ArticleJournal of molecular biology2019
Overcoming Drug Resistance through the Development of Selective Inhibitors of UDP-Glucuronosyltransferase Enzymes.
Article in Journal of molecular biology, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 26 citations in OpenAlex.
- Trial
- The Dual Role of Human UDP-Glucuronosyltransferase-Mediated Metabolism in Tumor Drug Resistance: Mechanisms and Prospects.International journal of molecular sciences · 2026Review
- Innovative strategies to overcome cancer drug resistance: from nanodelivery systems to targeted therapeutics.Discover oncology · 2026Review
- eIF4E and Ezrin cooperate in pseudopods to drive a localized migratory translation program in acute myeloid leukemia.bioRxiv : the preprint server for biology · 2026Article
- Multipurpose RNA maturation factors dysregulate multiple mRNA processing steps simultaneously and provide new therapeutic opportunities.RNA biology · 2025Review
- Inhibition of ABCG2 by SCO-101 Enhances Chemotherapy Efficacy in Cancer.International journal of molecular sciences · 2025Article
- Insight into the structure, oligomerization, and the role in drug resistance of human UDP-glucuronosyltransferases.Archives of toxicology · 2025Review
- Interactive effects of morphine and the HIV integrase inhibitor, cabotegravir, in male and female mice.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2025Article
- Medicinal Chemistry and NMR Driven Discovery of Novel UDP-glucuronosyltransferase 1A Inhibitors That Overcome Therapeutic Resistance in Cells.Journal of molecular biology · 2024Article
- A novel approach to overcome drug resistance in acute myeloid leukemia.Haematologica · 2023Article
- Review
- Cellular resistance mechanisms in cancer and the new approaches to overcome resistance mechanisms chemotherapy.Saudi medical journal · 2023Article
- Unravelling the clinicopathological and functional significance of replication protein A (RPA) heterotrimeric complex in breast cancers.NPJ breast cancer · 2023Article
- The NSAID glafenine rescues class 2 CFTR mutants via cyclooxygenase 2 inhibition of the arachidonic acid pathway.Scientific reports · 2022Article
- Untangling the clinicopathological significance of MRE11-RAD50-NBS1 complex in sporadic breast cancers.NPJ breast cancer · 2021Article
- Article
- Targeting Drug Chemo-Resistance in Cancer Using Natural Products.Biomedicines · 2021Review
- UGT1A Gene Family Members Serve as Potential Targets and Prognostic Biomarkers for Pancreatic Cancer.BioMed research international · 2021Article
- Metabolic Reprogramming of Chemoresistant Cancer Cells and the Potential Significance of Metabolic Regulation in the Reversal of Cancer Chemoresistance.Metabolites · 2020Review
- Mechanisms of Multidrug Resistance in Cancer Chemotherapy.International journal of molecular sciences · 2020Review
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
Abstract
Drug resistance is a major cause of cancer-related mortality. Glucuronidation of drugs via elevation of UDP-glucuronosyltransferases (UGT1As) correlates with clinical resistance. The nine UGT1A family members have broad substrate specificities attributed to their variable N-terminal domains and share a common C-terminal domain. Development of UGT1As as pharmacological targets has been hampered by toxicity of pan-UGT inhibitors and by difficulty in isolating pure N-terminal domains or full-length proteins. Here, we developed a strategy to target selected UGT1As which exploited the biochemical tractability of the C-domain and its ability to allosterically communicate with the catalytic site. By combining NMR fragment screening with in vitro glucuronidation assays, we identified inhibitors selective for UGT1A4. Significantly, these compounds selectively restored sensitivity in resistant cancer cells only for substrates of the targeted UGT1A. This strategy represents a crucial first step toward developing compounds to overcome unwanted glucuronidation thereby reversing resistance in patients.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.