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Identifying the core concepts of pharmacology education.

Paul J White, Elizabeth A Davis, Marina Santiago, Tom Angelo, Alison Shield, Anna-Marie Babey, Barbara Kemp-Harper, Gregg Maynard, Hesham S Al-Sallami, Ian F Musgrave, Lynette B Fernandes, Suong N T Ngo, Tina Hinton,

Pharmacology education currently lacks an agreed knowledge curriculum. Evidence from physics and biology education indicates that core concepts are useful and effective structures around which such a curriculum can be designed to facilitate student learning. Building on previous work, we developed a novel, criterion-based method to identify the core concepts ... Read more >>

Pharmacol Res Perspect (Pharmacology research & perspectives)
[2021, 9(4):e00836]

Cited: 0 times

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Pharmacological Insights Into Safety and Efficacy Determinants for the Development of Adenosine Receptor Biased Agonists in the Treatment of Heart Failure.

Patricia Rueda, Jon Merlin, Stefano Chimenti, Michel Feletou, Jerome Paysant, Paul J White, Arthur Christopoulos, Patrick M Sexton, Roger J Summers, William N Charman, Lauren T May, Christopher J Langmead,

Adenosine A<sub>1</sub> receptors (A<sub>1</sub>R) are a potential target for cardiac injury treatment due to their cardioprotective/antihypertrophic actions, but drug development has been hampered by on-target side effects such as bradycardia and altered renal hemodynamics. Biased agonism has emerged as an attractive mechanism for A<sub>1</sub>R-mediated cardioprotection that is haemodynamically safe. Here ... Read more >>

Front Pharmacol (Frontiers in pharmacology)
[2021, 12:628060]

Cited: 0 times

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Biased agonism at adenosine receptors.

Samantha M McNeill, Jo-Anne Baltos, Paul J White, Lauren T May,

Adenosine modulates many aspects of human physiology and pathophysiology through binding to the adenosine family of G protein-coupled receptors, which are comprised of four subtypes, the A<sub>1</sub>R, A<sub>2A</sub>R, A<sub>2B</sub>R and A<sub>3</sub>R. Modulation of adenosine receptor function by exogenous agonists, antagonists and allosteric modulators can be beneficial for a number of ... Read more >>

Cell Signal (Cellular signalling)
[2021, 82:109954]

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Predictors of Pharmacy Student Performance on Written and Clinical Examinations in a Flipped Classroom Curriculum.

Kayley M Lyons, Tina P Brock, Daniel T Malone, Lubna Freihat, Paul J White,

<b>Objective.</b> To examine the effects of student demographics, prior academic performance, course engagement, and time management on pharmacy students' performance on course examinations and objective structured clinical examinations (OSCEs).<b>Methods.</b> Study participants were one cohort of pharmacy students enrolled in a five-year combined Bachelor and Master of Pharmacy degree program at ... Read more >>

Am J Pharm Educ (American journal of pharmaceutical education)
[2020, 84(12):8038]

Cited: 0 times

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The adenosine A2B G protein-coupled receptor: Recent advances and therapeutic implications.

Elizabeth A Vecchio, Paul J White, Lauren T May,

The adenosine A2B receptor (A2BAR) is one of four adenosine receptor subtypes belonging to the Class A family of G protein-coupled receptors (GPCRs). Until recently, the A2BAR remained poorly characterised, in part due to its relatively low affinity for the endogenous agonist adenosine and therefore presumed minor physiological significance. However, ... Read more >>

Pharmacol Ther (Pharmacology & therapeutics)
[2019, 198:20-33]

Cited: 9 times

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Development of a self-report instrument for measuring in-class student engagement reveals that pretending to engage is a significant unrecognized problem.

Kathryn A Fuller, Nilushi S Karunaratne, Som Naidu, Betty Exintaris, Jennifer L Short, Michael D Wolcott, Scott Singleton, Paul J White,

Student engagement during classes includes behavioural, cognitive and emotional components, and is a pre-requisite for successful active learning environments. A novel approach to measuring student engagement was developed, involving triangulation of real-time student-self report, observation by trained observers and heart rate measurement. The self-report instrument was evaluated in four separate ... Read more >>

PLoS One (PloS one)
[2018, 13(10):e0205828]

Cited: 0 times

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Effect of the 5-HT4 receptor agonist tegaserod on the expression of GRK2 and GRK6 in the rat gastrointestinal tract.

Teshome Nedi, Paul J White, Ian M Coupar, Helen R Irving,

<h4>Objective</h4>Tegaserod is a 5-hydroxytryptamine type 4 (5-HT<sub>4</sub>) receptor agonist, formerly used in treating constipation predominant irritable bowel syndrome, which desensitizes 5-HT<sub>4</sub> receptors in rat oesophagus and colon in vitro. Desensitization of 5-HT<sub>4</sub> receptors is regulated by G-protein coupled receptor kinases. This study was designed to assess the effect of 5-HT<sub>4</sub> ... Read more >>

BMC Res Notes (BMC research notes)
[2018, 11(1):362]

Cited: 1 time

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New paradigms in adenosine receptor pharmacology: allostery, oligomerization and biased agonism.

Elizabeth A Vecchio, Jo-Anne Baltos, Anh T N Nguyen, Arthur Christopoulos, Paul J White, Lauren T May,

Adenosine receptors are a family of GPCRs containing four subtypes (A<sub>1</sub> , A<sub>2A</sub> , A<sub>2B</sub> and A<sub>3</sub> receptors), all of which bind the ubiquitous nucleoside adenosine. These receptors play an important role in physiology and pathophysiology and therefore represent attractive drug targets for a range of conditions. The theoretical framework ... Read more >>

Br J Pharmacol (British journal of pharmacology)
[2018, 175(21):4036-4046]

Cited: 12 times

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A Structure-Activity Relationship Study of Bitopic N6-Substituted Adenosine Derivatives as Biased Adenosine A1 Receptor Agonists.

Luigi Aurelio, Jo-Anne Baltos, Leigh Ford, Anh T N Nguyen, Manuela Jörg, Shane M Devine, Celine Valant, Paul J White, Arthur Christopoulos, Lauren T May, Peter J Scammells,

The adenosine A<sub>1</sub> receptor (A<sub>1</sub>AR) is a potential novel therapeutic target for myocardial ischemia-reperfusion injury. However, to date, clinical translation of prototypical A<sub>1</sub>AR agonists has been hindered due to dose limiting adverse effects. Recently, we demonstrated that the biased bitopic agonist 1, consisting of an adenosine pharmacophore linked to an ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2018, 61(5):2087-2103]

Cited: 3 times

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α1A-Adrenoceptors activate mTOR signalling and glucose uptake in cardiomyocytes.

Masaaki Sato, Bronwyn A Evans, Anna L Sandström, Ling Yeong Chia, Saori Mukaida, Bui San Thai, Anh Nguyen, Linzi Lim, Christina Y R Tan, Jo-Anne Baltos, Paul J White, Lauren T May, Dana S Hutchinson, Roger J Summers, Tore Bengtsson,

The capacity of G protein-coupled receptors to modulate mechanistic target of rapamycin (mTOR) activity is a newly emerging paradigm with the potential to link cell surface receptors with cell survival. Cardiomyocyte viability is linked to signalling pathways involving Akt and mTOR, as well as increased glucose uptake and utilization. Our ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2018, 148:27-40]

Cited: 10 times

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Student Engagement with a Flipped Classroom Teaching Design Affects Pharmacology Examination Performance in a Manner Dependent on Question Type.

Paul J White, Som Naidu, Elizabeth Yuriev, Jennifer L Short, Jacqueline E McLaughlin, Ian C Larson,

Objective: To investigate the relationship between student engagement with the key elements of a flipped classroom approach (preparation and attendance), their attitudes to learning, including strategy development, and their performance on two types of examination questions (knowledge recall and providing rational predictions when faced with novel scenarios). Methods. This study ... Read more >>

Am J Pharm Educ (American journal of pharmaceutical education)
[2017, 81(9):5931]

Cited: 2 times

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A suicidal strain of Listeria monocytogenes is effective as a DNA vaccine delivery system for oral administration.

Shubhra Sinha, Cheng-Yi Kuo, Joan K Ho, Paul J White, Jalal A Jazayeri, Colin W Pouton,

In this study we determined the in vivo activity of model ovalbumin vaccines delivered by direct intramuscular delivery of plasmid DNA or oral delivery using a recombinant suicidal Listeria monocytogenes strain (rsΔ2). In a previous report we described how rsΔ2 is capable of delivering luciferase, as protein or DNA, in ... Read more >>

Vaccine (Vaccine)
[2017, 35(38):5115-5122]

Cited: 4 times

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Virtual reality body motion induced navigational controllers and their effects on simulator sickness and pathfinding.

Cassandra N Aldaba, Paul J White, Ahmad Byagowi, Zahra Moussavi,

Virtual reality (VR) navigation is usually constrained by plausible simulator sickness (SS) and intuitive user interaction. The paper reports on the use of four different degrees of body motion induced navigational VR controllers, a TiltChair, omni-directional treadmill, a manual wheelchair joystick (VRNChair), and a joystick in relation to a participant's ... Read more >>

Annu Int Conf IEEE Eng Med Biol Soc (Annual International Conference of the IEEE Engineering in Medicine and Biology Society. IEEE Engineering in Medicine and Biology Society. Annual International Conference)
[2017, 2017:4175-4178]

Cited: 3 times

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Targeting Adenosine Receptors for the Treatment of Cardiac Fibrosis.

Elizabeth A Vecchio, Paul J White, Lauren T May,

Adenosine is a ubiquitous molecule with key regulatory and cytoprotective mechanisms at times of metabolic imbalance in the body. Among a plethora of physiological actions, adenosine has an important role in attenuating ischaemia-reperfusion injury and modulating the ensuing fibrosis and tissue remodeling following myocardial damage. Adenosine exerts these actions through ... Read more >>

Front Pharmacol (Frontiers in pharmacology)
[2017, 8:243]

Cited: 15 times

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Capadenoson, a clinically trialed partial adenosine A1 receptor agonist, can stimulate adenosine A2B receptor biased agonism.

Jo-Anne Baltos, Elizabeth A Vecchio, Matthew A Harris, Cheng Xue Qin, Rebecca H Ritchie, Arthur Christopoulos, Paul J White, Lauren T May,

The adenosine A<sub>2B</sub> receptor (A<sub>2B</sub>AR) has been identified as an important therapeutic target in cardiovascular disease, however in vitro and in vivo targeting has been limited by the paucity of pharmacological tools, particularly potent agonists. Interestingly, 2-((6-amino-3,5-dicyano-4-(4-(cyclopropylmethoxy)phenyl)-2-pyridinyl)thio)acetamide (BAY60-6583), a potent and subtype-selective A<sub>2B</sub>AR agonist, has the same core structure as ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2017, 135:79-89]

Cited: 11 times

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Novel Irreversible Agonists Acting at the A1 Adenosine Receptor.

Manuela Jörg, Alisa Glukhova, Alaa Abdul-Ridha, Elizabeth A Vecchio, Anh T N Nguyen, Patrick M Sexton, Paul J White, Lauren T May, Arthur Christopoulos, Peter J Scammells,

The A<sub>1</sub> adenosine receptor (A<sub>1</sub>AR) is an important G protein-coupled receptor that regulates a range of physiological functions. Herein we report the discovery of novel irreversible agonists acting at the A<sub>1</sub>AR, which have the potential to serve as useful research tools for studying receptor structure and function. A series of ... Read more >>

J Med Chem (Journal of medicinal chemistry)
[2016, 59(24):11182-11194]

Cited: 6 times

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Developing a Framework for Objective Structured Clinical Examinations Using the Nominal Group Technique.

Safeera Y Hussainy, Matthew F Crum, Paul J White, Ian Larson, Daniel T Malone, David T Manallack, Joseph A Nicolazzo, Jennifer McDowell, Angelina S Lim, Carl M Kirkpatrick,

<b>Objective.</b> To use the nominal group technique to develop a framework to improve existing and develop new objective structured clinical examinations (OSCEs) within a four-year bachelor of pharmacy course. <b>Design.</b> Using the nominal group technique, a unique method of group interview that combines qualitative and quantitative data collection, focus groups ... Read more >>

Am J Pharm Educ (American journal of pharmaceutical education)
[2016, 80(9):158]

Cited: 2 times

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Role of the Second Extracellular Loop of the Adenosine A1 Receptor on Allosteric Modulator Binding, Signaling, and Cooperativity.

Anh T N Nguyen, Elizabeth A Vecchio, Trayder Thomas, Toan D Nguyen, Luigi Aurelio, Peter J Scammells, Paul J White, Patrick M Sexton, Karen J Gregory, Lauren T May, Arthur Christopoulos,

Allosteric modulation of adenosine A1 receptors (A1ARs) offers a novel therapeutic approach for the treatment of numerous central and peripheral disorders; however, despite decades of research, there is a relative paucity of structural information regarding the A1AR allosteric site and mechanisms governing cooperativity with orthosteric ligands. We combined alanine-scanning mutagenesis ... Read more >>

Mol Pharmacol (Molecular pharmacology)
[2016, 90(6):715-725]

Cited: 14 times

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Neurocognitive Treatment for a Patient with Alzheimer's Disease Using a Virtual Reality Navigational Environment.

Paul J F White, Zahra Moussavi,

In this case study, a man at the onset of Alzheimer's disease (AD) was enrolled in a cognitive treatment program based upon spatial navigation in a virtual reality (VR) environment. We trained him to navigate to targets in a symmetric, landmark-less virtual building. Our research goals were to determine whether ... Read more >>

J Exp Neurosci (Journal of experimental neuroscience)
[2016, 10:129-135]

Cited: 13 times

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Extracellular Loop 2 of the Adenosine A1 Receptor Has a Key Role in Orthosteric Ligand Affinity and Agonist Efficacy.

Anh T N Nguyen, Jo-Anne Baltos, Trayder Thomas, Toan D Nguyen, Laura López Muñoz, Karen J Gregory, Paul J White, Patrick M Sexton, Arthur Christopoulos, Lauren T May,

The adenosine A<sub>1</sub> G protein-coupled receptor (A<sub>1</sub>AR) is an important therapeutic target implicated in a wide range of cardiovascular and neuronal disorders. Although it is well established that the A<sub>1</sub>AR orthosteric site is located within the receptor's transmembrane (TM) bundle, prior studies have implicated extracellular loop 2 (ECL2) as having ... Read more >>

Mol Pharmacol (Molecular pharmacology)
[2016, 90(6):703-714]

Cited: 23 times

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The hybrid molecule, VCP746, is a potent adenosine A2B receptor agonist that stimulates anti-fibrotic signalling.

Elizabeth A Vecchio, Chung Hui Chuo, Jo-Anne Baltos, Leigh Ford, Peter J Scammells, Bing H Wang, Arthur Christopoulos, Paul J White, Lauren T May,

We have recently described the rationally-designed adenosine receptor agonist, 4-(5-amino-4-benzoyl-3-(3-(trifluoromethyl)phenyl)thiophen-2-yl)-N-(6-(9-((2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxylmethyl)tetrahydro-furan-2-yl)-9H-purin-6-ylamino)hexyl)benzamide (VCP746), a hybrid molecule consisting of an adenosine moiety linked to an adenosine A1 receptor (A1AR) allosteric modulator moiety. At the A1AR, VCP746 mediated cardioprotection in the absence of haemodynamic side effects such as bradycardia. The current study has now ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2016, 117:46-56]

Cited: 11 times

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VCP746, a novel A1 adenosine receptor biased agonist, reduces hypertrophy in a rat neonatal cardiac myocyte model.

Chung H Chuo, Shane M Devine, Peter J Scammells, Henry Krum, Arthur Christopoulos, Lauren T May, Paul J White, Bing H Wang,

VCP746 is a novel A1 adenosine receptor (A1 AR) biased agonist previously shown to be cytoprotective with no effect on heart rate. The aim of this study was to investigate the potential anti-hypertrophic effect of VCP746 in neonatal rat cardiac myocytes (NCM). NCM hypertrophy was stimulated with interleukin (IL)-1β (10 ng/mL), ... Read more >>

Clin Exp Pharmacol Physiol (Clinical and experimental pharmacology & physiology)
[2016, 43(10):976-982]

Cited: 11 times

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Quantification of adenosine A(1) receptor biased agonism: Implications for drug discovery.

Jo-Anne Baltos, Karen J Gregory, Paul J White, Patrick M Sexton, Arthur Christopoulos, Lauren T May,

Adenosine A1 receptor (A1AR) stimulation is a powerful protective mechanism in cerebral and cardiac ischemia-reperfusion injury. Despite this, therapeutic targeting of the A1AR for the treatment of ischemia-reperfusion injury has been largely unsuccessful, as high concentrations of prototypical A1AR agonists impart significant hemodynamic effects, particularly pronounced bradycardia, atrioventricular block and ... Read more >>

Biochem Pharmacol (Biochemical pharmacology)
[2016, 99:101-112]

Cited: 23 times

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Ligand-Independent Adenosine A2B Receptor Constitutive Activity as a Promoter of Prostate Cancer Cell Proliferation.

Elizabeth A Vecchio, Christina Y R Tan, Karen J Gregory, Arthur Christopoulos, Paul J White, Lauren T May,

Aberrant ligand-independent G protein-coupled receptor constitutive activity has been implicated in the pathophysiology of a number of cancers. The adenosine A2B receptor (A2BAR) is dynamically upregulated under pathologic conditions associated with a hypoxic microenvironment, including solid tumors. This, in turn, may amplify ligand-independent A2BAR signal transduction. The contribution of A2BAR ... Read more >>

J Pharmacol Exp Ther (The Journal of pharmacology and experimental therapeutics)
[2016, 357(1):36-44]

Cited: 25 times

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Effect of viewing mode on pathfinding in immersive Virtual Reality.

Paul J White, Ahmad Byagowi, Zahra Moussavi,

The use of Head Mounted Displays (HMDs) to view Virtual Reality Environments (VREs) has received much attention recently. This paper reports on the difference between actual humans' navigation in a VRE viewed through an HMD compared to that in the same VRE viewed on a laptop PC display. A novel ... Read more >>

Annu Int Conf IEEE Eng Med Biol Soc (Annual International Conference of the IEEE Engineering in Medicine and Biology Society. IEEE Engineering in Medicine and Biology Society. Annual International Conference)
[2015, 2015:4619-4622]

Cited: 3 times

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