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10d
Revealing the mechanism of Tilvestamab in treating cancer from a single-molecule perspective using atomic force microscopy. (PubMed, Anal Chim Acta)
Our study reveals that tilvestamab's anti-cancer efficacy arises from superior kinetic stability in AXL binding and direct modulation of cellular biomechanics. By enhancing membrane rigidity, tilvestamab impairs cancer cell migration and proliferation-key drivers of metastasis. These findings provide the biomechanical rationale for tilvestamab's therapeutic activity, positioning it as a promising agent for targeting AXL-dependent cancers through mechanopharmacological mechanisms.
Journal
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GAS6 (Growth arrest specific 6)
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tilvestamab (BGB149)
2ms
Paratope mapping of tilvestamab, an anti-AXL function-blocking antibody, using high-throughput bacterial expression of secreted scFv-ompY fusion proteins. (PubMed, Biosci Rep)
Glu2 near the N terminus of AXL is essential for binding. The data give a structural view into the AXL-tilvestamab complex and allow for further optimisation of the binding interface.
Journal
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AXL (AXL Receptor Tyrosine Kinase)
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tilvestamab (BGB149)
almost4years
AXL targeting by a specific small molecule or monoclonal antibody inhibits renal cell carcinoma progression in an orthotopic mice model. (PubMed, Physiol Rep)
Remarkably, their in vivo antitumor effectiveness was not significantly enhanced by concomitant administration of a multi-target tyrosine kinase inhibitor. Bemcentinib and tilvestamab qualify as compounds of potentially high clinical interest in AXL overexpressing RCC.
Preclinical • Journal
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AXL (AXL Receptor Tyrosine Kinase) • VIM (Vimentin) • GAS6 (Growth arrest specific 6)
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AXL expression • AXL overexpression • VIM expression
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bemcentinib (BGB324) • tilvestamab (BGB149)