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Photothermally Triggered Copper Payload Release for Cuproptosis-Promoted Cancer Synergistic Therapy.

Angewandte Chemie, 2022
Cuproptosis is a new form of programmed cell death and exhibits enormous potential in cancer treatment. However, reducing the undesirable Cu ion release in normal tissue and maximizing the Cu-induced therapeutic effect in cancer sites are two main ...
Jie Zhou   +7 more
semanticscholar   +1 more source

Novel formats of antibody conjugates: recent advances in payload diversity, conjugation, and linker chemistry

Expert Opinion on Biological Therapy, 2023
Introduction In the field of bioconjugates, the focus on antibody – drug conjugates (ADCs) with novel payloads beyond the traditional categories of potent cytotoxic agents is increasing.
Tomohiro Fujii, Yutaka Matsuda
semanticscholar   +1 more source

Use of Payload Binding Selectivity Enhancers to Improve Therapeutic Index of Maytansinoid-Antibody-Drug Conjugates.

Molecular Cancer Therapeutics, 2023
Systemic exposure to released cytotoxic payload contributes to the dose-limiting off-target toxicities of anti-cancer antibody-drug conjugates (ADC).
T. D. Nguyen   +2 more
semanticscholar   +1 more source

Antibody−Drug Conjugates: Linking Cytotoxic Payloads to Monoclonal Antibodies

Bioconjugate Chemistry, 2009
Antibody-drug conjugates (ADCs) combine the specificity of monoclonal antibodies (mAbs) with the potency of cytotoxic molecules, thereby taking advantage of the best characteristics of both components. Along with the development of the mAbs and cytotoxins, the design of chemical linkers to covalently bind these building blocks is making rapid progress ...
Laurent, Ducry, Bernhard, Stump
openaire   +2 more sources

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties.

Journal of Medicinal Chemistry, 2021
The biological and medicinal impacts of proteolysis-targeting chimeras (PROTACs) and related chimeric molecules that effect intracellular degradation of target proteins via ubiquitin ligase-mediated ubiquitination continue to grow.
P. Dragovich   +36 more
semanticscholar   +1 more source

Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

Bioorganic & Medicinal Chemistry Letters, 2016
Trastuzumab conjugates consisting of exatecan derivatives were prepared and their biological activities and physicochemical properties were evaluated. The ADCs showed strong efficacy and a low aggregation rate. The exatecan derivatives were covalently connected via a peptidyl spacer (Gly-Gly-Phe-Gly), which is assumed to be stable in circulation, and ...
Takashi, Nakada   +11 more
openaire   +2 more sources

Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads

Journal of Medicinal Chemistry, 2020
Bicycles are constrained bicyclic peptides that represent a promising binding modality for use in targeted drug conjugates. A phage display screen against EphA2, a receptor tyrosine kinase highly expressed in a number of solid tumors, identified a number of Bicycle families with low nanomolar affinity.
Gemma E. Mudd   +9 more
openaire   +2 more sources

Natural Products as Exquisitely Potent Cytotoxic Payloads for Antibody- Drug Conjugates

Current Topics in Medicinal Chemistry, 2015
Antibody-drug conjugates (ADCs) are an emerging area of study within medicinal chemistry and are thought of as sophisticated drug delivery systems due to their specificity to a disease-targeted antigen. ADCs have been actively utilized as therapeutics for hematological and solid tumor cancers due to their capability to deliver a cytotoxic compound to a
Samantha M, Gromek, Marcy J, Balunas
openaire   +2 more sources

Enhanced cytotoxicity of a polymer–drug conjugate with triple payload of paclitaxel

Bioorganic & Medicinal Chemistry, 2009
The development of targeting approaches to selectively release chemotherapeutic drugs into malignant tissue is a major challenge in anticancer therapy. We have synthesized an N-(2-hydroxypropyl)-methacrylamide (HPMA) copolymer-drug conjugate with an AB(3) self-immolative dendritic linker.
Rotem, Erez   +4 more
openaire   +2 more sources

Double-Chambered Ferritin Platform: Dual-Function Payloads of Cytotoxic Peptides and Fluorescent Protein

Biomacromolecules, 2015
Ferritin cage nanoparticles are promising platforms for targeted delivery of imaging and therapeutic agents. One of the main advantages of cage nanoparticles is the ability to display multiple functionalities through genetic modification so as to achieve desired therapeutic or diagnostic functions.
Soyoun, Kim   +7 more
openaire   +2 more sources

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