Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_00131
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| PDC Name |
D-Lys6-GnRH-gemcitabine(GSHG)
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Tumor
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| Structure |
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| Peptide Name |
[D-Lys6]-LH-RH
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Peptide Info | ||||
| Receptor Name |
Gonadotropin-releasing hormone receptor (GNRHR)
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Receptor Info | ||||
| Drug Name |
Gemcitabine
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Drug Info | ||||
| Therapeutic Target |
Ribonucleoside-diphosphate reductase subunit M2 (RRM2)
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Target Info | ||||
| Linker Name |
GSHG
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Linker Info | ||||
| Formula |
C78H108F2N22O20
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| #Ro5 Violations (Lipinski): 5 | Molecular Weight | 1711.852 | ||||
| Lipid-water partition coefficient (xlogp) | -3.78993 | |||||
| Hydrogen Bond Donor Count (hbonddonor) | 21 | |||||
| Hydrogen Bond Acceptor Count (hbondacc) | 25 | |||||
| Rotatable Bond Count (rotbonds) | 48 | |||||
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 | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2.40 nM
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| Description |
The presented data show that 2G2, 2G1 and GSHG bind to GnRH-R with 95.5-, 15.2-, and 4.4-fold higher affinity, respectively, than that of the native peptide D-Lys6-GnRH (10.5 ± 0.2 nM, according to our former study [3]).
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| In Vitro Model | Normal | HEK293 cell | CVCL_0045 | ||
| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
55.5 nM
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| Description |
GSHGpossesses the highest cytotoxic effect among the three conjugates, which is comparable with that of gemcitabine in the examined cell lines and especially regarding MCF-7 cells.
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| In Vitro Model | Invasive breast carcinoma | MCF-7 cell | CVCL_0031 | ||
| Experiment 3 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
684 nM
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| Description |
GSHGpossesses the highest cytotoxic effect among the three conjugates, which is comparable with that of gemcitabine in the examined cell lines and especially regarding MCF-7 cells.
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| In Vitro Model | Prostate carcinoma | DU145 cell | CVCL_0105 | ||
| Experiment 4 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
937 nM
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| Description |
GSHGpossesses the highest cytotoxic effect among the three conjugates, which is comparable with that of gemcitabine in the examined cell lines and especially regarding MCF-7 cells.
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| In Vitro Model | Prostate carcinoma | PC-3 cell | CVCL_0035 | ||
| Experiment 5 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Tumor | ||||
| Efficacy Data | Half Maximal Inhibitory Concentration (IC50) |
2387 nM
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| Description |
GSHGpossesses the highest cytotoxic effect among the three conjugates, which is comparable with that of gemcitabine in the examined cell lines and especially regarding MCF-7 cells.
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| In Vitro Model | Breast adenocarcinoma | MDA-MB-231 cell | CVCL_0062 | ||
References