Fyn, Blk, and Lyn kinase inhibitors: A mini-review on medicinal attributes, research progress, and future insights

Bioorg Med Chem Lett. 2024 Apr 1:102:129674. doi: 10.1016/j.bmcl.2024.129674. Epub 2024 Feb 24.

Abstract

Fyn, Blk, and Lyn are part of a group of proteins called Src family kinases. They are crucial in controlling cell communication and their response to the growth, changes, and immune system. Blocking these proteins with inhibitors can be a way to treat diseases where these proteins are too active. The primary mode of action of these inhibitors is to inhibit the phosphorylation of Fyn, Blk, and Lyn receptors, which in turn affects how signals pass within the cells. This review shows the structural and functional aspects of Fyn, Blk, and Lyn kinases, highlighting the significance of their dysregulation in diseases such as cancer and autoimmune disorders. The discussion encompasses the design strategies, SAR analysis, and chemical characteristics of effective inhibitors, shedding light on their specificity and potency. Furthermore, it explores the progress of clinical trials of these inhibitors, emphasizing their potential therapeutic applications.

Keywords: Autoimmune disorders; Blk inhibitors; Cancer; Fyn inhibitors; Kinase signalling; Lyn inhibitors; Protein tyrosine kinases.

Publication types

  • Review

MeSH terms

  • Phosphorylation
  • Protein-Tyrosine Kinases* / metabolism
  • Proto-Oncogene Proteins c-fyn / metabolism
  • Proto-Oncogene Proteins* / metabolism
  • src-Family Kinases

Substances

  • Protein-Tyrosine Kinases
  • Proto-Oncogene Proteins c-fyn
  • Proto-Oncogene Proteins
  • src-Family Kinases