Biomedical Engineering Reference
In-Depth Information
12
EXPERIMENTAL APPROACHES TO
RAPID IDENTIFICATION, PROFILING,
AND CHARACTERIZATION OF
SPECIFIC BIOLOGICAL EFFECTS
OF DOS COMPOUNDS
EDUARD A. SERGIENKO AND SUSANNE HEYNEN-GENEL
12.1
INTRODUCTION
Historically, a small number of protein classes provided a disproportionally large
pool of current medications. Arguably, this suggests that some target classes are more
amenable to regulation with small molecules. Alternatively, this prevalence may also
have emerged stochastically through a predominant reliance on specific approaches
for identification of initial drugs and their targets. Completion of sequencing and
mapping the human genome promises to infuse the drug discovery field with new
representatives and classes of therapeutically relevant targets. Gene microarrays and
RNA
i
-based approaches for detection and quantification of the transcriptional prod-
ucts have already benefited immensely from identification of novel genes. These
techniques are now used routinely in research labs and provide invaluable informa-
tion on overall correlations between pathophysiological conditions and certain genes.
Changes in the level of gene transcriptional activity in the cells, bearing disease phe-
notypes, are taken to indicate a potential association for protein products of the genes
affected with the disease. Unfortunately, ascribing a link between a disease and a
specific protein function is not always possible: many proteins are known to take part
in multiple, frequently unrelated cellular activities.
