Now showing items 2061-2070 of 2082
Peptide and Nonpeptide Approaches to Target Protein-protein Interactions for the Treatment of Cancer.
(2015)
Protein-protein interactions (PPIs) are macromolecular contacts critical in physiological processes and they play a role in both normal cellular processes and disease pathogenesis. Targeting PPIs represents a new but poorly ...
High Throughput Experimentation Facilitated Development of Amine-Acid Cross Coupling Reactions
(2023)
High throughput experimentation (HTE) is an important technique which can expedite the hit-to-lead process in drug discovery. The first chapter of this thesis reviews reported applications using HTE in medicinal chemistry ...
Understanding the Solution Phase Chemistry and Solid State Thermodynamic Behavior of Pharmaceutical Cocrystals.
(2012)
This dissertation focuses on the thermodynamic stability and solubility of pharmaceutical cocrystals. Specifically, the objectives are to; (i) investigate the influence of coformer properties such as solubility and ionization ...
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 ...
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 ...
Thermodynamic and Mathematical Relationships for Predicting Cocrystal Stability and Controlling Dissolution - Supersaturation - Precipitation Behavior
(2020)
Although pharmaceutical cocrystals have emerged as a useful strategy for enhancing the solubility, dissolution, and oral bioavailability of poorly water-soluble drugs, their development has thus far been marked by a lack ...
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 ...