2. Academic Validation
  3. Research progress of DDR1 inhibitors in the treatment of multiple human diseases

Research progress of DDR1 inhibitors in the treatment of multiple human diseases

  • Eur J Med Chem. 2024 Mar 15:268:116291. doi: 10.1016/j.ejmech.2024.116291.
Mengying Liu 1,  Jifa Zhang 1,  Xiaoxue Li 2,  Yuxi Wang 3
Affiliations

Affiliations

  • 1 Department of Pulmonary and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Research Center, Neuro-system and Multimorbidity Laboratory, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; Frontiers Medical Center, Tianfu Jincheng Laboratory, Chengdu, 610212, Sichuan, China.
  • 2 Department of Dermatology, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China.
  • 3 Department of Pulmonary and Critical Care Medicine, Targeted Tracer Research and Development Laboratory, Institute of Respiratory Health, Frontiers Science Center for Disease-related Molecular Network, Precision Medicine Key Laboratory of Sichuan Province & Precision Medicine Research Center, Neuro-system and Multimorbidity Laboratory, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu, 610041, Sichuan, China; Frontiers Medical Center, Tianfu Jincheng Laboratory, Chengdu, 610212, Sichuan, China. Electronic address: [email protected].
PMID: 38452728 DOI: 10.1016/j.ejmech.2024.116291
Abstract

Discoidin Domain Receptor 1 (DDR1) is a collagen-activated receptor tyrosine kinase (RTK) and plays pivotal roles in regulating cellular functions such as proliferation, differentiation, invasion, migration, and matrix remodeling. DDR1 is involved in the occurrence and progression of many human diseases, including Cancer, fibrosis, and inflammation. Therefore, DDR1 represents a highly promising therapeutic target. Although no selective small-molecule inhibitors have reached clinical trials to date, many molecules have shown therapeutic effects in preclinical studies. For example, BK40143 has demonstrated significant promise in the therapy of neurodegenerative diseases. In this context, our perspective aims to provide an in-depth exploration of DDR1, encompassing its structure characteristics, biological functions, and disease relevance. Furthermore, we emphasize the importance of understanding the structure-activity relationship of DDR1 inhibitors and highlight the unique advantages of dual-target or multitarget inhibitors. We anticipate offering valuable insights into the development of more efficacious DDR1-targeted drugs.

Keywords

DDR1; Drug discovery; Human diseases; Structure-activity relationship.

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