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Articles 1 - 30 of 458

Full-Text Articles in Medicinal and Pharmaceutical Chemistry

Medication Overdoses In The Emergency Department: Oral Hypoglycemic Agents, Atypical Antipsychotic Agents, Beta-Blockers, Calcium Channel Blockers, And Digoxin, Brooke Marlowe, Tara Tokar, Kayti Kintner, Kelsey Fink, Grant Walliser Oct 2019

Medication Overdoses In The Emergency Department: Oral Hypoglycemic Agents, Atypical Antipsychotic Agents, Beta-Blockers, Calcium Channel Blockers, And Digoxin, Brooke Marlowe, Tara Tokar, Kayti Kintner, Kelsey Fink, Grant Walliser

Pharmacy and Wellness Review

The number of medication toxicities has been steadily increasing with more patients presenting to the emergency department for both intentional and unintentional overdoses. Oral hypoglycemics, atypical antipsychotics, betablockers, calcium channel blockers and digoxin overdoses are some of the more common medication toxicities health care professionals may see in practice. Toxic doses of oral hypoglycemic agents, beta-blockers, calcium channel blockers and digoxin have more definitive options for treatment, while atypical antipsychotic overdoses are managed with supportive care. Pharmacists in particular play a pivotal role in identifying presenting symptoms and recommending appropriate treatment options in toxicological emergencies.


Understanding The Pharmacokinetic Interaction Betweenalcohol And Long-Acting Opioids, Emily Blum, Brittany Crowe, Tanya Wilsmann, Heather Helsel, David Kisor Oct 2019

Understanding The Pharmacokinetic Interaction Betweenalcohol And Long-Acting Opioids, Emily Blum, Brittany Crowe, Tanya Wilsmann, Heather Helsel, David Kisor

Pharmacy and Wellness Review

In response to the fatal interaction of alcohol with extended-release hydromorphone, the U.S. Food and Drug Administration (FDA) approved a class-wide Risk Evaluation and Mitigation Strategy (REMS) for extended-release (ER) and long-acting (LA) opioid analgesics in July 2012. Due to the rising concern of dose-dumping effects, it is important for pharmacists to understand the pharmacokinetic interaction between two of the most commonly prescribed LA opioids (oxycodone and morphine) and alcohol. Clinical trials have looked at the pharmacokinetic profile of these long-acting formulations in conjunction with alcohol, and the results have varied depending on the formulation. For this reason, it ...


Truvada® Recommended By Fda Committee For Pre-Exposure Prophylaxis In Highriskhiv-Negative Individuals, Justin Steele, Emily Blum, Alison Steinbrunner, Lara Long, Andrew M. Roecker Oct 2019

Truvada® Recommended By Fda Committee For Pre-Exposure Prophylaxis In Highriskhiv-Negative Individuals, Justin Steele, Emily Blum, Alison Steinbrunner, Lara Long, Andrew M. Roecker

Pharmacy and Wellness Review

Once-daily combination tenofofovir disoproxil fumarate (TDF) and emtricitabine (FTC) has received Food and Drug Administration (FDA) approval for use in pre-exposure prophylaxis (PrEP) against Human Immunodeficiency Virus (HIV) infection in high-risk individuals. In clinical trials, FTC/TDF has been shown to reduce the risk of HIV acquisition by 62 percent in sexually active heterosexual men and women. Similarly, use of FTC/TDF demonstrated a 44 percent reduction in HIV infection within the men who have sex with men population.7 When used compliantly and in conjunction with safe sex practices, it appears that FTC/TDF can play an important role ...


Comparing The Glp-1 Receptor Agonists: Byetta®, Victoza® And Once-Weeklybydureon™, Todd A. Tucker Jr., Sarah Turley, Kaila Bollinger, Jessica Beck, Sandra L. Hrometz Oct 2019

Comparing The Glp-1 Receptor Agonists: Byetta®, Victoza® And Once-Weeklybydureon™, Todd A. Tucker Jr., Sarah Turley, Kaila Bollinger, Jessica Beck, Sandra L. Hrometz

Pharmacy and Wellness Review

Type 2 diabetes mellitus (T2DM) has traditionally been managed with oral medications. However, in the last few years, subcutaneous glucagon-like peptide-1 (GLP-1) receptor agonists have risen to fame. These agents serve as a reliable addition to current monotherapy. GLP-1 receptor agonists offer a significant reduction in hemoglobin AlC (HbAlc), fasting plasma glucose, and have the added benefit of weight loss. They work primarily by enhancing glucose-dependent insulin secretion while inhibiting glucagon secretion. The available GLP-1 agonists are Byetta® (exenatide), Victoza® (liraglutide), and Bydureon™ (exenatide extended-release). Studies suggest that they are similar in safety and efficacy, with the longer acting GLP-1 ...


Sildenafil As An Appropriate Monotherapy Option In The Treatment Of Pulmonaryarterial Hypertension (Pah), Kaitlin Horton, Kent Wilin, Sarah Ginty, Lara Long, David Bright Oct 2019

Sildenafil As An Appropriate Monotherapy Option In The Treatment Of Pulmonaryarterial Hypertension (Pah), Kaitlin Horton, Kent Wilin, Sarah Ginty, Lara Long, David Bright

Pharmacy and Wellness Review

Pulmonary arterial hypertension (PAH) is a debilitating disease characterized by constriction in the diameter of the pulmonary arterial lumen.1,2 This leads to increased pressure and stress on the right ventricle of the heart, which may lead to heart failure and death.2,3 Currently there are only a few treatment options for patients with PAH. Sildenafil, a phosphodiesterase type 5 (PDE-5) inhibitor, can be used to treat PAH. Sildenafil inhibits the degradation of cyclic guanosine monophosphate (cGMP). Increased cGMP concentration results in pulmonary vasculature relaxation. Current clinical trials have indicated that sildenafil can significantly improve many of the ...


Overview Of Stevens-Johnson Syndrome And Toxic Epidermal Necrolysis, Christina Spinaris, Sarah Kradel, Tara Tokar, Zachary Crawford, Michael M. Milks Oct 2019

Overview Of Stevens-Johnson Syndrome And Toxic Epidermal Necrolysis, Christina Spinaris, Sarah Kradel, Tara Tokar, Zachary Crawford, Michael M. Milks

Pharmacy and Wellness Review

Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN) are immunologic reactions that typically present due to drug hypersensitivity. These reactions present with serious mucocutaneous manifestations that can lead to significant morbidity and mortality. The pathogeneses of SJS and TEN have yet to be clearly elucidated, but three potential immunologic mechanisms have been defined in literature: granulysin, Fas-FasL, and perforin and granzyme B. Medications have been immunologically linked as the primary causative agents of SJS/TEN. Corticosteroids, intravenous immunoglobulin administration (IVIG) and cyclosporine have been employed as treatments; however, none have resulted in consistent positive outcomes. Pharmacists have a significant role ...


The Impact Of Pharmacogenomics On Chemotherapeutic Drug Development And Use, Lara Long, Amy Pasternak, Ellen Hazelet, David Kisor Oct 2019

The Impact Of Pharmacogenomics On Chemotherapeutic Drug Development And Use, Lara Long, Amy Pasternak, Ellen Hazelet, David Kisor

Pharmacy and Wellness Review

Cancer therapy is largely dependent on general treatment guidelines, and patients undergoing chemotherapy often experience treatment failure with standard drugs. The development of individualized drug therapy through pharmacogenomics has the potential to enhance chemotherapy regimen selection and improve patient outcomes. Antineoplastic agents such as cetuximab and trastuzumab are effective in treating cancers possessing specific genetic biomarker characteristics. Patients need to undergo genetic testing before these agents are administered to ensure appropriate use. Cetuximab has been shown to improve outcomes in metastatic colorectal cancers and head and neck squamous cell carcinomas positive for EGFR. Trastuzumab has shown benefit in human epidermal ...


Improving Maternal And Fetal Health: A Look At Thyroid Function During Pregnancy, Sarah Ginty, Jessica Beck, Taylor Gauthier, Amanda Meyer, Michelle R. Musser Oct 2019

Improving Maternal And Fetal Health: A Look At Thyroid Function During Pregnancy, Sarah Ginty, Jessica Beck, Taylor Gauthier, Amanda Meyer, Michelle R. Musser

Pharmacy and Wellness Review

Maintenance of thyroid function during pregnancy is critical for both maternal and fetal health and development; therefore, knowledge regarding the relationship between thyroid hormones and pregnancy is essential. The American Thyroid Association task force has developed clinical guidelines on the diagnosis and treatment of thyroid disease during pregnancy. Gestational thyroid diseases are divided into two classifications, hypothyroidism and hyperthyroidism, which are further divided into more specific classifications based on clinical presentation. Differentiation, diagnosis, and monitoring of thyroid diseases throughout pregnancy require assessing symptoms, as well as obtaining levels of thyroid-stimulating hormone (TSH) and free thyroxine (FT4) concentration by a simple ...


Dronedarone: An Update To A Controversial Therapy For Atrial Fibrillation, Zachary Crawford, Sara Mcallister, Amanda Hoersten, Jennifer Bauer, Megan Keller, David Bright Oct 2019

Dronedarone: An Update To A Controversial Therapy For Atrial Fibrillation, Zachary Crawford, Sara Mcallister, Amanda Hoersten, Jennifer Bauer, Megan Keller, David Bright

Pharmacy and Wellness Review

As of 2004, it was estimated that 2.2 million Americans were diagnosed with paroxysmal or persistent atrial fibrillation (AF) resulting in one out of every six strokes in the United States. AF leads to a reduction in pumping efficiency of the heart increasing the risk of several serious sequelae such as thromboembolic stroke and congestive heart failure (CHF). It also results in a reduced quality of life for the patients suffering from the disease. Patients with AF require appropriate antiarrhythmic therapy to control symptoms and prevent adverse effects of the condition. Multaq® (dronedarone), an antiarrhythmic drug approved for AF ...


Lysteda® For Heavy Menstrual Bleeding, Erica B. Schoenberger, Todd A. Tucker Jr., Justin W. Steele, Amanda Meyer, Sandra L. Hrometz Oct 2019

Lysteda® For Heavy Menstrual Bleeding, Erica B. Schoenberger, Todd A. Tucker Jr., Justin W. Steele, Amanda Meyer, Sandra L. Hrometz

Pharmacy and Wellness Review

Lysteda®, a novel formulation of tranexamic acid, is an antifibrinolytic medication recently approved by the Food and Drug Administration (FDA) for the treatment of heavy menstrual bleeding. Tranexamic acid has been shown to significantly reduce menstrual blood loss while simultaneously allowing a woman to safely become pregnant. The major advantage of Lysteda® (an oral modified-release formulation of tranexamic acid) compared to oral immediate-release tranexamic acid, is the decreased occurrence of gastrointestinal side effects. As there are no therapeutic equivalents to Lysteda® for heavy menstrual bleeding, it is important for pharmacists to be able to counsel patients appropriately on the specific ...


The Emerging Role Of Ticagrelor In Acute Coronary Syndromes, Jennifer Bauer, Brittany Dye, Kimberly Baucher, Megan Keller, David Bright, Karen L. Kier Oct 2019

The Emerging Role Of Ticagrelor In Acute Coronary Syndromes, Jennifer Bauer, Brittany Dye, Kimberly Baucher, Megan Keller, David Bright, Karen L. Kier

Pharmacy and Wellness Review

Antiplatelet therapy has become a mainstay in the treatment of acute coronary syndromes (ACS). Until recently, options were somewhat limited when it came to individualizing drug selection. Plavix® (clopidogrel) has been successfully used for many years but requires activation by CYP enzymes. Depending on an individual patient's genetic makeup, function of these CYP enzymes may be altered, which may increase the risk for clots. The recent approval of Effient® (prasugrel) and Brilinta® (ticagrelor) has provided physicians and pharmacists with more options and may hopefully lead to improved clinical outcomes. Ticagrelor specifically exhibits clinically different pharmacologic characteristics that require twice ...


Synthesizing Galactose Modified Polymeric Nanoparticles For Biofilm Inhibition Of Pseudomonas Aeruginosa, Tyler R. Flockton Sep 2019

Synthesizing Galactose Modified Polymeric Nanoparticles For Biofilm Inhibition Of Pseudomonas Aeruginosa, Tyler R. Flockton

Theses and Dissertations

Treating patients with antibiotics is becoming harder with the increase in antibiotic resistance. This is due to the widespread antibiotic use in clinical and agricultural settings. With antibiotic resistance outpacing new drugs making it to the market, developing new options to treat bacterial infections is and will be important. We created sugar modified nanoparticles to inhibit the biofilm formation of Pseudomonas aeruginosa.

P. aeruginosa is a gram-negative opportunistic pathogen that infects its host that has a compromised immune system. This makes it one of the most significant bacterial infection in hospitals. P. aeruginosa uses biofilms as an attack mechanism on ...


Sipuleucel-T (Provenge®): Therapeutic Use And Financial Implications, Courtney Porter, Joshua Ilenin, Lisa Berni, Ashley Overy, Karen L. Kier Sep 2019

Sipuleucel-T (Provenge®): Therapeutic Use And Financial Implications, Courtney Porter, Joshua Ilenin, Lisa Berni, Ashley Overy, Karen L. Kier

Pharmacy and Wellness Review

Although mortality rates have been declining, prostate cancer accounts for a large percentage of cancer diagnoses around the world. Sipuleucel-T (Provenge®), an autologous cellular immunotherapy targeted against the antigen expressed in most prostate cancers, has been shown to increase the median survival rate of castration-resistant prostate cancer. Even so, the therapeutic risks and benefits, as well as financial implications, all currently play a role in the governmental decision to reimburse for this new therapy.


The Pharmacogenetics Of Opioid Pain Management, Maryanne Ventura, Lauren Desko, Kimberly Gathers, Ashley Overy, David Kisor Sep 2019

The Pharmacogenetics Of Opioid Pain Management, Maryanne Ventura, Lauren Desko, Kimberly Gathers, Ashley Overy, David Kisor

Pharmacy and Wellness Review

High rates of interpatient variability in drug metabolism and drug response for nearly all medications lead to the hypothesis that assessment of an individual patient's genotype with respect to their ability metabolize certain drugs can be a useful tool in predicting a patient's responsiveness to certain medications. Evaluating patients using pharmacogenomics as a basis for assessment could allow pharmacists to decide which treatment options would be most efficacious in a given patient and, thereby, have significant impact in the clinical setting. This holds true especially in the case of prodrugs, which require in vivo activation to an active ...


Synthesis Of Betulinic Acid Via Baylis-Hillman Reaction, Sai Krishna Kommineni Aug 2019

Synthesis Of Betulinic Acid Via Baylis-Hillman Reaction, Sai Krishna Kommineni

Theses and Dissertations

Betulin is readily isolated from the bark of birch trees using simple extraction techniques and this molecule as well as its derivatives (eg. betulinic acid) exhibit impressive levels of biological activity. While it is naturally available and shows selective toxicity towards certain cancers, betulin suffers from a general lack of solubility in aqueous conditions. In this regard, we took up a project involving the synthesis of conjugates of betulin with improved solubility characteristics and we were able to identify a series of compounds that showed cytotoxicity against breast and pancreatic cancer cells.

This thesis describes our efforts on the development ...


Development Of Functionalized Imidazoles As Potential Therapeutical Agents, Drew Christopher Morgan Aug 2019

Development Of Functionalized Imidazoles As Potential Therapeutical Agents, Drew Christopher Morgan

Theses and Dissertations

Imidazoles are heterocyclic small molecules that play a major role in medicinal chemistry and drug discovery. There are several drugs in the market which contain imidazoles as the pharmacophore. Metronidazole, an imidazole containing compound, is a prominent antibiotic and antiprotozoal medication used for the treatment of a variety of infections such as amoebiasis, trichomoniasis, bacterial vaginosis, etc. The current work involves the synthesis of small molecule libraries of imidazoles derived from metronidazole using Baylis-Hillman (BH) reaction. BH reaction is a carbon-carbon bond forming reaction and involves the coupling of aldehydes or imines with activated alkenes such as acrylates, acrolein, or ...


Functionalized Heterocyclics As Potential Therapeutics, Anupama Indukuri Aug 2019

Functionalized Heterocyclics As Potential Therapeutics, Anupama Indukuri

Theses and Dissertations

Heterocyclic compounds play an important role in pharmaceutical drug development. Several natural products and biologically active compounds contain heterocyclic motifs in them. Multicomponent coupling reactions offer an excellent platform for the synthesis of diverse libraries of heterocyclic compounds. We have been working on the synthesis of novel heterocyclic small molecules utilizing reactions such as Baylis-Hillman reaction, Passerini reaction, Click reaction, reductive amination aldol condensation, etc.

In the current project, we prepared three series of heterocyclic compounds using Passerini and Baylis-Hillman reactions as key steps. Owing to the importance of heterocyclic chemistry in drug discovery and the ease of synthesis, the ...


Development Of An Imaging Analysis Algorithm For Fluorescence-Based High Content Screening In Parkinson’S Disease, Ryan Arlinghaus Aug 2019

Development Of An Imaging Analysis Algorithm For Fluorescence-Based High Content Screening In Parkinson’S Disease, Ryan Arlinghaus

The Journal of Purdue Undergraduate Research

No abstract provided.


A Pharmacological Model Of Trpa1-Mediated Nociception In Zebrafish For Therapeutic Discovery, Emre Coskun Aug 2019

A Pharmacological Model Of Trpa1-Mediated Nociception In Zebrafish For Therapeutic Discovery, Emre Coskun

The Journal of Purdue Undergraduate Research

No abstract provided.


Edb-Fn Targeted Peptide–Drug Conjugates For Use Against Prostate Cancer, Shang Eun Park, Kiumars Shamloo, Timothy A. Kristedja, Shaban Darwish, Marco Bisoffi, Keykavous Parang, Rakesh Tiwari Jul 2019

Edb-Fn Targeted Peptide–Drug Conjugates For Use Against Prostate Cancer, Shang Eun Park, Kiumars Shamloo, Timothy A. Kristedja, Shaban Darwish, Marco Bisoffi, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

Prostate cancer (PCa) is the most common malignancy in men and is the leading cause of cancer-related male mortality. A disulfide cyclic peptide ligand [CTVRTSADC] 1 has been previously found to target extra domain B of fibronectin (EDB-FN) in the extracellular matrix that can dierentiate aggressive PCa from benign prostatic hyperplasia. We synthesized and optimized the stability of ligand 1 by amide cyclization to obtain [KTVRTSADE] 8 using Fmoc/tBu solid-phase chemistry. Optimized targeting ligand 8 was found to be stable in phosphate buered saline (PBS, pH 6.5, 7.0, and 7.5) and under redox conditions, with a ...


Molecular Recognition Of M1-Linked Ubiquitin Chains By Native And Phosphorylated Uban Domains, Lina Herhaus, Henry Van Den Bedem, Sean Teng, Innokentiy Maslennikov, Soichi Wakatsuki, Ivan Dikic, Simin Rahighi Jun 2019

Molecular Recognition Of M1-Linked Ubiquitin Chains By Native And Phosphorylated Uban Domains, Lina Herhaus, Henry Van Den Bedem, Sean Teng, Innokentiy Maslennikov, Soichi Wakatsuki, Ivan Dikic, Simin Rahighi

Pharmacy Faculty Articles and Research

Although the Ub-binding domain in ABIN proteins and NEMO (UBAN) is highly conserved, UBAN-containing proteins exhibit different Ub-binding properties, resulting in their diverse biological roles. Post-translational modifications further control UBAN domain specificity for poly-Ub chains. However, precisely, how the UBAN domain structurally confers such functional diversity remains poorly understood. Here we report crystal structures of ABIN-1 alone and in complex with one or two M1-linked di-Ub chains. ABIN-1 UBAN forms a homo-dimer that provides two symmetrical Ub-binding sites on either side of the coiled-coil structure. Moreover, crystal structures of ABIN1 UBAN in complex with di-Ub chains reveal a concentration-dependency of ...


A Comprehensive Review Of Pegvaliase, An Enzyme Substitution Therapy For The Treatment Of Phenylketonuria, Tasmina Hydery, Valerie Azzopardi Coppenrath Jun 2019

A Comprehensive Review Of Pegvaliase, An Enzyme Substitution Therapy For The Treatment Of Phenylketonuria, Tasmina Hydery, Valerie Azzopardi Coppenrath

Open Access Articles

Objective: To review the pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of a phenylalanine-metabolizing enzyme indicated to reduce blood phenylalanine concentrations, pegvaliase injection.

Data Sources: Searches of MEDLINE (1946-September 1, 2018) were conducted using the terms pegvaliase and phenylalanine ammonia lyase (PAL). Additional data were obtained from the prescribing information, the product dossier obtained from the manufacturer, and Clinicaltrials.gov.

Study Selection and Data Extraction: All English language articles related to pharmacology, pharmacokinetics, efficacy, or safety of the combination therapy in human subjects were reviewed.

Data Synthesis: Pegvaliase is a pegylated PAL enzyme that converts phenylalanine to ammonia and ...


Modification And Characterization Of Chloro-Sugar Derivatives As Anti-Bacterial Agents, Mansi Jani Jun 2019

Modification And Characterization Of Chloro-Sugar Derivatives As Anti-Bacterial Agents, Mansi Jani

Theses and Dissertations

Sucralose is an artificial sugar substitute which is most commonly used sweetener among other artificial sweeteners. It is derived from sucrose through a complex chemical process that selectively substitutes three atoms of chlorine for three hydroxyl groups on sucrose molecule, which have shown some inhibition of bacterial growth in gut. The goal of the project was to substitute halide in sucralose in a way that it sustains potential anti-bacterial activity along with sweetening effect, which can be then incorporated into mouthwash formulation. Sucralose is very stable molecule and it also has other physico-chemical advantages which are suitable for our anticipated ...


Integration Of Native American Medicinal Plants Into The Heber W. Youngken Jr. Garden, Emily Lyn Murray May 2019

Integration Of Native American Medicinal Plants Into The Heber W. Youngken Jr. Garden, Emily Lyn Murray

Senior Honors Projects

Healthcare among Native American tribes was focused on all aspects of a patient’s life, such as physical, spiritual, and environmental elements. Healthy outcomes were obtained by maintaining a balance among all of these components. This “bio-psycho-socio-spiritual” approach to healthcare was thought to not only play a role in the health of a certain individual, but the health of the tribe as a whole. An illness was not only precipitated by a physical source, but by an imbalance of these components. Medicinal plants served as an integral role in direct physical healing, as well as an important element for the ...


Experimental Pharmacological Research Regarding Some New Quinazolin-4-Ones Derivatives, Cornel Chiriță, Emil Ștefănescu, Cristina E. Zbârcea, Simona Negreș, Mihaela Bratu, Diana C. Nuță, Carmen Limban, Ileana C. Chiriță, Cristina D. Marineci Apr 2019

Experimental Pharmacological Research Regarding Some New Quinazolin-4-Ones Derivatives, Cornel Chiriță, Emil Ștefănescu, Cristina E. Zbârcea, Simona Negreș, Mihaela Bratu, Diana C. Nuță, Carmen Limban, Ileana C. Chiriță, Cristina D. Marineci

Journal of Mind and Medical Sciences

A series of new compounds with quinazolin-4-one structure, synthesized by the Pharmaceutical Chemistry Department of the Faculty of Pharmacy of the University of Medicine and Pharmacy “Carol Davila” Bucharest, was studied. Five of them were selected, conventionally named S1, S2, S3, S4, S5, and investigated in terms of their potential influence on the central nervous system (CNS). For this purpose, the antidepressant effect was determined using the forced swimming test; the anxiolytic/ anxiogenic effect was determined using the suspended plus-shaped maze (Ugo Basile); the effect on the motor activity was determined using the Ugo Basile activity cage; and the potential ...


Sensory Primary Cilium Is A Responsive Camp Microdomain In Renal Epithelia, Rinzhin T. Sherpa, Ashraf M. Mohieldin, Rajasekharreddy Pala, Dagmar Wachten, Rennolds S. Ostrom, Surya M. Nauli Apr 2019

Sensory Primary Cilium Is A Responsive Camp Microdomain In Renal Epithelia, Rinzhin T. Sherpa, Ashraf M. Mohieldin, Rajasekharreddy Pala, Dagmar Wachten, Rennolds S. Ostrom, Surya M. Nauli

Pharmacy Faculty Articles and Research

Primary cilia are hair-like cellular extensions that sense microenvironmental signals surrounding cells. The role of adenylyl cyclases in ciliary function has been of interest because the product of adenylyl cyclase activity, cAMP, is relevant to cilia-related diseases. In the present study, we show that vasopressin receptor type-2 (V2R) is localized to cilia in kidney epithelial cells. Pharmacologic inhibition of V2R with tolvaptan increases ciliary length and mechanosensory function. Genetic knockdown of V2R, however, does not have any effect on ciliary length, although the effect of tolvaptan on ciliary length is dampened. Our study reveals that tolvaptan may have a cilia-specific ...


Amphiphilic Peptides For Efficient Sirna Delivery, Saghar Mozaffari, Emira Bousoik, Farideh Amirrad, Robert Lamboy, Melissa Coyle, Ryley Hall, Abdulaziz Alasmari, Parvin Mahdipoor, Keykavous Parang, Hamidreza Montazeri Aliabadi Apr 2019

Amphiphilic Peptides For Efficient Sirna Delivery, Saghar Mozaffari, Emira Bousoik, Farideh Amirrad, Robert Lamboy, Melissa Coyle, Ryley Hall, Abdulaziz Alasmari, Parvin Mahdipoor, Keykavous Parang, Hamidreza Montazeri Aliabadi

Pharmacy Faculty Articles and Research

A number of amphiphilic cyclic peptides—[FR]4, [WR]5, and [WK]5—containing hydrophobic and positively-charged amino acids were synthesized by Fmoc/tBu solid-phase peptide methods and evaluated for their efficiency in intracellular delivery of siRNA to triple-negative breast cancer cell lines, MDA-MB-231 and MDA-MB-468, in the presence and absence of 1,2-dioleoyl-sn-glycero-3-phosphoethanolamine (DOPE). Among the peptides, [WR]5, which contains alternate tryptophan (W) and arginine (R) residues, was found to be the most efficient in the delivery of siRNA by improving the delivery by more than 3-fold when compared to other synthesized cyclic peptides that were not efficient ...


Iron-Containing Nanoparticles For The Treatment Of Chrionic Biofilm Infections In Cystic Fibrosis, Leisha M. A. Martin Apr 2019

Iron-Containing Nanoparticles For The Treatment Of Chrionic Biofilm Infections In Cystic Fibrosis, Leisha M. A. Martin

Nanoscience and Microsystems ETDs

Cystic fibrosis (CF) is the most common genetic disease resulting in the morbidity and mortality of Caucasian children and adults worldwide. Due to a genetic mutation resulting in malfunction of the Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) protein, CF patients produce highly viscous mucus in their respiratory tract. This leads to impairment of the mucociliary clearance of inhaled microbes. In addition to reduced microbial clearance, anoxic environmental conditions in the lungs promote biofilm-mode growth of the pathogenic bacterial species Pseudomonas aeruginosa. Chronic infections of P. aeruginosa begin in early childhood and typically persist until respiratory failure and death result. The ...


Synthesis And Antiproliferative Activities Of Conjugates Of Paclitaxel And Camptothecin With A Cyclic Cell-Penetrating Peptide, Naglaa Salem El-Sayed, Amir Nasrolahi Shirazi, Muhammad Imran Sajid, Shang Eun Park, Keykavous Parang, Rakesh Tiwari Apr 2019

Synthesis And Antiproliferative Activities Of Conjugates Of Paclitaxel And Camptothecin With A Cyclic Cell-Penetrating Peptide, Naglaa Salem El-Sayed, Amir Nasrolahi Shirazi, Muhammad Imran Sajid, Shang Eun Park, Keykavous Parang, Rakesh Tiwari

Pharmacy Faculty Articles and Research

Cell-penetrating peptide [WR]5 has been previously shown to be an efficient molecular transporter for various hydrophilic and hydrophobic molecules. The peptide was synthesized using Fmoc/tBu solid-phase chemistry, and one arginine was replaced with one lysine to enable the conjugation with the anticancer drugs. Paclitaxel (PTX) was functionalized with an esterification reaction at the C20 hydroxyl group of PTX with glutaric anhydride and conjugated with the cyclic peptide [W(WR)4K(bAla)] in DMF to obtain the peptide-drug conjugate PTX1. Furthermore, camptothecin (CPT) was modified at the C(20)-hydroxyl group through the reaction with triphosgene. Then, it was ...


Meta-Analysis To Identify And Evaluate Factors Associated With Regulatory Approval Of Orphan Drugs (Od) To Develop An Algorithm For Predicting Regulatory Approval (Success) And To Develop A Standardized Tool To Improve Orphan Drug Portfolio Decision-Making, Milky C. Florent Mar 2019

Meta-Analysis To Identify And Evaluate Factors Associated With Regulatory Approval Of Orphan Drugs (Od) To Develop An Algorithm For Predicting Regulatory Approval (Success) And To Develop A Standardized Tool To Improve Orphan Drug Portfolio Decision-Making, Milky C. Florent

Seton Hall University Dissertations and Theses (ETDs)

Background and Purpose of the Study: Developed an algorithm (AODI) for predicting probability of regulatory success (PRS) for new orphan drugs after phase II testing has been conductedwith the objective of providing a tool to improve drug portfolio decision-making.Methods: Examined 132 studies from recent publications (2005 onwards). Data on safety, efficacy, operational, market, and company characteristics were obtained from public sources. Meta-analysis and meta-regressions were used to provide an unbiased approach to assess overall predictability and to identify the most important individual predictors.Results: Found that a simple three-factor model (disease prevalence, clinical trial duration and clinical trial participation ...