• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

9-脱氮鸟嘌呤衍生物:作为哺乳动物嘌呤核苷磷酸化酶多底物类似物抑制剂的合成及抑制特性

9-Deazaguanine derivatives: synthesis and inhibitory properties as multi-substrate analogue inhibitors of mammalian PNPs.

作者信息

Yatsu Tomoyuki, Hashimoto Mariko, Hikishima Sadao, Magnowska Lucyna, Bzowska Agnieszka, Yokomatsu Tsutomu

机构信息

School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, Hachiouji, Tokyo 192-0392, Japan.

出版信息

Nucleic Acids Symp Ser (Oxf). 2008(52):661-2. doi: 10.1093/nass/nrn334.

DOI:10.1093/nass/nrn334
PMID:18776553
Abstract

9-(5',5'-Difluoro-5'-phosphonopentyl)-9-deazaguanine (DFPP-DG) and its related analogues were designed as multi-substrate analogue inhibitors of purine nucleoside phosphorylase (PNP) on the basis of the X-ray crystallographic data obtained for the binary complex of 9-(5',5'-difluoro-5'-phosphonopentyl)guanine (DFPP-G) with calf spleen PNP. One of these analogues, homo-DFPP-DG was found to be a very potent PNP inhibitor at an intracellular (approximately 1 mM) phosphate concentration.

摘要

9-(5',5'-二氟-5'-膦酰戊基)-9-脱氮鸟嘌呤(DFPP-DG)及其相关类似物,是基于9-(5',5'-二氟-5'-膦酰戊基)鸟嘌呤(DFPP-G)与小牛脾脏嘌呤核苷磷酸化酶(PNP)二元复合物的X射线晶体学数据,设计而成的嘌呤核苷磷酸化酶(PNP)多底物类似物抑制剂。其中一种类似物,高同型DFPP-DG,发现在细胞内磷酸盐浓度(约1 mM)下是一种非常有效的PNP抑制剂。

相似文献

1
9-Deazaguanine derivatives: synthesis and inhibitory properties as multi-substrate analogue inhibitors of mammalian PNPs.9-脱氮鸟嘌呤衍生物:作为哺乳动物嘌呤核苷磷酸化酶多底物类似物抑制剂的合成及抑制特性
Nucleic Acids Symp Ser (Oxf). 2008(52):661-2. doi: 10.1093/nass/nrn334.
2
Synthesis and evaluation of 9-deazaguanine derivatives as multi-substrate analogue inhibitors of PNP.9-脱氮鸟嘌呤衍生物作为嘌呤核苷磷酸化酶多底物类似物抑制剂的合成与评价
Nucleic Acids Symp Ser (Oxf). 2007(51):431-2. doi: 10.1093/nass/nrm216.
3
Synthesis and biological evaluation of 9-deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid as multi-substrate analogue inhibitors of PNP.通过连接基与二氟亚甲基膦酸相连的9-脱氮鸟嘌呤衍生物作为嘌呤核苷磷酸化酶多底物类似物抑制剂的合成及生物学评价
Bioorg Med Chem Lett. 2007 Aug 1;17(15):4173-7. doi: 10.1016/j.bmcl.2007.05.054. Epub 2007 May 21.
4
1.45 A resolution crystal structure of recombinant PNP in complex with a pM multisubstrate analogue inhibitor bearing one feature of the postulated transition state.1.45 重组 PNP 与带有推测过渡态特征之一的 pM 多底物类似物抑制剂复合物的分辨率晶体结构。
Biochem Biophys Res Commun. 2010 Jan 1;391(1):703-8. doi: 10.1016/j.bbrc.2009.11.124. Epub 2009 Nov 26.
5
Structural-based design and synthesis of novel 9-deazaguanine derivatives having a phosphate mimic as multi-substrate analogue inhibitors for mammalian PNPs.基于结构的新型 9-去氮杂鸟嘌呤衍生物的设计与合成,其作为多底物类似物抑制剂,模拟磷酸盐,用于哺乳动物 PNPs。
Bioorg Med Chem. 2010 Mar 15;18(6):2275-2284. doi: 10.1016/j.bmc.2010.01.062. Epub 2010 Feb 4.
6
Calf spleen purine-nucleoside phosphorylase: crystal structure of the binary complex with a potent multisubstrate analogue inhibitor.小牛脾脏嘌呤核苷磷酸化酶:与一种强效多底物类似物抑制剂形成的二元复合物的晶体结构
Acta Crystallogr D Biol Crystallogr. 2004 Aug;60(Pt 8):1417-24. doi: 10.1107/S0907444904013861. Epub 2004 Jul 21.
7
Synthesis and biological evaluation of 9-(5',5'-difluoro-5'-phosphonopentyl)guanine derivatives for PNP-inhibitors.用于PNP抑制剂的9-(5',5'-二氟-5'-膦酰基戊基)鸟嘌呤衍生物的合成及生物学评价
Bioorg Med Chem. 2006 Mar 1;14(5):1660-70. doi: 10.1016/j.bmc.2005.10.017. Epub 2005 Nov 2.
8
9-Deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid are slow-binding picomolar inhibitors of trimeric purine nucleoside phosphorylase.通过连接子将 9-去氮鸟嘌呤衍生物与二氟亚甲基膦酸连接的化合物是三聚合嘌呤核苷磷酸化酶的缓慢结合皮摩尔抑制剂。
FEBS J. 2010 Apr;277(7):1747-60. doi: 10.1111/j.1742-4658.2010.07598.x. Epub 2010 Feb 24.
9
Thermodynamic studies of interactions of calf spleen PNP with acyclic phosphonate inhibitors.小牛脾磷酸核糖焦磷酸酶与无环膦酸酯抑制剂相互作用的热力学研究。
Nucleic Acids Symp Ser (Oxf). 2008(52):663-4. doi: 10.1093/nass/nrn335.
10
Antiproliferative activity of purine nucleoside phosphorylase multisubstrate analogue inhibitors containing difluoromethylene phosphonic acid against leukaemia and lymphoma cells.含二氟亚甲基膦酸的嘌呤核苷磷酸化酶多底物类似物抑制剂对白血病和淋巴瘤细胞的抗增殖活性。
Chem Biol Drug Des. 2010 Apr;75(4):392-9. doi: 10.1111/j.1747-0285.2009.00939.x. Epub 2010 Jan 19.