Key Laboratory of Molecular Medicine and Biotherapy in the Ministry of Industry and Information Technology, Department of Biology, School of Life Sciences, Beijing Institute of Technology, Beijing, China.
Department of Biosciences, COMSATS University Islamabad, Sahiwal Campus, Islamabad, Pakistan.
J Cell Physiol. 2019 Aug;234(8):13263-13276. doi: 10.1002/jcp.27999. Epub 2018 Dec 19.
Schizophrenia (SZ) is a complex disabling disorder that leads to the mental disability and afflicts 1% of the world's total population and placed in top ten medical disorders. In current work, bioinformatics analyses were carried out on Trace amine (TA)-associated receptor 6 (TAAR6) to recognize the potential drugs and compounds against SZ. Comparative modeling and threading-based approaches were utilized for the structure prediction of TAAR6. Fifty-nine predicted structures were evaluated by various model assessment techniques and final model having only eight amino acids in the outlier region and 98.5% overall quality factor was chosen for further pharmacoinformatics and molecular docking analyses. From an extensive literature review, 11 Food and Drug Administration (FDA) approved drugs were analyzed by computational techniques and Aripiprazole was found as the most effective drug against SZ by targeting TAAR6. Here, we report five novel molecules which exhibited the highest binding affinity, effective drug properties, and interestingly, observed better results than the approved selected drugs against SZ by targeting TAAR6. The docking analyses revealed that Arg-92, Trp-98, Gln-191, Thr-192, Ala-290, Cys-291, Tyr-293, and Glu-294 residues were observed as critical interacting residues in receptor-ligand interactions. Absorption, distribution, metabolism, excretion, and toxicity (ADMET) properties, Lipinski rule of five, highest binding affinity coupled with virtual screening (VS), and pharmacophore modeling approach illustrated that aripiprazole (-8.6 kcal/mol) and TAAR6_0094 (-9.3 kcal/mol) are potential inhibitors for targeting TAAR6. It is suggested that schizophrenic patients have to use Aripiprazole for the medication of SZ by targeting TAAR6 and develop effective therapies by utilizing scrutinized novel compound.
精神分裂症(SZ)是一种复杂的致残性疾病,导致精神残疾,影响全球总人口的 1%,位列十大医学疾病之列。在当前的工作中,对痕量胺(TA)相关受体 6(TAAR6)进行了生物信息学分析,以识别潜在的抗 SZ 药物和化合物。采用比较建模和基于对接的方法进行 TAAR6 的结构预测。利用各种模型评估技术对 59 个预测结构进行了评估,最终选择了只有 8 个氨基酸处于异常区且整体质量系数为 98.5%的模型进行进一步的药物信息学和分子对接分析。通过广泛的文献回顾,对 11 种已获美国食品和药物管理局(FDA)批准的药物进行了计算技术分析,发现阿立哌唑通过靶向 TAAR6 是治疗 SZ 最有效的药物。在这里,我们报告了五个新分子,它们表现出最高的结合亲和力、有效的药物特性,并且有趣的是,通过靶向 TAAR6 观察到它们对 SZ 的治疗效果优于已批准的选定药物。对接分析表明,Arg-92、Trp-98、Gln-191、Thr-192、Ala-290、Cys-291、Tyr-293 和 Glu-294 残基被观察为受体-配体相互作用中的关键相互作用残基。吸收、分布、代谢、排泄和毒性(ADMET)特性、Lipinski 五规则、最高结合亲和力与虚拟筛选(VS)以及药效团建模方法表明,阿立哌唑(-8.6 kcal/mol)和 TAAR6_0094(-9.3 kcal/mol)是潜在的 TAAR6 靶向抑制剂。建议精神分裂症患者通过靶向 TAAR6 使用阿立哌唑治疗 SZ,并利用经过仔细筛选的新型化合物开发有效的治疗方法。