Tyrosine kinase domain

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=== Role and significance in cancer:  ===
 
=== Role and significance in cancer:  ===
  
[[Tyrosine_kinase|Tyrosine kinases]] are important mediators of the [[signalling cascade|signalling cascade]], determining key roles in diverse biological processes like growth, differentiation, [[Metabolism|metabolism]] and [[Apoptosis|apoptosis]] in response to external and internal stimuli.  
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[[Tyrosine kinase|Tyrosine kinases]] are important mediators of the [[Signalling cascade|signalling cascade]], determining key roles in diverse biological processes like growth, differentiation, [[Metabolism|metabolism]] and [[Apoptosis|apoptosis]] in response to external and internal[[Stimulus|stimuli]].  
  
Recent advances have implicated the role of tyrosine kinases in the [[pathophysiology|pathophysiology]] of [[cancer|cancer]]. Though their activity is tightly regulated in normal [[Cells|cells]], they may acquire transforming functions due to mutation(s), overexpression and autocrine, paracrine stimulation, leading to malignancy. Constitutive oncogenic activation in cancer cells can be blocked by selective tyrosine kinase inhibitors and thus considered as a promising approach for innovative [[genome|genome]] based therapeutics. The modes of [[oncogenic activation|oncogenic activation]] and the different approaches for tyrosine kinase inhibition, like small molecule inhibitors, [[Monoclonal_antibodies|monoclonal antibodies]], [[heat shock proteins|heat shock proteins]], immunoconjugates, antisense and peptide drugs are reviewed in light of the important molecules. As angiogenesis is a major event in cancer growth and proliferation, tyrosine kinase inhibitors as a target for anti-angiogenesis can be aptly applied as a new mode of cancer therapy. The review concludes with a discussion on the application of modern techniques and knowledge of the kinome as means to gear up the tyrosine kinase drug discovery process.
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Recent advances have implicated the role of tyrosine kinases in the [[Pathophysiology|pathophysiology]] of [[Cancer|cancer]]. Though their activity is tightly regulated in normal [[Cells|cells]], they may acquire transforming functions due to [[Mutation|mutation]](s), overexpression and [[Autocrine|autocrine]], paracrine stimulation, leading to [[malignancy|malignancy]]. Constitutive [[oncogenic activation|oncogenic activation]] in [[Cancer|cancer]] cells can be blocked by selective tyrosine kinase [[inhibitors|inhibitors ]]and thus considered as a promising approach for innovative [[Genome|genome]] based therapeutics. The modes of [[Oncogenic activation|oncogenic activation]] and the different approaches for tyrosine kinase inhibition, like small molecule inhibitors, [[Monoclonal antibodies|monoclonal antibodies]], [[Heat shock proteins|heat shock proteins]], immunoconjugates, antisense and peptide drugs are reviewed in light of the important molecules. As angiogenesis is a major event in cancer growth and proliferation, tyrosine kinase inhibitors as a target for anti-angiogenesis can be aptly applied as a new mode of cancer therapy. The review concludes with a discussion on the application of modern techniques and knowledge of the kinome as means to gear up the tyrosine kinase drug discovery process.

Revision as of 18:33, 2 December 2017

Role and significance in cancer:

Tyrosine kinases are important mediators of the signalling cascade, determining key roles in diverse biological processes like growth, differentiation, metabolism and apoptosis in response to external and internalstimuli.

Recent advances have implicated the role of tyrosine kinases in the pathophysiology of cancer. Though their activity is tightly regulated in normal cells, they may acquire transforming functions due to mutation(s), overexpression and autocrine, paracrine stimulation, leading to malignancy. Constitutive oncogenic activation in cancer cells can be blocked by selective tyrosine kinase inhibitors and thus considered as a promising approach for innovative genome based therapeutics. The modes of oncogenic activation and the different approaches for tyrosine kinase inhibition, like small molecule inhibitors, monoclonal antibodies, heat shock proteins, immunoconjugates, antisense and peptide drugs are reviewed in light of the important molecules. As angiogenesis is a major event in cancer growth and proliferation, tyrosine kinase inhibitors as a target for anti-angiogenesis can be aptly applied as a new mode of cancer therapy. The review concludes with a discussion on the application of modern techniques and knowledge of the kinome as means to gear up the tyrosine kinase drug discovery process.

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