6BT5

Human mGlu8 Receptor complexed with L-AP4

6BT5 の概要

• エントリーDOI: 10.2210/pdb6bt5/pdb
• 分子名称: Metabotropic glutamate receptor 8, (2S)-2-amino-4-phosphonobutanoic acid, 2-acetamido-2-deoxy-beta-D-glucopyranose, ... (4 entities in total)
• 機能のキーワード: mglur8, grm8, l-ap4, gene id: 2918, signaling protein
• 由来する生物種: Homo sapiens (Human)
• 細胞内の位置: Cell membrane; Multi-pass membrane protein: O00222
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 107819.47

構造登録者

Schkeryantz, J.M.,Chen, Q.,Ho, J.D.,Atwell, S.,Zhang, A.,Vargas, M.C.,Wang, J.,Monn, J.A.,Hao, J. (登録日: 2017-12-05, 公開日: 2018-02-07, 最終更新日: 2024-11-06)

主引用文献

Schkeryantz, J.M.,Chen, Q.,Ho, J.D.,Atwell, S.,Zhang, A.,Vargas, M.C.,Wang, J.,Monn, J.A.,Hao, J.
Determination of L-AP4-bound human mGlu8 receptor amino terminal domain structure and the molecular basis for L-AP4's group III mGlu receptor functional potency and selectivity.
Bioorg. Med. Chem. Lett., 28:612-617, 2018

PubMed Abstract: L-2-Amino-4-phosphonobutyric acid (L-AP4) is a known potent and selective agonist for the Group III mGlu receptors. However, it does not show any selectivity among the individual group III mGlu subtypes. In order to understand the molecular basis for this group selectivity, we solved the first human mGlu8 amino terminal domain (ATD) crystal structures in complex with L-glu and L-AP4. In comparison with other published L-glu-bound mGlu ATD structures, we have observed L-glu binds in a significantly different manner in mGlu1. Furthermore, these new structures provided evidence that both the electronic and steric nature of the distal phosphate of L-AP4 contribute to its exquisite Group III functional agonist potency and selectivity.

PubMed: 29402739
DOI: 10.1016/j.bmcl.2018.01.037

実験手法

X-RAY DIFFRACTION (2.92 Å)