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Hello, and welcome to the Henry Stewart
lecture series on Small
Molecule Drug Discovery.
My name is Mark Wigglesworth, and
I'm the Director at the Global High
Throughput Screening
organization within AstraZeneca.
Today I have a
presentation for you on,
G-Protein Coupled Receptors
in Drug Discovery.
I've had a long interest
in both screening
and in G-protein coupled receptors.
I hope the presentation that
follows will give you some insight
into both and how their
impacting to discovery
both today and in the future.
0:36
I'm going to start with some
information which I'm sure you're
all already aware of,
and that is GPCRs,
the size of the super family,
and that this is actually
a very significant
opportunity for all
of us that work
within drug discovery.
The graph that you're
looking at on this slide
simply shows the number of proteins
targets within some major target
super families.
And GPCR showed, on this graph, as
having around 800 family members,
by far the largest single
protein class that are
successfully targeted
by drugs today.
1:17
And as drug targets, GPCRs are
involved in almost all diseases
throughout the human body.
Perhaps more importantly for
drug discovery, of course,
is that this family
of proteins are highly
tractable and highly profitable.
They are the most exploited
class of drug targets,
with approximately 36% of
all drugs targeting them.
And just taking a moment
to think about that,
that's quite phenomenal.
The effects that this target
class and drugs acting upon them
has had on human health
historically is very significant.
Indeed, according to
data from IMS Health,
six out of the top 20 drugs in
terms of global sales in 2010,
targeted GPCRs.
That is 30%.
