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Novel adenosine-derived inhibitors of Cryptosporidium parvum inosine 5 '-monophosphate dehydrogenase

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Please use this identifier to cite or link to this item:http://hdl.handle.net/2115/78287

Title: Novel adenosine-derived inhibitors of Cryptosporidium parvum inosine 5 '-monophosphate dehydrogenase
Authors: Shigetomi, Kengo Browse this author →KAKEN DB
Sarwono, Albertus Eka Yudistira Browse this author
Ichikawa, Satoshi Browse this author →KAKEN DB
Ubukata, Makoto Browse this author →KAKEN DB
Issue Date: Dec-2019
Publisher: Nature Publishing Group
Journal Title: Journal of antibiotics
Volume: 72
Issue: 12
Start Page: 934
End Page: 942
Publisher DOI: 10.1038/s41429-019-0199-3
PMID: 31296916
Abstract: We have found cyclophane-type adenosine derivatives having p-quinone amide moieties (1 and 2) as weak inhibitors of Cryptosporidium parvum inosine 5'-monophosphate dehydrogenase (CpIMPDH) from the Hokkaido University Chemical Library via the luciferase-based high-throughput screening. To obtain more potent inhibitors, we synthesized four new derivatives free from cyclophane rings (3-6). The N-H derivatives 3 and 5 showed more potent activities (24.4 and 11.1 mu M, respectively) in the presence of dithiothreitol (DTT), whereas the N-methyl derivative 4 indicated more potent activity (2.1 mu M) without DTT. Conformational analysis of compounds 3 and 4 suggested that N-H amide 3 binds to IMP-binding site in the DTT mediated manner.
Type: article (author version)
URI: http://hdl.handle.net/2115/78287
Appears in Collections:農学院・農学研究院 (Graduate School of Agriculture / Faculty of Agriculture) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 重冨 顕吾

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