Bryostatin-1: Pharmacology and Therapeutic Potential as a CNS Drug

Miao-Kun Sun, Daniel L. Alkon
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引用次数: 95

Abstract

Bryostatin-1 is a powerful protein kinase C (PKC) agonist, activating PKC isozymes at nanomolar concentrations. Pharmacological studies of bryostatin-1 have mainly been focused on its action in preventing tumor growth. Emerging evidence suggests, however, that bryostatin-1 exhibits additional important pharmacological activities. In preclinical studies bryostatin-1 has been shown at appropriate doses to have cognitive restorative and antidepressant effects. The underlying pharmacological mechanisms may involve an activation of PKC isozymes, induction of synthesis of proteins required for long-term memory, restoration of stress-evoked inhibition of PKC activity, and reduction of neurotoxic amyloid accumulation and tau protein hyperphosphorylation. The therapeutic potential of bryostatin-1 as a CNS drug should be further explored.

苔藓虫素-1:作为中枢神经系统药物的药理学和治疗潜力
苔藓虫素-1是一种强大的蛋白激酶C (PKC)激动剂,在纳摩尔浓度下激活PKC同工酶。苔藓虫素-1的药理研究主要集中在其抑制肿瘤生长的作用上。然而,新出现的证据表明苔藓虫素-1具有其他重要的药理活性。在临床前研究中,苔藓抑素-1在适当剂量下具有认知恢复和抗抑郁作用。潜在的药理学机制可能涉及PKC同工酶的激活,诱导长期记忆所需蛋白质的合成,恢复应激引起的PKC活性抑制,减少神经毒性淀粉样蛋白积累和tau蛋白过度磷酸化。苔藓虫素-1作为中枢神经系统药物的治疗潜力有待进一步挖掘。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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