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趋化因子受体信号转导中的偏倚。

Bias in chemokine receptor signalling.

机构信息

Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.

Division of Medicinal Chemistry, Leiden Academic Centre for Drug Research, Leiden University, Einsteinweg 55, 2333 CC Leiden, The Netherlands.

出版信息

Trends Immunol. 2014 Jun;35(6):243-52. doi: 10.1016/j.it.2014.02.004. Epub 2014 Mar 26.

Abstract

Chemokine receptors are widely expressed on a variety of immune cells and play a crucial role in normal physiology as well as in inflammatory and infectious diseases. The existence of 23 chemokine receptors and 48 chemokine ligands guarantees a tight control and fine-tuning of the immune system. Here, we discuss the multiple regulatory mechanisms of chemokine signalling at a systemic, cellular, and molecular level. In particular, we focus on the impact of biased signalling at the receptor level; an emerging concept in molecular pharmacology. An improved understanding of these mechanisms may provide a framework for more effective drug discovery and development at a target class that is so relevant for immune function.

摘要

趋化因子受体广泛表达于各种免疫细胞上,在正常生理以及炎症和感染性疾病中发挥着至关重要的作用。23 种趋化因子受体和 48 种趋化因子配体的存在保证了免疫系统的严密控制和精细调节。在这里,我们在系统、细胞和分子水平上讨论了趋化因子信号的多种调节机制。特别是,我们关注的是受体水平上偏向信号传递的影响,这是分子药理学中的一个新兴概念。对这些机制的更好理解可能为在这个与免疫功能密切相关的靶点类别中进行更有效的药物发现和开发提供一个框架。

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