1. Academic Validation
  2. Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide

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

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.

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