Computational Biomedicine, Institute for Advanced Simulation IAS-5/Institute for Neuroscience and Medicine INM-9, Forschungszentrum Jülich GmbH, Wilhelm-Johnen-Straße, D-52428 Jülich, Germany.
Dipartimento di Bioscienze, Università degli Studi di Milano, Via Celoria 26, I-20133 Milan, Italy.
J Chem Inf Model. 2023 May 22;63(10):2911-2917. doi: 10.1021/acs.jcim.3c00380. Epub 2023 May 5.
Atomistic-level investigation of olfactory receptors (ORs) is a challenging task due to the experimental/computational difficulties in the structural determination/prediction for members of this family of G-protein coupled receptors. Here, we have developed a protocol that performs a series of molecular dynamics simulations from a set of structures predicted by recent machine learning algorithms and apply it to a well-studied receptor, the human OR51E2. Our study demonstrates the need for simulations to refine and validate such models. Furthermore, we demonstrate the need for the sodium ion at a binding site near D and E to stabilize the inactive state of the receptor. Considering the conservation of these two acidic residues across human ORs, we surmise this requirement also applies to the other ∼400 members of this family. Given the almost concurrent publication of a CryoEM structure of the same receptor in the active state, we propose this protocol as an complement to the growing field of ORs structure determination.
由于在结构测定/预测方面存在实验/计算上的困难,对嗅觉受体(OR)进行原子水平的研究是一项具有挑战性的任务。 在这里,我们开发了一种方案,该方案可以根据最近的机器学习算法预测的一组结构执行一系列分子动力学模拟,并将其应用于研究充分的受体,即人 OR51E2。 我们的研究表明,需要模拟来完善和验证此类模型。 此外,我们还证明了在 D 和 E 附近的结合部位需要钠离子来稳定受体的非活性状态。 考虑到这两个酸性残基在人类 OR 中的保守性,我们推测这一要求也适用于该家族的其他约 400 个成员。 鉴于同一受体的活性状态的 CryoEM 结构几乎同时发表,我们建议将该方案作为 OR 结构测定领域不断发展的补充。