A5064790610- Ubiquitin and proteasome pathways
- Inhalation and Respiratory Drug Delivery
- Cancer, Hypoxia, and Metabolism
- Epigenetics and DNA Methylation
- Microtubule and mitosis dynamics
- Nanoparticle-Based Drug Delivery
- Click Chemistry and Applications
- Autophagy in Disease and Therapy
- Pancreatic function and diabetes
- Drug Solubulity and Delivery Systems
- Peptidase Inhibition and Analysis
- Computational Drug Discovery Methods
- NF-κB Signaling Pathways
- Cell Adhesion Molecules Research
- Polyamine Metabolism and Applications
- Amino Acid Enzymes and Metabolism
- Monoclonal and Polyclonal Antibodies Research
- Catalytic Cross-Coupling Reactions
- Neutrophil, Myeloperoxidase and Oxidative Mechanisms
- Cytokine Signaling Pathways and Interactions
- Signaling Pathways in Disease
- Catalytic C–H Functionalization Methods
- Histone Deacetylase Inhibitors Research
- GABA and Rice Research
- Toxin Mechanisms and Immunotoxins
St. John's University
2017-2024
University of Central Florida
2012-2019
University of Massachusetts Chan Medical School
2016-2018
University of Kansas
2014-2016
Florida College
2013
Middle Tennessee State University
2007-2008
Johannes Gutenberg University Mainz
1982
Neutrophils release neutrophil extracellular traps (NETs) which ensnare pathogens and have pathogenic functions in diverse diseases. We examined the NETosis pathways induced by five stimuli; PMA, calcium ionophore A23187, nigericin, Candida albicans Group B Streptococcus. studied NET production neutrophils from healthy donors with inhibitors of molecules crucial to PMA-induced NETs including protein kinase C, calcium, reactive oxygen species, enzymes myeloperoxidase (MPO) elastase....
Heightened citrullination promotes the expression of inflammatory cytokines in rheumatoid arthritis.
Protein arginine deiminase 2 (PAD2) plays a key role in the onset and progression of multiple sclerosis, rheumatoid arthritis, breast cancer. To date, no PAD2-selective inhibitor has been developed. Such compound will be critical for elucidating biological roles this isozyme may ultimately useful treating specific diseases which PAD2 activity is dysregulated. achieve goal, we synthesized series benzimidazole-based derivatives Cl-amidine, hypothesizing that scaffold would allow access to...
Non-small cell lung cancer (NSCLC) is a global disorder, treatment options for which remain limited with resistance development by cells and off-target events being major roadblocks current therapies. The discovery of new drug molecules remains time-consuming, expensive, prone to failure in safety/efficacy studies. Drug repurposing (i.e., investigating FDA-approved use against indications) provides an opportunity shorten the cycle. In this project, we propose repurpose pirfenidone (PFD),...
This study aimed at developing metformin hydrochloride (Met) encapsulated liposomal vesicles for enhanced therapeutic outcomes reduced doses against breast cancer. Liposomal Met was prepared using thin-film hydration through various loading methods; passive loading, active and drug-loaded lipid film. The film method exhibited maximum entrapment efficiency (~65%) as compared to (~25%) (~5%) Met-loaded liposomes. efficacy of these optimized liposomes evaluated cellular uptake, cytotoxicity,...
The development of polyamine transport inhibitors (PTIs), in combination with the biosynthesis inhibitor difluoromethylornithine (DFMO), provides a method to target cancers high requirements. DFMO+PTI therapy results sustained intracellular depletion and cell death. A series substituted benzene derivatives were evaluated for their ability inhibit import spermidine DFMO-treated Chinese hamster ovary (CHO) L3.6pl human pancreatic cancer cells. Several design features discovered which strongly...
Glucose regulated protein 94 (Grp94) is the endoplasmic reticulum resident of heat shock 90 kDa (Hsp90) family molecular chaperones. Grp94 associates with many proteins involved in cell adhesion and signaling, including integrins, Toll-like receptors, immunoglobulins, mutant myocilin. has been implicated as a target for several therapeutic areas glaucoma, cancer metastasis, multiple myeloma. While 85% identical to other Hsp90 isoforms, N-terminal ATP-binding site possesses unique hydrophobic...
Abstract Peptidylarginine deiminase (PADI) enzymes are increasingly being associated with the regulation of chromatin structure and gene activity via histone citrullination. As one PADI family members, PADI1 has been mainly reported to be expressed in epidermis uterus, where protein keratinocytes is thought promote differentiation by citrullinating filament proteins. However, roles preimplantation development have not addressed. Using a PADI1-specific inhibitor Padi1-morpholino knockdown, we...
A one-pot procedure leading to disubstituted pyridines from the starting dibromopyridines is described. Key features include ability couple a range of aryl and even alkenylboronic acids at 2,3 and/or 2,5 positions with excellent regiocontrol under standard set conditions. Further, isolated yields are greatly improved by use neutral alumina in place silica for product purification. Finally, intrinsic electronic bias pyridine ring can be overcome using bromoiodopyridine.
There is growing evidence that repurposed drugs demonstrate excellent efficacy against many cancers, while facilitating accelerated drug development process. In this study, bedaquiline (BDQ), an FDA approved anti-mycobacterial agent, was and inhalable cyclodextrin complex formulation developed to explore its anti-cancer activity in non-small cell lung cancer (NSCLC). A sulfobutyl ether derivative of β-cyclodextrin (SBE-β-CD) selected based on phase solubility studies molecular modeling...
Polyamine homeostasis is critical for life and accomplished via a balance of polyamine biosynthesis, degradation, transport. Rapidly dividing cancer cells have been shown to high transport activity compared normal cells, likely due their requirement metabolites. The system (PTS) therapeutically relevant target, as it can provide selective drug delivery cells. This report describes the synthesis biological evaluation multimeric derivatives efficient PTS ligands. Arylmethyl-polyamine were...