磷酸二酯酶4的新型抑制剂Brilacidin治疗自身免疫和炎症疾病的潜力

2018-10-14 MedSci MedSci原创

Innovation生物制药公司近日提供了磷酸二酯酶4(PDE4)的新型抑制剂Brilacidin的最新信息。磷酸二酯酶4(PDE4)被认为是炎症治疗的新机制。

Innovation生物制药公司近日提供了磷酸二酯酶4PDE4)的新型抑制剂Brilacidin的最新信息。磷酸二酯酶4PDE4)被认为是炎症治疗的新机制。PDE4抑制剂,例如apremilastcrisaborole已陆续用于治疗各种自身免疫和炎性疾病。目前正在研究PDE4抑制剂治疗炎性肠病(IBD)的可能性。

由于介导多种免疫调节功能,防御素在皮肤和粘膜表面以及中性粒细胞中广泛表达,产生的小型抗微生物肽在介导人类健康和疾病中起关键作用。Brilacidin的设计以防御素为模型,已被证明是免疫反应的有效调节剂。它能够抑制各种促炎介质(例如,TNF-αIL-1βIL-8IL-6MMP-9MCP-1)。Brilacidin作用机制的一个潜在核心就是抑制磷酸二酯酶4PDE4)以及磷酸二酯酶3PDE3)的能力以调节环磷酸腺苷(cAMP)途径,这是一种既定的治疗靶点。

更详细地,临床前研究已经证明Brilacidin以剂量依赖性方式在体外抑制PDE4B2PDE3A。在基于细胞的测定中,表明Brilacidin具有良好的细胞膜通透性。


原始出处:

http://www.firstwordpharma.com/node/1597080#axzz5Trc0A3L7

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    2019-08-29 xlxchina
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    2019-03-20 zhouqu_8
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    2018-10-14 1241a1f8m26暂无昵称

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