The cyclic dinucleotide c-di-GMP is known as an important second messenger in bacteria, which controls various important cellular processes, such as cell differentiation, biofilm formation and virulence factors production. It is extremely vital for the development of new antibacterial agents by virtue of blocking c-di-GMP signal conduction. Current research indicates that there are three potential targets for discovering new antibacterial agents based on c-di-GMP regulated signal pathway, which are c-di-GMP synthases, c-di-GMP degrading enzymes and c-di-GMP receptors. Herein, we review small molecules that have been developed to inhibit c-di-GMP related enzymes and indicate perspectives of c-di-GMP inhibitors.
环二鸟苷酸 (Bis-(3′-5′) cyclic diguanylic acid, c-di-GMP) 是细菌所特有的一类核酸类第二信使，参与并调节细菌多种生理功能，包括细胞分化、生物被膜的形成以及致病因子的产生等。阻断c-di-GMP 信号的传导对于发展新型抗菌药物具有重要的意义。现有研究结果表明，基于c-di-GMP 调控的信号通路开发新型抗菌药物具有3 类潜在的靶点，分别是c-di-GMP 合成酶 (DGCs)、c-di-GMP 降解酶 (PDEs) 以及c-di-GMP 受体。文中根据上述3 类关键靶点，介绍了相关小分子抑制剂的研究进展，并展望了c-di-GMP 信号分子抑制剂的发展方向。.
Keywords: c-di-GMP; diguanylatecyclases; inhibitors; phosphodiesterases; receptors.