ArticleScientific reports2016
pH-Selective Cytotoxicity of pHLIP-Antimicrobial Peptide Conjugates.
Article in Scientific reports, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers.
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Who cites it
30 citing papers in PubMed.
- Nano-Engineered Delivery of the Pro-Apoptotic KLA Peptide: Strategies, Synergies, and Future Directions.Biomolecules · 2026Review
- Review
- Cationic antimicrobial peptides: potential templates for anticancer agents.Frontiers in medicine · 2025Review
- The solid tumor microenvironment and related targeting strategies: a concise review.Frontiers in immunology · 2025Review
- Selective Recruitment of Antibodies to Cancer Cells and Immune Cell-mediated Killing via In Situ Click Chemistry.ChemMedChem · 2024Article
- Combination of STING agonist with anti-vascular RGD-(KLAKLAK)Cancer immunology, immunotherapy : CII · 2024Article
- Targeted acidosis mediated delivery of antigenic MHC-binding peptides.Frontiers in immunology · 2024Article
- Aiming the magic bullet: targeted delivery of imaging and therapeutic agents to solid tumors by pHLIP peptides.Frontiers in pharmacology · 2024Review
- Promoting the activity of a receptor tyrosine phosphatase with a novel pH-responsive transmembrane agonist inhibits cancer-associated phenotypes.Protein science : a publication of the Protein Society · 2023Article
- Selective Display of a Chemoattractant Agonist on Cancer Cells Activates the Formyl Peptide Receptor 1 on Immune Cells.Chembiochem : a European journal of chemical biology · 2022Article
- Eradication of tumors and development of anti-cancer immunity using STINGa targeted by pHLIP.Frontiers in oncology · 2022Article
- PET Imaging of Acidic Tumor Environment WithFrontiers in oncology · 2022Article
- Bioactive cationic peptides as potential agents for breast cancer treatment.Bioscience reports · 2021Article
- Therapeutic targeting of the hypoxic tumour microenvironment.Nature reviews. Clinical oncology · 2021Review
- An Experimental Study on [Molecular imaging · 2021Article
- Ku80-Targeted pH-Sensitive Peptide-PNA Conjugates Are Tumor Selective and Sensitize Cancer Cells to Ionizing Radiation.Molecular cancer research : MCR · 2020Article
- pH-Dependent Grafting of Cancer Cells with Antigenic Epitopes Promotes Selective Antibody-Mediated Cytotoxicity.Journal of medicinal chemistry · 2020Article
- pHLIP(Var7)-P1AP suppresses tumor cell proliferation in MDA-MB-231 triple-negative breast cancer by targeting protease activated receptor 1.Breast cancer research and treatment · 2020Article
- Tumor-Targeted, Cytoplasmic Delivery of Large, Polar Molecules Using a pH-Low Insertion Peptide.Molecular pharmaceutics · 2020Article
- Co-delivery of D-(KLAKLAK)Pharmaceutics · 2019Article
Corrections and comments
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Authors and funding
3 authors.
Funding
Abstract
Positively charged antimicrobial peptides have become promising agents for the treatment of cancer by inducing apoptosis though their preferential binding and disruption of negatively charged membranes, such as the mitochondrial membrane. (KLAKLAK)2 is such a peptide but due to its polarity, it cannot cross the cellular membrane and therefore relies on the use of a delivery agent. For targeted delivery, previous studies have relied on cell penetrating peptides, nanoparticles or specific biomarkers. Herein, we investigated the first use of pHLIP to selectively target and directly translocate (KLAKLAK)2 into the cytoplasm of breast cancer cells, based on the acidic tumor micro-environment. With the goal of identifying a lead conjugate with optimized selective cytotoxicity towards cancer cells, we analyzed a family of (KLAKLAK)2 analogs with varying size, polarity and charge. We present a highly efficacious pHLIP conjugate that selectively induces concentration- and pH-dependent toxicity in breast cancer cells.
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