Plateforme de Physiologie et Physiopathologie Cardiovasculaires (P2C), Laboratoire des Biomolécules, Venins et Applications Théranostiques (LR20IPT01), Institut Pasteur de Tunis, Université Tunis El Manar, Tunis 1068, Tunisia.
Laboratory of Biotechnology and Bio-Geo Resources Valorization (LR11ES31), Higher Institute of Biotechnology of Sidi Thabet (ISBST), University of Manouba, Tunis 2010, Tunisia.
Toxins (Basel). 2022 Nov 11;14(11):787. doi: 10.3390/toxins14110787.
Lebetin 2 (L2), a natriuretic-like peptide (NP), exerts potent cardioprotection in myocardial infarction (MI), with stronger effects than B-type natriuretic peptide (BNP). To determine the molecular mechanisms underlying its cardioprotection effect, we used molecular modeling, molecular docking and molecular dynamics (MD) simulation to describe the binding mode, key interaction residues as well as mechanistic insights into L2 interaction with NP receptors (NPRs). L2 binding affinity was determined for human, rat, mouse and chicken NPRs, and the stability of receptor-ligand complexes ascertained during 100 ns-long MD simulations. We found that L2 exhibited higher affinity for all human NPRs compared to BNP, with a rank preference for NPR-A > NPR-C > NPR-B. Moreover, L2 affinity for human NPR-A and NPR-C was higher in other species. Both docking and MD studies revealed that the NPR-C-L2 interaction was stronger in all species compared to BNP. Due to its higher affinity to human receptors, L2 could be used as a therapeutic approach in MI patients. Moreover, the stronger interaction of L2 with NPR-C could highlight a new L2 signaling pathway that would explain its additional effects during cardiac ischemia. Thus, L2 is a promising candidate for drug design toward novel compounds with high potency, affinity and stability.
利贝汀 2(L2)是一种利尿钠肽(NP),在心肌梗死(MI)中具有强大的心脏保护作用,其效果强于 B 型利钠肽(BNP)。为了确定其心脏保护作用的分子机制,我们使用分子建模、分子对接和分子动力学(MD)模拟来描述 L2 与 NP 受体(NPRs)的结合模式、关键相互作用残基以及相互作用的机制见解。我们确定了 L2 与人、大鼠、小鼠和鸡 NPRs 的结合亲和力,并在 100ns 长的 MD 模拟过程中确定了受体-配体复合物的稳定性。我们发现,与 BNP 相比,L2 对所有人类 NPRs 的亲和力更高,对 NPR-A>NPR-C>NPR-B 的亲和力偏好程度更高。此外,L2 对人类 NPR-A 和 NPR-C 的亲和力在其他物种中更高。对接和 MD 研究均表明,与 BNP 相比,L2 与 NPR-C 的相互作用在所有物种中更强。由于其对人类受体的亲和力更高,L2 可作为 MI 患者的治疗方法。此外,L2 与 NPR-C 的更强相互作用可能突出了一种新的 L2 信号通路,该通路可以解释其在心脏缺血期间的额外作用。因此,L2 是一种很有前途的候选药物,可用于设计具有高效力、亲和力和稳定性的新型化合物。