Structure–Activity Relationship Study on Col-003, a Protein–Protein Interaction Inhibitor between Collagen and Hsp47
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- Yoshida Masahito
- Graduate School of Pharmaceutical Science, Tohoku University
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- Saito Masazumi
- Graduate School of Pharmaceutical Science, Tohoku University
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- Ito Shinya
- Institute for Protein Dynamics, Kyoto Sangyo University
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- Ogawa Koji
- National Institute of Advanced Industrial Science and Technology (AIST)
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- Goshima Naoki
- National Institute of Advanced Industrial Science and Technology (AIST)
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- Nagata Kazuhiro
- Institute for Protein Dynamics, Kyoto Sangyo University
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- Doi Takayuki
- Graduate School of Pharmaceutical Science, Tohoku University Graduate School of Life Sciences, Tohoku University
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<p>This study demonstrates the structure–activity relationship of Col-003, a potent collagen–heat-shock protein 47 (Hsp47) interaction inhibitor. Col-003 analogues were successfully synthesized by Pd(0)-catalyzed cross-coupling reactions of 5-bromosalicylaldehyde derivatives with alkyl–metal species, and the inhibitory activities of the synthetic analogues were evaluated using surface plasmon resonance analysis (BIAcore). We succeeded in discovering two potent inhibitors that showed 85 and 81% inhibition at a concentration of 1.9 µM against the collagen–Hsp47 interaction. This indicates that elongation of an alkyl linker between two aromatic rings could considerably improve inhibitory activity due to the adjustment of a pendant phenyl moiety to an appropriate position, in addition to the hydrophobic interaction with an alkyl linker moiety.</p>
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 68 (3), 220-226, 2020-03-01
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390002184879012224
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- NII論文ID
- 130007804070
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- HANDLE
- 2241/0002001710
- 10097/00128316
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- NDL書誌ID
- 030275072
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- PubMed
- 31582590
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- 本文言語コード
- en
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- データソース種別
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- IRDB
- NDL
- Crossref
- PubMed
- CiNii Articles
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