An Innovative High-Throughput Screening Approach for Discovery of Small Molecules That Inhibit TNF Receptors.

Author: BawaskarPrachi, BrummelBenjamin E, ChiuTing-Lan, GrantBenjamin D, LewisAndrew K, LoChih Hung, SachsJonathan N, SchaafTory M, ThomasDavid D, VunnamNagamani

Paper Details 
Original Abstract of the Article :
Tumor necrosis factor receptor 1 (TNFR1) is a transmembrane receptor that binds tumor necrosis factor or lymphotoxin-alpha and plays a critical role in regulating the inflammatory response. Upregulation of these ligands is associated with inflammatory and autoimmune diseases. Current treatments redu...See full text at original site
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引用元:
https://pubmed.ncbi.nlm.nih.gov/28530838

データ提供:米国国立医学図書館(NLM)

Targeting the Root of Inflammation: A Novel Approach

Inflammation is a complex process, often involving the interplay of multiple receptors and signaling pathways. The tumor necrosis factor receptor 1 (TNFR1), a key player in the inflammatory response, has long been a target for drug development. This study delves into a novel approach for inhibiting TNFR1 activation, focusing on the interactions between the receptor itself rather than the ligands that bind to it.

Unlocking the Secrets of Receptor Interactions

The authors developed a TNFR1 FRET biosensor, a clever tool that allowed them to screen for compounds that disrupt the interactions between TNFR1 molecules. Through this innovative high-throughput screening approach, they identified two small-molecule compounds, zafirlukast and triclabendazole, that inhibit TNFR1-induced IκBα degradation and NF-κB activation. Imagine a camel caravan, where the camels are TNFR1 molecules, and the researchers are finding ways to disrupt the caravan's formation and prevent its journey. This research offers a promising new avenue for developing targeted anti-inflammatory therapies.

A New Era of Anti-Inflammatory Therapies

This study highlights the potential for developing drugs that specifically target the interactions between receptor molecules, rather than relying on blocking the ligands that bind to them. This approach could lead to more effective and selective anti-inflammatory therapies, with fewer off-target effects. Imagine a camel caravan traveling through the desert, where the researchers are able to specifically disrupt the communication between the camels, without affecting the caravan's overall journey. This research offers a glimpse into a new era of anti-inflammatory therapies, where we can precisely target the root of inflammation.

Dr.Camel's Conclusion

This groundbreaking study introduces a new approach to inhibiting TNFR1 activation, focusing on the interactions between the receptor molecules themselves. The authors demonstrate the feasibility of this approach through the identification of two promising small-molecule compounds. This research offers a promising new avenue for developing targeted anti-inflammatory therapies, with the potential to improve patient outcomes and reduce the side effects associated with current treatment options. It's a reminder that even in the vast and complex desert of inflammatory diseases, there are new oases of innovation waiting to be discovered.
Date :
  1. Date Completed 2019-06-27
  2. Date Revised 2022-08-30
Further Info :

Pubmed ID

28530838

DOI: Digital Object Identifier

S2472-5552(22)07026-5

SNS
PICO Info
in preparation
Languages

English

Positive IndicatorAn AI analysis index that serves as a benchmark for how positive the results of the study are. Note that it is a benchmark and requires careful interpretation and consideration of different perspectives.

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