Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide

Ying Wu; Lei Wang; Yahui Huang; Shuqiang Chen; Shanchao Wu; Guoqiang Dong; Chunquan Sheng

doi:10.1021/acsmedchemlett.9b00407

Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide

ACS Med Chem Lett. 2019 Dec 13;11(1):40-44. doi: 10.1021/acsmedchemlett.9b00407. eCollection 2020 Jan 9.

Authors

Ying Wu¹, Lei Wang¹, Yahui Huang¹, Shuqiang Chen¹, Shanchao Wu¹, Guoqiang Dong¹, Chunquan Sheng^{1

2}

Affiliations

¹ Department of Medicinal Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China.
² School of Pharmaceutical Sciences, Zhengzhou University, Zhengzhou 450001, China.

Abstract

Chidamide is a histone deacetylase (HDAC) inhibitor that is currently used to treat cutaneous T-cell lymphoma in clinic. Herein nicotinamide phosphoribosyltransferase (NAMPT) was identified to be a new target of chidamide on the basis of the pharmacophore analysis, molecular docking, biological assays, inhibitor design, and structure-activity relationship study. The polypharmacology of chidamide will provide important information for better understanding its antitumor mechanism. Also, design of dual NAMPT/HDAC inhibitors may serve as an effective strategy to develop novel antitumor agents.