Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00235
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| PDC Name |
LWJ-M30
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Colorectal cancer
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| Structure |
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| Peptide Name |
B6
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Peptide Info | ||||
| Receptor Name |
Transferrin receptor protein 1 (TFRC)
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Receptor Info | ||||
| Drug Name |
Maytansine
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Drug Info | ||||
| Therapeutic Target |
Microtubule (MT)
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Target Info | ||||
| Linker Name |
Disulfide bond
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Linker Info | ||||
| Formula |
C80H126ClN21O21S2
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| #Ro5 Violations (Lipinski): 4 | Molecular Weight | 1817.601 | ||||
| Lipid-water partition coefficient (xlogp) | -1.7436 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 18 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 28 | |||||
| Rotatable Bond Count (rotbonds) | 51 | |||||
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 | Colorectal cancer | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
0.047 µM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| MOA of PDC |
Given these findings, we employed tissue-specific drug delivery approaches PDC to overcome those adverse effects. Several TfR-targeted peptides sequence with different affinity have been reported, so we synthesized a series of TfR-targeted peptide-DM1 conjugates for screening the effects of TfR-targeted drug candidates. It is speculated that the conjugates can specifically target tumor with high expression of TfR and can be uptake more than that of the normal cells. We succeeded found LWJ-M30, a conjugate of DM1 and B6, had a significant therapeutic effect after preliminary screening. In order to further reveal the improved therapeutic effects and mechanism of the LWJ-M30 on cancer with high TfR expression, in this study, we investigated the role of the LWJ-M30 in the targeted therapy for colorectal cancer in vitro and in vivo and explored the therapeutic mechanism.
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| Description |
To determine the activity of the compounds, we analyzed the effects of them on cell growth and migration in HCT116 cells. We found that LWJ-M30 displayed significant inhibition of cell proliferation and clone formation ability. The IC50 of LWJ-M30 was 0.047 uM which was close to DM1 (0.026 uM). According to the results of wound-healing assay and transwell migration assay, LWJ-M30 also dramatically showed a inhibitory effect on cells migration. These results suggested that LWJ-M30 could inhibit the cells proliferation and migration.
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| In Vitro Model | Colon carcinoma | HCT 116 cell | CVCL_0291 | ||
References