A high proportion of drugs currently coming to market exert their action in the body by inhibition of a target enzyme involved in a particular body function or in a bacterium, protozoon, or virus causing an infection. This book extends the previous volume in providing a comprehensive coverage of more recently recognised target enzymes and their known inhibitors, and within this framework of knowledge demonstrates how the drug designer uses all available information to develop aspecific therapeutic agent. Drug design is an interdisciplinary art and the text illustrates the pathway followed from the initial design concept and synthesis of an inhibitor through its in vitro and in vivo assessments to clinical trial, a process involving chemists, biochemists, pharmacologies, andclinicians.
Preface; Enzyme inhibitors as drugs:: from design to the clinic; Computer-aided molecular design of enzyme inhibitors; Protein serine - threonine kinases; Inhibitors of protein tyrosine kinases; Inhibitors of non-protein kinases; Enzyme targets as an approach to therapy for HIV infections; Inhibitors of viral DNA Polymerase; Fungal enzyme targets; Steroidogenesis pathway enzymes; HMG-Co A reductase inhibitors; DNA topoisomerases; Catecholamine - O- methyltrasnferase (COMT) and COMT inhibitors; Inhibitors of Phospholipase A; Inhibitors of gastric H+, K+ ATPase; Inhibitors of mammalian collagenases; Inhibitors of Aldose Reductase; Miscellaneous topics;
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