期刊
EXPERT OPINION ON DRUG DISCOVERY
卷 4, 期 8, 页码 799-821出版社
TAYLOR & FRANCIS LTD
DOI: 10.1517/17460440903052559
关键词
anticancer drugs; apoptosis; ATF6; cancer; cancer drug discovery; ERAD; ERS; GADD153/CHOP; GRP78/BiP; heat shock proteins; IRE1; Mdm2; oncogenes; p53; PERK; signal transduction; turnout suppressors; UPR; UPS; XBP1
资金
- University of the Western Cape
- University of Cape Town
- Ackerman Family Educational Trust
Background: In eukaryotes, endoplasmic reticulum stress (ERS) and the unfolded protein response (UPR) are coordinately regulated to maintain steady-state levels and activities of various cellular proteins to ensure cell survival. Objective: This review (Part I of II) focuses on specific ERS and UPR signalling regulators, their expression in the cancer phenotype and apoptosis, and proposes how their implication in these processes can be rationalised into proteasome inhibition, apoptosis induction and the development of more efficacious targeted molecular cancer therapies. Method: in this review, we contextualise many ERS and UPR client proteins that are deregulated or mutated in cancers and show links between ERS and the UPR, their implication in oncogenic transformation, tumour progression and escape from immune surveillance, apoptosis inhibition, angiogenesis, metastasis, acquired drug resistance and poor cancer prognosis. Conclusion: Evasion of programmed cell death or apoptosis is a hallmark of cancer that enables tumour cells to proliferate uncontrollably. Successful eradication of cancer cells through targeting ERS- and UPR-associated proteins to induce apoptosis is currently being pursued as a central tenet of anticancer drug discovery.
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