TY - JOUR
T1 - Ubiquitin–proteasome system (UPS) as a target for anticancer treatment
AU - Park, Jinyoung
AU - Cho, Jinhong
AU - Song, Eun Joo
N1 - Funding Information:
This work was supported by a National Research Foundation of Korea (NRF) Grant funded by the Korean government (MSIP) (2020R1A4A4079494 and 2019R1A2C2004052).
Publisher Copyright:
© 2020, The Pharmaceutical Society of Korea.
PY - 2020/11
Y1 - 2020/11
N2 - The ubiquitin–proteasome system (UPS) plays an important role in the cellular processes for protein quality control and homeostasis. Dysregulation of the UPS has been implicated in numerous diseases, including cancer. Indeed, components of UPS are frequently mutated or abnormally expressed in various cancers. Since Bortezomib, a proteasome inhibitor, received FDA approval for the treatment of multiple myeloma and mantle cell lymphoma, increasing numbers of researchers have been seeking drugs targeting the UPS as a cancer therapeutic strategy. Here, we introduce the essential component of UPS, including ubiquitinating enzymes, deubiquitinating enzymes and 26S proteasome, and we summarize their targets and mechanisms that are crucial for tumorigenesis. In addition, we briefly discuss some UPS inhibitors, which are currently in clinical trials as cancer therapeutics.
AB - The ubiquitin–proteasome system (UPS) plays an important role in the cellular processes for protein quality control and homeostasis. Dysregulation of the UPS has been implicated in numerous diseases, including cancer. Indeed, components of UPS are frequently mutated or abnormally expressed in various cancers. Since Bortezomib, a proteasome inhibitor, received FDA approval for the treatment of multiple myeloma and mantle cell lymphoma, increasing numbers of researchers have been seeking drugs targeting the UPS as a cancer therapeutic strategy. Here, we introduce the essential component of UPS, including ubiquitinating enzymes, deubiquitinating enzymes and 26S proteasome, and we summarize their targets and mechanisms that are crucial for tumorigenesis. In addition, we briefly discuss some UPS inhibitors, which are currently in clinical trials as cancer therapeutics.
KW - Cancer
KW - Deubiquitinating enzymes (DUBs)
KW - E3 ligase
KW - Proteasome
KW - Small molecule inhibitors
KW - Ubiquitin–proteasome system (UPS)
UR - http://www.scopus.com/inward/record.url?scp=85095605596&partnerID=8YFLogxK
U2 - 10.1007/s12272-020-01281-8
DO - 10.1007/s12272-020-01281-8
M3 - Review article
C2 - 33165832
AN - SCOPUS:85095605596
SN - 0253-6269
VL - 43
SP - 1144
EP - 1161
JO - Archives of Pharmacal Research
JF - Archives of Pharmacal Research
IS - 11
ER -