AI Article Synopsis
- Angiogenesis, the formation of new blood vessels, is linked to cancer, making VEGFR-2 inhibitors important targets for treatment.
- Researchers developed 29 compounds as VEGFR-2 inhibitors and tested their effectiveness; B1, PB11, and PB16 showed strong antiangiogenic activity with low IC scores.
- In assays, B1 and PB16 demonstrated significant capability to curb capillary formation and migration of human umbilical vein endothelial cells (HUVECs), with B1 and PB16 effectively interacting with VEGFR-2's ATP site and allosteric pocket.
Article Abstract
Angiogenesis deregulation is often linked to cancer and is thus an essential target. Twenty-nine compounds were developed as VEGFR-2 inhibitors. Compounds were evaluated to determine their antiangiogenic activity. B1, PB11 and PB16 showed HUVEC's IC scores in the submicromolar range. B1, B2 and PB16 reduced cellular migration and capillary tube formation of HUVECs. VEGFR-2 inhibitory activity was found in the nanomolar range: 200 nM of B1, 500 nM of B2 and 600 nM of PB16. B1 and PB16 suppressed the formation of new capillaries on growing CAMs. B1 and PB16 occupied the ATP site and allosteric pocket of VEGFR-2 in docking studies. These compounds can target VEGFR-2 and are endowed with and antiangiogenic activity.
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| http://dx.doi.org/10.4155/fmc-2021-0139 | DOI Listing |
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