Panorama dos nutlins como protótipo para terapia do câncer
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Data
2014
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Resumo
p53 is a tumor suppressor protein that acts in cell defense against
deleterious mutations and cancer transformations. The signaling
pathway of p53 protein is inactivated in all types of cancer and this fact
has attracted the attention of many researchers in order to develop new
drug therapies based on the reestablishment of this pathway. The levels
of p53 in the cell are under the strict control of the negative regulator
MDM2 ubiquitination pathway. p53 also controls the transcription of
MDM2 generating a feedback regulation that the two proteins mutually
control their cellular levels. Thus, it was thought that blocking the
MDM2-p53 interaction could lead to different pharmacological effects
and antitumor inhibitory molecules have been tested for this purpose,
among them a family of imidazoline tetrasubstituted called nutlins.
These compounds can selectively activate the p53 signaling pathway in
vitro and in vivo human tumor lines that show high expression of
HDM2 (human type MDM2) leading to inhibition of cell growth and
apoptosis. MDM2 inhibitors represent a promising class of activators of
p53 that may become drugs effective in the treatment of cancer and also
in diagnostic imaging.
Descrição
Palavras-chave
Nutlins, p53, MDM2, Cancer, p53, Nutlins, MDM2, Câncer
Citação
RODRIGUES, Caroline Rego; CUNHA, Luiz Carlos da; GUILLO, Lídia Andeu. Panorama dos nutlins como protótipo para terapia do câncer. Revista de Biotecnologia & Ciência, Goiânia, v. 3, n. 1, p. 77-89, 2014.