Cyclin-dependent kinase 7 inhibitor THZ1 in cancer therapy

Bin-Bin Li; Bo Wang; Cheng-Ming Zhu; Di Tang; Jun Pang; Jing Zhao; Chun-Hui Sun; Miao-Juan Qiu; Zhi-Rong Qian

doi:10.1016/j.cdtm.2019.08.006

Cyclin-dependent kinase 7 inhibitor THZ1 in cancer therapy

Chronic Dis Transl Med. 2019 Oct 18;5(3):155-169. doi: 10.1016/j.cdtm.2019.08.006. eCollection 2019 Sep.

Authors

Bin-Bin Li^{1

2}, Bo Wang², Cheng-Ming Zhu², Di Tang², Jun Pang², Jing Zhao², Chun-Hui Sun^{2

3}, Miao-Juan Qiu², Zhi-Rong Qian²

Affiliations

¹ School of Biological Sciences, Nanyang Technological University, Singapore 639798, Singapore.
² Scientific Research Center, The Seventh Affiliated Hospital, Sun Yat-sen University, Shenzhen, Guangdong 518107, China.
³ Equipe Communication Intercellulaire et Infections Microbiennes, Centre de Recherche Interdisciplinaire en Biologie (CIRB), College de France, Paris 75005, France.

Abstract

Current cancer therapies have encountered adverse response due to poor therapeutic efficiency, severe side effects and acquired resistance to multiple drugs. Thus, there are urgent needs for finding new cancer-targeted pharmacological strategies. In this review, we summarized the current understanding with THZ1, a covalent inhibitor of cyclin-dependent kinase 7 (CDK7), which demonstrated promising anti-tumor activity against different cancer types. By introducing the anti-tumor behaviors and the potential targets for different cancers, this review aims to provide more effective approaches to CDK7 inhibitor-based therapeutic agents and deeper insight into the diverse tumor proliferation mechanisms.

Keywords: Cancer therapy; Cyclin-dependent kinase 7; Super-enhancer; THZ1; Transcription.