Drug discovery approaches targeting the incretin pathway

Xinxian Deng, Mojdeh S. Tavallaie, Ran Sun, Juntao Wang, Qingqing Cai, Jian Shen, Shuwen Lei, Lei Fu*, Faqin Jiang

*Corresponding author for this work

Research output: Contribution to journalReview articlepeer-review

11 Citations (Scopus)


Incretin pathway plays an important role in the development of diabetes medications. Interventions in DPP-4 and GLP-1 receptor have shown remarkable efficacy in experimental and clinical studies and imperatively become one of the most promising therapeutic approaches in the T2DM drug discovery pipeline. Herein, we analyzed the action mechanisms of DPP-4 and GLP-1 receptor targeting the incretin pathway in T2DM treatment. We gave an insight into the structural requirements for the potent DPP-4 inhibitors and revealed a classification of DPP-4 inhibitors by stressing on the binding modes of these ligands to the enzyme. We then reviewed the drug discovery strategies for the development of peptide and non-peptide GLP-1 receptor agonists (GLP-1 RAs). Furthermore, the drug design strategies for DPP-4 inhibitors and GLP-1R agonists were detailed accurately. This review might provide an efficient evidence for the highly potent and selective DPP-4 inhibitors and the GLP-1 RAs, as novel medicines for patients suffering from T2DM.

Original languageEnglish
Article number103810
JournalBioorganic Chemistry
Publication statusPublished - Jun 2020
Externally publishedYes


  • DPP-4 inhibitors
  • Drug discovery
  • GLP-1 receptor agonists
  • Incretin pathway
  • Ligand-receptor interactions


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