PI3K inhibitors: review and new strategies.

Author: JangHyunbum, NussinovRuth, ZhangMingzhen

Paper Details 
Original Abstract of the Article :
The search is on for effective specific inhibitors for PI3Kα mutants. PI3Kα, a critical lipid kinase, has two subunits, catalytic and inhibitory. PIK3CA, the gene that encodes the p110α catalytic subunit is a highly mutated protein in cancer. Dysregulation of PI3Kα signalling is commonly associated ...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7472334/

データ提供:米国国立医学図書館(NLM)

Targeting PI3Kα Mutants in Cancer: New Strategies on the Horizon

The field of cancer research is continuously seeking innovative approaches to combat this devastating disease. This study delves into the intricate world of PI3Kα, a crucial lipid kinase implicated in tumorigenesis and drug resistance. Researchers are actively pursuing strategies to develop effective and specific inhibitors for PI3Kα mutants, aiming to disrupt the aberrant signaling pathways that fuel cancer growth. The study explores various avenues, including the development of allosteric and orthosteric inhibitor combinations, as well as the exploitation of allosteric rescue mutations to guide drug discovery. These efforts hold promise for advancing personalized cancer therapies.

Reimagining PI3Kα Inhibition

The study sheds light on the challenges and opportunities associated with targeting PI3Kα mutants. While current ATP-competitive drugs often lead to concentration-dependent side effects, the researchers propose innovative approaches that hold promise for more effective and targeted therapies. These strategies include the development of allosteric inhibitors, which target different regions of the PI3Kα protein, and the exploitation of allosteric rescue mutations to guide drug discovery. These novel approaches offer hope for overcoming the limitations of existing therapies and advancing personalized cancer treatment.

The Promise of Personalized Cancer Therapies

This research underscores the importance of personalized medicine approaches in cancer treatment. By targeting the specific mutations that drive cancer growth, researchers can develop therapies that are more effective and have fewer side effects. This study serves as a testament to the ongoing pursuit of innovative strategies to combat cancer, offering hope for a future where personalized therapies are the norm.

Dr. Camel's Conclusion

The battle against cancer is like a relentless desert wind, constantly shifting and challenging. This study offers a beacon of hope, highlighting promising strategies for targeting PI3Kα mutants. These new approaches hold promise for more effective and personalized cancer therapies, offering the potential to harness the power of precision medicine to combat this formidable foe.

Date :
  1. Date Completed n.d.
  2. Date Revised 2023-11-04
Further Info :

Pubmed ID

32953006

DOI: Digital Object Identifier

PMC7472334

Related Literature

SNS
PICO Info
in preparation
Languages

English

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