Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic.
The development of small molecules that disrupt protein-protein interactions is a key goal in addressing a number of disease states. The alpha-helix is commonly found at protein interaction interfaces and has been the focus of substantial small molecule mimetic efforts. One of the primary drawbacks...
| Main Authors: | , , , |
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| Format: | Journal article |
| Language: | English |
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2009
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| _version_ | 1797095061581725696 |
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| author | Cummings, C Ross, N Katt, W Hamilton, A |
| author_facet | Cummings, C Ross, N Katt, W Hamilton, A |
| author_sort | Cummings, C |
| collection | OXFORD |
| description | The development of small molecules that disrupt protein-protein interactions is a key goal in addressing a number of disease states. The alpha-helix is commonly found at protein interaction interfaces and has been the focus of substantial small molecule mimetic efforts. One of the primary drawbacks of many small molecule alpha-helix mimetics is their hydrophobic core structures. To address this problem we have developed a novel scaffold based on a more water soluble 5-6-5 imidazole-phenyl-thiazole core. An inhibitor of this class has been shown to disrupt the Cdc42/Dbs protein-protein interaction at micromolar concentrations and may be useful in overcoming Cdc42-induced tumor resistance to anticancer therapies. |
| first_indexed | 2024-03-07T04:22:40Z |
| format | Journal article |
| id | oxford-uuid:cb8bec52-4b00-4ba3-8040-c5ae5b4fd552 |
| institution | University of Oxford |
| language | English |
| last_indexed | 2024-03-07T04:22:40Z |
| publishDate | 2009 |
| record_format | dspace |
| spelling | oxford-uuid:cb8bec52-4b00-4ba3-8040-c5ae5b4fd5522022-03-27T07:15:39ZSynthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic.Journal articlehttp://purl.org/coar/resource_type/c_dcae04bcuuid:cb8bec52-4b00-4ba3-8040-c5ae5b4fd552EnglishSymplectic Elements at Oxford2009Cummings, CRoss, NKatt, WHamilton, AThe development of small molecules that disrupt protein-protein interactions is a key goal in addressing a number of disease states. The alpha-helix is commonly found at protein interaction interfaces and has been the focus of substantial small molecule mimetic efforts. One of the primary drawbacks of many small molecule alpha-helix mimetics is their hydrophobic core structures. To address this problem we have developed a novel scaffold based on a more water soluble 5-6-5 imidazole-phenyl-thiazole core. An inhibitor of this class has been shown to disrupt the Cdc42/Dbs protein-protein interaction at micromolar concentrations and may be useful in overcoming Cdc42-induced tumor resistance to anticancer therapies. |
| spellingShingle | Cummings, C Ross, N Katt, W Hamilton, A Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title | Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title_full | Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title_fullStr | Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title_full_unstemmed | Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title_short | Synthesis and biological evaluation of a 5-6-5 imidazole-phenyl-thiazole based alpha-helix mimetic. |
| title_sort | synthesis and biological evaluation of a 5 6 5 imidazole phenyl thiazole based alpha helix mimetic |
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