Now showing items 121-130 of 130
Combining Active Site and Allosteric Inhibitors to Study Protein Tyrosine Kinases
(2016)
Kinases play a crucial role in a variety of cell signaling pathways that control processes such as: growth, motility, and angiogenesis. Not surprisingly, dysregulation of proper kinase signaling often leads to cancer. Since ...
Synthesis and Biochemical Evaluation of Multifunctional Acetylcholinesterase Inhibitor Hybrids for Treatment of Alzheimer's Disease.
(2014)
Alzheimer’s disease (AD) places a significant and dramatically increasing burden on society. While pathological hallmarks of this neurodegenerative disorder are known, the exact cause remains unclear. Acetylcholinesterase ...
Development, Synthesis, and Characterization of G Protein-Coupled Receptor Kinase Inhibitors Using Structure Based Drug Design for the Advancement of Heart Failure Therapeutics
(2017)
In heart failure, the β-adrenergic receptors (βARs) become desensitized and uncoupled from heterotrimeric G proteins. This process is initiated by G protein-coupled receptor kinases (GRKs), some of which are upregulated ...
The Function of the ASH1L Histone Methyltransferase in Cancer: A Chemical Biology Approach
(2018)
ASH1L (absent, small, or homeotic-like 1) is a histone lysine methyltransferase (KMTase) that is overexpressed in cancer and activates oncogenic HOX genes. Small molecule inhibitors of ASH1L would be invaluable tools to ...
Mass Spectrometry Based Techniques for In Vivo Neurochemical Monitoring.
(2012)
Neurotransmitter concentration in vivo reflects various behavioral and pharmacological events. Therefore, the measurement of neurochemical dynamics in live behaving animals’ brain is of crucial importance for the fundamental ...
Incorporation of Protein Flexibility in Structure-Based Drug Discovery of HIV-1 Protease and Bacterial Hsp70 Chaperone.
(2013)
Damm et al. utilized a multiple protein structure (MPS)-based method and discovery an allosteric site of HIV-1 protease (HIV-1p) that had not been described before. Based on this new site, a MPS-based pharmacophore model ...
Chemical Modulation of Phospho-Signaling Pathways Involved in Cancer.
(2015)
Advancements in our understanding of the molecular causes of cancer have led to the therapeutic targeting of key enzymes involved in cell growth. Kinase inhibitors have been the most successful forms of such targeted therapy ...
Hsp70 chaperone Proteins and their Interactions with Various Drugs as Studied by Nuclear Magnetic Resonance.
(2011)
Chaperone proteins and their cochaperones are perhaps one of the most intriguing systems for investigation. Ubiquitous in nature, they can be found in every organism and that perhaps is the reason that their sequence shows ...
Molecular Dynamics Simulation of Phase and Structural Transitions in Model Lung Surfactant Mixtures.
(2010)
Lung surfactant (LS) is a complex mixture of lipids and proteins that reduces and regulates the surface tension in the lungs, thereby decreasing the work of breathing. A thorough understanding of LS function is critical ...
Solid State NMR Investigations of Lipid Bilayers and Biomembrane Binding Molecules: Dendrimers and Amylin.
(2010)
The goal of this project was to investigate the interaction between lipid binding molecules, such as peptides and drug compounds, with biological lipid bilayers. The results demonstrate that human amylin, a peptide hormone ...