Process development, inhibitor enzymes

Many substances can affect metabolic processes by influencing the activity of enzymes. Enzyme inhibitors are particularly important here. A large proportion of medicines act as enzyme inhibitors. Enzyme-kinetic experiments are therefore an important aspect of drug development and testing procedures. Natural metabolites are also involved in regulatory processes as inhibitors (see p.ll4). 

In conjunction with our overview of glycomimetics that block protein-carbohydrate interactions, we also discuss strategies to develop inhibitors of carbohydrate-processing enzymes this section focuses on the enzymes involved in bacterial cell wall biosynthesis because it is an area in which many new advances have been made. Enzymes that utilize sugars and synthesize glycoconjugates unique to pathogens have been identified, and cell-permeable inhibitors can be used to explore their biological roles or validate a potential... 

Overview and Future Development Inhibitors of Carbohydrate-processing Enzymes... 

Substituted nicotinic acid derivatives, such as 6-hydroxy nicotinic acid are important building blocks for the synthesis of pesticides and pharmaceuticals, acting as specific inhibitors of NAD/NADP-dependent enzymes. In a process developed by Lonza (Switzerland), 6-hydroxy nicotinic acid is produced by whole-cell microbial hydroxylation of nicotinic acid with Achromobacter xylosoxidans (yield > 100 g 1 ) (Fig. 16). A similar process for the production of 6-hydroxypicolinic acid (98 g l-1) and derivatives from picolinic acid (derivatives), based on Alcaligenes faecalis, has also been established [174,175]. 

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