Leitch A E, Haslett C, Rossi A G
MRC Centre for Inflammation Research, The Queen's Medical Research Institute, University of Edinburgh Medical School, 47 Little France Crescent, Edinburgh, UK.
Br J Pharmacol. 2009 Oct;158(4):1004-16. doi: 10.1111/j.1476-5381.2009.00402.x. Epub 2009 Sep 23.
The cyclin-dependent kinase inhibitor (CDKi) drugs such as R-roscovitine have emerged as potential anti-inflammatory, pharmacological agents that can influence the resolution of inflammation. Usually, once an inciting inflammatory stimulus has been eliminated, resolution proceeds by prompt, safe removal of dominant inflammatory cells. This is accomplished by programmed cell death (apoptosis) of prominent effector, inflammatory cells typified by the neutrophil. Apoptosis of neutrophils ensures that toxic neutrophil granule contents are securely packaged in apoptotic bodies and expedites phagocytosis by professional phagocytes such as macrophages. A panel of CDKi drugs have been shown to promote neutrophil apoptosis in a concentration- and time-dependent manner and the archetypal CDKi drug, R-roscovitine, overrides the anti-apoptotic effects of powerful survival factors [including lipopolysaccharide (LPS) and granulocyte macrophage-colony stimulating factor (GM-CSF)]. Inflammatory cell longevity and survival signalling is integral to the inflammatory process and any putative anti-inflammatory agent must unravel a complex web of redundancy in order to be effective. CDKi drugs have also been demonstrated to have significant effects on other cell types including lymphocytes and fibroblasts indicating that they may have pleiotropic anti-inflammatory, pro-resolution activity. In keeping with this, CDKi drugs like R-roscovitine have been reported to be efficacious in resolving established animal models of neutrophil-dominant and lymphocyte-driven inflammation. However, the mechanism of action behind these powerful effects has not yet been fully elucidated. CDKs play an integral role in the regulation of the cell cycle but are also recognized as participants in processes such as apoptosis and transcriptional regulation. Neutrophils have functional CDKs, are transcriptionally active and demonstrate augmented apoptosis in response to CDKi drugs, while lymphocyte proliferation and secretory function are inhibited. This review will discuss current understanding of the processes of inflammation and resolution but will focus on CDKis and their potential mechanisms of action.
细胞周期蛋白依赖性激酶抑制剂(CDKi)药物,如R - 罗可替尼,已成为具有潜在抗炎作用的药物,能够影响炎症的消退。通常,一旦引发炎症的刺激因素被消除,炎症的消退通过迅速、安全地清除主要炎症细胞来进行。这是通过以中性粒细胞为代表的主要效应炎症细胞的程序性细胞死亡(凋亡)来实现的。中性粒细胞的凋亡确保了有毒的中性粒细胞颗粒内容物被安全地包裹在凋亡小体中,并加速巨噬细胞等专业吞噬细胞的吞噬作用。一组CDKi药物已被证明能以浓度和时间依赖性方式促进中性粒细胞凋亡,而典型的CDKi药物R - 罗可替尼能克服强大的生存因子[包括脂多糖(LPS)和粒细胞巨噬细胞集落刺激因子(GM - CSF)]的抗凋亡作用。炎症细胞的寿命和生存信号是炎症过程不可或缺的一部分,任何假定的抗炎药物都必须解开一个复杂的冗余网络才能有效。CDKi药物也已被证明对包括淋巴细胞和成纤维细胞在内的其他细胞类型有显著影响,表明它们可能具有多效性的抗炎、促消退活性。与此一致的是,据报道,像R - 罗可替尼这样的CDKi药物在解决已建立的中性粒细胞为主和淋巴细胞驱动的炎症动物模型中是有效的。然而,这些强大作用背后的作用机制尚未完全阐明。细胞周期蛋白依赖性激酶(CDK)在细胞周期调控中起着不可或缺的作用,但也被认为参与凋亡和转录调控等过程。中性粒细胞具有功能性CDK,具有转录活性,并对CDKi药物表现出增强的凋亡反应,而淋巴细胞的增殖和分泌功能则受到抑制。本综述将讨论目前对炎症和消退过程的理解,但将重点关注CDKi及其潜在的作用机制。