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  3. Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy

Nonpeptidic quinazolinone derivatives as dual nucleotide-binding oligomerization domain-like receptor 1/2 antagonists for adjuvant cancer chemotherapy

  • Eur J Med Chem. 2020 Dec 1;207:112723. doi: 10.1016/j.ejmech.2020.112723.
Yao Ma 1,  Jingshu Yang 2,  Xiduan Wei 2,  Yameng Pei 2,  Jingjia Ye 2,  Xueyuan Li 2,  Guangxu Si 2,  Jingyuan Tian 2,  Yi Dong 3,  Gang Liu 4
Affiliations

Affiliations

  • 1 Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 2A Nanwei Rd, Xicheng Dist, Beijing, 100050, PR China.
  • 2 School of Pharmaceutical Sciences, Tsinghua University, Haidian Dist, Beijing, 100084, PR China.
  • 3 Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, 2A Nanwei Rd, Xicheng Dist, Beijing, 100050, PR China. Electronic address: dongyi@imm.ac.cn.
  • 4 School of Pharmaceutical Sciences, Tsinghua University, Haidian Dist, Beijing, 100084, PR China. Electronic address: gangliu27@tsinghua.edu.cn.
PMID: 32920426 DOI: 10.1016/j.ejmech.2020.112723
Abstract

Nucleotide-binding oligomerization domain-containing protein 1 and 2 (NOD1/2) receptors are potential immune checkpoints. In this article, a quinazolinone derivative (36b) as a NOD1/2 dual antagonist was identified that significantly sensitizes B16 tumor-bearing mice to paclitaxel treatment by inhibiting both nuclear factor κB (NF-κB) and mitogen-activated protein kinase inflammatory signaling that mediated by NOD1/2.

Keywords

B16 tumor; Dual NOD1/2 antagonists; Quinazolinone; Retroamide.

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