ArticlePharmaceuticals (Basel, Switzerland)2021
Inhibition of XPO-1 Mediated Nuclear Export through the Michael-Acceptor Character of Chalcones.
Article in Pharmaceuticals (Basel, Switzerland), 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 9 papers.
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Who cites it
9 citing papers in PubMed, 16 citations in OpenAlex.
- Design and mechanistic evaluation of chalcone-quinoline-triazole hybrids as antifungal CYP51 inhibitors.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026Article
- Gluing the allosteric way.Nature chemical biology · 2025Article
- KPT-330, A New Candidate Drug for Targeting NOTCH1 Overexpression in T-cell Acute Lymphoblastic Leukemia, An In Vitro and Silico Study.Cell biochemistry and biophysics · 2025Article
- Targeting deubiquitinase USP7-mediated stabilization of XPO1 contributes to the anti-myeloma effects of selinexor.Journal of translational medicine · 2025Article
- Medicinally Privileged Natural Chalcones: Abundance, Mechanisms of Action, and Clinical Trials.International journal of molecular sciences · 2024Review
- Azacitidine Is Synergistically Lethal with XPO1 Inhibitor Selinexor in Acute Myeloid Leukemia by Targeting XPO1/eIF4E/c-MYC Signaling.International journal of molecular sciences · 2023Article
- Chalcone: A Promising Bioactive Scaffold in Medicinal Chemistry.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Identification of Novel Covalent XPO1 Inhibitors Based on a Hybrid Virtual Screening Strategy.Molecules (Basel, Switzerland) · 2022Article
- Special Issue "Anticancer Drugs 2021".Pharmaceuticals (Basel, Switzerland) · 2022Article
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7 authors at 2 institutions in 2 countries.
Funding
Abstract
The nuclear export receptor exportin-1 (XPO1, CRM1) mediates the nuclear export of proteins that contain a leucine-rich nuclear export signal (NES) towards the cytoplasm. XPO1 is considered a relevant target in different human diseases, particularly in hematological malignancies, tumor resistance, inflammation, neurodegeneration and viral infections. Thus, its pharmacological inhibition is of significant therapeutic interest. The best inhibitors described so far (leptomycin B and SINE compounds) interact with XPO1 through a covalent interaction with Cys528 located in the NES-binding cleft of XPO1. Based on the well-established feature of chalcone derivatives to react with thiol groups via hetero-Michael addition reactions, we have synthesized two series of chalcones. Their capacity to react with thiol groups was tested by incubation with GSH to afford the hetero-Michael adducts that evolved backwards to the initial chalcone through a retro-Michael reaction, supporting that the covalent interaction with thiols could be reversible. The chalcone derivatives were evaluated in antiproliferative assays against a panel of cancer cell lines and as XPO1 inhibitors, and a good correlation was observed with the results obtained in both assays. Moreover, no inhibition of the cargo export was observed when the two prototype chalcones
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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 Socratic graph.