{"database":"biostudies-literature","file_versions":[],"scores":null,"additional":{"submitter":["Ziaei E"],"funding":["National Cancer Institute","NCI NIH HHS"],"pagination":["3098-3106"],"full_dataset_link":["https://www.ebi.ac.uk/biostudies/studies/S-EPMC7965737"],"repository":["biostudies-literature"],"omics_type":["Unknown"],"volume":["30(12)"],"pubmed_abstract":["In this study, we have designed and synthesized two novel peptide-drug conjugates (PDCs) where the drug, doxorubicin (Dox), is linked to the peptide via a succinimidyl thioether bond or a hydrazone linker. A highly specific and proteolytically stable breast cancer cell targeting peptide (WxEAAYQrFL) is conjugated to Dox to synthesize peptide-Dox thioether (<b>1</b>) or hydrazone (<b>2</b>) conjugate. The evaluation of the stability in water, media, and human serum showed that the conjugate <b>1</b> with the succinimidyl thioether linkage is more stable compared to the acid-sensitive hydrazone containing conjugate <b>2</b>. The cytotoxicity studies showed that the two PDCs were as toxic as free Dox toward the triple negative breast cancer (TNBC) cells and were 7-30 times less toxic (IC<sub>50</sub> 1.2-4.7 μM for TNBC cells versus 15-39 μM for noncancerous cells) toward the noncancerous breast cells compared to the free doxorubicin (IC<sub>50</sub> 0.35-1.5 μM for TNBC cells versus 0.24 μM for noncancerous cells). The results from the comparative study of the two PDCs suggest that both may have translational potential for TNBC treatment."],"journal":["Bioconjugate chemistry"],"pubmed_title":["Targeting Triple Negative Breast Cancer Cells with Novel Cytotoxic Peptide-Doxorubicin Conjugates."],"pmcid":["PMC7965737"],"funding_grant_id":["R15 CA208656","R15CA208656"],"pubmed_authors":["Saghaeidehkordi A","Kaur K","Dill C","Chen S","Maslennikov I","Ziaei E"],"additional_accession":[]},"is_claimable":false,"name":"Targeting Triple Negative Breast Cancer Cells with Novel Cytotoxic Peptide-Doxorubicin Conjugates.","description":"In this study, we have designed and synthesized two novel peptide-drug conjugates (PDCs) where the drug, doxorubicin (Dox), is linked to the peptide via a succinimidyl thioether bond or a hydrazone linker. A highly specific and proteolytically stable breast cancer cell targeting peptide (WxEAAYQrFL) is conjugated to Dox to synthesize peptide-Dox thioether (<b>1</b>) or hydrazone (<b>2</b>) conjugate. The evaluation of the stability in water, media, and human serum showed that the conjugate <b>1</b> with the succinimidyl thioether linkage is more stable compared to the acid-sensitive hydrazone containing conjugate <b>2</b>. The cytotoxicity studies showed that the two PDCs were as toxic as free Dox toward the triple negative breast cancer (TNBC) cells and were 7-30 times less toxic (IC<sub>50</sub> 1.2-4.7 μM for TNBC cells versus 15-39 μM for noncancerous cells) toward the noncancerous breast cells compared to the free doxorubicin (IC<sub>50</sub> 0.35-1.5 μM for TNBC cells versus 0.24 μM for noncancerous cells). The results from the comparative study of the two PDCs suggest that both may have translational potential for TNBC treatment.","dates":{"release":"2019-01-01T00:00:00Z","publication":"2019 Dec","modification":"2025-04-21T18:52:36.903Z","creation":"2025-04-05T17:25:28.729Z"},"accession":"S-EPMC7965737","cross_references":{"pubmed":["31715102"],"doi":["10.1021/acs.bioconjchem.9b00755"]}}