The development of novel and selective p56lck tyrosine kinase inhibitors

J L Bullington; J C Cameron; J E Davis; J H Dodd; C A Harris; J R Henry; J L Pellegrino-Gensey; K C Rupert; J J Siekierka

doi:10.1016/s0960-894x(98)00445-4

The development of novel and selective p56lck tyrosine kinase inhibitors

Bioorg Med Chem Lett. 1998 Sep 22;8(18):2489-94. doi: 10.1016/s0960-894x(98)00445-4.

Authors

J L Bullington¹, J C Cameron, J E Davis, J H Dodd, C A Harris, J R Henry, J L Pellegrino-Gensey, K C Rupert, J J Siekierka

Affiliation

¹ R. W. Johnson Pharmaceutical Research Institute, Raritan, NJ 08869, USA.

PMID: 9873567
DOI: 10.1016/s0960-894x(98)00445-4

Abstract

Early T-cell receptor mediated signal transduction involves the activation of several tyrosine protein kinases. One of these tyrosine kinases, p56lck, is expressed primarily in T-cells and Natural Killer (NK) cells and has been shown to be critical for their proliferative and effector functions. Indandiones have been identified as a potent and selective chemical class that inhibits p56lck.

MeSH terms

CSK Tyrosine-Protein Kinase
Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors
Enzyme Activation
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology
Indans / chemistry
Indans / pharmacology
Killer Cells, Natural / enzymology
Lymphocyte Specific Protein Tyrosine Kinase p56(lck) / antagonists & inhibitors*
Models, Chemical
Protein-Tyrosine Kinases / antagonists & inhibitors
Signal Transduction
T-Lymphocytes / enzymology
src-Family Kinases

Substances

Enzyme Inhibitors
Indans
Protein-Tyrosine Kinases
CSK Tyrosine-Protein Kinase
Lymphocyte Specific Protein Tyrosine Kinase p56(lck)
src-Family Kinases
Cyclic AMP-Dependent Protein Kinases