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