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The spectacular advances of medicinal chemistry in the last few
decades have been triggered by a greater understanding of cellular
processes at the molecular level. The understanding of biochemical
processes and diseases at molecular level has revolutionized the
field. This volume summarizes recent developments in the area of
biological inhibitors such as squalene epoxidase inhibitors, dual
inhibitors of 5-lipoxygenase and cycloxgenase, inhibition of
cholestrol biosynthesis, HIV proteinase inhibitors, nonpeptide
antagonists at peptide receptors, and binding interaction of
thyroid hormones.
The goal of an activity-directed isolation process is to isolate
bioactive compounds which may provide structural leads of
therapeutic importance. Whereas the traditional process of drug
development is long and expensive, simple and rapid bioassays can
serve as the starting point for drug discovery. This book presents
a range of "bench top" bioassay techniques useful for natural
product and pharmaceutical chemists involved in drug discovery and
pharmacognosy. The contents detail a number of enzyme-based assays,
cell-based functional bioassays and receptor radioligand binding
assays along with detailed descriptions of each type. The majority
of these bioassays are presented in a step-by-step format, so they
could even be implemented by technical personnel with little
background in microbiology, biochemistry or pharmacology.
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