ArticleHaematologica2024
A first-in-class Wiskott-Aldrich syndrome protein activator with antitumor activity in hematologic cancers.
Article in Haematologica, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
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Who cites it
4 citing papers in PubMed.
- N-WASP is downregulated in patients with acute myeloid leukemia (AML) and is associated with poor prognosis.Scientific reports · 2026Article
- HIV Nef amplifies mechanical heterogeneity to promote immune evasion.bioRxiv : the preprint server for biology · 2025Article
- Multifaceted role of the actin-binding protein WIP: Promotor and inhibitor of tumor progression and dissemination.Cytoskeleton (Hoboken, N.J.) · 2025Review
- New insights into Wiskott-Aldrich syndrome: ten novelFrontiers in immunology · 2025Article
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Authors and funding
43 authors.
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Abstract
Hematologic cancers are among the most common cancers in adults and children. Despite significant improvements in therapies, many patients still succumb to the disease. Therefore, novel therapies are needed. The Wiskott-Aldrich syndrome protein (WASp) family regulates actin assembly in conjunction with the Arp2/3 complex, a ubiquitous nucleation factor. WASp is expressed exclusively in hematopoietic cells and exists in two allosteric conformations: autoinhibited or activated. Here, we describe the development of EG-011, a first-in-class small molecule activator of the autoinhibited form of WASp. EG-011 possesses in vitro and in vivo antitumor activity as a single agent in lymphoma, leukemia, and multiple myeloma, including models of secondary resistance to PI3K, BTK, and proteasome inhibitors. The in vitro activity was confirmed in a lymphoma xenograft. Actin polymerization and WASp binding were demonstrated using multiple techniques. Transcriptome analysis highlighted homology with drugs inducing actin polymerization.
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