Zhijia Yan, Yongli Du, Haibin Zhang, Yong Zheng, Huiting Lv, Ning Dong and Fang He
RSC Med. Chem., 2023,14, 1629-1644
Abstract
Structural optimization progress and future research directions of CDK12 inhibitors.
Pompom Ghosh, Maximilian Schmitz, Thiyagamurthy Pandurangan, Solomon Tadesse Zeleke, Sean Chin Chan, John Mosior, Luxin Sun, Vinayak Palve, Dylan Grassie, Kanchan Anand, Sylvia Frydman, William R. Roush, Ernst Schönbrunn, Matthias Geyer, Derek Duckett and Andrii Monastyrskyi
RSC Chem. Biol., 2025,6, 36-55
From themed collection:
Celebrating International Women’s day 2026: Women in Chemical Biology
Abstract
De novo design of molecular glues transforming CDK12 inhibitors, including dinaciclib, into cyclin K degraders.
Yasmin Y. Omar, Ghada F. Elmasry, Dina S. El-kady, Ahmed A. Abd-Rabou, Samir M. El-Moghazy, Fadi M. Awadallah, Gamal A. Elmegeed and Ghada H. Elsayed
RSC Med. Chem., 2026,17, 932-950
Abstract
This study developed novel progesterone-based CDK8 inhibitors and demonstrated their anticancer activity against A549 cells in CS-PEG nanoform, supported by gene expression analysis, CDK8 inhibition, and molecular docking studies.
Yumeng Wang, Cencen Lei, Quan Wang, Xingxing Zhang, Liping Zhi and Xinhua Liu
RSC Med. Chem., 2024,15, 3180-3195
Abstract
A new compound exhibiting excellent inhibitory activity against CDK8 was discovered. The mechanism was explored.
Xingxing Zhang, Qingsong Chen, Cencen Lei, Da Long Jin, Hao Dong Liu, Yumeng Wang, Chenyu zhao, Liping Zhi and Xinhua Liu
RSC Med. Chem., 2026, Accepted Manuscript
Abstract
CDK8 exerts important physiological functions, particularly in CRC, by forming intermediate complexes with Cyclic C, MED12, and MED13. In this work, different from the design of traditional single CDK8 protac...