Article
HER2-Mediated Internalization of Cytotoxic Agents in ERBB2 Amplified or Mutant Lung Cancers.
Cancer discovery - 1 May 2020
Li Bob T, Michelini Flavia, Misale Sandra, Cocco Emiliano, Baldino Laura, Cai Yanyan, Shifman Sophie, Tu Hai-Yan, Myers Mackenzie L, Xu Chongrui, Mattar Marissa, Khodos Inna, Little Megan, Qeriqi Besnik, Weitsman Gregory, Wilhem Clare J, Lalani Alshad S, Diala Irmina, Freedman Rachel A, Lin Nancy U, Solit David B, Berger Michael F, Barber Paul R, Ng Tony, Offin Michael, Isbell James M, Jones David R, Yu Helena A, Thyparambil Sheeno, Liao Wei-Li, Bhalkikar Anuja, Cecchi Fabiola, Hyman David M, Lewis Jason S, Buonocore Darren J, Ho Alan L, Makker Vicky, Reis-Filho Jorge S, Razavi Pedram, Arcila Maria E, Kris Mark G, Poirier John T, Shen Ronglai, Tsurutani Junji, Ulaner Gary A, de Stanchina Elisa, Rosen Neal, Rudin Charles M, Scaltriti Maurizio
Abstract excerpt
Amplification of and oncogenic mutations in ERBB2, the gene encoding the HER2 receptor tyrosine kinase, promote receptor hyperactivation and tumor growth. Here we demonstrate that HER2 ubiquitination and internalization, rather than its overexpression, are key mechanisms underlying endocytosis and consequent efficacy of the anti-HER2 antibody-drug conjugates (ADC) ado-trastuzumab emtansine (T-DM1) and trastuzumab...
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