Please wait while the transcript is being prepared...
0:00
The title of today's talk
is 'Epigenetics as a Paradigm
for Cancer Treatment:
Chemically Targeting
the Histone Lysine
Methyltransferase EZH2.
My name is Sharad Verma
and I work for GlaxoSmithKline,
and I support
the Oncology Therapeutic area
in the area
of early development.
0:24
The objectives of today's
presentation are as follows.
I would like
to provide the viewer
with an improved
understanding of first,
cancer as an unmet medical need,
and then discuss epigenetics
as a paradigm
for treating cancer.
In this regard,
I will discuss epigenetics
from a structural
mechanistic standpoint,
and then focus on
one particular class
of enzymes called
histone methyltransferases.
I will then discuss
EZH2 as an example
within this target class.
Specifically, what is EZH2
and what it does
and the rationale
for targeting EZH2 in oncology.
Further discussion
will then focus on
the development
of EZH2 inhibitors.
First, some general
drug discovery themes,
and then discussion around
some of the lead molecules
that have arisen from
those discovery efforts,
and then finally a summary
and future outlook.
1:33
Cancer is a major unmet medical
need of global significance.
It is the leading cause
of death worldwide
and the second leading cause
of death in the United States,
following coronary
heart disease.
It is estimated by
the American Cancer Society
that in 2015,
there will be 1.66 million
new cases of cancer diagnosed.
The number of cancer cases
is continually rising
especially in the United States
and European Union countries.
This is in large part driven
by an aging population,
as cancer cases
are more prominent
in an elderly population.
2/3rds of all cases
are in patients 65 and older.
