TY - JOUR
T1 - Parthenolide
T2 - From plant shoots to cancer roots
AU - Ghantous, Akram
AU - Sinjab, Ansam
AU - Herceg, Zdenko
AU - Darwiche, Nadine
PY - 2013/9
Y1 - 2013/9
N2 - Parthenolide (PTL), a sesquiterpene lactone (SL) originally purified from the shoots of feverfew (Tanacetum parthenium), has shown potent anticancer and anti-inflammatory activities. It is currently being tested in cancer clinical trials. Structure-activity relationship (SAR) studies of parthenolide revealed key chemical properties required for biological activities and epigenetic mechanisms, and led to the derivatization of an orally bioavailable analog, dimethylamino-parthenolide (DMAPT). Parthenolide is the first small molecule found to be selective against cancer stem cells (CSC), which it achieves by targeting specific signaling pathways and killing cancer from its roots. In this review, we highlight the exciting journey of parthenolide, from plant shoots to cancer roots.
AB - Parthenolide (PTL), a sesquiterpene lactone (SL) originally purified from the shoots of feverfew (Tanacetum parthenium), has shown potent anticancer and anti-inflammatory activities. It is currently being tested in cancer clinical trials. Structure-activity relationship (SAR) studies of parthenolide revealed key chemical properties required for biological activities and epigenetic mechanisms, and led to the derivatization of an orally bioavailable analog, dimethylamino-parthenolide (DMAPT). Parthenolide is the first small molecule found to be selective against cancer stem cells (CSC), which it achieves by targeting specific signaling pathways and killing cancer from its roots. In this review, we highlight the exciting journey of parthenolide, from plant shoots to cancer roots.
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U2 - 10.1016/j.drudis.2013.05.005
DO - 10.1016/j.drudis.2013.05.005
M3 - Review article
C2 - 23688583
AN - SCOPUS:84883233659
SN - 1359-6446
VL - 18
SP - 894
EP - 905
JO - Drug Discovery Today
JF - Drug Discovery Today
IS - 17-18
ER -