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Tyrosine kinase - Role and significance in Cancer.

Paul MK, Mukhopadhyay AK - Int J Med Sci (2004)

Bottom Line: Tyrosine kinases are important mediators of the signaling cascade, determining key roles in diverse biological processes like growth, differentiation, metabolism and apoptosis in response to external and internal stimuli.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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Biotechnology, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S Nagar, Mohali, Punjab, India-160062.

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

No MeSH data available.


Related in: MedlinePlus

Mechanism of action of tyrosine kinase. 1. Receptor expression at membrane claveola 2. Ligand binding 3. Hetero/homodimerization leading to tyrosine kinase activation and tyrosine transphosphorylation 4. Signal transduction 5. Receptor internalization 6. Receptor degradation or re-expression.
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Figure 2: Mechanism of action of tyrosine kinase. 1. Receptor expression at membrane claveola 2. Ligand binding 3. Hetero/homodimerization leading to tyrosine kinase activation and tyrosine transphosphorylation 4. Signal transduction 5. Receptor internalization 6. Receptor degradation or re-expression.


Tyrosine kinase - Role and significance in Cancer.

Paul MK, Mukhopadhyay AK - Int J Med Sci (2004)

Mechanism of action of tyrosine kinase. 1. Receptor expression at membrane claveola 2. Ligand binding 3. Hetero/homodimerization leading to tyrosine kinase activation and tyrosine transphosphorylation 4. Signal transduction 5. Receptor internalization 6. Receptor degradation or re-expression.
© Copyright Policy
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC1074718&req=5

Figure 2: Mechanism of action of tyrosine kinase. 1. Receptor expression at membrane claveola 2. Ligand binding 3. Hetero/homodimerization leading to tyrosine kinase activation and tyrosine transphosphorylation 4. Signal transduction 5. Receptor internalization 6. Receptor degradation or re-expression.
Bottom Line: Tyrosine kinases are important mediators of the signaling cascade, determining key roles in diverse biological processes like growth, differentiation, metabolism and apoptosis in response to external and internal stimuli.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.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.

View Article: PubMed Central - PubMed

Affiliation: Department of Biotechnology, National Institute of Pharmaceutical Education and Research, Sector-67, S.A.S Nagar, Mohali, Punjab, India-160062.

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

No MeSH data available.


Related in: MedlinePlus