5W8B

Carbonic anhydrase II in complex with activating histamine pyridinium derivative

5W8B の概要

• エントリーDOI: 10.2210/pdb5w8b/pdb
• 分子名称: Carbonic anhydrase 2, ZINC ION, Hexafluorophosphate anion, ... (6 entities in total)
• 機能のキーワード: complex, activator, ligand, lyase
• 由来する生物種: Homo sapiens (Human)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 29507.52

構造登録者

Bhatt, A.,Ilies, M.,McKenna, R. (登録日: 2017-06-21, 公開日: 2018-05-30, 最終更新日: 2023-10-04)

主引用文献

Bhatt, A.,Mondal, U.K.,Supuran, C.T.,Ilies, M.A.,McKenna, R.
Crystal Structure of Carbonic Anhydrase II in Complex with an Activating Ligand: Implications in Neuronal Function.
Mol. Neurobiol., 55:7431-7437, 2018

PubMed Abstract: Carbonic anhydrase (CA) plays a key role in neuronal signaling, providing bicarbonate and proton ions for GABAergic and glutamatergic neuronal function. Activation of CA isoforms expressed in neurons have been shown to have implications in the prognosis of Alzheimer's disease and dementia, while inhibitors of CAs are clinically used in the treatment of epilepsy, emphasizing the importance of this family of enzymes in both disease and normal neuronal function. Previously, compounds have been reported to enhance activity of CAs in an aging rat model, but their mechanism of action was not known. We report the 1.6 Å resolution structure of an imidazole-based CA activator in complex with the ubiquitously-expressed human CA II. Based on the structure, a proposed mechanism of CA activation by the compound and its potential applications in the neurobiology of aging are discussed.

PubMed: 29423818
DOI: 10.1007/s12035-017-0854-2

実験手法

X-RAY DIFFRACTION (1.601 Å)