Zhang Jing, Zhai Jiadai, Liu Hui, Liu Hongying, Sun Bingxia, Gao Jie, Sang Feng
School of Life Sciences and Medicine, Shandong University of Technology, Zibo, 255049, People's Republic of China.
Department of Pharmacy, Zibo Vocational Institute, Zibo, 255300, People's Republic of China.
Mol Divers. 2025 Jun 14. doi: 10.1007/s11030-025-11242-2.
The phosphodiesterase 4B (PDE4B) subtype, a member of the phosphodiesterase (PDE) family, plays a key role in promoting anti-inflammatory and antifibrotic effects by controlling the rate of cyclic adenosine phosphate degradation. To date, inhibitors targeting PDE4B have been widely used in the development of therapeutic agents for pulmonary fibrosis, inflammation, cancer, Alzheimer's disease, adipose tissue dysfunction and chronic liver injury. With the development of techniques such as molecular docking studies, more and more PDE4B inhibitors with different core scaffolds have been discovered, and at least six of these molecular structures have been approved for marketing or entered clinical studies. In this work, we reviewed the PDE4B inhibitors reported in the literature since 2014 and classified the most representative examples with different biological activities according to their structural characteristics. We also made a preliminary analysis of their structure-activity relationship based on the classification results and the conclusions reported in the relevant literature. In addition, we describe the inhibition selectivity of some compounds to PDE4B and PDE4D enzymes, as inhibition of PDE4D is often associated with side effects such as nausea and emesis. We hope that this work will help researchers in the design and optimization of novel PDE4B selective inhibitors and provide a reference for readers who are new to this field.
磷酸二酯酶4B(PDE4B)亚型是磷酸二酯酶(PDE)家族的成员之一,通过控制环磷酸腺苷的降解速率,在促进抗炎和抗纤维化作用中发挥关键作用。迄今为止,靶向PDE4B的抑制剂已广泛应用于肺纤维化、炎症、癌症、阿尔茨海默病、脂肪组织功能障碍和慢性肝损伤治疗药物的研发。随着分子对接研究等技术的发展,越来越多具有不同核心骨架的PDE4B抑制剂被发现,其中至少有六种分子结构已获批准上市或进入临床研究。在这项工作中,我们回顾了自2014年以来文献报道的PDE4B抑制剂,并根据其结构特征对具有不同生物活性的最具代表性的实例进行了分类。我们还根据分类结果和相关文献报道的结论,对它们的构效关系进行了初步分析。此外,我们描述了一些化合物对PDE4B和PDE4D酶的抑制选择性,因为抑制PDE4D通常会伴有恶心和呕吐等副作用。我们希望这项工作将有助于研究人员设计和优化新型PDE4B选择性抑制剂,并为该领域的新手读者提供参考。