Now showing items 421-430 of 438
Biophysical Approaches to Target Protein-Protein Interactions of Epigenetic Complexes by Small-Molecule Inhibitors
(2019)
Innumerable biological systems rely on Protein-Protein Interactions (PPIs) to govern basal physiological processes. Deregulation of PPIs is implicated in various human diseases, and PPIs have thus been frequently promoted ...
Structural and Biochemical Insights into Methylation Site and State Specificity of JMJD2 Lysine Demethylases.
(2012)
The human JMJD2/KDM4 family of histone lysine demethylases comprises four homologs: JMJD2A, JMJD2B, JMJD2C and JMJD2D. These enzymes have been implicated in a number of biological processes such as transcriptional activation, ...
Development of a Chemoproteomic Approach to Study Kinase-Substrate Interactions and the Discovery of CDK4 as a 4E-BP1 Kinase
(2019)
An instrumental aspect of cancer progression is the acquired deregulation of the cellular processes that regulate growth and proliferation. Most of these processes are, at some level, controlled by a kinase-catalyzed change ...
Examination of Aggregation Prone Proteins and their Higher Order Interactions by Ion Mobility-Mass Spectrometry.
(2015)
Amyloid forming peptides and proteins present an extreme challenge for modern analytical measurement techniques. When natively-folded biomolecules partition into misfolded forms, they produce a myriad of inherently unstable ...
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 ...
Directed Evolution of Stabilized Peptides with Bacterial Display
(2020)
Interactions between proteins govern cellular and the body’s states, including aberrant interactions found in diseases such as in cancers and infections. Small molecule drugs are not ideal in targeting these interactions ...
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 ...
Development and Discovery of Novel Inhibitors of Mycobacterium tuberculosis RNA Polymerase for the Treatment of Tuberculosis
(2022)
Tuberculosis (TB) is an infectious pulmonary disease caused by the pathogen Mycobacterium tuberculosis (MTB). It is the leading cause of death from a single bacterial pathogen and second, only to COVID-19, as the deadliest ...