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.
Ying Wu  1 ,  Lei Wang  1 ,  Yahui Huang  1 ,  Shuqiang Chen  1 ,  Shanchao Wu  1 ,  Guoqiang Dong  1 ,  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.
PMID: 31938461 DOI: 10.1021/acsmedchemlett.9b00407
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.