Tyrosine kinase inhibitors: Rationale, mechanisms of action, and implications for drug resistance

Dagmar Busse, F. Michael Yakes, Anne E.G. Lenferink, Carlos L. Arteaga

Research output: Contribution to journalArticlepeer-review

30 Scopus citations


Tyrosine kinases play a role in normal cellular regulatory processes. However, aberrant tyrosine kinase activity can lead to cellular transformation and can be causally associated with tumor maintenance and progression. In the last few years, high-throughput screening and the use of combinatorial, computational, and medicinal chemistry have led to the identification of small molecules that compete with the adenosine triphosphate binding site of the catalytic domain of several oncogenic tyrosine kinases. Some of these compounds are highly specific to a single tyrosine kinase, while others can inhibit several homologous kinase pockets simultaneously. At a practical level, the relative promiscuity of these inhibitors against more than one oncogenic tyrosine kinase may have clinical merit as well as implications for host tissue toxicity. Many of these small molecules are in different stages of preclinical and clinical development against several solid tumors and will be discussed.

Original languageEnglish (US)
Pages (from-to)47-55
Number of pages9
JournalSeminars in oncology
Issue number5 SUPPL. 16
StatePublished - 2001

ASJC Scopus subject areas

  • Hematology
  • Oncology


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