ArticleScientific reports2017
New insight on the structural features of the cytotoxic auristatins MMAE and MMAF revealed by combined NMR spectroscopy and quantum chemical modelling.
Article in Scientific reports, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed.
- Overcoming resistance to antibody-drug conjugates: from mechanistic insights to cutting-edge strategies.Journal of hematology & oncology · 2025Review
- In silico decrypting of the bystander effect in antibody-drug conjugates for breast cancer therapy.Scientific reports · 2025Article
- Molecular characterization of the CXCR4 / CXCR7 axis in germ cell tumors and its targetability using nanobody-drug-conjugates.Experimental hematology & oncology · 2023Article
- More than just an eagle killer: The freshwater cyanobacteriumProceedings of the National Academy of Sciences of the United States of America · 2023Article
- Targeting CLDN6 in germ cell tumors by an antibody-drug-conjugate and studying therapy resistance of yolk-sac tumors to identify and screen specific therapeutic options.Molecular medicine (Cambridge, Mass.) · 2023Article
- Review
- Article
- Conditional activation of an anti-IgM antibody-drug conjugate for precise B cell lymphoma targeting.Frontiers in immunology · 2023Article
- Antibody-drug conjugates for lymphoma patients: preclinical and clinical evidences.Exploration of targeted anti-tumor therapy · 2022Review
- Discovery of Dolastatinol: A Synthetic Analog of Dolastatin 10 and Low Nanomolar Inhibitor of Tubulin Polymerization.ACS medicinal chemistry letters · 2021Article
- Halogenation at the Phenylalanine Residue of Monomethyl Auristatin F Leads to a FavorableMolecular pharmaceutics · 2021Article
- Development of Marine-Derived Compounds for Cancer Therapy.Marine drugs · 2021Review
- Bioactive Compounds from Marine Heterobranchs.Marine drugs · 2020Review
- Site-Specific, Stoichiometric-Controlled, PEGylated Conjugates of Fibroblast Growth Factor 2 (FGF2) with Hydrophilic Auristatin Y for Highly Selective Killing of Cancer Cells Overproducing Fibroblast Growth Factor Receptor 1 (FGFR1).Molecular pharmaceutics · 2020Article
- Antibody-Drug Conjugate Using Ionized Cys-Linker-MMAE as the Potent Payload Shows Optimal Therapeutic Safety.Cancers · 2020Article
- Increasing the Potential of the Auristatin Cancer-Drug Family by Shifting the Conformational Equilibrium.Molecular pharmaceutics · 2019Article
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Authors and funding
3 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Antibody-drug conjugates (ADCs) are emerging as a promising class of selective drug delivery systems in the battle against cancer and other diseases. The auristatins monomethyl auristatin E (MMAE) and monomethyl auristatin F (MMAF) appear as the cytotoxic drug in almost half of the state-of-the-art ADCs on the market or in late stage clinical trials. Here, we present the first complete NMR spectroscopic characterisation of these challenging molecules, and investigate their structural properties by a combined NMR and quantum chemical modelling approach. We find that in solution, half of the drug molecules are locked in an inactive conformation, severely decreasing their efficiency, and potentially increasing the risk of side-effects. Furthermore, we identify sites susceptible to future modification, in order to potentially improve the performance of these drugs.
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