WIP1 phosphatase as pharmacological target in cancer therapy
Jazyk angličtina Země Německo Médium print-electronic
Typ dokumentu časopisecké články, přehledy, práce podpořená grantem
PubMed
28439615
PubMed Central
PMC5442293
DOI
10.1007/s00109-017-1536-2
PII: 10.1007/s00109-017-1536-2
Knihovny.cz E-zdroje
- Klíčová slova
- Cancer, Checkpoint, DNA damage response, Inhibitor, Phosphatase, p53,
- MeSH
- konformace proteinů MeSH
- lidé MeSH
- nádorový supresorový protein p53 metabolismus MeSH
- nádory farmakoterapie metabolismus MeSH
- onkogeny MeSH
- poškození DNA MeSH
- proteinfosfatasa 2C antagonisté a inhibitory chemie imunologie metabolismus MeSH
- protinádorové látky farmakologie MeSH
- zvířata MeSH
- Check Tag
- lidé MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- přehledy MeSH
- Názvy látek
- nádorový supresorový protein p53 MeSH
- proteinfosfatasa 2C MeSH
- protinádorové látky MeSH
DNA damage response (DDR) pathway protects cells from genome instability and prevents cancer development. Tumor suppressor p53 is a key molecule that interconnects DDR, cell cycle checkpoints, and cell fate decisions in the presence of genotoxic stress. Inactivating mutations in TP53 and other genes implicated in DDR potentiate cancer development and also influence the sensitivity of cancer cells to treatment. Protein phosphatase 2C delta (referred to as WIP1) is a negative regulator of DDR and has been proposed as potential pharmaceutical target. Until recently, exploitation of WIP1 inhibition for suppression of cancer cell growth was compromised by the lack of selective small-molecule inhibitors effective at cellular and organismal levels. Here, we review recent advances in development of WIP1 inhibitors and discuss their potential use in cancer treatment.
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