Bioingeniería, Universidad El Bosque, Bogotá 110121, Colombia.
Química Farmacéutica, Facultad de Ciencias, Universidad El Bosque, Bogotá 110121, Colombia.
Molecules. 2020 Nov 25;25(23):5509. doi: 10.3390/molecules25235509.
Dopamine (DA) is an important neurotransmitter with a fundamental role in regulatory functions related to the central, peripheral, renal, and hormonal nervous systems. Dopaminergic neurotransmission dysfunctions are commonly associated with several diseases; thus, in situ quantification of DA is a major challenge. To achieve this goal, enzyme-based biosensors have been employed for substrate recognition in the past. However, due to their sensitivity to changes in temperature and pH levels, new peptide bioreceptors have been developed. Therefore, in this study, four bioreceptors were designed in silico to exhibit a higher affinity for DA than the DA transporters (DATs). The design was based on the hot spots of the active sites of crystallized enzyme structures that are physiologically related to DA. The affinities between the chosen targets and designed bioreceptors were calculated using AutoDock Vina. Additionally, the binding free energy, ∆G, of the dopamine-4xp1 complex was calculated by molecular dynamics (MD). This value presented a direct relationship with the E_refine value obtained from molecular docking based on the ∆G functions obtained from MOE of the promising bioreceptors. The control variables in the design were amino acids, bond type, steric volume, stereochemistry, affinity, and interaction distances. As part of the results, three out of the four bioreceptor candidates presented promising values in terms of DA affinity and distance.
多巴胺(DA)是一种重要的神经递质,在与中枢、外周、肾脏和激素神经系统相关的调节功能中起着基础性作用。多巴胺能神经传递功能障碍通常与多种疾病有关;因此,DA 的原位定量是一个主要挑战。为了实现这一目标,过去曾采用基于酶的生物传感器进行底物识别。然而,由于其对温度和 pH 值变化的敏感性,已经开发出了新的肽类生物受体。因此,在这项研究中,设计了四个生物受体,以比多巴胺转运蛋白(DAT)具有更高的 DA 亲和力。设计是基于与生理上与 DA 相关的结晶酶结构的活性位点热点。使用 AutoDock Vina 计算所选靶标和设计生物受体之间的亲和力。此外,通过分子动力学(MD)计算多巴胺-4xp1 复合物的结合自由能,∆G。该值与基于有前途的生物受体的 MOE 获得的∆G 函数从分子对接获得的 E_refine 值呈直接关系。设计中的控制变量是氨基酸、键类型、立体体积、立体化学、亲和力和相互作用距离。作为结果的一部分,四个生物受体候选者中有三个在 DA 亲和力和距离方面表现出了有前途的价值。