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Bryostatin-1: pharmacology and therapeutic potential as a CNS drug.

机译:Bryostatin-1:作为CNS药物的药理学和治疗潜力。

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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.
机译:Bryostatin-1是一种功能强大的蛋白激酶C(PKC)激动剂,可在纳摩尔浓度下激活PKC同工酶。 bryostatin-1的药理研究主要集中在其预防肿瘤生长的作用上。然而,新兴证据表明,bryostatin-1表现出其他重要的药理活性。在临床前研究中,已经显示了适当剂量的bryostatin-1具有认知修复和抗抑郁作用。潜在的药理学机制可能涉及激活PKC同工酶,诱导长期记忆所需的蛋白质合成,恢复应激诱发的PKC活性抑制以及减少神经毒性淀粉样蛋白的积累和tau蛋白的过度磷酸化。 bryostatin-1作为CNS药物的治疗潜力应进一步探索。

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