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Updated: Jun 4, 2026

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking
11:57

Using an α-Bungarotoxin Binding Site Tag to Study GABA A Receptor Membrane Localization and Trafficking

Published on: March 28, 2014

断片の成長は,アセチルコリン結合タンパク質の構造変化を誘導する:構造的および熱力学的分析

Ewald Edink1, Prakash Rucktooa, Kim Retra

  • 1Leiden/Amsterdam Center of Drug Research (LACDR), Division of Medicinal Chemistry, Faculty of Sciences, VU University Amsterdam, The Netherlands.

Journal of the American Chemical Society
|February 17, 2011
PubMed
まとめ

フラグメントベース・ドラッグ・ディスカバリー (Fragment-based drug discovery, FBDD) は,フラグメントを高親和性鉛化合物に最適化するために使用されました. 熱力学分析とX線結晶学により,アセチルコリン結合タンパク質 (AChBP) 内での特定の結合相互作用が明らかになりました.

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Indirect-Acting Cholinergic Agonists: Mechanism of Action

Indirect-acting cholinergic agonists work by interacting with an enzyme called acetylcholinesterase (AChE) in the synaptic cleft. They can be reversible or irreversible inhibitors and have different effects on the enzyme.
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Direct-Acting Cholinergic Agonists: Chemistry and Structure-Activity Relationship

Cholinergic agonists or cholinomimetics mimic the action of acetylcholine to stimulate the parasympathetic nervous system. They are categorized into direct-acting and indirect-acting agents. The direct-acting cholinergic drugs induce the parasympathetic response by directly binding to the muscarinic or nicotine receptors. In comparison, the indirect-acting cholinergic drugs prevent acetylcholine hydrolysis, indirectly contributing to the extended parasympathetic response.
The direct-acting...