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State-of-the-art of small molecule inhibitors of the TAM family: The point of view of the chemist.

Authors :
Baladi, Tom
Abet, Valentina
Piguel, Sandrine
Source :
European Journal of Medicinal Chemistry. Nov2015, Vol. 105, p220-237. 18p.
Publication Year :
2015

Abstract

The TAM family of tyrosine kinases receptors (Tyro3, Axl and Mer) is implicated in cancer development, autoimmune reactions and viral infection and is therefore emerging as an effective and attractive therapeutic target. To date, only a few small molecules have been intentionally designed to block the TAM kinases, while most of the inhibitors were developed for blocking different protein kinases and then identified through selectivity profile studies. This minireview will examine in terms of chemical structure the different compounds able to act on either one, two or three TAM kinases with details about structure–activity relationships, drug-metabolism and pharmacokinetics properties where they exist. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
02235234
Volume :
105
Database :
Academic Search Index
Journal :
European Journal of Medicinal Chemistry
Publication Type :
Academic Journal
Accession number :
110632416
Full Text :
https://doi.org/10.1016/j.ejmech.2015.10.003