Pub. Date : 2021 Nov 10
PMID : 34648292
8 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | To this end, we report the crystal structure of CYP3A5 in complex with a previously reported selective inhibitor, clobetasol propionate (CBZ). | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 2 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 3 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 4 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 5 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 6 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 7 | Supported by structure-guided mutagenesis analyses, the CYP3A5-CBZ structure showed that a unique conformation of the F-F" loop in CYP3A5 enables selective binding of CBZ to CYP3A5. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |
| 8 | In addition, functional and biophysical assays using CBZ analogs highlight the importance of heme-adjacent moieties for selective CYP3A5 inhibition. | Carbamazepine | cytochrome P450 family 3 subfamily A member 5 | Homo sapiens |