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Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Targeting Small Molecule Tyrosine Kinases by Polyphenols: New Move Towards Anti-tumor Drug Discovery
Nikhil S Sakle1, Shweta A More1, Sachin A Dhawale1
1Dr. Rafiq Zakaria Campus, Y. B. Chavan College of Pharmacy, Aurangabad-431001, Maharashtra, India.
Background:
Cancer is a complex disease involving genetic and epigenetic alteration that allows cells to escape normal homeostasis. Kinases play a crucial role in signaling pathways that regulate cell functions. Deregulation of kinases leads to a variety of pathological changes, activating cancer cell proliferation and metastases. The molecular mechanism of cancer is complex and the dysregulation of tyrosine kinases like Anaplastic Lymphoma Kinase (ALK), Bcr-Abl (Fusion gene found in patient with Chronic Myelogenous Leukemia (CML), JAK (Janus Activated Kinase), Src Family Kinases (SFKs), ALK (Anaplastic lymphoma Kinase), c-MET (Mesenchymal- Epithelial Transition), EGFR (Epidermal Growth Factor receptor), PDGFR (Platelet-Derived Growth Factor Receptor), RET (Rearranged during Transfection) and VEGFR (Vascular Endothelial Growth Factor Receptor) plays major role in the process of carcinogenesis. Recently, kinase inhibitors have overcome many problems of traditional cancer chemotherapy as they effectively separate out normal, non-cancer cells as well as rapidly multiplying cancer cells.
Methods:
Electronic databases were searched to explore the small molecule tyrosine kinases by polyphenols with the help of docking study (Glide-7.6 program interfaced with Maestro-v11.3 of Schrödinger 2017) to show the binding energies of polyphenols inhibitor with different tyrosine kinases in order to differentiate between the targets.
Results:
From the literature survey, it was observed that the number of polyphenols derived from natural sources alters the expression and signaling cascade of tyrosine kinase in various tumor models. Therefore, the development of polyphenols as a tyrosine kinase inhibitor against targeted proteins is regarded as an upcoming trend for chemoprevention.
Conclusion:
In this review, we have discussed the role of polyphenols as chemoreceptive which will help in future for the development and discovery of novel semisynthetic anticancer agents coupled with polyphenols.
Insights
Polyphenols from natural sources show potential as tyrosine kinase inhibitors for cancer chemoprevention. This study explores their role in altering tyrosine kinase signaling pathways for targeted cancer therapy.
Area of Science:
- Oncology
- Molecular Biology
- Pharmacology
Background:
- Cancer involves genetic and epigenetic alterations, with kinase deregulation driving proliferation and metastasis.
- Tyrosine kinases such as ALK, Bcr-Abl, JAK, and EGFR are critical in carcinogenesis.
- Kinase inhibitors offer a targeted approach to cancer therapy, distinguishing between normal and cancer cells.
Purpose of the Study:
- To explore small molecule tyrosine kinases targeted by polyphenols.
- To investigate the binding energies of polyphenol inhibitors with various tyrosine kinases using docking studies.
- To differentiate between polyphenol targets for potential anticancer drug development.
Main Methods:
- Electronic databases were searched for relevant studies.
- Docking studies were performed using Glide-7.6 and Maestro-v11.3 (Schrödinger 2017).
- Binding energies of polyphenol inhibitors with tyrosine kinases were analyzed.
Main Results:
- Polyphenols from natural sources can modulate tyrosine kinase expression and signaling in tumor models.
- This suggests polyphenols are a promising class of compounds for targeted cancer therapy.
- The development of polyphenols as tyrosine kinase inhibitors is an emerging trend in chemoprevention.
Conclusions:
- Polyphenols act as chemoreceptive agents with potential in cancer treatment.
- Further research can lead to the discovery of novel semisynthetic anticancer agents incorporating polyphenols.
- Polyphenols represent a viable strategy for developing targeted anticancer therapies.
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