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利用合成配体和天然配体在体内靶向G蛋白偶联受体以调控炎症反应的可能性。

Possible targeting of G protein coupled receptors to manipulate inflammation in vivo using synthetic and natural ligands.

作者信息

Kinsel J F, Sitkovsky M V

出版信息

Ann Rheum Dis. 2003 Nov;62 Suppl 2(Suppl 2):ii22-4. doi: 10.1136/ard.62.suppl_2.ii22.

Abstract

Cyclic AMP elevating Gs protein coupled receptors were considered for a long time to be immunosuppressive. One of these receptors, adenosine A(2A) receptor, was implicated in a physiological mechanism that down regulates inflammation and protects tissues from excessive immune mediated damage. Targeting of these receptors by selective agonists may lead to better protocols of anti-inflammatory treatments. At the same time inhibiting the Gs protein coupled mediated signalling with antagonists could be explored in studies of approaches to enhance inflammation and tissue damage. Enhancement of targeted tissue damage is highly desirable when it is cancerous tissue, while enhancement of inflammatory events might be desirable in the development of new vaccine adjuvants.

摘要

长期以来,环磷酸腺苷(cAMP)升高的Gs蛋白偶联受体被认为具有免疫抑制作用。这些受体之一,即腺苷A(2A)受体,参与了一种下调炎症并保护组织免受过度免疫介导损伤的生理机制。通过选择性激动剂靶向这些受体可能会带来更好的抗炎治疗方案。同时,在增强炎症和组织损伤的研究中,可以探索用拮抗剂抑制Gs蛋白偶联介导的信号传导。当靶向组织为癌组织时,增强靶向组织损伤是非常可取的,而在开发新型疫苗佐剂时,增强炎症反应可能是可取的。

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