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TI-3D Seed Grants
Fortilin
The NS1 Protein
Regulation of sGC
function by non-heme tetrapyrrole macrocycles
FastLab
Virtual
Screening
Protein Kinases
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Postdoctoral Research Initiatives

Protein Kinases
Kevin Dalby, PhD - College of
Pharmacy, The University of Texas at Austin
Eric Anslyn, PhD - Department of Chemistry & Biochemistry, The
University of Texas at Austin
Pengyu Ren, PhD - Biomedical Engineering, The University of Texas at
Austin
Alexey Ryazanov, PhD - Department of Pharmacology, Robert Wood
Johnson Medical School
Protein kinases currently represent one of
the most attractive families of drug targets occupying the
pharmaceutical industry, having an unprecedented involvement in the
pathogenesis of human disease. Consequently, they have been dubbed
the drug targets of the 21st century, reflecting the view that many
of the new drugs to surface in the future will be inhibitors of
protein kinases.
Our multi-disciplined team of enzymologists, synthetic chemists,
computer scientists and pharmacologists will focus on a number of
protein kinases, which include the mitogen-activated protein kinases
as well as several structurally distinct family members. While MAPK
signaling pathways mediate a variety of cellular processes including
proliferation, differentiation, apoptosis and survival, a huge
amount of evidence highlights the potential of the MAP kinase
signaling pathways as therapeutic targets, because the loss of their
regulation is associated with many diseases. These include a growing
number of cancers, including prostate cancer, colorectal cancer, and
chronic myeloid leukemia, as well as neurological diseases such as
Alzheimer disease, and also several inflammatory diseases.
Through TI-3D we are optimizing the expression and purification of
specific protein kinases. In addition, we are also embarking on the
synthesis of kinase-focused inhibitor libraries for high-throughput
screening. Ultimately, structures of lead compounds will be
determined and these structures will provide the basis for further
refinement of inhibitor design using in silico approaches. These
latter studies will be performed on a state-of-the-art computer
cluster dedicated to TI-3D research.
As part of this work we collaborate with Alexey G. Ryazanov who is
an associate professor in the Dept. of Pharmacology at Robert Wood
Johnson Medical School, Piscataway, NJ. Dr. Ryazanov’s role on the
project is to provide cell-based assays and in some cases transgenic
animals to develop lead compounds.
Dalby Lab
Anslyn
Lab
Ren Lab
Ryazanov Lab
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