Offers essential guidance for discovering and optimizing novel drug therapies Using
detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers …

Drugs that function as enzyme inhibitors constitute a significant portion of the orally
bioavailable therapeutic agents that are in clinical use today. Likewise, much of drug …

Enzymes offer unique opportunities for drug design that are not available to cell surface
receptors, nuclear hormone receptors, ion channels, transporters, and DNA. Here, we …

Highlights•Enzymes are highly druggable due to the presence of discrete substrate
pockets.•Enzymology contributes throughout the value chain of lead discovery.•Quantitative …

Enzymes catalyze multistep chemical reactions and achieve phenomenal rate accelerations
by matching protein and substrate chemical groups in the transition state. Inhibitors that take …

This article presents several covalent inhibitors, including examples of successful drugs, as
well as highly selective, irreversible inhibitors of emerging therapeutic targets, such as fatty …

As medicinal chemists become more and more involved in the “rational”** design of enzyme
inhibitors as potential drugs, it may be useful to consider a comment made by the late BR …

Given the therapeutic and commercial success of small-molecule enzyme inhibitors, as
exemplified by kinase inhibitors in oncology, a major focus of current drug-discovery and …

Drug research encompasses several diverse disciplines united by a common goal, namely
the development of novel therapeutic agents. The search for new drugs can be divided …

Enzymes as drugs have two important features that distinguish them from all other types of
drugs. First, enzymes often bind and act on their targets with great affinity and specificity …