MEDI 65 |
| Residue-specific incorporation of 5',5',5'-trifluoroleucine (TFL) into chloramphenicol acetyltransferase (CAT) results in reduction in the thermal stability of the protein. To deconvolute which TFL residues participate in the loss of thermal stability, a highly sensitive microplate-based cell lysate thermostability and activity screen was developed. Thirteen single-isoleucine mutants were created and screened. From the assay, fluorinated mutants L82I T and L208I T exhibited large losses in thermal stability while the fluorinated mutant L158I T was determined to be more active than the parent CAT T at elevated temperatures. Additional secondary structure characterization of L158I T confirmed the enhanced thermal stability suggesting that TFL at position 158 contributes to some of the loss in thermostability upon fluorination. |
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Poster Session
7:00 PM-9:00 PM, Sunday, August 19, 2007 BCEC -- Exhibit Hall - B2, Poster
Division of Medicinal Chemistry |