The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme.
The structure of mouse L1210 dihydrofolate reductase (DHFR) complexed with NADPH and trimethoprim has been refined at 2.0 A resolution. The analogous complex with NADPH and methotrexate has been refined at 2.5 A resolution. These structures reveal for the first time details of drug interactions with...
| Egile Nagusiak: | , , , , , , , |
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| Formatua: | Journal article |
| Hizkuntza: | English |
| Argitaratua: |
1987
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| _version_ | 1826292431115517952 |
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| author | Stammers, D Champness, J Beddell, C Dann, J Eliopoulos, E Geddes, A Ogg, D North, A |
| author_facet | Stammers, D Champness, J Beddell, C Dann, J Eliopoulos, E Geddes, A Ogg, D North, A |
| author_sort | Stammers, D |
| collection | OXFORD |
| description | The structure of mouse L1210 dihydrofolate reductase (DHFR) complexed with NADPH and trimethoprim has been refined at 2.0 A resolution. The analogous complex with NADPH and methotrexate has been refined at 2.5 A resolution. These structures reveal for the first time details of drug interactions with a mammalian DHFR, which are compared with those observed from previous X-ray investigations of DHFR/inhibitor complexes. The refined L1210 structure has been used as the basis for the construction of a model of the human enzyme. There are only twenty-one sequence differences between mouse L1210 and human DHFRs, and all but two of these are located close to the molecular surface: a strong indication that the active sites are essentially identical in these two mammalian enzymes. |
| first_indexed | 2024-03-07T03:14:35Z |
| format | Journal article |
| id | oxford-uuid:b55acfb9-a49d-4914-a21d-eaba9309d917 |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T03:14:35Z |
| publishDate | 1987 |
| record_format | dspace |
| spelling | oxford-uuid:b55acfb9-a49d-4914-a21d-eaba9309d9172022-03-27T04:32:51ZThe structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:b55acfb9-a49d-4914-a21d-eaba9309d917EnglishSymplectic Elements at Oxford1987Stammers, DChampness, JBeddell, CDann, JEliopoulos, EGeddes, AOgg, DNorth, AThe structure of mouse L1210 dihydrofolate reductase (DHFR) complexed with NADPH and trimethoprim has been refined at 2.0 A resolution. The analogous complex with NADPH and methotrexate has been refined at 2.5 A resolution. These structures reveal for the first time details of drug interactions with a mammalian DHFR, which are compared with those observed from previous X-ray investigations of DHFR/inhibitor complexes. The refined L1210 structure has been used as the basis for the construction of a model of the human enzyme. There are only twenty-one sequence differences between mouse L1210 and human DHFRs, and all but two of these are located close to the molecular surface: a strong indication that the active sites are essentially identical in these two mammalian enzymes. |
| spellingShingle | Stammers, D Champness, J Beddell, C Dann, J Eliopoulos, E Geddes, A Ogg, D North, A The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title | The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title_full | The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title_fullStr | The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title_full_unstemmed | The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title_short | The structure of mouse L1210 dihydrofolate reductase-drug complexes and the construction of a model of human enzyme. |
| title_sort | structure of mouse l1210 dihydrofolate reductase drug complexes and the construction of a model of human enzyme |
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