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Optimisation of 2-cyano-pyrimidine inhibitors of cathepsin K: improving selectivity over hERG

Zoran Rankovic1, Jiaqiang Cai, Jennifer Kerr

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Bioorganic & Medicinal Chemistry Letters
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Catalytically Perfect Enzymes01:07

Catalytically Perfect Enzymes

The theory of catalytically perfect enzymes was first proposed by W.J. Albery and J. R. Knowles in 1976. These enzymes catalyze biochemical reactions at high-speed. Their catalytic efficiency values range from 108-109 M-1s-1. These enzymes are also called 'diffusion-controlled' as the only rate-limiting step in the catalysis is that of the substrate diffusion into the active site. Examples include triose phosphate isomerase, fumarase, and superoxide dismutase.