Scientific American, 3/97, William A. Haseltine, page 78
Discovering Genes for New Medicines
By identifying human genes involved in disease, researchers can create potentially
therapeutic proteinsand speed the development of powerful drugs
Most readers of this magazine are probably familiar with the idea of a gene as
something that transmits inherited traits from one generation to the next. Less well
appreciated is that malfunctioning genes are deeply involved in most diseases, not only
inherited ones. Cancer, atherosclerosis, osteoporosis, arthritis and Alzheimer's disease,
for example, are all characterized by specific changes in the activities of genes. Even
infectious disease usually provokes the activation of identifiable genes in a patient's
immune system. Moreover, accumulated damage to genes from a lifetime of exposure to
ionizing radiation and injurious chemicals probably underlies some of the changes
associated with aging.
A few years ago I and some likeminded colleagues decided that knowing where and when
different genes are switched on in the human body would lead to far-reaching advances in
our ability to predict, prevent, treat and cure disease. When a gene is active, or as a
geneticist would say, "expressed," the sequence of the chemical units, or bases,
in its DNA is used as a blueprint to produce a specific protein. Proteins direct, in
various ways, all of a cell's functions. They serve as structural components, as catalysts
that carry out the multiple chemical processes of life and as control elements that
regulate cell reproduction, cell specialization and physiological activity at all levels.
The development of a human from fertilized egg to mature adult is, in fact, the
consequence of an orderly change in the pattern of gene expression in different tissues.
Knowing which genes are expressed in healthy and diseased tissues, we realized, would
allow us to identify both the proteins required for normal functioning of tissues and the
aberrations involved in disease. With that information in hand, it would be possible to
develop new diagnostic tests for various illnesses and new drugs to alter the activity of
affected proteins or genes. Investigators might also be able to use some of the proteins
and genes we identified as therapeutic agents in their own right. We envisaged, in a
sense, a high-resolution description of human anatomy descending to the molecular level of
detail.
It was clear that identifying all the expressed genes in each of the dozens of tissues in
the body would be a huge task. There are some 100,000 genes in a typical human cell. Only
a small proportion of those genes (typically about 15,000) is expressed in any one type of
cell, but the expressed genes vary from one cell type to another. So looking at just one
or two cell types would not reveal the genes expressed in the rest of the body. We would
also have to study tissues from all the stages of human development. Moreover, to identify
the changes in gene expression that contribute to sickness, we would have to analyze
diseased as well as healthy tissues.
Technological advances have provided a way to get the job done. Scientists can now rapidly
discover which genes are expressed in any given tissue. Our strategy has proved the
quickest way to identify genes of medical importance.
Take the example of atherosclerosis. In this common condition, a fatty substance called
plaque accumulates inside arteries, notably those supplying the heart. Our strategy
enables us to generate a list of genes expressed in normal arteries, along with a measure
of the level of expression of each one. We can then compare the list with one derived from
patients with atherosclerosis. The difference between the lists corresponds to the genes
(and thus the proteins) involved in the disease. It also indicates how much the genes'
expression has been increased or decreased by the illness. Researchers can then make the
human proteins specified by those genes.
Once a protein can be manufactured in a pure form, scientists can fairly easily fashion a
test to detect it in a patient. A test to reveal overproduction of a protein found in
plaque might expose early signs of atherosclerosis, when better options exist for treating
it. In addition, pharmacologists can use pure proteins to help them find new drugs. A
chemical that inhibited production of a protein found in plaque might be considered as a
drug to treat atherosclerosis.
Our approach,. which I call medical genomics, is somewhat outside the mainstream of
research in human genetics. A great many scientists are involved in the Human Genome
Project, an international collaboration devoted to the discovery of the complete sequence
of the chemical bases in human DNA. (All the codes in DNA are constructed from an alphabet
consisting of just four bases.) That information will be important for studies of gene
action and evolution and will particularly benefit research on inherited diseases. Yet the
genome project is not the fastest way to discover genes, because most of the bases that
ma