4LKM

Crystal structure of Plk1 Polo-box domain in complex with PL-74

4LKM の概要

• エントリーDOI: 10.2210/pdb4lkm/pdb
• 関連するPDBエントリー: 4LKL
• 関連するBIRD辞書のPRD_ID: PRD_001159
• 分子名称: Serine/threonine-protein kinase PLK1, PL-74, SULFATE ION, ... (5 entities in total)
• 機能のキーワード: polo-box domain, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Nucleus: P53350
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 55909.71

構造登録者

Lee, W.C.,Song, J.H.,Kim, H.Y. (登録日: 2013-07-08, 公開日: 2013-12-11, 最終更新日: 2024-10-09)

主引用文献

Murugan, R.N.,Ahn, M.,Lee, W.C.,Kim, H.Y.,Song, J.H.,Cheong, C.,Hwang, E.,Seo, J.H.,Shin, S.Y.,Choi, S.H.,Park, J.E.,Bang, J.K.
Exploring the binding nature of pyrrolidine pocket-dependent interactions in the polo-box domain of polo-like kinase 1
Plos One, 8:e80043-e80043, 2013

PubMed Abstract: Over the years, a great deal of effort has been focused on the design and synthesis of potent, linear peptide inhibitors targeting the polo-like kinase 1 (Plk1), which is critically involved in multiple mitotic processes and has been established as an adverse prognostic marker for tumor patients. Plk1 localizes to its intracellular anchoring sites via its polo-box domain, and inhibiting the Plk1 polo-box domain has been considered as an approach to circumvent the specificity problems associated with inhibiting the conserved adenosine triphosphate-binding pocket. The polo-box domain consists of two different binding regions, such as the unique, broader pyrrolidine-binding pocket and the conserved, narrow, Tyr-rich hydrophobic channel, among the three Plk polo-box domains (Plks 1-3), respectively. Therefore, the studies that provide insights into the binding nature of the unique, broader pyrrolidine-binding pocket might lead to the development of selective Plk1-inhibitory compounds.

PubMed: 24223211
DOI: 10.1371/journal.pone.0080043

実験手法

X-RAY DIFFRACTION (2 Å)