Kandjani Omid Jamshidi, Yaqoubi Shadi, Vahdati Samad Shams, Borhannejad Behnam, Dastmalchi Siavoush, Alizadeh Ali Akbar
Biotechnology Research Center, Tabriz University of Medical Sciences, Tabriz, Iran; Parmaceutical Analysis Research Center, Tabriz University of Medical Sciences, Tabriz, Iran.
Research Center for Integrative Medicine in Aging, Aging Research Institute, Tabriz University of Medical Sciences, Tabriz, Iran.
Eur J Med Chem. 2023 Mar 15;250:115182. doi: 10.1016/j.ejmech.2023.115182. Epub 2023 Feb 4.
Multiple sclerosis (MS) is a neurological disease that leads to severe physical and cognitive disabilities. Drugs used in the treatment of MS vary from small synthetic molecules to large macromolecules such as antibodies. Sphingosine 1-phosphate receptor modulators are frequently used for the treatment of MS. These medicines prevent the egress of lymphocytes from secondary lymphoid organs leading to immune system suppression. Currently, four S1PR modulators are on the market and several potential drug candidates are in clinical trials for the treatment of MS. These compounds differ in chemical structure, adverse effects, and efficacy points of view. The current article reviews the latest studies on S1PR1 modulators and compares them with other MS drugs in terms of efficacy, tolerability, and safety. A special focus was dedicated to discussing the structure-activity relationships of these compounds and performing a three-dimensional quantitative structure-activity relationship (3D-QSAR) analysis to gain better insight into the ligand-receptor interaction mode.
多发性硬化症(MS)是一种导致严重身体和认知残疾的神经系统疾病。用于治疗MS的药物从小分子合成物到诸如抗体等大分子各不相同。1-磷酸鞘氨醇受体调节剂常用于治疗MS。这些药物可防止淋巴细胞从次级淋巴器官流出,从而导致免疫系统受到抑制。目前,有四种1-磷酸鞘氨醇受体(S1PR)调节剂已上市,还有几种潜在的候选药物正在进行治疗MS的临床试验。从化学结构、不良反应和疗效角度来看,这些化合物各有不同。本文综述了关于S1PR1调节剂的最新研究,并在疗效、耐受性和安全性方面将它们与其他MS药物进行了比较。特别着重讨论了这些化合物的构效关系,并进行了三维定量构效关系(3D-QSAR)分析,以更好地洞察配体-受体相互作用模式。