Development of Src tyrosine kinase substrate binding site inhibitors

G. Ye, R. Tiwari, K. Parang

Research output: Contribution to journalArticlepeer-review

24 Scopus citations


The majority of marketed drugs or drug candidates that target protein kinases and which are currently undergoing clinical trials are ATP binding site inhibitors. The process of designing a selective inhibitor as an ATP mimic is challenging, mainly because of the presence of a large number of protein kinases that show a conserved ATP binding site. The substrate binding site of protein kinases is less conserved than the ATP binding site, and provides an opportunity to design valuable chemical tools which can be utilized to understand the catalytic mechanism of the enzyme, or to develop inhibitors with enhanced specificity. In this review, the latest developments of four classes of substrate binding site inhibitors of Src tyrosine kinase are discussed.

Original languageEnglish (US)
Pages (from-to)605-613
Number of pages9
JournalCurrent Opinion in Investigational Drugs
Issue number6
StatePublished - Jun 2008
Externally publishedYes


  • Bisubstrate inhibitor
  • Cyclic peptide
  • Pseudosubstrate
  • Small molecule
  • Src tyrosine kinase
  • Substrate binding site inhibitor

ASJC Scopus subject areas

  • Pharmacology


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