title: Developing a photoreactive antagonist.
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.
authors.affiliation: Department of Pharmaceutical Chemistry, University of California San Francisco, San Francisco, CA, USA.
authors.forename: Pamela M
authors.initials: PM
authors.lastname: England
mesh_terms: D000818:Animals; D001386:Azides / Q000737:chemistry / Q000528:radiation effects; D001577:Benzophenones / Q000737:chemistry / Q000528:radiation effects; D003432:Cross-Linking Reagents / Q000737:chemistry / Q000528:radiation effects; D015195:Drug Design; D018691:Excitatory Amino Acid Antagonists / Q000737:chemistry / Q000528:radiation effects; D008027:Light; D055668:Photochemical Processes; D011810:Quinoxalines / Q000737:chemistry / Q000528:radiation effects; D018091:Receptors, AMPA / Q000037:antagonists & inhibitors*
chemical_list: D001386:Azides; D001577:Benzophenones; D003432:Cross-Linking Reagents; D018691:Excitatory Amino Acid Antagonists; D011810:Quinoxalines; D018091:Receptors, AMPA