Open Access. Powered by Scholars. Published by Universities.®
- Institution
- Keyword
-
- Amino Acids (1)
- Antibiotic resistance (1)
- Antiproliferative (1)
- Beta-lactam (1)
- Combretastatin A-4 prodrug (1)
-
- Crystallography (1)
- Driving group (1)
- Drug delivery system (1)
- Drug discovery (1)
- Glycopeptide (1)
- Guanine (1)
- Imaging probe (1)
- Inhibitor of vertebrate lysozyme (1)
- Metals (1)
- NMR-based drug optimization (1)
- PET imaging (1)
- Proteins (1)
- Rhenium (1)
- SPECT imaging (1)
- Selenophene (1)
- Solubility (1)
- Synthesis (1)
- Theranostics (1)
- Tubulin (1)
- Publication
- Publication Type
Articles 1 - 6 of 6
Full-Text Articles in Heterocyclic Compounds
Visible Light Kinetics Of N-Heterocyclic Carbenes As Additives For Native Chemical Ligation, Hannah M. Werle, Kaitlyn S. Marley, John P. Morgan
Visible Light Kinetics Of N-Heterocyclic Carbenes As Additives For Native Chemical Ligation, Hannah M. Werle, Kaitlyn S. Marley, John P. Morgan
SURF Posters 2026
Spectroscopic data have been obtained demonstrating that N-heterocyclic carbenes are effective catalysts for linking shorter peptides to form longer ones, a reaction known as “native chemical ligation” (NCL). This reaction is key to the preparation of GLP-1 agonists, such as Zepbound®, Ozempic®, and Wegovy®, which are currently undergoing an explosion in popularity due to their treatment of diabetes, obesity, and cardiac issues. To assess which catalysts are faster, the kinetics model developed by Raines et al., involving the reaction of N-acetylphenylalanine p-nitrophenylthioester and L-cysteine, is being utilized. This published model allows for easy monitoring of the rate of reaction for …
Design, Synthesis, And Nmr-Guided Characterization Of A Targeted Covalent Inhibitor-Like Molecule Against Ivyp1 From P. Aeruginosa, Samuel Taylor Moore
Design, Synthesis, And Nmr-Guided Characterization Of A Targeted Covalent Inhibitor-Like Molecule Against Ivyp1 From P. Aeruginosa, Samuel Taylor Moore
Master's Theses
Multi-drug resistance poses a serious threat to future generations and historical antibiotic pipelines; consequently, the medical and economic burdens associated with treating multidrug-resistant bacteria are substantiated. In this context, P. aeruginosa (PA) emerges as one of the most significant healthcare challenges, being a leading cause of resistance-associated mortality worldwide. Despite modern efforts to combat these poor outcomes, drug-resistant cases continue to rise, and the need for novel antibiotic treatment is apparent. To this end, we investigated relevant resistance mechanisms and past antibiotic targets within PA, and in doing so, we identified relationships between peptidoglycan biology and a periplasmic protein, Inhibitor …
Designing And Synthesizing A Warhead-Fragment Inhibitory Ligand For Ivyp1 Through Fragment-Based Drug Discovery, Samuel Moore
Designing And Synthesizing A Warhead-Fragment Inhibitory Ligand For Ivyp1 Through Fragment-Based Drug Discovery, Samuel Moore
Symposium of Student Scholars
Fragment-based drug discovery (FBDD) is a powerful tool for developing anticancer and antimicrobial agents. Within this, magnetic resonance spectroscopy (NMR) provides a comprehensive qualitative and quantitative approach to screening and validating weak and robust binders with targeted proteins, making NMR among the most attractive strategies in FBDD. Inhibitor of vertebrate lysozyme (Ivyp1) of P. aeruginosa serves as an excellent target because of its active cellular location and implications in clinical prognosis for cystic fibrosis and immunocompromised patients. This study uses current NMR and biophysical techniques to develop a covalent, fragment-linked warhead inhibitor for Ivyp1 through synthetic methods, warhead linking, and …
Synthesis Of Selenotryptophan For Protein Elucidation, James P. Reiselman
Synthesis Of Selenotryptophan For Protein Elucidation, James P. Reiselman
[Archive] Belmont University Research Symposium (BURS)
Through complex intermolecular and intramolecular forces, proteins conformationally change to form complex 3-d geometry that carries out biochemical processes and mapping their structures is becoming a field of interest in the biological community. Techniques for modeling protein’s structure typically follow the path of X-ray crystallography, which has an intrinsic phase problem that can make reading the electron density map they produce very difficult. This can be mitigated by appending a heavy-atom containing amino acid analogue into a crystal sample of the protein being studied. A selenium containing tryptophan analogue will be synthesized to be appended into proteins as a chemical …
Design, Synthesis And Development Of Transporter Targeting Agents For Image-Guided Therapy And Drug Delivery, Ning Tsao
Dissertations and Theses (Open Access)
The purpose of this study was to design, synthesize and develop novel transporter targeting agents for image-guided therapy and drug delivery. Two novel agents, N4-guanine (N4amG) and glycopeptide (GP) were synthesized for tumor cell proliferation assessment and cancer theranostic platform, respectively. N4amG and GP were synthesized and radiolabeled with 99mTc and 68Ga. The chemical and radiochemical purities as well as radiochemical stabilities of radiolabeled N4amG and GP were tested. In vitro stability assessment showed both 99mTc-N4amG and 99mTc-GP were stable up to 6 hours, whereas 68Ga-GP was stable up to 2 hours. Cell culture studies …
Synthesis And Biochemical Activities Of Antiproliferative Amino Acid And Phosphate Derivatives Of Microtubule-Disrupting Beta-Lactam Combretastatins, Niamh M. O'Boyle, Lisa M. Greene, Niall O. Keely, Shu Wang, Tadhg S. Cotter, Daniela M. Zisterer, Mary J. Meegan
Synthesis And Biochemical Activities Of Antiproliferative Amino Acid And Phosphate Derivatives Of Microtubule-Disrupting Beta-Lactam Combretastatins, Niamh M. O'Boyle, Lisa M. Greene, Niall O. Keely, Shu Wang, Tadhg S. Cotter, Daniela M. Zisterer, Mary J. Meegan
Articles
The synthesis and biochemical activities of novel water-soluble β-lactam analogues of combretastatin A-4 are described. The first series of compounds investigated, β-lactam phosphate esters 7a, 8a and 9a, exhibited potent antiproliferative activity and caused microtubule disruption in human breast carcinoma-derived MCF-7 cells. They did not inhibit tubulin polymerisation in vitro, indicating that biotransformation was necessary for their antiproliferative and tubulin binding effects in MCF-7 cells. The second series of compounds, β-lactam amino acid amides (including 10k and 11l) displayed potent antiproliferative activity in MCF-7 cells, disrupted microtubules in MCF-7 cells and also inhibited the polymerisation of …