代谢型谷氨酸受体4（mGlu4）调节剂专利更新：2017年至今。
Update on mGlu4 modulator patents: 2017 to present.
作者信息
Rahman Fahad Imtiaz, Webster Thomas M, Hopkins Corey R
机构信息
Department of Pharmaceutical Sciences, College of Pharmacy, University of Nebraska Medical Center, Omaha, NE, USA.
Eppley Institute for Cancer Research, University of Nebraska Medical Center, Omaha, NE, USA.
出版信息
Expert Opin Ther Pat. 2025 May;35(5):463-475. doi: 10.1080/13543776.2025.2467679. Epub 2025 Feb 22.
INTRODUCTION
Metabotropic glutamate receptor 4 (mGluR4) regulates disease by modulating neurotransmitter release and synaptic plasticity and has been implicated in various diseases, including neurodegenerative disorders and psychiatric conditions, where its dysregulation can impact synaptic function and neuronal signaling.
AREAS COVERED
This review covers the patents and key literature concerning mGluR4 PAMs by utilizing the search engines: SciFinder, Google Patents, and PubMed from 2017 to 2024. It summarizes the key exemplified compounds, relevant SAR, and key biological data presented in the patents and primary literature. The key findings and potential path forward are also discussed.
EXPERT OPINION
The mGluR4 receptor serves as a novel target for the treatment of neurodegenerative disorders (namely Parkinson's disease), multiple sclerosis, and chronic pain along with other brain disorders. Two compounds have been advanced to early-stage clinical trials from Prexton Therapeutics and Appello Pharmaceuticals. The first compound from Prexton failed due to efficacy and the Appello compound has yet to have results disclosed. The results from this trial will be an important test for whether future mGluR4 PAMs are advanced into clinical trials.
引言
代谢型谷氨酸受体4（mGluR4）通过调节神经递质释放和突触可塑性来调控疾病，并且与包括神经退行性疾病和精神疾病在内的多种疾病有关，在这些疾病中其失调会影响突触功能和神经元信号传导。
涵盖领域
本综述利用2017年至2024年期间的SciFinder、谷歌专利和PubMed搜索引擎，涵盖了有关mGluR4正变构调节剂（PAMs）的专利和关键文献。它总结了专利和主要文献中呈现的关键示例化合物、相关的构效关系（SAR）以及关键生物学数据。还讨论了关键发现和潜在的前进方向。
专家观点
mGluR4受体是治疗神经退行性疾病（即帕金森病）、多发性硬化症和慢性疼痛以及其他脑部疾病的新靶点。来自Prexton Therapeutics和Appello Pharmaceuticals的两种化合物已进入早期临床试验。Prexton的第一种化合物因疗效问题失败，Appello的化合物尚未公布结果。该试验的结果对于未来mGluR4 PAMs是否推进到临床试验将是一项重要测试。
Zotero 插件