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-Structure paper
タイトル | E-site drug specificity of the human pathogen ribosome. |
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ジャーナル・号・ページ | Sci Adv, Vol. 8, Issue 21, Page eabn1062, Year 2022 |
掲載日 | 2022年5月27日 |
![]() | Yury Zgadzay / Olga Kolosova / Artem Stetsenko / Cheng Wu / David Bruchlen / Konstantin Usachev / Shamil Validov / Lasse Jenner / Andrey Rogachev / Gulnara Yusupova / Matthew S Sachs / Albert Guskov / Marat Yusupov / ![]() ![]() ![]() ![]() |
PubMed 要旨 | is a widespread commensal fungus with substantial pathogenic potential and steadily increasing resistance to current antifungal drugs. It is known to be resistant to cycloheximide (CHX) that binds ... is a widespread commensal fungus with substantial pathogenic potential and steadily increasing resistance to current antifungal drugs. It is known to be resistant to cycloheximide (CHX) that binds to the E-transfer RNA binding site of the ribosome. Because of lack of structural information, it is neither possible to understand the nature of the resistance nor to develop novel inhibitors. To overcome this issue, we determined the structure of the vacant 80 ribosome at 2.3 angstroms and its complexes with bound inhibitors at resolutions better than 2.9 angstroms using cryo-electron microscopy. Our structures reveal how a change in a conserved amino acid in ribosomal protein eL42 explains CHX resistance in and forms a basis for further antifungal drug development. |
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手法 | EM (単粒子) |
解像度 | 2.32 - 2.77 Å |
構造データ | EMDB-13737: Cryo-EM map of the vacant Candida albicans 80S ribosome EMDB-13741, PDB-7q08: EMDB-13744: Cryo-EM map of Candida albicans 80S ribosome in complex with phyllanthoside EMDB-13749: Cryo-EM map of the Candida albicans 80S ribosome in complex with anisomycin EMDB-13750: Cryo-EM map of the Candida albicans 80S ribosome in complex with blasticidin s |
化合物 | ![]() ChemComp-SPD: ![]() ChemComp-PUT: ![]() ChemComp-MG: ![]() ChemComp-ZN: ![]() ChemComp-HOH: ![]() ChemComp-3HE: ![]() ChemComp-3K5: ![]() ChemComp-ANM: ![]() ChemComp-BLS: |
由来 |
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![]() | RIBOSOME / Candida albicans / cryo-EM / cycloheximide / drug design / phyllanthoside / anisomycin / peptidyl transferase center / blasticidin s |