Abstract

Advances in molecular and cellular biology, as well as the development of chemical synthesis and modern technologies, enriched the contemporary experimental research with new directions in which light plays a key role as a tool for modulating biological functions. One of them is photopharmacology, a field that uses chemically synthesized light-controlled compounds that can modulate the functions of proteins. When illuminated at specific wavelengths, these synthetic photoswitches are capable of modulating functions of receptors, ion channels and enzymes. This review briefly describes compounds that modulate the functions of ionotropic Cys-loop receptors for acetylcholine, GABA, and glycine. The nicotinic acetylcholine receptor (nAChR) is the first receptor-operated channel for which a way of modulation using light-dependent molecules has been discovered. In the 1970s–80s, blockers and activators of nAChR were created, consisting of azobenzene (light-controlled switch) and agonists. In the current millennium, new compounds have been created to provide light-controlled modulation of nAChR activity. These new photochromes are selective to muscle and neuronal nAChR, and are promising to study the physiological role of nAChRs in the nervous system. An extensive library of photochromic compounds is available for light-controlling of GABA receptor function. Some of them modulate the activity via interaction with the agonist site, the others are light-controlled blockers of chloride-selective ion channels. Recently, the first two photochromic modulators of glycine receptor activity have also been developed. These achievements demonstrate that photopharmacology opens up unique possibilities for remote control of physiological functions, as well as for studying the processes of inhibition and excitation in neural networks and models of neuronal pathologies.

中文翻译：

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半胱氨酸环配体门离子通道的光致变色调制。

摘要

分子和细胞生物学的进步以及化学合成和现代技术的发展，以新的方向丰富了当代的实验研究，其中光在调节生物学功能中起着关键作用。其中之一是光药理学，该领域使用化学合成的光控化合物来调节蛋白质的功能。当以特定波长照射时，这些合成光电开关能够调节受体，离子通道和酶的功能。这篇综述简要描述了可调节离子性Cys环受体的乙酰胆碱，GABA和甘氨酸功能的化合物。烟碱乙酰胆碱受体（nAChR）是第一个受体操纵的通道，已为其发现了一种使用光依赖性分子的调节方式。在1970年代至80年代，nAChR的阻滞剂和激活剂被创造出来，其中包括偶氮苯（光控开关）和激动剂。在当前的千年中，已经开发出新的化合物以提供nAChR活性的光控调节。这些新的光致色素对肌肉和神经元nAChR具有选择性，并有望研究nAChR在神经系统中的生理作用。大量的光致变色化合物库可用于GABA受体功能的光控制。它们中的一些通过与激动剂位点的相互作用来调节活性，其他的是氯离子选择性离子通道的光控阻滞剂。最近，甘氨酸受体活性的前两个光致变色调节剂也已经开发出来。这些成就表明，光药理学为生理功能的远程控制以及研究神经网络和神经元病理模型中的抑制和兴奋过程开辟了独特的可能性。