Nicotinic Acid Adenine Dinucleotide Phosphate Analogues Substituted on the Nicotinic Acid and Adenine Ribosides. Effects on ReceptorMediated Ca²⁺ Release.
Nicotinic Acid Adenine Dinucleotide Phosphate Analogues Substituted on the Nicotinic Acid and Adenine Ribosides. Effects on ReceptorMediated Ca²⁺ Release.
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烟酸腺嘌呤二核苷酸磷酸类似物在烟酸和腺嘌呤核苷上取代。对受体介导的Ca²⁺释放的影响。
DOI：
10.1021/acs.jmedchem.5b00279
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发表时间：
2015-04-23
影响因子：
7.3
通讯作者：
Slama, James T.
中科院分区：
文献类型：
--
作者：
Trabbic, Christopher J.;Zhang, Fan;Walseth, Timothy F.;Slama, James T.
烟酸腺嘌呤二核苷酸磷酸（NAADP）是哺乳动物和棘皮动物细胞内释放Ca ~（2+）的第二信使。我们报告，在烟酸5-位引入的大的官能化取代基被海胆受体识别，尽管激动剂效力损失20-500倍。5-（3-叠氮基丙基）-NAADP释放Ca 2+的EC 50为31 µM，与NAADP竞争受体结合的IC 50为56 nM。带电荷的基团连接到NAADP的烟酸与活性的丧失有关，这表明烟酸核苷部分被认为是中性的两性糖基化酶。取代基（Br-和N3-）可以在NAADP的8-腺苷位置引入，同时保持高效力和激动剂功效，并且还认识到在烟酸的5-位置和8-腺苷位置两者处取代的NAADP衍生物，尽管激动剂效力显著降低。
Nicotinic acid adenine dinucleotide phosphate (NAADP) is a Ca2+ releasing intracellular second messenger in both mammals and echinoderms. We report that large functionalized substituents introduced at the nicotinic acid 5-position are recognized by the sea urchin receptor, albeit with a 20–500 fold loss in agonist potency. 5-(3-Azidopropyl)-NAADP was shown to release Ca2+ with an EC50 of 31 µM and to compete with NAADP for receptor binding with an IC50 of 56 nM. Attachment of charged groups to the nicotinic acid of NAADP is associated with loss of activity, suggesting that the nicotinate riboside moiety is recognized as a neutral zwitterion. Substituents (Br- and N3-) can be introduced at the 8-adenosyl position of NAADP while preserving high potency and agonist efficacy and an NAADP derivative substituted at both the 5-position of the nicotinic acid and at the 8-adenosyl position was also recognized although the agonist potency was significantly reduced.
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影响因子：
9.2
作者：
Bak, J;Billington, RA;Genazzani, AA
通讯作者：
Genazzani, AA
影响因子：
16.6
作者：
Dowden, J;Moreau, C;Potter, BVL
通讯作者：
Potter, BVL
DOI：
10.1083/jcb.150.3.581
发表时间：
2000-08-07
期刊：
The Journal of cell biology
影响因子：
--
作者：
Berg I;Potter BV;Mayr GW;Guse AH
通讯作者：
Guse AH
影响因子：
64.5
作者：
Cang C;Zhou Y;Navarro B;Seo YJ;Aranda K;Shi L;Battaglia-Hsu S;Nissim I;Clapham DE;Ren D
通讯作者：
Ren D
影响因子：
4.8
作者：
Aarhus, R;Dickey, DM;Lee, HC
通讯作者：
Lee, HC