ArticleScientific reports2014
YLT192, a novel, orally active bioavailable inhibitor of VEGFR2 signaling with potent antiangiogenic activity and antitumor efficacy in preclinical models.
Article in Scientific reports, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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Who cites it
20 citing papers in PubMed, 33 citations in OpenAlex.
- Exploring the therapeutic mechanisms of Coptidis Rhizoma in gastric precancerous lesions: a network pharmacology approach.Discover oncology · 2024Article
- Molecular Mechanisms and Future Implications of VEGF/VEGFR in Cancer Therapy.Clinical cancer research : an official journal of the American Association for Cancer Research · 2023Review
- The use of machine learning modeling, virtual screening, molecular docking, and molecular dynamics simulations to identify potential VEGFR2 kinase inhibitors.Scientific reports · 2022Article
- Inhibition of AXL and VEGF-A Has Improved Therapeutic Efficacy in Uterine Serous Cancer.Cancers · 2021Article
- Nifuroxazide Mitigates Angiogenesis in Ehlrich's Solid Carcinoma: Molecular Docking, Bioinformatic and Experimental Studies on Inhibition of Il-6/Jak2/Stat3 Signaling.Molecules (Basel, Switzerland) · 2021Article
- The Protective Effect of Aspirin Eugenol Ester on Oxidative Stress to PC12 Cells Stimulated with HOxidative medicine and cellular longevity · 2021Article
- Protective Activity of Aspirin Eugenol Ester on Paraquat-Induced Cell Damage in SH-SY5Y Cells.Oxidative medicine and cellular longevity · 2021Article
- Alkaloid extract of Corydalis yanhusuo inhibits angiogenesis via targeting vascular endothelial growth factor receptor signaling.BMC complementary and alternative medicine · 2019Article
- Repositioning antipsychotic fluphenazine hydrochloride for treating triple negative breast cancer with brain metastases and lung metastases.American journal of cancer research · 2019Article
- Antipsychotic Drug Trifluoperazine Suppresses Colorectal Cancer by Inducing G0/G1 Arrest and Apoptosis.Frontiers in pharmacology · 2019Article
- The enhanced antitumour response of pimozide combined with the IDO inhibitor L‑MT in melanoma.International journal of oncology · 2018Article
- Tumor-secreted anterior gradient-2 binds to VEGF and FGF2 and enhances their activities by promoting their homodimerization.Oncogene · 2017Article
- Disruption of Angiogenesis by Anthocyanin-Rich Extracts ofInternational journal of scientific and engineering research · 2017Article
- The novel VEGF receptor 2 inhibitor YLL545 inhibits angiogenesis and growth in breast cancer.Oncotarget · 2016Article
- Salinomycin exerts anti-angiogenic and anti-tumorigenic activities by inhibiting vascular endothelial growth factor receptor 2-mediated angiogenesis.Oncotarget · 2016Article
- Nifuroxazide exerts potent anti-tumor and anti-metastasis activity in melanoma.Scientific reports · 2016Article
- Gamabufotalin, a major derivative of bufadienolide, inhibits VEGF-induced angiogenesis by suppressing VEGFR-2 signaling pathway.Oncotarget · 2016Article
- Niclosamide inhibits the inflammatory and angiogenic activation of human umbilical vein endothelial cells.Inflammation research : official journal of the European Histamine Research Society ... [et al.] · 2015Article
- Vascular endothelial growth factor receptor-2 (VEGFR-2) inhibitors: development and validation of predictive 3-D QSAR models through extensive ligand- and structure-based approaches.Journal of computer-aided molecular design · 2015Article
- Nifuroxazide induces apoptosis and impairs pulmonary metastasis in breast cancer model.Cell death & disease · 2015Article
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Authors and funding
18 authors at 3 institutions in 1 country.
Funding
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Abstract
Antagonizing vascular endothelial growth factor receptor 2 (VEGFR2) to block angiogenesis has been applied toward cancer therapy for its role in promoting cancer growth and metastasis. However, most these clinical anticancer drugs have unexpected side effects. Development of novel VEGFR2 inhibitors with less toxicity remains an urgent need. In this study, we describe a novel, well-tolerated, and orally active VEGFR2 inhibitor, YLT192, which inhibits tumor angiogenesis and growth. YLT192 significantly inhibited kinase activity of VEGFR2 and suppressed proliferation, migration, invasion, and tube formation of human umbilical vascular endothelial cells (HUVEC) in vitro. In addition, it inhibited VEGF-induced phosphorylation of VEGFR2 and its downstream signaling regulator in HUVEC. Zebrafish embryonic models and alginate-encapsulated tumor cell assays indicated YLT192 also inhibited angiogenesis in vivo. Moreover, YLT192 could directly inhibit proliferation and induce apoptosis of cancer cells in vitro and in vivo. Oral administration of YLT192 at a dose of 100 mg/kg/day could markedly inhibited human tumor xenograft growth without causing obvious toxicities. It decreased microvessel densities (MVD) in tumor sections. It also shows good safety profiles in the studies with mice and rats. Taken together, these preclinical evaluations suggest that YLT192 inhibits angiogenesis and may be a promising anticancer drug candidate.
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