Improving the Potency of Cancer Immunotherapy by Dual Targeting of IDO1 and DNA

Kun Fang, Guoqiang Dong, Hongyu Wang, Shipeng He, Shanchao Wu, Wei Wang, Chunquan Sheng

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Herein we report the first exploration of a dual-targeting drug design strategy to improve the efficacy of small-molecule cancer immunotherapy. New hybrids of indoleamine 2,3-dioxygenase 1 (IDO1) inhibitors and DNA alkylating nitrogen mustards that respectively target IDO1 and DNA were rationally designed. As the first-in-class examples of such molecules, they were found to exhibit significantly enhanced anticancer activity in vitro and in vivo with low toxicity. This proof-of-concept study has established a critical step toward the development of a novel and effective immunotherapy for the treatment of cancers.

Original languageEnglish (US)
Pages (from-to)30-36
Number of pages7
JournalChemMedChem
Volume13
Issue number1
DOIs
StatePublished - Jan 8 2018
Externally publishedYes

Keywords

  • IDO1
  • antitumor activity
  • cancer immunotherapy
  • multitarget drug design

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Pharmacology, Toxicology and Pharmaceutics(all)
  • Organic Chemistry

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