开发一种光反应性拮抗剂。

Developing a photoreactive antagonist.

作者信息

England Pamela M

机构信息

Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA, USA.

出版信息

Methods Mol Biol. 2013;995:121-9. doi: 10.1007/978-1-62703-345-9_9.

DOI:10.1007/978-1-62703-345-9_9

PMID:23494376

Abstract

Light is an exquisite reagent for controlling the activity of biological systems, often offering improved temporal and spatial resolution over strictly genetic, biochemical, or pharmacological manipulations. This chapter describes a general approach for developing small molecules that, upon irradiation with light, may be used to rapidly inactivate targeted proteins expressed on the surfaces of cells. Highlighted is ANQX, a photoreactive AMPA receptor antagonist developed to irreversibly inactivate a subtype of glutamate-gated ion channels natively expressed on neurons.

摘要

光作为一种用于控制生物系统活性的精妙试剂，相较于单纯的基因、生化或药理学操作，它往往能提供更高的时间和空间分辨率。本章描述了一种开发小分子的通用方法，这些小分子在光照后可用于快速使细胞表面表达的靶向蛋白质失活。重点介绍的是ANQX，一种光反应性AMPA受体拮抗剂，其开发目的是不可逆地使神经元天然表达的谷氨酸门控离子通道的一个亚型失活。