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Molecular tools that block maturation of the nuclear lamin A and decelerate cancer cell migration.

Abstract：

:Lamin A contributes to the structure of nuclei in all mammalian cells and plays an important role in cell division and migration. Mature lamin A is derived from a farnesylated precursor protein, known as prelamin A, which undergoes post-translational cleavage catalyzed by the zinc metalloprotease STE24 (ZPMSTE24). Accumulation of farnesylated prelamin A in the nuclear envelope compromises cell division, impairs mitosis and induces an increased expression of inflammatory gene products. ZMPSTE24 has been proposed as a potential therapeutic target in oncology. A library of peptidomimetic compounds were synthesized and screened for their ability to induce accumulation of prelamin A in cancer cells and block cell migration in pancreatic ductal adenocarcinoma cells. The results of this study suggest that inhibitors of lamin A maturation may interfere with cell migration, the biological process required for cancer metastasis.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Matralis AN,Xanthopoulos D,Huot G,Lopes-Paciencia S,Cole C,de Vries H,Ferbeyre G,Tsantrizos YS

doi

10.1016/j.bmc.2018.10.001

subject

Has Abstract

pub_date

2018-11-01 00:00:00

pages

5547-5554

issue

20

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(18)31504-9

journal_volume

26

pub_type

杂志文章

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