Identification of new EphA4 inhibitors by virtual screening of FDA-approved drugs.

Author: FuAmy K Y, FuWing-Yu, GuShuo, HuangXuhui, IpFanny C F, IpNancy Y, TongEstella Pui Sze

Paper Details 
Original Abstract of the Article :
The receptor tyrosine kinase, erythropoietin-producing hepatocellular A4 (EphA4), was recently identified as a molecular target for Alzheimer's disease (AD). We found that blockade of the interaction of the receptor and its ligands, ephrins, alleviates the disease phenotype in an AD transgenic mouse...See full text at original site
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引用元:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5943255/

データ提供:米国国立医学図書館(NLM)

Identification of New EphA4 Inhibitors by Virtual Screening of FDA-Approved Drugs

The quest for new Alzheimer's disease (AD) treatments, like searching for a hidden oasis in the desert, requires innovative approaches. This research explores the potential of repurposing existing FDA-approved drugs to target EphA4, a receptor tyrosine kinase implicated in AD. The researchers employed a virtual screening approach to identify five FDA-approved drugs - ergoloid, cyproheptadine, nilotinib, abiraterone, and retapamulin - as potential inhibitors of EphA4. Further biochemical and cellular assays confirmed the inhibitory activity of these drugs, highlighting nilotinib as a promising candidate due to its ability to inhibit the binding of EphA4 and its ligand, ephrin-A, at micromolar scale.

A New Oasis in the Desert of AD Research: Repurposing FDA-Approved Drugs

This study presents a novel approach to drug discovery, suggesting that repurposing existing FDA-approved drugs can offer a faster and more efficient path to developing new AD treatments. The identification of nilotinib as a potential EphA4 inhibitor opens up exciting new avenues for exploring the therapeutic potential of existing medications.

Navigating the Desert of AD: Hope for a Healthier Future

The search for effective treatments for AD is ongoing. This research offers a glimmer of hope by exploring new strategies to combat this debilitating disease. Continued research and innovation are crucial for developing new therapies and improving the lives of individuals affected by AD.

Dr. Camel's Conclusion

This study demonstrates the potential of repurposing FDA-approved drugs to identify new treatments for Alzheimer's disease. The identification of nilotinib as a potential EphA4 inhibitor offers a promising new avenue for research and development.

Date :
  1. Date Completed 2019-10-17
  2. Date Revised 2023-11-12
Further Info :

Pubmed ID

29743517

DOI: Digital Object Identifier

PMC5943255

Related Literature

SNS
PICO Info
in preparation
Languages

English

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