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Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine
https://repo.qst.go.jp/records/49236
https://repo.qst.go.jp/records/4923612b460ca-c4c0-4187-a7b3-b35853d1e390
| Item type | 学術雑誌論文 / Journal Article(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2018-10-29 | |||||
| タイトル | ||||||
| タイトル | Identification of Highly Potent Human Immunodeficiency Virus Type-1 Protease Inhibitors against Lopinavir and Darunavir Resistant Viruses from Allophenylnorstatine-Based Peptidomimetics with P2 Tetrahydrofuranylglycine | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
| 資源タイプ | journal article | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 著者 |
Hidaka, Koushi
× Hidaka, Koushi× Kimura, Tooru× Sankaranarayanan, Rajesh× Wang, Jun× F. McDaniel, Keith× J. Kempf, Dale× Kameoka, Masanori× Adachi, Motoyasu× Kuroki, Ryota× Jeffrey-Tri, Nguyen× Hayashi, Yoshio× Kiso, Yoshiaki× Adachi, Motoyasu |
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| 抄録 | ||||||
| 内容記述タイプ | Abstract | |||||
| 内容記述 | The emergence of drug-resistant HIV from a wide spreading anti-viral chemotherapy targeting the HIV protease in the past decades is unavoidable and provides a challenge to develop alternative inhibitors. We synthesized a series of allophenylnorstatine-based peptidomimetics with various P3, P2 and P2´ moieties. The derivatives with P2 tetrahydrofuranylglycine (Thfg) were found to be potent against wild type HIV-1 protease and the virus, identifying a highly potent compound 21f (KNI-1657) against lopinavir/ritonavir- or darunavir-resistant strains. Co-crystal structures of 21f and the wild-type protease revealed numerous key hydrogen bonding interactions with the Thfg. These results suggest that the strategy to design allophenylnorstatine-based peptidomimetics combined with Thfg residue would be promising for generating candidates to overcome multi-drug resistance. | |||||
| 書誌情報 |
Journal of Medicinal Chemistry 巻 61, 号 12, p. 5138-5153, 発行日 2018-11 |
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| 出版者 | ||||||
| 出版者 | ELSEVIER | |||||
| ISSN | ||||||
| 収録物識別子タイプ | ISSN | |||||
| 収録物識別子 | 0022-2623 | |||||
| DOI | ||||||
| 識別子タイプ | DOI | |||||
| 関連識別子 | 10.1021/acs.jmedchem.7b01709 | |||||
