4KXM

Crystal structure of DNPH1 (RCL) WITH N6-ISOPENTENYL-AMP

4KXM の概要

• エントリーDOI: 10.2210/pdb4kxm/pdb
• 関連するPDBエントリー: 4FYI 4KXL 4KXN
• 分子名称: 2'-deoxynucleoside 5'-phosphate N-hydrolase 1, N6-ISOPENTENYL-ADENOSINE-5'-MONOPHOSPHATE (3 entities in total)
• 機能のキーワード: deoxyribonucleoside 5'-monophosphate n-glycosidase, hydrolase
• 由来する生物種: Rattus norvegicus (brown rat,rat,rats)
• 細胞内の位置: Cytoplasm (By similarity): O35820
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 70362.75

構造登録者

Padilla, A.,Labesse, G.,Kaminski, P.A. (登録日: 2013-05-27, 公開日: 2014-02-05, 最終更新日: 2023-09-20)

主引用文献

Amiable, C.,Pochet, S.,Padilla, A.,Labesse, G.,Kaminski, P.A.
N (6)-substituted AMPs inhibit mammalian deoxynucleotide N-hydrolase DNPH1.
Plos One, 8:e80755-e80755, 2013

PubMed Abstract: The gene dnph1 (or rcl) encodes a hydrolase that cleaves the 2'-deoxyribonucleoside 5'-monophosphate (dNMP) N-glycosidic bond to yield a free nucleobase and 2-deoxyribose 5-phosphate. Recently, the crystal structure of rat DNPH1, a potential target for anti-cancer therapies, suggested that various analogs of AMP may inhibit this enzyme. From this result, we asked whether N (6)-substituted AMPs, and among them, cytotoxic cytokinin riboside 5'-monophosphates, may inhibit DNPH1. Here, we characterized the structural and thermodynamic aspects of the interactions of these various analogs with DNPH1. Our results indicate that DNPH1 is inhibited by cytotoxic cytokinins at concentrations that inhibit cell growth.

PubMed: 24260472
DOI: 10.1371/journal.pone.0080755

実験手法

X-RAY DIFFRACTION (2.24 Å)