Tsai Yung-Fong, Yang Shun-Chin, Hwang Tsong-Long
Department of Anesthesiology, Chang Gung Memorial Hospital, Linkou Medical Center, Taoyuan, Taiwan.
Graduate Institute of Clinical Medical Sciences, College of Medicine, Chang Gung University, Taoyuan, Taiwan.
Expert Opin Ther Pat. 2025 Aug;35(8):839-857. doi: 10.1080/13543776.2025.2515882. Epub 2025 Jun 11.
Formyl peptide receptors (FPRs) belong to the family of class A G-protein-coupled receptors that are important for immune modulation and inflammation and are emerging as potential therapeutic targets for several inflammatory diseases. FPRs have shown therapeutic roles in the management of cardiovascular diseases, neuroinflammation, and cancer. Biased agonists are an active topic in the further revisions that encompass the utilization of a definite subset of signaling pathways to improve therapeutic maladies, in parallel with reducing the negative effects.
This review surveys the modulators of FPR1 and FPR2 that have been published in patents from 2021 to 2024, to summarize the categorization of agonists and antagonists and discuss their possible clinical uses. A targeted patent search was performed using the Taiwan Patent GO Showcases database (https://tiponet.tipo.gov.tw/gpss/).
We examine newly disclosed patents concerning FPR modulators, with all specified compounds classified as either FPR1 or FPR2 modulators. Receptor cross-reactivity, ligand promiscuity, and receptor variations across species are challenges encountered during drug formulation. Further research into different types of biased agonists and the synthesis of potent and selective ligands is essential to overcome these obstacles and facilitate the eventual therapeutic use of biased signaling in inflammation and diseases.
甲酰肽受体(FPRs)属于A类G蛋白偶联受体家族,对免疫调节和炎症反应至关重要,并且正成为多种炎症性疾病潜在的治疗靶点。FPRs在心血管疾病、神经炎症和癌症的治疗中已显示出治疗作用。偏向性激动剂是进一步研究中的一个热门话题,包括利用特定的信号通路子集来改善治疗疾病,同时减少负面影响。
本综述调查了2021年至2024年专利中公布的FPR1和FPR2调节剂,总结激动剂和拮抗剂的分类,并讨论它们可能的临床用途。使用台湾专利GO展示数据库(https://tiponet.tipo.gov.tw/gpss/)进行了有针对性的专利检索。
我们研究了有关FPR调节剂的新公开专利,所有指定化合物分为FPR1或FPR2调节剂。受体交叉反应性、配体混杂性以及物种间的受体变异是药物研发过程中遇到的挑战。进一步研究不同类型的偏向性激动剂以及合成强效和选择性配体对于克服这些障碍并促进偏向性信号在炎症和疾病中的最终治疗应用至关重要。