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Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes

Abstract: Nearly 50% of human malignancies exhibit unregulated RAS-ERK signaling; inhibiting it is a valid strategy for antineoplastic intervention. Upon activation, ERK dimerize, which is essential for ERK extranuclear, but not for nuclear, signaling. Here, we describe a small molecule inhibitor for ERK dimerization that, without affecting ERK phosphorylation, forestalls tumorigenesis driven by RAS-ERK pathway oncogenes. This compound is unaffected by resistance mechanisms that hamper classical RAS-ERK pathway inhibitors. Thus, ERK dimerization inhibitors provide the proof of principle for two understudied concepts in cancer therapy: (1) the blockade of sub-localization-specific sub-signals, rather than total signals, as a means of impeding oncogenic RAS-ERK signaling and (2) targeting regulatory protein-protein interactions, rather than catalytic activities, as an approach for producing effective antitumor agents.

Otras publicaciones de la misma revista o congreso con autores/as de la Universidad de Cantabria

 Fuente: Cancer Cell. 2015 Aug 10;28(2):170-82

Editorial: Cell Press

 Fecha de publicación: 10/08/2015

Nº de páginas: 13

Tipo de publicación: Artículo de Revista

 DOI: 10.1016/j.ccell.2015.07.001.

ISSN: 1535-6108,1878-3686

Proyecto español: RD/12/0036/0033 ; SAF2011-25020 ; RD12/0036/0012

Autores/as

ANA HERRERO MIER

ADAN PINTO FERNANDEZ

PAULA COLON BOLEA

JONES, MARY

REBECA VIDAL CASADO

TENBAUM, STEPHAN P.

NUCIFORO, PAOLO

ELSA MARIA VALDIZAN RUIZ

HORVATH, ZOLTAN

ORFI, LASZLO

PINEDA LUCENA, ANTONIO

BONY, EMILIE

KERI, GYORGY

RIVAS, GERMÁN

GOZALBES, RAFAEL

PALMER, HÉCTOR G.

HURLSTONE, ADAM