My
research interests center around a few key questions:
How
do DNA-binding proteins discriminate against
non-cognate sites?
While the
current database of protein-DNA complex structures
determined by crystallographic and NMR methods has
contributed greatly to our understanding of the
positive forces involved in the
high affinity binding of DNA by sequence-specific
DNA-binding proteins, our understanding of the
mechanisms that these proteins use to discriminate
against the myriad of similar but incorrect sites in
the genome lags far behind. The central theme of this
project is the application of crystallographic
methods to elucidating the mechanisms involved in
discrimination against sub-optimal ligands; i.e.,
What is the structural basis for the higher energy
state of the complex between a DNA-binding protein
and a minimally-suboptimal DNA oligonucleotide?
Can
small molecules be found or designed to interfere
with sequence-specific protein-DNA recognition?
The
apparently fragile nature of the protein-DNA
interface, coupled with the delicate balance between
affinity and specificity, suggests that it may be
possible to find or devise small molecules which
could interfere with sequence-specific protein-DNA
recognition. The central theme of this second project
is to discover, design, and characterize these
substances and determine their mechanisms of action,
preferentially targetting the DNA-binding surface of
the protein rather than the DNA.
Collaborative
Projects:
uvsY
- DNA Prof. Scott Morrical and Hans Beernink, Ph.D.
Proteins
such as gp32 from phage T4 stabilize and protect
single-stranded DNA by tightly binding to and coating
it - so tightly that the subsequent binding of the
replication and recombination machinery is hindered.
Additional proteins are required to mediate the
efficient loading of the R & R machinery onto
gp32-coated ssDNA, such as the uvsY protein from
phage T4. The current model for the action of uvsY is
that it binds to the coated ssDNA, disrupts the
cooperative binding of gp32 on DNA, and mediates the
exchange of the filamentous recombination protein
uvsX for the displaced gp32. Towards understanding
the detailed molecular mechanism of this process,
Hans Beernink crystallized the uvsY-ssDNA complex
while he was a graduate student in Scott Morrical's
lab. As a post-doc, Hans is continuing the
crystallographic structure determination of this
complex in a collaboration between the Morrical and
Rould Labs.
Structural
Studies of Myosin Function Prof. Kathy Trybus, Prof.
Susan Lowey, and Terri Messier
The
3-dimensional crystal structure of a smooth muscle
motor domain-essential light chain complex with
several bound nucleotides has provided the first
snapshot of the molecule in the pre-power stroke
conformation (Cell 94: 559-571, 1998). These studies
are being extended to other nucleotide analogs, as
well as to mutants that have impaired function or
which are stalled at various stages of the
crossbridge cycle. A large body of supporting
biochemical and mechanical data has been obtained for
the proteins that have been chosen for the structural
studies. Crystallization of double-headed heavy
meromyosin is also being pursued, with the goal of
understanding the head-head interactions that are
required for phosphorylation-dependent regulation of
this motor's activity. We are also pursuing the
crystallization of an unconventional myosin motor
(myosin V and its calmodulin-binding domain), which
is involved in vesicular transport within the cell.