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Crystal structure of human RIOK2 bound to a specific inhibitor
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| Zeitschriftentitel: | Open Biology |
|---|---|
| Personen und Körperschaften: | , , , |
| In: | Open Biology, 9, 2019, 4 |
| Format: | E-Article |
| Sprache: | Englisch |
| veröffentlicht: |
The Royal Society
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| Schlagwörter: |
| author_facet |
Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. |
|---|---|
| author |
Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. |
| spellingShingle |
Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. Open Biology Crystal structure of human RIOK2 bound to a specific inhibitor General Biochemistry, Genetics and Molecular Biology Immunology General Neuroscience |
| author_sort |
wang, jing |
| spelling |
Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. 2046-2441 The Royal Society General Biochemistry, Genetics and Molecular Biology Immunology General Neuroscience http://dx.doi.org/10.1098/rsob.190037 <jats:p>The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure of an inhibitor-bound RIO kinase reveals the binding mode of the inhibitor and explains the structure–activity relationship of the inhibitor series. The inhibitor binds in the ATP-binding site and forms extensive hydrophobic interactions with residues at the entrance to the ATP-binding site. Analysis of the conservation of active site residues reveals the reasons for the specificity of the inhibitor for RIOK2 over RIOK1 and RIOK3, and it provides a template for inhibitor design against the human RIOK family.</jats:p> Crystal structure of human RIOK2 bound to a specific inhibitor Open Biology |
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| title |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_unstemmed |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_full |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_fullStr |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_full_unstemmed |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_short |
Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_sort |
crystal structure of human riok2 bound to a specific inhibitor |
| topic |
General Biochemistry, Genetics and Molecular Biology Immunology General Neuroscience |
| url |
http://dx.doi.org/10.1098/rsob.190037 |
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2019 |
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<jats:p>The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure of an inhibitor-bound RIO kinase reveals the binding mode of the inhibitor and explains the structure–activity relationship of the inhibitor series. The inhibitor binds in the ATP-binding site and forms extensive hydrophobic interactions with residues at the entrance to the ATP-binding site. Analysis of the conservation of active site residues reveals the reasons for the specificity of the inhibitor for RIOK2 over RIOK1 and RIOK3, and it provides a template for inhibitor design against the human RIOK family.</jats:p> |
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| author | Wang, Jing, Varin, Thibault, Vieth, Michal, Elkins, Jonathan M. |
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| description | <jats:p>The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure of an inhibitor-bound RIO kinase reveals the binding mode of the inhibitor and explains the structure–activity relationship of the inhibitor series. The inhibitor binds in the ATP-binding site and forms extensive hydrophobic interactions with residues at the entrance to the ATP-binding site. Analysis of the conservation of active site residues reveals the reasons for the specificity of the inhibitor for RIOK2 over RIOK1 and RIOK3, and it provides a template for inhibitor design against the human RIOK family.</jats:p> |
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| spelling | Wang, Jing Varin, Thibault Vieth, Michal Elkins, Jonathan M. 2046-2441 The Royal Society General Biochemistry, Genetics and Molecular Biology Immunology General Neuroscience http://dx.doi.org/10.1098/rsob.190037 <jats:p>The RIO kinases (RIOKs) are a universal family of atypical kinases that are essential for assembly of the pre-40S ribosome complex. Here, we present the crystal structure of human RIO kinase 2 (RIOK2) bound to a specific inhibitor. This first crystal structure of an inhibitor-bound RIO kinase reveals the binding mode of the inhibitor and explains the structure–activity relationship of the inhibitor series. The inhibitor binds in the ATP-binding site and forms extensive hydrophobic interactions with residues at the entrance to the ATP-binding site. Analysis of the conservation of active site residues reveals the reasons for the specificity of the inhibitor for RIOK2 over RIOK1 and RIOK3, and it provides a template for inhibitor design against the human RIOK family.</jats:p> Crystal structure of human RIOK2 bound to a specific inhibitor Open Biology |
| spellingShingle | Wang, Jing, Varin, Thibault, Vieth, Michal, Elkins, Jonathan M., Open Biology, Crystal structure of human RIOK2 bound to a specific inhibitor, General Biochemistry, Genetics and Molecular Biology, Immunology, General Neuroscience |
| title | Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_full | Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_fullStr | Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_full_unstemmed | Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_short | Crystal structure of human RIOK2 bound to a specific inhibitor |
| title_sort | crystal structure of human riok2 bound to a specific inhibitor |
| title_unstemmed | Crystal structure of human RIOK2 bound to a specific inhibitor |
| topic | General Biochemistry, Genetics and Molecular Biology, Immunology, General Neuroscience |
| url | http://dx.doi.org/10.1098/rsob.190037 |