Targeting Ultrasmall Gold Nanoparticles with cRGD Peptide Increases the Uptake and Efficacy of Cytotoxic Payload [PDF]
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 +18 more sources
Lysosomal P-gp-MDR1 Confers Drug Resistance of Brentuximab Vedotin and Its Cytotoxic Payload Monomethyl Auristatin E in Tumor Cells [PDF]
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 +7 more sources
Facile protein conjugation of platinum for light-activated cytotoxic payload release
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 +5 more sources
Adnectin–drug conjugates for Glypican-3-specific delivery of a cytotoxic payload to tumors [PDF]
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
Payload diversification: a key step in the development of antibody–drug conjugates [PDF]
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that currently combines the selectivity of monoclonal antibodies with the potency of a payload consisting of cytotoxic agents. For many years microtubule targeting and DNA-
Warren Viricel +2 more
exaly +3 more sources
Monomethyl Auristatin E, a Potent Cytotoxic Payload for Development of Antibody-Drug Conjugates against Breast Cancer [PDF]
Background: Breast cancer is a heterogeneous disease characterized by differential responses to targeted and chemotherapeutic agents. Antibody-drug conjugates are one of the promising strategies for the treatment of breast cancer. Monomethyl auristatin E
Meghdad Abdollahpour-alitappeh +9 more
doaj +4 more sources
DNA-programmed bispecific peptide assemblies for delivering cytotoxic payload to cells expressing EGFR and MET receptors. [PDF]
Bispecific 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
Ghosh P, Dinh H, Seitz O.
europepmc +4 more sources
Antibody-drug conjugates in breast cancer: Progress and future directions [PDF]
Summary: Antibody-drug conjugates (ADCs) have transformed the treatment landscape of breast cancer, enabling targeted delivery of potent cytotoxic payloads to antigen-expressing tumor cells.
Alexandra Bili Newman +2 more
doaj +2 more sources
Antibody–Drug Conjugates (ADCs): A Review of Structural Design, Technological Evolution, and Future Perspectives [PDF]
Antibody–drug conjugates (ADCs) have become an important class of targeted anticancer therapeutics by integrating the tumor selectivity of monoclonal antibodies with the potent cytotoxicity of small-molecule payloads through rational linker design.
Guiying Wu +5 more
doaj +2 more sources
Site-Specific Glycan Conjugation Improves Stability and Efficacy of an Antibody-Drug Conjugates Bearing DXd as a Cytotoxic Payload. [PDF]
This 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 ...
Manabe S +10 more
europepmc +3 more sources

