Department of Neurobiology and Anatomy, W.M. Keck Center for the Neurobiology of Learning and Memory, McGovern Medical School of the University of Texas Health Science Center at Houston, Houston, TX, 77030, USA.
Department of Neurobiology and Behavior, University of California Irvine, Irvine, CA, 92697, USA.
J Comput Neurosci. 2021 Feb;49(1):37-56. doi: 10.1007/s10827-020-00771-4. Epub 2020 Nov 11.
Genetic disorders such as Rubinstein-Taybi syndrome (RTS) and Coffin-Lowry syndrome (CLS) cause lifelong cognitive disability, including deficits in learning and memory. Can pharmacological therapies be suggested that improve learning and memory in these disorders? To address this question, we simulated drug effects within a computational model describing induction of late long-term potentiation (L-LTP). Biochemical pathways impaired in these and other disorders converge on a common target, histone acetylation by acetyltransferases such as CREB binding protein (CBP), which facilitates gene induction necessary for L-LTP. We focused on four drug classes: tropomyosin receptor kinase B (TrkB) agonists, cAMP phosphodiesterase inhibitors, histone deacetylase inhibitors, and ampakines. Simulations suggested each drug type alone may rescue deficits in L-LTP. A potential disadvantage, however, was the necessity of simulating strong drug effects (high doses), which could produce adverse side effects. Thus, we investigated the effects of six drug pairs among the four classes described above. These combination treatments normalized impaired L-LTP with substantially smaller individual drug 'doses'. In addition three of these combinations, a TrkB agonist paired with an ampakine and a cAMP phosphodiesterase inhibitor paired with a TrkB agonist or an ampakine, exhibited strong synergism in L-LTP rescue. Therefore, we suggest these drug combinations are promising candidates for further empirical studies in animal models of genetic disorders that impair histone acetylation, L-LTP, and learning.
遗传疾病,如 Rubinstein-Taybi 综合征(RTS)和 Coffin-Lowry 综合征(CLS),会导致终身认知障碍,包括学习和记忆缺陷。是否可以提出药物治疗方法来改善这些疾病的学习和记忆能力?为了解决这个问题,我们在描述晚期长时程增强(L-LTP)诱导的计算模型中模拟了药物效应。这些和其他疾病中受损的生化途径汇聚到一个共同的靶点,即乙酰转移酶 CREB 结合蛋白(CBP)引起的组蛋白乙酰化,这有助于 L-LTP 所需的基因诱导。我们专注于四类药物:原肌球蛋白受体激酶 B(TrkB)激动剂、cAMP 磷酸二酯酶抑制剂、组蛋白去乙酰化酶抑制剂和ampakines。模拟表明,每种药物类型单独使用都可能挽救 L-LTP 缺陷。然而,一个潜在的缺点是需要模拟强药物效应(高剂量),这可能会产生不良反应。因此,我们研究了上述四类药物中的六种药物组合的效果。这些联合治疗用显著较小的单个药物“剂量”使受损的 L-LTP 正常化。此外,这六种组合中的三种,TrkB 激动剂与ampakine 联合,以及 cAMP 磷酸二酯酶抑制剂与 TrkB 激动剂或 ampakine 联合,在 L-LTP 挽救方面表现出很强的协同作用。因此,我们建议这些药物组合是进一步在遗传疾病动物模型中进行实验研究的有前途的候选药物,这些疾病会损害组蛋白乙酰化、L-LTP 和学习能力。