The Therapeutic Potential Of Targeting Cardiac Rgs4.,
2023
Nova Southeastern University
The Therapeutic Potential Of Targeting Cardiac Rgs4., Giselle Del Calvo, Teresa Baggio Lopez, Anastasios Lymperopoulos
HPD Articles
G protein-coupled receptors (GPCRs) play pivotal roles in regulation of cardiac function and homeostasis. To function properly, every cell needs these receptors to be stimulated only when a specific extracellular stimulus is present, and to be silenced the moment that stimulus is removed. The regulator of G protein signaling (RGS) proteins are crucial for the latter to occur at the cell membrane, where the GPCR normally resides. Perturbations in both activation and termination of G protein signaling underlie numerous heart pathologies. Although more than 30 mammalian RGS proteins have been identified, each RGS protein seems to interact only with a …
Structural Features Of Thyroglobulin Linked To Protein Trafficking,
2023
Chapman University
Structural Features Of Thyroglobulin Linked To Protein Trafficking, Cintia E. Citterio, Kookjoo Kim, Bhavana Rajesh, Kevin Pena, Oliver Biggs Clark, Peter Arvan
Pharmacy Faculty Articles and Research
Thyroglobulin must pass endoplasmic reticulum (ER) quality control to become secreted for thyroid hormone synthesis. Defective thyroglobulin, blocked in trafficking, can cause hypothyroidism. Thyroglobulin is a large protein (~2750 residues) spanning regions I–II–III plus a C-terminal cholinesterase-like domain. The cholinesterase-like domain functions as an intramolecular chaperone for regions I–II–III, but the folding pathway leading to successful thyroglobulin trafficking remains largely unknown. Here, informed by the recent three-dimensional structure of thyroglobulin as determined by cryo-electron microscopy, we have bioengineered three novel classes of mutants yielding three entirely distinct quality control phenotypes. Specifically, upon expressing recombinant thyroglobulin, we find that first, mutations …
A Causal Inference Study: The Impact Of The Combined Administration Of Donepezil And Memantine On Decreasing Hospital And Emergency Department Visits Of Alzheimer’S Disease Patients,
2023
Chapman University
A Causal Inference Study: The Impact Of The Combined Administration Of Donepezil And Memantine On Decreasing Hospital And Emergency Department Visits Of Alzheimer’S Disease Patients, Ehsan Yaghmaei, Albert Pierce, Hongxia Lu, Yesha M. Patel, Louis Ehwerhemuepha, Ahmad Rezaie, Seyed Ahmad Sajjadi, Cyril Rakovski
Mathematics, Physics, and Computer Science Faculty Articles and Research
Alzheimer’s disease is the most common type of dementia that currently affects over 6.5 million people in the U.S. Currently there is no cure and the existing drug therapies attempt to delay the mental decline and improve cognitive abilities. Two of the most commonly prescribed such drugs are Donepezil and Memantine. We formally tested and confirmed the presence of a beneficial drug-drug interaction of Donepezil and Memantine using a causal inference analysis. We applied doubly robust estimators to one of the largest and high-quality medical databases to estimate the effect of two commonly prescribed Alzheimer’s disease (AD) medications, Donepezil and …
Anti-Inflammatory And Antioxidant Effects Of Sea Urchin Spine Extract,
2023
The American University in Cairo
Anti-Inflammatory And Antioxidant Effects Of Sea Urchin Spine Extract, Dina Magdy El Gamal
The Undergraduate Research Journal
Diadema savignyi spine extract in an experimental setup using L929 cell line in vitro. The cell metabolic activity of L929 cells is tested through an MTT assay. The sea urchin spine extract is applied to the cells in two concentrations: 100 μg/ml (136% viability) and 200 μg/ml (95% viability). The bioactive components of the sea urchin spine are identified via GC-MS, and the antioxidant and anti-inflammatory activities are evaluated using catalase assay (CAT), glutathione (GSH), and nitric oxide (NO) tests. Results show that the GC-MS identified bioactive components including the anti-inflammatory and anti-irritant bisabolol oxide and the pro-inflammatory oleic acid. …
Steamed Broccoli Sprouts Alleviate Dss-Induced Inflammation And Retain Gut Microbial Biogeography In Mice,
2023
Binghamton University--SUNY
Steamed Broccoli Sprouts Alleviate Dss-Induced Inflammation And Retain Gut Microbial Biogeography In Mice, Johanna M. Holman, Louisa Colucci, Dorien Baudewyns, Joe Balkan, Timothy Hunt, Benjamin Hunt, Marissa Kinney, Lola Holcomb, Allesandra Stratigakis, Grace Chen, Peter L. Moses, Gary M. Mawe, Tao Zhang, Yanyan Li, Suzanne L. Ishaq
Pharmacy Faculty Scholarship
Inflammatory bowel diseases (IBDs) are devastating conditions of the gastrointestinal tract with limited treatments, and dietary intervention may be effective and affordable for managing symptoms. Glucosinolate compounds are highly concentrated in broccoli sprouts, especially glucoraphanin (GLR), and can be metabolized by certain mammalian gut bacteria into antiinflammatory isothiocyanates, such as sulforaphane. Gut microbiota exhibit biogeographic patterns, but it is unknown if colitis alters these or whether the location of glucoraphanin-metabolizing bacteria affects antiinflammatory benefits. We fed specific pathogen-free C57BL/6 mice either a control diet or a 10% steamed broccoli sprout diet and gave a three-cycle regimen of 2.5% dextran sodium …
Folate Conjugated Nanomedicines For Selective Inhibition Of Mtor Signaling In Polycystic Kidneys At Clinically Relevant Doses,
2023
Chapman University
Folate Conjugated Nanomedicines For Selective Inhibition Of Mtor Signaling In Polycystic Kidneys At Clinically Relevant Doses, Rajasekharreddy Pala, Ayan K. Barui, Ashraf M. Mohieldin, Jing Zhou, Surya M. Nauli
Pharmacy Faculty Articles and Research
Although rapamycin is a very effective drug for rodents with polycystic kidney disease (PKD), it is not encouraging in the clinical trials due to the suboptimal dosages compelled by the off-target side effects. We here report the generation, characterization, specificity, functionality, pharmacokinetic, pharmacodynamic and toxicology profiles of novel polycystic kidney-specific-targeting nanoparticles (NPs). We formulated folate-conjugated PLGA-PEG NPs, which can be loaded with multiple drugs, including rapamycin (an mTOR inhibitor) and antioxidant 4-hydroxy-TEMPO (a nephroprotective agent). The NPs increased the efficacy, potency and tolerability of rapamycin resulting in an increased survival rate and improved kidney function by decreasing side effects and …
Intranasal Sufentail Vs. Intravenous Morphine For Acute Pain In The Emergency Department,
2023
Long Island University
Intranasal Sufentail Vs. Intravenous Morphine For Acute Pain In The Emergency Department, Billy Sin, Lilia Davenport, Gabriella Sikorska, Joi Yam Yau Lin
Discovery Day
Introduction: Acute pain management in the emergency department (ED) requires prompt administration of safe and effective analgesia. ¬Traditional routes of administration for analgesia includes the oral (PO), intravenous (IV), or intramuscular routes (IM). When these routes of administration are not feasible, the intranasal (IN) route may be considered. Furthermore, a rapid onset of therapeutic effects may be observed due to the rich capillary network of the respiratory mucosa that is able to promptly transport the drug into systemic circulation. There is emerging literature that supports the use of analgesia via the IN route in the Emergency Department (ED). However, its …
A Fleeting Glimpse Of Functional Benefit Of The Complete Dmd Gene In A Large Animal Model Of Duchenne Muscular Dystrophy,
2023
Binghamton University -- SUNY
A Fleeting Glimpse Of Functional Benefit Of The Complete Dmd Gene In A Large Animal Model Of Duchenne Muscular Dystrophy, Eric P. Hoffman
Pharmacy Faculty Scholarship
No abstract provided.
Probing The Activation Mechanisms Of Agonist Dpi-287 To Delta-Opioid Receptor And Novel Agonists Using Ensemble-Based Virtual Screening With Molecular Dynamics Simulations.,
2023
Rowan University
Probing The Activation Mechanisms Of Agonist Dpi-287 To Delta-Opioid Receptor And Novel Agonists Using Ensemble-Based Virtual Screening With Molecular Dynamics Simulations., Emily Dean, Annemarie Dominique, Americus Palillero, Annie Tran, Nicholas Paradis, Chun Wu
College of Science & Mathematics Departmental Research
Pain drugs targeting mu-opioid receptors face major addiction problems that have caused an epidemic. The delta-opioid receptor (DOR) has shown to not cause addictive effects when bound to an agonist. While the active conformation of the DOR in complex with agonist DPI-287 has been recently solved, there are still no FDA-approved agonists targeting it, providing the opportunity for structure-based virtual screening. In this study, the conformational plasticity of the DOR was probed using molecular dynamics (MD) simulations, identifying two representative conformations from clustering analysis. The two MD conformations as well as the crystal conformation of DOR were used to screen …
Clustering Microbiome Data Using Mixtures Of Logistic Normal Multinomial Models,
2023
Binghamton University–SUNY
Clustering Microbiome Data Using Mixtures Of Logistic Normal Multinomial Models, Yuan Fang, Sanjeena Subedi
Pharmacy Faculty Scholarship
Discrete data such as counts of microbiome taxa resulting from next-generation sequencing are routinely encountered in bioinformatics. Taxa count data in microbiome studies are typically high-dimensional, over-dispersed, and can only reveal relative abundance therefore being treated as compositional. Analyzing compositional data presents many challenges because they are restricted to a simplex. In a logistic normal multinomial model, the relative abundance is mapped from a simplex to a latent variable that exists on the real Euclidean space using the additive log-ratio transformation. While a logistic normal multinomial approach brings flexibility for modeling the data, it comes with a heavy computational cost …
The Price Of Competition: Analyzing Anticompetitive Tactics In Pharmaceutical Markets During The Hatch-Waxman Era,
2023
Notre Dame Law School
The Price Of Competition: Analyzing Anticompetitive Tactics In Pharmaceutical Markets During The Hatch-Waxman Era, William Ulrich
Notre Dame Journal on Emerging Technologies
Pharmaceutical manufacturers can delay the generic entry for a blockbuster drug. In order to keep the generic system on track, it is critical to expose the various avenues of generic delay. Part I of this Note briefly describes the generic entry process as prescribed by the Hatch-Waxman Act. Part II details four well-known tactics used by brand-name manufacturers to block or delay the entry of generic competition, highlighting how the tactics are successful. Part III concludes by examining the nature of the various problems and arguing that the first step towards ending the different forms of anticompetitive behavior is through …
The High Cost Of Pharmaceutical Acquisitions: Increasing Social Welfare Or Furthering Inequality?,
2023
Notre Dame Law School
The High Cost Of Pharmaceutical Acquisitions: Increasing Social Welfare Or Furthering Inequality?, Timothy J. Haltermann
Notre Dame Journal on Emerging Technologies
This note will argue that government and regulatory authorities should focus on easing access to downstream innovation by broadening research exemptions to patent infringement. Part I of this note will focus on the current state of patent protection and exclusivity afforded to pharmaceutical companies. Part II will discuss incentives created that lead rational actors to engage in M&A instead of through internal R&D. Part III will address the development of innovation as a standalone theory of harm in merger review, and the fallacies associated with labeling certain transactions as “killer acquisitions.” Finally, Part IV of the note will look at …
Artificial Intelligence Is Revolutionizing Controlled Substance Diversion Detection,
2023
Marshall University
Artificial Intelligence Is Revolutionizing Controlled Substance Diversion Detection, Brian Cox, Alberto Coustasse, Craig Kimble
Management Faculty Research
In community and institutional health care sectors, artificial intelligence (AI) use is expanding. AI is being tapped broadly in operations, customer service, and scheduling, with major pharmacy chains such as Kroger, CVS, and Walgreens, already starting to implement AI applications in their pharmacies. So far, Kroger has begun to use AI for employee onboarding and training processes, CVS is applying AI in negotiations with suppliers, and Walgreens is using it to streamline vaccine scheduling. With these advances in major pharmacy chains, the next extensive application for AI has become clearer: diversion monitoring. Diversion occurs in health care settings when a …
Equine In Vivo Metabolite Profiling Of The Selective Androgen Receptor Modulator Lgd-3303 For Doping Control,
2023
Uppsala University
Equine In Vivo Metabolite Profiling Of The Selective Androgen Receptor Modulator Lgd-3303 For Doping Control, Malin Nilsson Broberg, Heather Knych, Ulf Bondesson, Curt Pettersson, Börje Tidstedt, Scott Stanley, Mario Thevis, Mikael Hedeland
UK CARES Faculty Publications
LGD-3303 is a Selective Androgen Receptor Modulator (SARM) that is prohibited in both equine and human sports due to its anabolic properties. The aim of this study was to investigate the equine in vivo metabolite profile of LGD-3303 and identify drug metabolites that can be suitable as new and improved analytical targets for equine doping control. This was performed by an oral administration of 0.05 mg⋅kg 1 LGD-3303 to horses, where blood and urine samples were collected up to 96 h after administration. The in vivo samples consisting of plasma, urine and hydrolyzed urine were analyzed utilizing ultra-high performance liquid …
A Real-World Comparison Of Apixaban And Rivaroxaban In Obese And Morbidly Obese Patients With Nonvalvular Atrial Fibrillation,
2023
University of Texas at Tyler
A Real-World Comparison Of Apixaban And Rivaroxaban In Obese And Morbidly Obese Patients With Nonvalvular Atrial Fibrillation, Kevin T. Burnham, Tianrui Yang, Jessica Wooster
Pharmacy Faculty Publications and Presentations
Background: Contemporary guidelines for managing nonvalvular atrial fibrillation (NVAF) include apixaban and rivaroxaban as first-line anticoagulation treatment options. Minimal guidance is available regarding selecting anticoagulants for patients with class I-III obesity. Objective: This study aims to evaluate the comparative effectiveness and safety of apixaban and rivaroxaban in both obese and morbidly obese patients with NVAF. Methods: A retrospective cohort study was conducted at an outpatient cardiovascular clinic after Institutional Review Board approval. Patients were eligible if they were ≥18 years of age, had a BMI ≥30 kg/m2, and took apixaban or rivaroxaban for NVAF for ≥3 months. The primary endpoint …
Isatin-Pyrimidine Hybrid Derivatives As Enoyl Acyl Carrier Protein Reductase (Inha) Inhibitors Against Mycobacterium Tuberculosis,
2023
Department of Pharmaceutical Chemistry- Department of Pharmaceutical Chemistry, Faculty of Pharmacy, The British University in Egypt, El-Sherouk City, Cairo 11837, Egypt
Isatin-Pyrimidine Hybrid Derivatives As Enoyl Acyl Carrier Protein Reductase (Inha) Inhibitors Against Mycobacterium Tuberculosis, Amira Khalil, Samy Mohamady, Amgad Albohy, Marwa M. Abdel-Aziz, Abdalrahman Khalifa
Pharmacy
Tuberculosis is a worldwide problem that impose a burden on the economy due to continuous development of resistant strains. The development of new antitubercular drugs is a need and can be achieved through inhibition of druggable targets. Mycobacterium tuberculosis enoyl acyl carrier protein (ACP) reductase (InhA) is an important enzyme for Mycobacterium tuberculosis survival. In this study, we report the synthesis of isatin derivatives that could treat TB through inhibition of this enzyme. Compound 4l showed IC50 value (0.6 ± 0.94 µM) similar to isoniazid but is also effective against MDR and XDR Mycobacterium tuberculosis strains (MIC of 0.48 and …
Unleashing The Potential Of 1,3-Diketone Analogues As Selective Lh2 Inhibitors,
2023
The University of Texas at Austin
Unleashing The Potential Of 1,3-Diketone Analogues As Selective Lh2 Inhibitors, Juhoon Lee, Hou-Fu Guo, Shike Wang, Yazdan Maghsoud, Erik Antonio Vázquez-Montelongo, Zhifeng Jing, Rae M. Sammons, Eun Jeong Cho, Pengyu Ren, G. Andrés Cisneros, Jonathan M. Kurie, Kevin N. Dalby
Markey Cancer Center Faculty Publications
Lysyl hydroxylase 2 (LH2) catalyzes the formation of highly stable hydroxylysine aldehyde-derived collagen cross-links (HLCCs), thus promoting lung cancer metastasis through its capacity to modulate specific types of collagen cross-links within the tumor stroma. Using 1 and 2 from our previous high-throughput screening (HTS) as lead probes, we prepared a series of 1,3-diketone analogues, 1−18, and identified 12 and 13 that inhibit LH2 with IC50’s of approximately 300 and 500 nM, respectively. Compounds 12 and 13 demonstrate selectivity for LH2 over LH1 and LH3. Quantum mechanics/molecular mechanics (QM/MM) modeling indicates that the selectivity of 12 and 13 may stem from …
Significant Improvement Of Fidelity For Encoded Quantum Bell Pairs At Long And Short-Distance Communication Along With Generalized Circuit,
2023
The Texas Medical Center Library
Significant Improvement Of Fidelity For Encoded Quantum Bell Pairs At Long And Short-Distance Communication Along With Generalized Circuit, Syed Emad Uddin Shubha, Md Saifur Rahman, M R C Mahdy
Faculty, Staff and Student Publications
Quantum entanglement is a unique criterion of the quantum realm and an essential tool to secure quantum communication. Ensuring high-fidelity entanglement has always been a challenging task owing to interaction with the hostile channel environment created due to quantum noise and decoherence. Though several methods have been proposed, correcting almost all arbitrary errors is still a gigantic task. As one of the main contributions of this work, a new model for 'large distance communication' has been proposed, which may correct all bit flip errors or other errors quite extensively if proper encoding and subspace measurements are used. To achieve this …
Solid Lipid Nanoparticles (Sln): Formulation And Fabrication,
2023
Faculty of Pharmacy, Universitas Indonesia, Depok, West Java, Indonesia
Solid Lipid Nanoparticles (Sln): Formulation And Fabrication, Gabriella F. Punu, Yahdiana Harahap, Qonita Kurnia Anjani, Pietradewi Hartrianti, Ryan F. Donnelly, Delly Ramadon
Pharmaceutical Sciences and Research
Solid lipid nanoparticles (SLN) have emerged as a novel drug delivery system and have been utilized for delivering various kinds of drugs since the 1990s. These particles may consist of multiple solid lipids, including glycerides, waxes, and fatty acids, and can be stabilized by a wide range of surfactants. SLN have garnered significant attention from researchers due to its innovative and versatile nature. Moreover, such delivery system has numerous advantages over traditional colloidal carriers, such as liposomes, polymeric nanoparticles, and emulsions. Several research groups have been developing SLN formulations and fabrication techniques based on their intended purpose, and this research …
Optimization Of Lubrication And Compression Process Parameters Of Vitamin C Film-Coated Caplets,
2023
School of Pharmacy, Institute of Technology Bandung, West Java, Indonesia
Optimization Of Lubrication And Compression Process Parameters Of Vitamin C Film-Coated Caplets, Ernestine Arianditha Pranasti, Ratna Annisa Utami, Yuda Prasetya Nugraha
Pharmaceutical Sciences and Research
Tablet production is a very intricate process influenced by numerous process variables or parameters. This study aimed to identify the critical processing variables that affect Critical Quality Attributes (CQAs) of vitamin C film-coated caplets utilizing a statistical experimental design. A two-level complete factorial design with two central points was used to examine the process parameters that posed the greatest risk to CQAs. The process variables investigated included mesh size and duration for the lubrication process, as well as speed and main thickness for compression. Statistical results showed that mesh number, lubrication time, and their interaction significantly affect flow rate, Hausner …
