Peptide Information
General Information of This Peptide
| Peptide ID |
PEP00081
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| Peptide Name |
Heptapeptide
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| Structure |
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| Sequence |
LPLTPLP
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| Peptide Type |
Linear
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| Receptor Name |
Heat shock protein HSP 90-alpha (HSP90AA1)
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Receptor Info | ||||
| PDC Transmembrane Types | Cell targeting peptides (CTPs) | |||||
| Formula |
C37H63N7O9
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| Isosmiles |
[H]N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@]([H])(C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)O)[C@@H](C)O[H]
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| InChI |
InChI=1S/C37H63N7O9/c1-20(2)17-24(38)34(49)42-14-8-11-27(42)32(47)39-25(18-21(3)4)31(46)41-30(23(7)45)36(51)43-15-9-12-28(43)33(48)40-26(19-22(5)6)35(50)44-16-10-13-29(44)37(52)53/h20-30,45H,8-19,38H2,1-7H3,(H,39,47)(H,40,48)(H,41,46)(H,52,53)/t23-,24+,25+,26+,27+,28+,29+,30+/m1/s1
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| InChIKey |
SZIINWGROOJTLF-DFXDLVLWSA-N
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| Pharmaceutical Properties |
Molecule Weight
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749.951
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Polar area
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231.78
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Complexity
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749.4687266
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xlogp Value
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0.3448
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Heavy Count
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53
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Rot Bonds
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19
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Hbond acc
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9
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Hbond Donor
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6
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The Activity Data of This Peptide
| Peptide Activity Information 1 | [1] | |||||
| KD | 65.3 μM | |||||
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| Binding Affinity Assay |
One flow cell of CM5 sensor chip was activated with a 1:1 mixture of 0.2 M EDC and 0.05 M NHS in water as described by the manufacturer. Hsp90 of 50 μg/ml was injected over the flow cell for 5 min in 10 mM sodium acetate, pH 4.5 at a flow rate of 10 μl/min. The remaining binding sites were blocked by 1 M ethanolamine, pH 8.5. 7200 RU of Hsp90 was immobilized.Peptides with different concentrations were injected over the Hsp90 surface and blank flow cell for 1 min at a flow rate of 30 μl/min. No specific binding to a blank flow cell was subtracted to obtain the corrected sensorgrams. Data were analyzed with the BIAcore T100 evaluation software by fitting to steady state affinity model.
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| Experimental Condition | CM5 sensor chip in the vitro | |||||
Each Peptide-drug Conjugate Related to This Peptide
Full Information of The Activity Data of The PDC(s) Related to This Peptide
DTX-P7 [Preclinical]
Discovered Using Cell Line-derived Xenograft Model
| Experiment 1 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Non-small cell lung cancer | ||||
| Efficacy Data | Tumor Growth Inhibition value (TGI) |
93.2% (Day 28)
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| Administration Time | Once a week for 4 weeks | ||||
| Administration Dosage | 20 mg/kg | ||||
| Evaluation Method | Tumor volume detection assay | ||||
| MOA of PDC |
Collecitvely, by force of active targeting delivery of DTX via membrane-bound Hsp90, DTX-P7 induces unfolded protein response and subsequent apoptosis by degrading Hsp90, meanwhile awakens and kills the dormant cancer stem cells.
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| Description |
Intraperitoneal administration of 20 mg/kg DTX-P7 (equivalent to DTX dose calculated as DTX) reduced tumor growth by 93.2% compared with control mice, whereas the tumor growth inhibition of DTX was only 35.9%.
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| In Vivo Model | A549 cells mouse xenograft model. | ||||
| In Vitro Model | Lung adenocarcinoma | A-549 cell | CVCL_0023 | ||
Revealed Based on the Cell Line Data
| Experiment 1 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Non-small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.62 nM
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Collecitvely, by force of active targeting delivery of DTX via membrane-bound Hsp90, DTX-P7 induces unfolded protein response and subsequent apoptosis by degrading Hsp90, meanwhile awakens and kills the dormant cancer stem cells.
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| Description |
Intraperitoneal administration of 20 mg/kg DTX-P7 (equivalent to DTX dose calculated as DTX) reduced tumor growth by 93.2% compared with control mice, whereas the tumor growth inhibition of DTX was only 35.9%.
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| In Vitro Model | Lung adenocarcinoma | H1975 cell | CVCL_1511 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [2] | ||||
| Indication | Non-small cell lung cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
11.4 nM
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| Administration Time | 48 h | ||||
| Evaluation Method | CCK-8 assay | ||||
| MOA of PDC |
Collecitvely, by force of active targeting delivery of DTX via membrane-bound Hsp90, DTX-P7 induces unfolded protein response and subsequent apoptosis by degrading Hsp90, meanwhile awakens and kills the dormant cancer stem cells.
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| Description |
Intraperitoneal administration of 20 mg/kg DTX-P7 (equivalent to DTX dose calculated as DTX) reduced tumor growth by 93.2% compared with control mice, whereas the tumor growth inhibition of DTX was only 35.9%.
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| In Vitro Model | Lung adenocarcinoma | A-549 cell | CVCL_0023 | ||
References