Results 241 to 250 of about 15,170 (273)
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ChemMedChem, 2019
AbstractWe describe the characterization of antigen binding fragments (Fab)–drug conjugates prepared using a dual maleimide pyrrolobenzodiazepine dimer cytotoxic payload (SG3710). Pyrrolobenzodiazepine dimers, which are DNA cross‐linkers, are a class of payloads used in antibody–drug conjugates (ADCs).
Nazzareno Dimasi, Changshou Gao
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AbstractWe describe the characterization of antigen binding fragments (Fab)–drug conjugates prepared using a dual maleimide pyrrolobenzodiazepine dimer cytotoxic payload (SG3710). Pyrrolobenzodiazepine dimers, which are DNA cross‐linkers, are a class of payloads used in antibody–drug conjugates (ADCs).
Nazzareno Dimasi, Changshou Gao
exaly +3 more sources
Journal of the American Chemical Society
Antibody-drug conjugates (ADCs) for the treatment of cancer aim to achieve selective delivery of a cytotoxic payload to tumor cells while sparing normal tissue. In vivo, multiple tumor-dependent and -independent processes act on ADCs and their released payloads to impact tumor-versus-normal delivery, often resulting in a poor therapeutic window. An ADC
Jack Sadowsky +2 more
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Antibody-drug conjugates (ADCs) for the treatment of cancer aim to achieve selective delivery of a cytotoxic payload to tumor cells while sparing normal tissue. In vivo, multiple tumor-dependent and -independent processes act on ADCs and their released payloads to impact tumor-versus-normal delivery, often resulting in a poor therapeutic window. An ADC
Jack Sadowsky +2 more
exaly +3 more sources
Traditional Cytotoxic Agents as Antibody–Drug Conjugate (ADC) Payloads [PDF]
, 2019 In the second half of the last century, when the antibody–drug conjugate (ADC) approach was still in its infancy, the choice of potential payloads was based on a small group of cytotoxic molecules already exploited clinically as cancer chemotherapeutic agents.
Ilona Pysz +2 more
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FDA approves ADC Therapeutics’ loncastuximab tesirine, ushering in a new cytotoxic payload
Nature Reviews Drug Discovery, 2021Mullard Asher
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Identification and Optimization of EphA2-Selective Bicycles for the Delivery of Cytotoxic Payloads
Journal of Medicinal Chemistry, 2020Bicycles 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
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Enhanced cytotoxicity of a polymer–drug conjugate with triple payload of paclitaxel
Bioorganic & Medicinal Chemistry, 2009The 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
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Antibody−Drug Conjugates: Linking Cytotoxic Payloads to Monoclonal Antibodies
Bioconjugate Chemistry, 2009Antibody-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
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Antibody drug conjugates beyond cytotoxic payloads
2023For many years, antibody drug conjugates (ADC) have teased with the promise of targeted payload delivery to diseased cells, embracing the targeting of the antibody to which a cytotoxic payload is conjugated. During the past decade this promise has started to be realised with the approval of more than a dozen ADCs for the treatment of various cancers ...
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Natural Products as Exquisitely Potent Cytotoxic Payloads for Antibody- Drug Conjugates
Current Topics in Medicinal Chemistry, 2015Antibody-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
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Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads
Bioorganic & Medicinal Chemistry Letters, 2016Trastuzumab 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
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