4.6 Review

Drug Development Targeting the Ubiquitin-Proteasome System (UPS) for the Treatment of Human Cancers

期刊

CANCERS
卷 12, 期 4, 页码 -

出版社

MDPI
DOI: 10.3390/cancers12040902

关键词

ubiquitin; cancer; targeted therapy; chemoresistance

类别

资金

  1. Department of Defense Ovarian Cancer Research Program [OC160377]
  2. Minnesota Ovarian Cancer Alliance
  3. Randy Shaver Cancer Research Funds
  4. NIH [1R01GM130800-01A1]
  5. CDMRP [OC160377, 917602] Funding Source: Federal RePORTER

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Cancer cells are characterized by a higher rate of protein turnover and greater demand for protein homeostasis compared to normal cells. In this scenario, the ubiquitin-proteasome system (UPS), which is responsible for the degradation of over 80% of cellular proteins within mammalian cells, becomes vital to cancer cells, making the UPS a critical target for the discovery of novel cancer therapeutics. This review systematically categorizes all current reported small molecule inhibitors of the various essential components of the UPS, including ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), ubiquitin ligases (E3s), the 20S proteasome catalytic core particle (20S CP) and the 19S proteasome regulatory particles (19S RP), as well as their mechanism/s of action and limitations. We also discuss the immunoproteasome which is considered as a prospective therapeutic target of the next generation of proteasome inhibitors in cancer therapies.

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