Peptide-drug Conjugate Information
General Information of This Peptide-drug Conjugate (PDC)
| PDC ID |
PDC_02142
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| PDC Name |
MAHNP-Dox conjugate
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| PDC Status |
Investigative
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| Indication |
In total 1 Indication(s)
Breast cancer
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| Structure |
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| Peptide Name |
AHNP
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Peptide Info | ||||
| Receptor Name |
Receptor tyrosine-protein kinase erbB-2 (ERBB2)
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Receptor Info | ||||
| Drug Name |
Doxorubicin
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Drug Info | ||||
| Therapeutic Target |
DNA topoisomerase 2-alpha (TOP2A)
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Target Info | ||||
| Linker Name |
Glutaric acid
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Linker Info | ||||
| Peptide Modified Type |
Cyclization modification
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| Modified Segment |
Side-chain cyclization
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| ChEBI ID | ||||||
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 | Breast cancer | ||||
| Efficacy Data | Half maximal inhibitory concentration (IC50) |
110.1 ± 12.7 nM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| MOA of PDC |
You et al. developed a unique approach for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer. A peptide fragment from the heavy chain 3 of the full-length antibody trastuzumab was obtained and termed AHNP. The 12-mer AHNP binds the extracellular domain of HER2 with high affinity and displays similar potency as trastuzumab. The peptide mimetic AHNP was then conjugated via an MMP-2 sensitive linker with doxorubicin (Dox) to form MAHNP-Dox conjugate essentially using ester/amide bonds.
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| Description |
Conjugate MAHNP-Dox was compared to Dox using HER2 positive breast cancer cell lines BT474 and SKBR3. Cellular toxicity analysis showed that MAHNP-Dox was more potent than free Dox, as indicated by lower IC50 values for both cell lines. The BT474 and SKBR3 cell lines had an IC50 of 746.8 ± 81.5 nM and 110.1 ± 12.7 nM for MAHNP-DOX and 2075.0 ± 368.0 nM and 172.9 ± 19.2 nM for Dox, respectively.
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| Experiment 2 Reporting the Activity Data of This PDC | [1] | ||||
| Indication | Breast cancer | ||||
| Efficacy Data | Half maximal inhibitory concentration (IC50) |
746.8 ± 81.5 nM
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| Administration Time | 48 h | ||||
| Evaluation Method | MTT assay | ||||
| MOA of PDC |
You et al. developed a unique approach for the treatment of human epidermal growth factor receptor 2 (HER2)-positive breast cancer. A peptide fragment from the heavy chain 3 of the full-length antibody trastuzumab was obtained and termed AHNP. The 12-mer AHNP binds the extracellular domain of HER2 with high affinity and displays similar potency as trastuzumab. The peptide mimetic AHNP was then conjugated via an MMP-2 sensitive linker with doxorubicin (Dox) to form MAHNP-Dox conjugate essentially using ester/amide bonds.
Click to Show/Hide
|
||||
| Description |
Conjugate MAHNP-Dox was compared to Dox using HER2 positive breast cancer cell lines BT474 and SKBR3. Cellular toxicity analysis showed that MAHNP-Dox was more potent than free Dox, as indicated by lower IC50 values for both cell lines. The BT474 and SKBR3 cell lines had an IC50 of 746.8 ± 81.5 nM and 110.1 ± 12.7 nM for MAHNP-DOX and 2075.0 ± 368.0 nM and 172.9 ± 19.2 nM for Dox, respectively.
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References