Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.

Cationic anticancer peptides (CAPs) refer to peptide-based molecules possessing a net positive charge, allowing them to preferentially combined with cancer cells which exhibit an overabundance of anionic components on their surface. Cationic peptides additionally induce cell membrane destabilization through carpet-like, toroidal pore or sinking raft et al. mechanism, or penetrate cell membrane and act on cellular sub-structures. Besides, cell-penetrating peptides (CPPs) represent a special subset of CAPs, renowned for their rapid and low-toxic cellular translocation abilities, making them promising vehicles for drug delivery. Therefore, CAPs are emerging as a class of potential anticancer agents and gaining widespread attention by researchers. As reported, the construction of bioactive peptides with cytotoxic payloads via a chemical linker provides a kind of prodrugs known as peptide-drug conjugates (PDCs), which represents an efficient approach to address the limitations of small molecules by leveraging the properties of peptides. In previous study, we have discovered the CAP of KM8-Aib (sequence: Lys-Leu-Leu-Lys-Lys-Asn-Leu-Lys-Aib-Leu-Ala-Ala-Leu-Ala-Lys-Lys-Ile-Leu-NH2), which derived from venom peptide Mastoparan, exhibiting favorable antiproliferative effect against several cancer cells but less toxic to benign cells. Herein, we attempted to integrate CPT with KM8-Aib, obtaining a series of peptide-CPT conjugates, to improve the solubility, selectivity of CPT, and achieve enhanced therapeutic outcomes. Based on preliminary in vitro assays, the PDC Kb-CC07 demonstrated exceptional selective cytotoxicity against various cancer cell lines, including drug-resistant variants, surpassing that of other conjugates. The solubility of Kb-CC07 was also significantly increased, which is ˜ 100 fold higher than that of CPT. In addition, we evaluated the in vivo antitumor efficacy of Kb-CC07 via nude-xenograft model. It is showed that mice treated with Kb-CC07 had substantially lower tumor volumes and minimum organ toxicities than CPT-treated group. As such, Kb-CC07 is suggested to be a promising anticancer agent and warrant thorough exploration.