DUAL INHIBITION OF EZH2 AND HDAC IS SYNERGISTIC IN EZH2 DYSREGULATED LYMPHOMAS
Sign Up to like & getrecommendations! Published in 2017 at "Hematological Oncology"
DOI: 10.1002/hon.2438_120
Abstract: rubicin, epirubicin, vinblastine, etoposide, paclitaxel, and topotecan. RTI‐79's PK characteristics are similar to rifabutin and exhibited no overt toxicity in mice at high doses. RTI‐79 did not exacerbate the known cardiotoxicity associated with doxorubicin as… read more here.
Keywords: rti; ezh2 hdac; dual inhibition; ezh2 ... See more keywords
Design of First-in-Class Dual EZH2/HDAC Inhibitor: Biochemical Activity and Biological Evaluation in Cancer Cells.
Sign Up to like & getrecommendations! Published in 2020 at "ACS medicinal chemistry letters"
DOI: 10.1021/acsmedchemlett.0c00014
Abstract: Since the histone modifying enzymes EZH2 and HDACs control a number of epigenetic-dependent carcinogenic pathways, we designed the first-in-class dual EZH2/HDAC inhibitor 5 displaying (sub)micromolar inhibition against both targets. When tested in several cancer cell… read more here.
Keywords: class dual; dual ezh2; ezh2 hdac; hdac inhibitor ... See more keywords
Combating castration-resistant prostate cancer by co-targeting the epigenetic regulators EZH2 and HDAC
Sign Up to like & getrecommendations! Published in 2023 at "PLOS Biology"
DOI: 10.1371/journal.pbio.3002038
Abstract: While screening and early detection have reduced mortality from prostate cancer, castration-resistant disease (CRPC) is still incurable. Here, we report that combined EZH2/HDAC inhibitors potently kill CRPCs and cause dramatic tumor regression in aggressive human… read more here.
Keywords: prostate cancer; ezh2 hdac; prostate; castration resistant ... See more keywords