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The Use of α-fetoprotein for the Delivery of Cytotoxic Payloads to Cancer Cells
Therapeutic Delivery, 2014One approach to improving the activity of anticancer drugs is to bind them to the human α-fetoprotein (HAFP) that recognizes the tumor-associated cell-surface HAFP receptor. A drug can be bound to the HAFP by covalent conjugation or within a non-covalent complex.
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Cancer Research, 2021
Abstract BT5528 was developed as a Bicycle® toxin conjugate to deliver monomethyl auristatin E (MMAE) -payload to EphA2 overexpressing tumors. It consists of a bicyclic peptide targeting the tumor antigen EphA2, linked to the cytotoxin MMAE via a molecular spacer and cleavable linker.
Johanna Lahdenranta +6 more
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Abstract BT5528 was developed as a Bicycle® toxin conjugate to deliver monomethyl auristatin E (MMAE) -payload to EphA2 overexpressing tumors. It consists of a bicyclic peptide targeting the tumor antigen EphA2, linked to the cytotoxin MMAE via a molecular spacer and cleavable linker.
Johanna Lahdenranta +6 more
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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
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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
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Factors Involved in the Design of Cytotoxic Payloads for Antibody–Drug Conjugates
2012Selective targeting of cancer can be accomplished by the use of monoclonal antibodies (mAbs) that bind to tumor-associated antigens expressed preferentially on the surface of cancer cells. Several of these non-derivatized antibodies, or naked antibodies, have been approved for the treatment of various cancer types.
Wayne C. Widdison, Ravi V. J. Chari
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Immune Reprogramming of Tumor Microenvironments by Cytotoxic Antibody–Drug Conjugate Payloads
Molecular Cancer TherapeuticsAbstract Antibody–drug conjugates (ADC) have recently emerged as an effective treatment option for cancer. Although the fundamental mechanisms of direct tumor cell killing by various ADC payloads have been established, their impact on the tumor microenvironment (TME) remains underexplored.
Srishti Chakravorty +10 more
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Cytotoxic Payloads for Antibody – Drug Conjugates
2019Antibody–drug conjugates (ADCs) represent one of the most promising and exciting areas of anticancer drug discovery. Five ADCs are now approved in the US and EU [i.e., ado-trastuzumab emtansine (Kadcyla™), brentuximab vedotin (Adcetris™), inotuzumab ozogamicin (Besponsa™), gemtuzumab ozogamicin (Mylotarg™) and moxetumomab pasudotox-tdfk (Lumoxiti ...
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RSC Medicinal Chemistry
HER2-targeted immunoliposomes with gold payloads exhibit greater accumulation than non-targeted liposomes and free gold compounds and localize in the mitochondria and endoplasmic reticulum leading to cell death at lower nanomolar drug concentrations.
Afruja Ahad +4 more
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HER2-targeted immunoliposomes with gold payloads exhibit greater accumulation than non-targeted liposomes and free gold compounds and localize in the mitochondria and endoplasmic reticulum leading to cell death at lower nanomolar drug concentrations.
Afruja Ahad +4 more
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Regulatory Toxicology and Pharmacology
The use of non-human primates (NHP) for the nonclinical development of biologics can be necessary to assess the potential safety risks in humans. An IQ DruSafe and 3Rs TPS Working Group (WG) conducted a survey on the use of NHP in toxicology studies used to develop antibody drug conjugates (ADCs) with cytotoxic payloads for oncology treatment.
Sherry L. Ralston +9 more
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The use of non-human primates (NHP) for the nonclinical development of biologics can be necessary to assess the potential safety risks in humans. An IQ DruSafe and 3Rs TPS Working Group (WG) conducted a survey on the use of NHP in toxicology studies used to develop antibody drug conjugates (ADCs) with cytotoxic payloads for oncology treatment.
Sherry L. Ralston +9 more
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Journal of Chromatography A, 2016
UV spectrophotometry is widely used to determine the molar extinction coefficients (MECs) of cytotoxic drugs as well as the drug antibody ratios (DARs) of antibody drug conjugates (ADCs). However, the unknown purity of a drug due to interfering impurities can lead to erroneous MECs and DARs.
Chunlei, Wang +5 more
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UV spectrophotometry is widely used to determine the molar extinction coefficients (MECs) of cytotoxic drugs as well as the drug antibody ratios (DARs) of antibody drug conjugates (ADCs). However, the unknown purity of a drug due to interfering impurities can lead to erroneous MECs and DARs.
Chunlei, Wang +5 more
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Cancer Research
Abstract Prostate-specific membrane antigen (PSMA), a type II transmembrane glycoprotein belonging to the folate receptor family, is highly expressed in metastatic castration-resistant prostate cancer (mCRPC), and increases following androgen deprivation therapy (ADT).
Daniela Impellizzieri +13 more
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Abstract Prostate-specific membrane antigen (PSMA), a type II transmembrane glycoprotein belonging to the folate receptor family, is highly expressed in metastatic castration-resistant prostate cancer (mCRPC), and increases following androgen deprivation therapy (ADT).
Daniela Impellizzieri +13 more
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