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3D-Informed Targeting of the Trop-2 Signal-Activation Site Drives Selective Cancer Vulnerability

15 Mar 2023

Abstract excerpt

Next-generation Trop-2-targeted therapy against advanced cancers is hampered by expression of Trop-2 in normal tissues. We discovered that Trop-2 undergoes proteolytic activation by ADAM10 in cancer cells, leading to the exposure of a previously inaccessible protein groove flanked by two N-glycosylation sites. We designed a recognition strategy for this region, to drive selective cancer vulnerability in patients....

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PMID: 36921314
DOI: 10.1158/1535-7163.mct-22-0352

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