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Article

Discovery of AL-GDa62 as a Potential Synthetic Lethal Lead for the Treatment of Gastric Cancer.

Journal of medicinal chemistry - 23 Dec 2021

Luxenburger Andreas, Bougen-Zhukov Nicola, Fraser Michael G, Beetham Henry, Harris Lawrence D, Schmidt Dorian, Cameron Scott A, Guilford Parry J, Evans Gary B

Abstract excerpt

Diffuse gastric cancer and lobular breast cancer are aggressive malignancies that are frequently associated with inactivating mutations in the tumor suppressor gene CDH1. Synthetic lethal (SL) vulnerabilities arising from CDH1 dysfunction represent attractive targets for drug development. Recently, SLEC-11 (1) emerged as a SL lead in E-cadherin-deficient cells. Here, we describe our efforts to optimize 1....

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PMID: 34878770
DOI: 10.1021/acs.jmedchem.1c01609

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