ||
| Experiment 2 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 | ||
References