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Full-Text Articles in Biochemistry, Biophysics, and Structural Biology

Synthesis Of An Ideal Inhibitor For The Lpxc Enzyme, Taejun Lee Apr 2019

Synthesis Of An Ideal Inhibitor For The Lpxc Enzyme, Taejun Lee

Honors Theses

Due to the growing need of antibiotics in modern day medicine, this study attempts to apply a method of medicinal chemistry that would create a novel inhibitor for a lesser known target of gram negative bacteria, the LpxC enzyme. This study proposes that a synthetic plan which consists of combining components of different molecules would create a more effective inhibitor. These components include a binding group for the active site of the enzyme, a hydrophobic chain which has been shown to interact with an allosteric site on the LpxC enzyme, and the isoxazoline ring which interacts with the zinc ion ...


Lysine Biosynthesis In Bacteria: A Metallodesuccinylase As A Potential Antimicrobial Target, Danuta M. Gillner, Daniel P. Becker Ph.D., Richard C. Holz Feb 2018

Lysine Biosynthesis In Bacteria: A Metallodesuccinylase As A Potential Antimicrobial Target, Danuta M. Gillner, Daniel P. Becker Ph.D., Richard C. Holz

Richard C. Holz

In this review, we summarize the recent literature on dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) enzymes, with an emphasis on structure–function studies that provide insight into the catalytic mechanism. Crystallographic data have also provided insight into residues that might be involved in substrate and hence inhibitor recognition and binding. These data have led to the design and synthesis of several new DapE inhibitors, which are described along with what is known about how inhibitors interact with the active site of DapE enzymes, including the efficacy of a moderately strong DapE inhibitor.


Environmental And Genetic Factors Affecting Antibiotic Resistance Of Extended Spectrum Î?-Lactamase Bacteria From The Rio Grande River In El Paso, Tx And Cd. Juarez, Mexico, Maria D. Fuentes Jan 2018

Environmental And Genetic Factors Affecting Antibiotic Resistance Of Extended Spectrum Î?-Lactamase Bacteria From The Rio Grande River In El Paso, Tx And Cd. Juarez, Mexico, Maria D. Fuentes

Open Access Theses & Dissertations

Background: The Rio Grande River provides a major source of potable and agricultural water for the population of the Texas/Mexico border region. Cattle farming and ranching are the most prevalent activities, which may contribute to the microbial burden of pharmaceuticals into our state's water resources. Antibiotics, presumably released into the environment by discharges originating from waste-water treatment plants, septic disposal systems, animal feeding operations and urban runoff have a definite impact on the ecosystem and may contribute to an increase in antibiotic resistance. We hypothesized that waters of the Rio Grande River contained Multi Drug Resistant Organisms (MDRO ...


Development Of In Vivo Systems For Detecting And Studying Ribosome Inhibition By Small Molecules, Shijie Huang Nov 2016

Development Of In Vivo Systems For Detecting And Studying Ribosome Inhibition By Small Molecules, Shijie Huang

Chemistry ETDs

The ribosome is the quintessential antibacterial drug target, with many structurally and mechanistically distinct classes of antibacterial agents acting by inhibiting ribosome function. Detecting and quantifying ribosome inhibition by small molecules and investigating their binding modes and mechanisms of action are critical to antibacterial drug discovery and development efforts. To develop a ribosome inhibition assay that is operationally simple, yet provides direct information on the drug target and the mechanism of action, we have developed engineered E. coli strains harboring an orthogonal ribosome controlled green fluorescent protein reporter that produce fluorescent signal when the O-ribosome is inhibited. As a proof ...


Lysine Biosynthesis In Bacteria: A Metallodesuccinylase As A Potential Antimicrobial Target, Danuta M. Gillner, Daniel P. Becker Ph.D., Richard C. Holz Feb 2013

Lysine Biosynthesis In Bacteria: A Metallodesuccinylase As A Potential Antimicrobial Target, Danuta M. Gillner, Daniel P. Becker Ph.D., Richard C. Holz

Chemistry: Faculty Publications and Other Works

In this review, we summarize the recent literature on dapE-encoded N-succinyl-l,l-diaminopimelic acid desuccinylase (DapE) enzymes, with an emphasis on structure–function studies that provide insight into the catalytic mechanism. Crystallographic data have also provided insight into residues that might be involved in substrate and hence inhibitor recognition and binding. These data have led to the design and synthesis of several new DapE inhibitors, which are described along with what is known about how inhibitors interact with the active site of DapE enzymes, including the efficacy of a moderately strong DapE inhibitor.


Anti-Germinants As A New Strategy To Prevent Clostridium Difficile Infections, Amber Janece Howerton Dec 2012

Anti-Germinants As A New Strategy To Prevent Clostridium Difficile Infections, Amber Janece Howerton

UNLV Theses, Dissertations, Professional Papers, and Capstones

Clostridium difficileinfections (CDI) have emerged as a leading cause of hospital-associated complications. CDI is the major cause of antibiotic-related cases of diarrhea and nearly all cases of pseudomembranous colitis. The infective form of C. difficileis the spore, a dormant and hardy structure that forms under stress. Germination of C. difficile spores into toxin producing bacteria in the GI tract of susceptible patients is the first step in CDI establishment. Patient susceptibility occurs with a disruption of the natural gut microbiota by broad-spectrum antibiotics. Antibiotic treatments usually resolve CDI but refractory cases are on the rise. Of great concern is the ...


Development Of Inhalable Dry Powder Antibiotics And On-Bead Transcription Strategies, J'Aime Manion Jan 2011

Development Of Inhalable Dry Powder Antibiotics And On-Bead Transcription Strategies, J'Aime Manion

Chemistry & Biochemistry Graduate Theses & Dissertations (1986-2018)

The global resurgence of tuberculosis (TB), the disease caused by Mycobacterium tuberculosis (Mtb) bacilli, has been driven by poverty, the development of drug resistance strains of Mtb, imperfect diagnostic assays, limited access to healthcare, poor healthcare infrastructure in the most highly infected areas, limited vaccine efficacy, lack of new drugs, and -- most profoundly -- the spread of HIV. Within this web of limitations dry powder inhalable antibiotics offer an opportunity to potentially reduce the lengthy treatment times associated with TB treatment. Incomplete tuberculosis treatment is the leading factor in the development of antibiotic resistant strains of Mtb. Inhalable antibiotics, by merit ...


Synthesis Of Some Valine Derivatives As Potential Antibacterial Agents , Frederick Nelson Minard Jan 1949

Synthesis Of Some Valine Derivatives As Potential Antibacterial Agents , Frederick Nelson Minard

Retrospective Theses and Dissertations

No abstract provided.