Format

Send to

Choose Destination
Trends Pharmacol Sci. 2015 Jul;36(7):422-39. doi: 10.1016/j.tips.2015.04.005. Epub 2015 May 12.

FDA-approved small-molecule kinase inhibitors.

Author information

1
Department of Chemistry, Technical University of Denmark, DK-2800 Kgs. Lyngby, Denmark. Electronic address: penwu@kemi.dtu.dk.
2
Protein and Peptide Chemistry, Novo Nordisk A/S, DK-2760 Måløv, Denmark.
3
Department of Chemistry, Technical University of Denmark, DK-2800 Kgs. Lyngby, Denmark; Center for Nanomedicine and Theranostics, Technical University of Denmark, DK-2800 Kgs. Lyngby, Denmark.

Abstract

Kinases have emerged as one of the most intensively pursued targets in current pharmacological research, especially for cancer, due to their critical roles in cellular signaling. To date, the US FDA has approved 28 small-molecule kinase inhibitors, half of which were approved in the past 3 years. While the clinical data of these approved molecules are widely presented and structure-activity relationship (SAR) has been reported for individual molecules, an updated review that analyzes all approved molecules and summarizes current achievements and trends in the field has yet to be found. Here we present all approved small-molecule kinase inhibitors with an emphasis on binding mechanism and structural features, summarize current challenges, and discuss future directions in this field.

KEYWORDS:

cancer; crystal structure; lipid kinase; protein kinase; serine/threonine kinase; tyrosine kinase

PMID:
25975227
DOI:
10.1016/j.tips.2015.04.005
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center