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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。

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