5b6i

Structure of fluorinase from Streptomyces sp. MA37

spinqualitylabelsall models 5b6i, resolution 1.95Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 5b6i is a 2 chain structure with sequence from Streptomyces sp. MA37. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Method: X-ray diffraction, Resolution 1.95Å Ligands: ADN, MET Resources: FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT Function W0W999_9ACTN Publication Abstract from PubMed Fluorinases offer an environmentally friendly alternative for selective fluorination under mild conditions. However, their diversity is limited in nature and they have yet to be engineered through directed evolution. Herein, we report the directed evolution of the fluorinase FlA1 for improved conversion of the non-native substrate 5'-chloro-5'-deoxyadenosine (5'-ClDA) into 5'-fluoro-5'-deoxyadenosine (5'-FDA). The evolved variants, fah2081 (A279Y) and fah2114 (F213Y, A279L), were successfully applied in the radiosynthesis of 5'-[18 F]FDA, with overall radiochemical conversion (RCC) more than 3-fold higher than wild-type FlA1. Kinetic studies of the two-step reaction revealed that the variants show a significantly improved kcat value in the conversion of 5'-ClDA into S-adenosyl-l-methionine (SAM) but a reduced kcat value in the conversion of SAM into 5'-FDA. Directed Evolution of a Fluorinase for Improved Fluorination Efficiency with a Non-native Substrate.,Sun H, Yeo WL, Lim YH, Chew X, Smith DJ, Xue B, Chan KP, Robinson RC, Robins EG, Zhao H, Ang EL Angew Chem Int Ed Engl. 2016 Oct 14. doi: 10.1002/anie.201606722. PMID:27739177 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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