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Mutation Information
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Mutation Site
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T174I |
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Mutation Type
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Amino acid level |
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Gene/Protein/Region Type
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IN |
Literature Information
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PubMed PMID
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33316407
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Published Year
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2021 |
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Journal
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Bioorganic & medicinal chemistry letters |
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Title
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Discovery of novel HIV-1 integrase-LEDGF/p75 allosteric inhibitors based on a pyridine scaffold forming an intramolecular hydrogen bond. |
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Author
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Sugiyama S,Akiyama T,Taoda Y,Iwaki T,Matsuoka E,Akihisa E,Seki T,Yoshinaga T,Kawasuji T |
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Evidence
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Compound 34f exhibited better antiviral potency against WT and the T174I mutant (EC50 (WT) = 6.6 nM, EC50 (T174I) = 270 nM) than BI 224436 (EC50 (WT) = 22 nM, EC50 (T174I) > 5000 nM).
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