1Z6P

Glycogen phosphorylase AMP site inhibitor complex

1Z6P の概要

• エントリーDOI: 10.2210/pdb1z6p/pdb
• 関連するPDBエントリー: 1Z6Q
• 分子名称: Glycogen phosphorylase, muscle form, 4-{2-[(3-NITROBENZOYL)AMINO]PHENOXY}PHTHALIC ACID (3 entities in total)
• 機能のキーワード: glycogen metabolism; glycogen phosphorylase b; inhibition; allosteric, transferase
• 由来する生物種: Oryctolagus cuniculus (rabbit)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 97941.66

構造登録者

Kristiansen, M.,Andersen, B.,Iversen, L.F.,Westergaard, N. (登録日: 2005-03-23, 公開日: 2005-04-12, 最終更新日: 2025-03-26)

主引用文献

Kristiansen, M.,Andersen, B.,Iversen, L.F.,Westergaard, N.
Identification, synthesis and chracterization of new glycogen phosphorylase inhibitors binding to the allosteric AMP site
J.Med.Chem., 47:3537-3545, 2004

PubMed Abstract: Inhibition of glycogen phosphorylase (GP) has attracted considerable attention during the last five to 10 years as a means of treating the elevated hepatic glucose production seen in patients with type 2 diabetes. Several different GP inhibitors binding to various binding sites of the GP enzyme have been reported in the literature. In this paper we report on a novel class of compounds that have been identified as potent GP inhibitors. Their synthesis, mode of binding to the allosteric AMP site as well as in vitro data on GP inhibition are shown. The most potent inhibitor was found to be 4-[2,4-bis-(3-nitrobenzoylamino)phenoxy]phthalic acid (4j) with an IC(50) value of 74 nM. This compound together with a closely related analogue was further characterized by enzyme kinetics and in primary rat hepatocytes.

PubMed: 15214781
DOI: 10.1021/jm031121n

実験手法

X-RAY DIFFRACTION (2.4 Å)