E7820 (NSC 719239) is an orally available anticancer and antiangiogenic agent that inhibits VEGF-2 or FGF-2-induced tube formation of HUVEC cells through the suppression of integrin α2. E7820 promotes selective proteasomal degradation of the U2AF-related splicing factor CAPERα (coactivator of activating protein-1 and estrogen receptors) by ubiquitination and degradation via CRL4DCAF15.
inducer of selective proteasomal degradation of CAPERα
E7820 is an orally active inhibitor of α(2)-integrin mRNA expression, currently tested in phases I and II. We aimed to evaluate what levels of inhibition of integrin expression are needed to achieve tumor stasis in mice, and to compare this
Most non-small-cell lung cancers (NSCLCs) harboring activating mutations in the epidermal growth factor receptor (EGFR) are initially responsive to EGFR tyrosine kinase inhibitors (EGFR-TKIs); however, they invariably develop resistance to these drugs. E7820 is an angiogenesis inhibitor that decreases integrin-α2
Nature chemical biology, 13(6), 675-680 (2017-04-25)
Target-protein degradation is an emerging field in drug discovery and development. In particular, the substrate-receptor proteins of the cullin-ubiquitin ligase system play a key role in selective protein degradation, which is an essential component of the anti-myeloma activity of immunomodulatory
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