Targeting Ultrasmall Gold Nanoparticles with cRGD Peptide Increases the Uptake and Efficacy of Cytotoxic Payload [PDF]
Nanomaterials, 2022 Cyclic arginyl-glycyl-aspartic acid peptide (cRGD) peptides show a high affinity towards αVβ3 integrin, a receptor overexpressed in many cancers. We aimed to combine the versatility of ultrasmall gold nanoparticles (usGNP) with the target selectivity of ...
Enrico Ferrari +2 more
exaly +9 more sources
Facile protein conjugation of platinum for light-activated cytotoxic payload release
Chemical Communications, 2021 This platinum anticancer complex can be conjugated to proteins, including antibodies, under mild conditions and activated by visible light, providing a basis for highly selective cancer phototherapy.
Frederik Lermyte +2 more
exaly +6 more sources
Adnectin–drug conjugates for Glypican-3-specific delivery of a cytotoxic payload to tumors [PDF]
Protein Engineering, Design and Selection, 2018 Tumor-specific delivery of cytotoxic agents remains a challenge in cancer therapy. Antibody-drug conjugates (ADC) deliver their payloads to tumor cells that overexpress specific tumor-associated antigens-but the multi-day half-life of ADC leads to high exposure even of normal, antigen-free, tissues and thus contributes to dose-limiting toxicity.
Dasa Lipovsek, Sanjeev Gangwar
exaly +5 more sources
Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells [PDF]
Frontiers in Pharmacology, 2019 Antibody-drug conjugates (ADCs) are composed of an antibody linked to cytotoxic anticancer payloads. ADCs recognize tumor-specific cell surface antigens and are internalized into lysosomes where proteolytic enzymes release the cytotoxic payloads.
Yurong Lai +2 more
exaly +5 more sources
Current Cancer Therapy Reviews, 2016 Over the last decade, Antibody Drug Conjugates (ADCs) have gained a great success due to their documented clinical efficacy and manageable toxicity. Generally the word "drug" is associated with a che-motherapeutic drug, however "drug" can also be associated with other cy-totoxic payloads such as radionuclides, termed more specifically, Anti-body ...
Caroline Rousseau +2 more
exaly +5 more sources
Site-Specific Glycan Conjugation Improves Stability and Efficacy of an Antibody–Drug Conjugates Bearing DXd as a Cytotoxic Payload [PDF]
ACS OmegaThis study developed a homogeneous ADC via site-specific conjugation of a potent antitumor agent, a camptothecin derivative, to the N-glycan in the Fc domain of an antibody, achieving a drug-to-antibody ratio (DAR) of 4. The resulting glycan-conjugated ADC exhibited improved thermal stability, reduced aggregation, and reduced premature payload release ...
Shino Manabe +10 more
exaly +4 more sources
A Novel Dual-Payload ADC for the Treatment of HER2+ Breast and Colon Cancer
Pharmaceutics, 2023 Antibody-drug conjugates (ADCs) have demonstrated a great therapeutic potential against cancer due to their target specificity and cytotoxicity. To exert a maximum therapeutic effect on cancerous cells, we have conjugated two different payloads to ...
Veysel Kayser, Candice Maria McKertish
exaly +4 more sources
From Unmet Medical Need to Drug Candidate: A Translational Therapeutic Development Roadmap Illustrated by Dual-Payload Antibody–Drug Conjugates [PDF]
BiomoleculesTransformative therapeutic innovation should not begin with a molecule—or even a molecular target. It should begin with a clearly defined unmet clinical need. Here, we present a seven-step Translational Therapeutic Development Roadmap that systematically
Takeshi Honda, Gui-Dong Zhu
doaj +2 more sources
DNA-programmed bispecific peptide assemblies for delivering cytotoxic payload to cells expressing EGFR and MET receptors [PDF]
RSC Chemical BiologyBispecific agents capable of simultaneously targeting two distinct cell surface receptors promise enhanced specificity and efficacy in cancer therapy. Here, we report a strategy for the rapid optimization of compact bispecific agents using nucleic acid hybridization to display peptide ligands for both the Epidermal Growth Factor Receptor (EGFR) and the
Pritam Ghosh, Huyen Dinh, Oliver Seitz
openaire +4 more sources
Clinical Pharmacology and Translational Science Considerations in the Development of Dual‐Payload Antibody Drug Conjugates [PDF]
Clinical and Translational ScienceAntibody‐drug conjugates (ADCs) have evolved in the last decade or two from carrying a single chemotherapy payload to carrying highly potent tubulin inhibitors and DNA damaging agents.
Paulien Ravenstijn +5 more
doaj +2 more sources