Enzymes and Coenzymes Commons^™

Biochemical Assay Optimization And Computational Screening Efforts To Identify Potential Luxs Inhibitors, Keeshia Q. Wang

Master's Theses

Quorum sensing (QS) is a process of coordination of bacterial gene expression in response to cell population. System two QS is regulated by the small signaling molecule autoinducer-2 (AI-2) and is implicated in the infectious behaviors of various bacterial species. AI-2 is biosynthesized from S-ribosylhomocysteine (SRH) by the enzyme LuxS and induces interspecies cell-to-cell communication. Inhibition of LuxS would therefore inhibit interspecies QS. Herein, a search for novel molecular species that will competitively bind with SRH in the LuxS binding site is performed in silico. Computational screening results are then validated in vitro using an optimized LuxS inhibition …

Investigation Of Commercial Milk Enzyme-Linked Immunosorbent Assay (Elisa) Kits: Specificity And Utility For Residues Of Foods Subjected To Proteolysis During Processing, Katherine O. Ivens

Department of Food Science and Technology: Dissertations, Theses, and Student Research

Analytical methods, such as enzyme-linked immunosorbent assays (ELISA), are used to detect and quantify residues from allergenic sources in food products. However, ELISAs have not been validated for use in foods that have been exposed to proteolysis. This thesis explores the specificities, sensitivities, and capabilities of commercially-available milk ELISA kits for detecting milk residues in cheeses that have undergone varying degrees of proteolysis.

The specificity, accuracy, and consistency of twelve commercially-available milk ELISA kits for individual milk proteins and commonly used milk-derived ingredients, including α-,β-, and κ-casein, β-lactoglobulin, α-lactalbumin, non-fat dry milk, sodium caseinate, and whey protein concentrate were evaluated. …

Radiosensitization Of Head & Neck Carcinoma Cells By Linifanib, A Receptor Tyrosine Kinase Inhibitor, Heng-Wei Hsu

Loma Linda University Electronic Theses, Dissertations & Projects

Tumor angiogenesis is a hallmark of advanced cancers and promotes invasion and metastasis. Over 90% of head and neck squamous cell carcinomas (HNSCC) express angiogenic factors such as vascular endothelial growth factor (VEGF). Since radiotherapy is one of the most commonly used treatments for HNSCC, it is imperative to identify the interactions between antiangiogenic therapy and radiotherapy, and to develop combination therapy to improve clinical outcome. The mechanisms between antiangiogenic agents and ionizing radiation are complicated and involve many interactions between the vasculature, tumor stroma and tumor cells. The proliferation and metastasis of tumor cells rely on angiogenesis/blood vessel formation. …

Enzymatic Hydrolysis Of Biomass At High-Solids Loadings – A Review, Alicia A. Modenbach, Sue E. Nokes

Biosystems and Agricultural Engineering Faculty Publications

Enzymatic hydrolysis is the unit operation in the lignocellulose conversion process that utilizes enzymes to depolymerize lignocellulosic biomass. The saccharide components released are the feedstock for fermentation. When performed at high-solids loadings (≥ 15% solids, w/w), enzymatic hydrolysis potentially offers many advantages over conversions performed at low- or moderate-solids loadings, including increased sugar and ethanol concentrations and decreased capital and operating costs.

The goal of this review is to provide a consolidated source of information on studies using high-solids loadings in enzymatic hydrolysis. Included in this review is a brief discussion of the limitations, such as a lack of available …

Rescuing Acetylcholinesterase From Nerve Agent Inhibition: Protein Dynamics Driven Drug Discovery, Aiyana M. Emigh, Brian Bennion

STAR Program Research Presentations

Severe morbidity and mortality consequences result from irreversible inhibition of human acetylcholinesterase by organophosphates (OPs). Oxime-based reactivators are currently the only available treatments but lack efficacy in the central nervous system (CNS) where the most damage occurs. Computational docking and molecular dynamics (MD) simulations reveal complex structural barriers that may reduce oxime efficacy. These results may guide future drug designs of more effective countermeasures.

Synthesis Of Pyrazolo[3,4-D]Pyrimidine Derivatives And Evaluation Of Their Src Kinase Inhibitory Activities, Anil Kumar, Guofeng Ye, Xianfeng Gu, Yuehao Wang, Gongqin Sun, Keykavous Parang

Pharmacy Faculty Articles and Research

A series of pyrazolo[3,4-d]pyrimidine derivatives was synthesized and evaluated for the Src kinase inhibitory activities. Compound 6e and 10c exhibited inhibition of Src kinase with an IC50 value of 5.6 and 5.1 μM, respectively. Hydroxamate derivative 15a was found to be a metal-mediated inhibitor for human Csk with an IC50 value of 2.0 μM showing 56-fold selectivity over Src kinase inhibition.

Biosynthetic Pathway Of The Aminoribosyl Component Of Lipopeptidyl Nucleoside Antibiotics, Xiuling Chi

Theses and Dissertations--Pharmacy

Several lipopeptidyl nucleoside antibiotics that inhibit bacterial translocase I (MraY) involved in peptidoglycan cell wall biosynthesis contain an aminoribosyl moiety, an unusual sugar appendage in natural products. A-90289 and muraminomicin are the two representative antibiotics that belong to this family. Bioinformatic analysis of the biosynthetic A-90289 gene clusters revealed that five enzymes are likely involved in the assembly and attachment of the aminoribosyl unit. These enzymes of A-90289 are functionally assigned by in vitro characterization. The results reveal a unique ribosylation pathway that highlighted by uridine-5′-monophosphate as the source of the sugar, a phosphorylase strategy to generate a sugar-1-phosphate, and …