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Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase
Nicotinamide adenine dinucleotide (NAD), one of the most important coenzymes in the cells, is a substrate of the signaling enzyme CD38, by which NAD is converted to a second messenger, cyclic ADP-ribose, which releases calcium from intracellular calcium stores. Starting with 2′-deoxy-2′-fluoroarabin...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271716/ https://www.ncbi.nlm.nih.gov/pubmed/25268725 http://dx.doi.org/10.3390/molecules191015754 |
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author | Wang, Shengjun Zhu, Wenjie Wang, Xuan Li, Jianguo Zhang, Kehui Zhang, Liangren Zhao, Yong-Juan Lee, Hon Cheung Zhang, Lihe |
author_facet | Wang, Shengjun Zhu, Wenjie Wang, Xuan Li, Jianguo Zhang, Kehui Zhang, Liangren Zhao, Yong-Juan Lee, Hon Cheung Zhang, Lihe |
author_sort | Wang, Shengjun |
collection | PubMed |
description | Nicotinamide adenine dinucleotide (NAD), one of the most important coenzymes in the cells, is a substrate of the signaling enzyme CD38, by which NAD is converted to a second messenger, cyclic ADP-ribose, which releases calcium from intracellular calcium stores. Starting with 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamide adenine dinucleotide (ara-F NAD), a series of NAD analogues were synthesized and their activities to inhibit CD38 NAD glycohydrolase (NADase) were evaluated. The adenosine-modified analogues showed potent inhibitory activities, among which 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamideguanine dinucleotide (ara-F NGD) was the most effective one. The structure-activity relationship of NAD analogues was also discussed. |
format | Online Article Text |
id | pubmed-6271716 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62717162018-12-27 Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase Wang, Shengjun Zhu, Wenjie Wang, Xuan Li, Jianguo Zhang, Kehui Zhang, Liangren Zhao, Yong-Juan Lee, Hon Cheung Zhang, Lihe Molecules Article Nicotinamide adenine dinucleotide (NAD), one of the most important coenzymes in the cells, is a substrate of the signaling enzyme CD38, by which NAD is converted to a second messenger, cyclic ADP-ribose, which releases calcium from intracellular calcium stores. Starting with 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamide adenine dinucleotide (ara-F NAD), a series of NAD analogues were synthesized and their activities to inhibit CD38 NAD glycohydrolase (NADase) were evaluated. The adenosine-modified analogues showed potent inhibitory activities, among which 2′-deoxy-2′-fluoroarabinosyl-β-nicotinamideguanine dinucleotide (ara-F NGD) was the most effective one. The structure-activity relationship of NAD analogues was also discussed. MDPI 2014-09-29 /pmc/articles/PMC6271716/ /pubmed/25268725 http://dx.doi.org/10.3390/molecules191015754 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Wang, Shengjun Zhu, Wenjie Wang, Xuan Li, Jianguo Zhang, Kehui Zhang, Liangren Zhao, Yong-Juan Lee, Hon Cheung Zhang, Lihe Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title | Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title_full | Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title_fullStr | Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title_full_unstemmed | Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title_short | Design, Synthesis and SAR Studies of NAD Analogues as Potent Inhibitors towards CD38 NADase |
title_sort | design, synthesis and sar studies of nad analogues as potent inhibitors towards cd38 nadase |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271716/ https://www.ncbi.nlm.nih.gov/pubmed/25268725 http://dx.doi.org/10.3390/molecules191015754 |
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