- Widely applicable background depletion step enables transaminase evolution through solid-phase screening
-
Directed evolution of transaminases is a widespread technique in the development of highly sought-after biocatalysts for industrial applications. This process, however, is challenged by the limited availability of effective high-throughput protocols to evaluate mutant libraries. Here we report a rapid, reliable, and widely applicable background depletion method for solid-phase screening of transaminase variants, which was successfully applied to a transaminase from Halomonas elongata (HEWT), evolved through rounds of random mutagenesis towards a series of diverse prochiral ketones. This approach enabled the identification of transaminase variants in viable cells with significantly improved activity towards para-substituted acetophenones (up to 60-fold), as well as tetrahydrothiophen-3-one and related substrates. Rationalisation of the mutants was assisted by determination of the high-resolution wild-type HEWT crystal structure presented herein.
- Planchestainer, Matteo,Hegarty, Eimear,Heckmann, Christian M.,Gourlay, Louise J.,Paradisi, Francesca
-
p. 5952 - 5958
(2019/06/19)
-
- A novel series of potent and selective EP4 receptor ligands: Facile modulation of agonism and antagonism
-
A novel series of EP4 ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic
- Boyd, Michael J.,Berthelette, Carl,Chiasson, Jean-Franois,Clark, Patsy,Colucci, John,Denis, Danielle,Han, Yongxin,Lévesque, Jean-Francois,Mathieu, Marie-Claude,Stocco, Rino,Therien, Alex,Rowland, Steve,Wrona, Mark,Xu, Daigen
-
scheme or table
p. 484 - 487
(2011/02/27)
-
- Synthesis, time-resolved luminescence, nmr spectroscopy, circular dichroism and circularly polarised luminescence studies of enantiopure macrocyclic lanthanide tetraamide complexes
-
The syntheses and properties of a series of lanthanide complexes (Ln = Eu, Tb, Dy, Yb) of C4 symmetric chiral tetraamide ligands based on 1,4,7,10- tetraazacyclododecane are reported. The configuration of the chiral centre at carbon in the amid
- Dickins, Rachel S.,Howard, Judith A.K.,Maupin, Christine L.,Moloney, Janet M.,Parker, David,Riehl, James P.,Siligardi, Giuliano,Williams, J.A. Gareth
-
p. 1095 - 1105
(2007/10/03)
-