Institute of Pharmacology and the Gaston H. Glock Research Laboratories for Exploratory Drug Development, Center of Physiology and Pharmacology, Medical University of Vienna, 1090 Vienna, Austria.
Int J Mol Sci. 2019 Oct 28;20(21):5365. doi: 10.3390/ijms20215365.
Kinetic models have been employed to understand the logic of substrate transport through transporters of the Solute Carrier (SLC) family. All SLC transporters operate according to the alternate access model, which posits that substrate transport occurs in a closed loop of partial reactions (i.e., a transport cycle). Kinetic models can help to find realistic estimates for conformational transitions between individual states of the transport cycle. When constrained by experimental results, kinetic models can faithfully describe the function of a candidate transporter at a pre-steady state. In addition, we show that kinetic models can accurately predict the intra- and extracellular substrate concentrations maintained by the transporter at a steady state, even under the premise of loose coupling between the electrochemical gradient of the driving ion and of the substrate. We define the criteria for the design of a credible kinetic model of the SLC transporter. Parsimony is the guiding principle of kinetic modeling. We argue, however, that the level of acceptable parsimony is limited by the need to account for the substrate gradient established by a secondary active transporter, and for random order binding of co-substrates and substrate. Random order binding has consistently been observed in transporters of the SLC group.
动力学模型已被用于理解溶质载体(SLC)家族转运体的底物运输逻辑。所有 SLC 转运体都按照交替访问模型运作,该模型假定底物运输发生在部分反应的闭环中(即运输循环)。动力学模型可以帮助找到运输循环中各个状态之间构象转变的现实估计值。当受到实验结果的限制时,动力学模型可以忠实地描述候选转运体在预稳定状态下的功能。此外,我们还表明,动力学模型即使在驱动离子和底物的电化学梯度之间存在松散耦合的前提下,也可以准确预测转运体在稳定状态下维持的细胞内和细胞外底物浓度。我们定义了 SLC 转运体可信动力学模型设计的标准。简约性是动力学建模的指导原则。然而,我们认为,可接受的简约程度受到需要考虑由二次主动转运体建立的底物梯度以及共底物和底物的随机顺序结合的限制。随机顺序结合在 SLC 组的转运体中一直被观察到。