dc.contributor.author |
Herrero Ana |
|
dc.contributor.author |
Pinto Adan |
|
dc.contributor.author |
Colon-Bolea Paula |
|
dc.contributor.author |
Casar Berta |
|
dc.contributor.author |
Jones Mary |
|
dc.contributor.author |
Agudo-Ibanez Lorena |
|
dc.contributor.author |
Vidal Rebeca |
|
dc.contributor.author |
Tenbaum Stephan P |
|
dc.contributor.author |
Nuciforo Paolo |
|
dc.contributor.author |
Valdizan Elsa M |
|
dc.contributor.author |
Horvath Zoltan |
|
dc.contributor.author |
Őrfi László |
|
dc.contributor.author |
Pineda-Lucena Antonio |
|
dc.contributor.author |
Bony Emilie |
|
dc.contributor.author |
Kéri György |
|
dc.contributor.author |
Rivas German |
|
dc.contributor.author |
Pazos Angel |
|
dc.contributor.author |
Gozalbes Rafael |
|
dc.contributor.author |
Palmer Hector G |
|
dc.contributor.author |
Hurlstone Adam |
|
dc.contributor.author |
Crespo Piero |
|
dc.date.accessioned |
2016-04-03T10:44:03Z |
|
dc.date.available |
2016-04-03T10:44:03Z |
|
dc.date.issued |
2015 |
|
dc.identifier.citation |
pagination=170-182;
journalVolume=28;
journalIssueNumber=2;
journalTitle=CANCER CELL; |
|
dc.identifier.uri |
http://repo.lib.semmelweis.hu//handle/123456789/2768 |
|
dc.identifier.uri |
doi:10.1016/j.ccell.2015.07.001 |
|
dc.description.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. |
|
dc.relation.ispartof |
urn:issn:1535-6108 |
|
dc.title |
Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes |
|
dc.type |
Journal Article |
|
dc.date.updated |
2015-11-25T16:18:56Z |
|
dc.language.rfc3066 |
en |
|
dc.identifier.mtmt |
2938537 |
|
dc.identifier.wos |
000359509200007 |
|
dc.identifier.pubmed |
26267534 |
|
dc.contributor.department |
SE/GYTK/Gyógyszerészi Kémiai Intézet |
|
dc.contributor.department |
SE/AOK/I/Orvosi Vegytani, Molekuláris Biológiai és Patobiokémiai Intézet |
|
dc.contributor.institution |
Semmelweis Egyetem |
|