Paper Details 
Original Abstract of the Article :
Dual TK inhibitors have shown significant clinical effects against many tumors, but with unmanageable side effects. Design approach and selectivity of these inhibitors plays substantial role in their potency and side-effects. Understanding the homology of binding sites in targeted receptors, and inv...See full text at original site
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引用元:
https://doi.org/10.1016/j.bioorg.2021.105358

データ提供:米国国立医学図書館(NLM)

Developing Targeted Anticancer Agents: A Pharmacophore-Based Approach

Cancer is a complex disease characterized by uncontrolled cell growth. One promising approach to treating cancer involves targeting specific proteins that are involved in tumor growth and development. This research focuses on the development of dual tyrosine kinase inhibitors (TKIs), which target two important proteins involved in cancer cell growth: VEGFR-2 and EGFR. These inhibitors are designed to block the signaling pathways that promote tumor growth.

This study used a pharmacophore-based approach to design new dual TKIs with improved selectivity and potency. The researchers identified key structural features of the inhibitors that are essential for binding to the target proteins. They then synthesized a series of benzylideneindolon-2-one derivatives based on these structural features.

The study found that one of the synthesized compounds, 5b, showed significant activity against both VEGFR-2 and EGFR. Moreover, this compound exhibited selective toxicity against cancer cells that overexpress these target proteins. These findings suggest that 5b has the potential to be a highly effective and selective anticancer agent.

The Promise of Targeted Therapy for Cancer

This research highlights the potential of targeted therapy for treating cancer. By specifically targeting proteins that drive tumor growth, these therapies can potentially kill cancer cells while minimizing damage to healthy cells. This approach could lead to more effective and less toxic cancer treatments.

The Importance of Selectivity in Anticancer Therapy

Selectivity is essential for the development of safe and effective anticancer agents. By targeting specific proteins involved in tumor growth, these agents can potentially kill cancer cells while minimizing damage to healthy cells. This research underscores the importance of designing anticancer drugs with high selectivity to maximize their effectiveness and minimize their side effects.

Dr.Camel's Conclusion

This research is like a journey through a vast and intricate desert, where every step leads to a new discovery. By exploring the intricate world of protein interactions, researchers are developing targeted therapies that can potentially revolutionize the treatment of cancer. It's a reminder that with perseverance and ingenuity, we can conquer even the most challenging obstacles.

Date :
  1. Date Completed 2022-01-04
  2. Date Revised 2022-01-04
Further Info :

Pubmed ID

34544029

DOI: Digital Object Identifier

10.1016/j.bioorg.2021.105358

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SNS
PICO Info
in preparation
Languages

English

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