TY - JOUR
T1 - Screening and identification of inhibitors of endoplasmic reticulum stress-induced activation of the IRE1α-XBP1 branch
AU - Tashiro, Etsu
PY - 2019/12/1
Y1 - 2019/12/1
N2 - Endoplasmic reticulum (ER) stress and the subsequent adaptive cellular response, termed the unfolded protein response (UPR), have been implicated in several diseases, including cancer. In this review, I present a brief introduction to ER stress and the UPR and then summarize the importance of the IRE1α-XBP1 branch as a target for anticancer drug discovery. In addition, I introduce our approach to the identification of inhibitors against the IRE1α-XBP1 branch from microbial cultures. As a result of our screening, toyocamycin has been identified and toyocamycin showed anticancer activity against multiple myeloma.
AB - Endoplasmic reticulum (ER) stress and the subsequent adaptive cellular response, termed the unfolded protein response (UPR), have been implicated in several diseases, including cancer. In this review, I present a brief introduction to ER stress and the UPR and then summarize the importance of the IRE1α-XBP1 branch as a target for anticancer drug discovery. In addition, I introduce our approach to the identification of inhibitors against the IRE1α-XBP1 branch from microbial cultures. As a result of our screening, toyocamycin has been identified and toyocamycin showed anticancer activity against multiple myeloma.
UR - http://www.scopus.com/inward/record.url?scp=85070250311&partnerID=8YFLogxK
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U2 - 10.1038/s41429-019-0219-3
DO - 10.1038/s41429-019-0219-3
M3 - Review article
C2 - 31399644
AN - SCOPUS:85070250311
SN - 0021-8820
VL - 72
SP - 899
EP - 905
JO - Journal of Antibiotics
JF - Journal of Antibiotics
IS - 12
ER -
