Characterisation of the Carboxypeptidase G2 Catalytic Site and Design of New Inhibitors for Cancer Therapy,ChemBioChem

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Characterisation of the Carboxypeptidase G2 Catalytic Site and Design of New Inhibitors for Cancer Therapy
ChemBioChem ( IF 2.6 ) Pub Date : 2018-08-13 , DOI: 10.1002/cbic.201800186
Dhadchayini Jeyaharan ₁ , Carla Brackstone ₁ , James Schouten ₂ , Paul Davis ₂ , Ann M. Dixon ₁

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The structural and functional impact of extensive point mutation across the entire putative CPG2 catalytic site and adjacent regions (shown) is reported, revealing that residues outside the catalytic region might direct substrate recognition. NMR spectroscopy was then used to map the binding epitopes and affinities of several novel CPG2 inhibitors that occupy new chemical space.