T.77. Tyrosine Kinases in Autoimmune Demyelination

Crespo, Oliver; Kang, Stacey; Daneman, Richard; Sobel, Raymond A.; Ho, Peggy P.; Steinman, Lawrence; Robinson, William H.

doi:10.1016/j.clim.2009.03.212

Cited by 1 publication

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“…Later, a broad spectrum of biological activities have been added like antioxidant, increase of cellular glutathione level, suppression of poly ADP (adenosine diphosphate)-ribose polymerase (PARP) activation 11 , as well as these compounds potentiate the expression of some redox-sensitive genes associated to mitogen-activated protein kinase (MAPK), AP-1 and Nrf2 factors 12,13 . TYK inhibitors, except being broadly used in cancer clinical trials 14 , have also been evaluated in animal models of type 1 diabetes 15,16 , multiple sclerosis 17 , intestinal inflammation 18 and septic shock 19 . A number of studies have shown that in general tyrphostins express their anti-inflammatory activity by modulation of pro-inflammatory gene expression, such as cyclooxygenase-2 (COX2), inducible nitric oxide synthase (iNOS) and several pivotal cytokines ( Figure 1).…”

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confidence: 99%

Tyrphostins as a promising therapeutic tool in inflammation-related conditions

Dimitrova¹,

Ivanovska²

2013

OA Inflammation

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IntroductionProtein kinases regulate the expression of many genes that are pivotal for inflammation. This review aims to summarise data on a group of small molecules capable to inhibit tyrosine kinases (TYKs), named tyrphostins. They are derivatives of benzylidenemalonitrile that decrease tyrosine phosphorylation, thereby affecting not a single mediator, but cell signalling transduction is affected. No single animal model fully represents the human disease, but these models provide valuable tools to understand particular pathways. In this review, we describe some of the recent investigations on tyrphostins as anti-inflammatory agents in vivo in animal models, and in vitro in cell culture systems. ConclusionIt is anticipated that tyrphostins are suitable for the treatment of inflammation-related diseases. Future research is required to understand the mechanisms of their action to pave way for gaining pharmacological benefits in clinical practice.

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