Paper Details

  1. Home
  2. Paper Details

Biased allosteric activation of ketone body receptor HCAR2 suppresses inflammation.

Author: ChengLin, FuHong, FuPing, HuHongbo, LiZiyan, LiuYing, MaLiang, ShaoZhenhua, ShenChenglong, TianXiaowen, WangBo, WangChuanxin, WangHeli, WuChao, YanWei, YangShengyong, YuJingjing, ZhaoChang

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Overview

Compound 9n is a G<sub>i</sub>-biased allosteric modulator (BAM) of HCAR2. This study characterized compound 9n as a BAM of HCAR2 and demonstrated its anti-inflammatory efficacy in macrophages. The study also revealed the structural basis of compound 9n's action.
Paper Details　
Original Abstract of the Article :
Hydroxycarboxylic acid receptor 2 (HCAR2), modulated by endogenous ketone body &#946;-hydroxybutyrate and exogenous niacin, is a promising therapeutic target for inflammation-related diseases. HCAR2 mediates distinct pathophysiological events by activating G<sub>i/o</sub> protein or &#946;-arrestin ...See full text at original site
Dr.Camel IconDr.Camel's Paper Summary Blogラクダ博士について

ラクダ博士は、Health Journal が論文の内容を分かりやすく解説するために作成した架空のキャラクターです。
難解な医学論文を、専門知識のない方にも理解しやすいように、噛み砕いて説明することを目指しています。

* ラクダ博士による解説は、あくまで論文の要点をまとめたものであり、原論文の完全な代替となるものではありません。詳細な内容については、必ず原論文をご参照ください。
* ラクダ博士は架空のキャラクターであり、実際の医学研究者や医療従事者とは一切関係がありません。
* 解説の内容は Health Journal が独自に解釈・作成したものであり、原論文の著者または出版社の見解を反映するものではありません。


引用元：
https://doi.org/10.1016/j.molcel.2023.07.030

データ提供：米国国立医学図書館（NLM）

HCAR2: A New Target for Taming Inflammation

The quest for effective treatments for [inflammation] continues, with researchers exploring novel targets and therapeutic approaches. This research investigates the potential of [HCAR2], a receptor activated by [ketone bodies] and [niacin], as a therapeutic target for inflammation. The researchers utilized a [RAW264.7 macrophage] model to explore the effects of a specific HCAR2 modulator, [compound 9n], on inflammation. They discovered that compound 9n exhibits anti-inflammatory efficacy through a specific HCAR2-Gi pathway. This research provides valuable insights into the intricate molecular mechanisms underlying HCAR2 activation and its potential to modulate inflammation. It highlights the potential of developing biased allosteric modulators (BAMs) of HCAR2 as a promising therapeutic strategy for inflammation-related diseases.

Targeting HCAR2: A New Frontier in Inflammation Research

The study found that compound 9n, a biased allosteric modulator of HCAR2, demonstrated anti-inflammatory effects in vitro. This research suggests that targeting HCAR2, specifically through biased allosteric modulation, could be a promising strategy for treating inflammatory conditions. The study also highlights the importance of understanding the specific molecular pathways involved in HCAR2 activation for developing targeted and effective therapies.

Harnessing the Power of HCAR2: Hope for the Future

This research offers a glimmer of hope for developing novel treatments for inflammation. By targeting HCAR2 with biased allosteric modulators, researchers may be able to harness the receptor's anti-inflammatory potential while minimizing potential side effects. Further research is needed to fully understand the therapeutic potential of HCAR2 modulation for a range of inflammatory diseases.

Dr. Camel's Conclusion

HCAR2 is emerging as a promising target for inflammation research, with biased allosteric modulation offering a new strategy for developing safe and effective anti-inflammatory therapies. This research is a testament to the power of scientific inquiry to unlock novel therapeutic approaches, offering hope for future treatments for inflammatory conditions.

Date :
  1. Date Completed 2023-09-13
  2. Date Revised 2023-09-18
Further Info :

Pubmed ID

37597514

DOI: Digital Object Identifier

10.1016/j.molcel.2023.07.030

Related Literature

Article Analysis
・Effects of monomethyl fumarate
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.

This site uses cookies. Visit our privacy policy page or click the link in any footer for more information and to change your preferences.