ArticleMolecular cancer therapeutics2019
EC359: A First-in-Class Small-Molecule Inhibitor for Targeting Oncogenic LIFR Signaling in Triple-Negative Breast Cancer.
Article in Molecular cancer therapeutics, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 54 papers.
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54 citing papers in PubMed, 72 citations in OpenAlex.
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- A humanized LIF-targeting antibody synergistically enhances chemo- and immunotherapy in pancreatic cancer.Journal of translational medicine · 2026Article
- Structural Model of the Oncostatin M (OSM)-OSMRβ-gp130 Ternary Complex Reveals Pathways of Allosteric Communication in OSM Signaling.Current medicinal chemistry · 2026Article
- Cryo-EM structures reveal the molecular mechanism of SUMO E1-E2 thioester transfer.Nature structural & molecular biology · 2025Article
- Stromal transcriptomics uncover LIF as a key effector in high tumor budding triple-negative breast cancer.Scientific reports · 2025Article
- Harnessing the Estradienone Scaffold to Develop Dual GPBAR1 and LIFR Modulators for Liver Fibrosis.Journal of medicinal chemistry · 2025Article
- EC359 Enhances Trametinib Efficacy inBiomolecules · 2025Article
- The Discovery and Characterization of HBS-101, a Novel Inhibitor of Midkine, as a Therapeutic Agent for the Treatment of Triple-Negative Breast Cancer.Molecular cancer therapeutics · 2025Article
- Targeting cancer-associated fibroblast-driven LIF/LIFR axis improves the therapeutic efficacy of gemcitabine and nab-paclitaxel in pancreatic cancer.NPJ precision oncology · 2025Article
- Fe-doped MOF nanoparticles: the LIFR and BMP4 dual-signaling pathways activated regulator for in vitro expansion of mouse embryonic stem cells.Materials today. Bio · 2025Article
- Exploring Boswellia serrata Triterpenes: A New Frontier in Leukemia Inhibitory Factor Receptor Modulation.ACS omega · 2025Article
- Blocking LIF and PD-L1 enhances the antitumor efficacy of SBRT in murine PDAC models.Journal for immunotherapy of cancer · 2025Article
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- Significance of LIF/LIFR Signaling in the Progression of Obesity-Driven Triple-Negative Breast Cancer.Cancers · 2024Article
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- Pharmacological inhibition of the LIF/LIFR autocrine loop reveals vulnerability of ovarian cancer cells to ferroptosis.NPJ precision oncology · 2024Article
- Emerging Therapies for Glioblastoma.Cancers · 2024Review
- The leukemia inhibitory factor regulates fibroblast growth factor receptor 4 transcription in gastric cancer.Cellular oncology (Dordrecht, Netherlands) · 2024Article
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26 authors at 7 institutions in 4 countries.
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Abstract
Leukemia inhibitory factor receptor (LIFR) and its ligand LIF play a critical role in cancer progression, metastasis, stem cell maintenance, and therapy resistance. Here, we describe a rationally designed first-in-class inhibitor of LIFR, EC359, which directly interacts with LIFR to effectively block LIF/LIFR interactions. EC359 treatment exhibits antiproliferative effects, reduces invasiveness and stemness, and promotes apoptosis in triple-negative breast cancer (TNBC) cell lines. The activity of EC359 is dependent on LIF and LIFR expression, and treatment with EC359 attenuated the activation of LIF/LIFR-driven pathways, including STAT3, mTOR, and AKT. Concomitantly, EC359 was also effective in blocking signaling by other LIFR ligands (CTF1, CNTF, and OSM) that interact at LIF/LIFR interface. EC359 significantly reduced tumor progression in TNBC xenografts and patient-derived xenografts (PDX), and reduced proliferation in patient-derived primary TNBC explants. EC359 exhibits distinct pharmacologic advantages, including oral bioavailability, and
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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 OpenQuestion graph.