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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]

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Do gabapentin or pregabalin directly modulate the µ receptor?

Preeti Manandhar, Bridin Patricia Murnion, Natasha L Grimsey, Mark Connor, Marina Santiago,

<h4>Background</h4>Pregabalin and gabapentin improve neuropathic pain symptoms but there are emerging concerns regarding their misuse. This is more pronounced among patients with substance use disorder, particularly involving opioids. Co-ingestion of gabapentinoids with opioids is increasingly identified in opioid related deaths, however, the molecular mechanism behind this is still unclear. We ... Read more >>

PeerJ (PeerJ)
[2021, 9:e11175]

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Lifetime-Engineered Ruby Nanoparticles (Tau-Rubies) for Multiplexed Imaging of μ-Opioid Receptors.

Xiaohong Yang, Alireza Maleki, Nikolay A Lipey, Xianlin Zheng, Marina Santiago, Mark Connor, Varun K A Sreenivasan, Judith M Dawes, Yiqing Lu, Andrei V Zvyagin,

To address the growing demand for simultaneous imaging of multiple biomarkers in highly scattering media such as organotypic cell cultures, we introduce a new type of photoluminescent nanomaterial termed "tau-ruby" composed of ruby nanocrystals (Al<sub>2</sub>O<sub>3</sub>:Cr<sup>3+</sup>) with tunable emission lifetime. The lifetime tuning range from 2.4 to 3.2 ms was achieved ... Read more >>

ACS Sens (ACS sensors)
[2021, 6(3):1375-1383]

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16S rRNA sequencing of samples from universal stool bank donors.

Marina Santiago, Scott W Olesen,

<h4>Objectives</h4>Universal stool banks provide stool to physicians for use in treating recurrent Clostridioides difficile infection via fecal microbiota transplantation. Stool donors providing the material are rigorously screened for diseases and disorders with a potential microbiome etiology, and they are likely healthier than the controls in most microbiome datasets. 16S rRNA ... Read more >>

BMC Res Notes (BMC research notes)
[2021, 14(1):108]

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Modulation of human T-type calcium channels by synthetic cannabinoid receptor agonists in vitro.

Chris Bladen, Somayeh Mirlohi, Marina Santiago, Mitchell Longworth, Michael Kassiou, Sam Banister, Mark Connor,

<h4>Background and purpose</h4>Consumption of Synthetic Cannabinoid Receptor agonists (SCRAs) is associated with severe adverse reactions including seizures, arrhythmias and death, but the molecular mechanisms surrounding SCRA toxicity are not yet established. These disease-like symptoms are also synonymous with altered T-type calcium channel activity which controls rhythmicity in the heart and ... Read more >>

Neuropharmacology (Neuropharmacology)
[2021, 187:108478]

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Modulation of Recombinant Human T-Type Calcium Channels by Δ9-Tetrahydrocannabinolic Acid In Vitro.

Somayeh Mirlohi, Chris Bladen, Marina Santiago, Mark Connor,

<b>Introduction:</b> Low voltage-activated T-type calcium channels (T-type <i>I</i><sub>Ca</sub>), Ca<sub>V</sub>3.1, Ca<sub>V</sub>3.2, and Ca<sub>V</sub>3.3, are opened by small depolarizations from the resting membrane potential in many cells and have been associated with neurological disorders, including absence epilepsy and pain. Δ<sup>9</sup>-tetrahydrocannabinol (THC) is the principal psychoactive compound in <i>Cannabis</i> and also directly modulates ... Read more >>

Cannabis Cannabinoid Res (Cannabis and cannabinoid research)
[2021, :]

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Evaluating Opioid-Mediated Adenylyl Cyclase Inhibition in Live Cells Using a BRET-Based Assay.

Preeti Manandhar, Shivani Sachdev, Marina Santiago,

Quantitative measurement of receptor signaling by different ligands is important for understanding the mechanism of drug action and screening of drugs. Here, we describe a simple and cost-effective method of measuring adenylyl cyclase inhibition, one of the hallmarks of opioid receptor activation. The assay is based on bioluminescence resonance energy ... Read more >>

Methods Mol Biol (Methods in molecular biology (Clifton, N.J.))
[2021, 2201:117-125]

Cited: 1 time

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Terpenoids Commonly Found in Cannabis sativa Do Not Modulate the Actions of Phytocannabinoids or Endocannabinoids on TRPA1 and TRPV1 Channels.

Marika Heblinski, Marina Santiago, Charlotte Fletcher, Jordyn Stuart, Mark Connor, Iain S McGregor, Jonathon C Arnold,

<b>Introduction:</b> <i>Cannabis sativa</i> produces hundreds of bioactive compounds, including cannabinoids and terpenoids. It has been proposed that cannabinoids act in synergy with terpenoids to produce the entourage effect, a concept used to explain the therapeutic benefits of medicinal cannabis. One molecular explanation for the entourage effect is that the terpenoids ... Read more >>

Cannabis Cannabinoid Res (Cannabis and cannabinoid research)
[2020, 5(4):305-317]

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Distinct Fecal and Plasma Metabolites in Children with Autism Spectrum Disorders and Their Modulation after Microbiota Transfer Therapy.

Dae-Wook Kang, James B Adams, Troy Vargason, Marina Santiago, Juergen Hahn, Rosa Krajmalnik-Brown,

Accumulating evidence has strengthened a link between dysbiotic gut microbiota and autism. Fecal microbiota transplant (FMT) is a promising therapy to repair dysbiotic gut microbiota. We previously performed intensive FMT called microbiota transfer therapy (MTT) for children with autism spectrum disorders (ASD) and observed a substantial improvement of gastrointestinal and ... Read more >>

mSphere (mSphere)
[2020, 5(5):]

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Exploring Stereochemical and Conformational Requirements at Cannabinoid Receptors for Synthetic Cannabinoids Related to SDB-006, 5F-SDB-006, CUMYL-PICA, and 5F-CUMYL-PICA.

Adam Ametovski, Christa Macdonald, Jamie J Manning, S A Syed Haneef, Marina Santiago, Lewis Martin, Eric Sparkes, Andrew Reckers, Roy R Gerona, Mark Connor, Michelle Glass, Samuel D Banister,

Synthetic cannabinoid receptor agonists (SCRAs) represent the most rapidly expanding class of new psychoactive substances (NPSs). Despite the prevalence and potency of recent chiral indole-3-carboxamide SCRAs, few pharmacological data are available regarding the enantiomeric bias of these NPSs toward human CB1 and CB2 receptors. A series of homochiral indole-3-carboxamides derived ... Read more >>

ACS Chem Neurosci (ACS chemical neuroscience)
[2020, 11(21):3672-3682]

Cited: 2 times

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Modulation of Recombinant Human T-type calcium Channels by Δ9-tetrahydrocannabinolic acid in vitro

Somayeh Mirlohi, Chris Bladen, Marina Santiago, Mark Connor,

<h4>Introduction</h4> Low voltage-activated T-type calcium channels (T-type I Ca ), Ca V 3.1, Ca V 3.2, and Ca V 3.3 are opened by small depolarizations from the resting membrane potential in many cells and have been associated with neurological disorders including absence epilepsy and pain. Δ 9 -tetrahydrocannabinol (THC) is ... Read more >>

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Structure and reconstitution of a hydrolase complex that may release peptidoglycan from the membrane after polymerization.

Kaitlin Schaefer, Tristan W Owens, Julia E Page, Marina Santiago, Daniel Kahne, Suzanne Walker,

Bacteria are encapsulated by a peptidoglycan cell wall that is essential for their survival<sup>1</sup>. During cell wall assembly, a lipid-linked disaccharide-peptide precursor called lipid II is polymerized and cross-linked to produce mature peptidoglycan. As lipid II is polymerized, nascent polymers remain membrane-anchored at one end, and the other end becomes ... Read more >>

Nat Microbiol (Nature microbiology)
[2021, 6(1):34-43]

Cited: 1 time

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Modulation of Human T-type Calcium Channels by Synthetic Cannabinoid Receptor Agonists in vitro

Chris Bladen, Somayeh Mirlohi, Marina Santiago, Mitchell Longworth, Michael Kassiou, Sam Banister, Mark Connor,

<h4>BACKGROUND AND PURPOSE</h4> Consumption of Synthetic Cannabinoid Receptor agonists (SCRAs) is associated with severe adverse reactions including seizures, arrhythmias and death, but the molecular mechanisms surrounding SCRA toxicity are not yet established. These disease-like symptoms are also synonymous with altered T-type calcium channel activity which controls rhythmicity in the heart ... Read more >>

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Structure and reconstitution of a hydrolase complex that releases peptidoglycan from the membrane after polymerization

Kaitlin Schaefer, Tristan Owens, Julia Page, Marina Santiago, Daniel Kahne, Suzanne Walker,

Bacteria are surrounded by a peptidoglycan cell wall that is essential for their survival 1 . During cell wall assembly, a lipid-linked disaccharide-peptide precursor called Lipid II is polymerized and crosslinked to produce mature peptidoglycan. As Lipid II is polymerized, nascent polymers remain membrane-anchored at one end and the other ... Read more >>

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Differential activation of G protein-mediated signaling by synthetic cannabinoid receptor agonists.

Shivani Sachdev, Samuel D Banister, Marina Santiago, Chris Bladen, Michael Kassiou, Mark Connor,

Synthetic cannabinoid receptor agonists (SCRAs) are new psychoactive substances associated with acute intoxication and even death. However, the molecular mechanisms through which SCRAs may exert their toxic effects remain unclear-including the potential differential activation of G protein subtypes by cannabinoid receptor type 1 (CB1), a major target of SCRA. We ... Read more >>

Pharmacol Res Perspect (Pharmacology research & perspectives)
[2020, 8(2):e00566]

Cited: 2 times

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Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of new opioid agonists.

Alexander Gillis, Arisbel B Gondin, Andrea Kliewer, Julie Sanchez, Herman D Lim, Claudia Alamein, Preeti Manandhar, Marina Santiago, Sebastian Fritzwanker, Frank Schmiedel, Timothy A Katte, Tristan Reekie, Natasha L Grimsey, Michael Kassiou, Barrie Kellam, Cornelius Krasel, Michelle L Halls, Mark Connor, J Robert Lane, Stefan Schulz, Macdonald J Christie, Meritxell Canals,

Biased agonism at G protein-coupled receptors describes the phenomenon whereby some drugs can activate some downstream signaling activities to the relative exclusion of others. Descriptions of biased agonism focusing on the differential engagement of G proteins versus β-arrestins are commonly limited by the small response windows obtained in pathways that ... Read more >>

Sci Signal (Science signaling)
[2020, 13(625):]

Cited: 24 times

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In vitro determination of the efficacy of illicit synthetic cannabinoids at CB1 receptors.

Shivani Sachdev, Kiran Vemuri, Samuel D Banister, Mitchell Longworth, Michael Kassiou, Marina Santiago, Alexandros Makriyannis, Mark Connor,

<h4>Background and purpose</h4>The morbidity and mortality associated with recreational use of synthetic cannabinoid receptor agonists (SCRAs) may reflect strong activation of CB<sub>1</sub> receptors and is a major health concern. The properties of SCRA at CB<sub>1</sub> receptors are not well defined. Here we have developed an assay to determine acute CB<sub>1</sub> ... Read more >>

Br J Pharmacol (British journal of pharmacology)
[2019, 176(24):4653-4665]

Cited: 8 times

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High-throughput transposon sequencing highlights the cell wall as an important barrier for osmotic stress in methicillin resistant Staphylococcus aureus and underlines a tailored response to different osmotic stressors.

Christopher F Schuster, David M Wiedemann, Freja C M Kirsebom, Marina Santiago, Suzanne Walker, Angelika Gründling,

Staphylococcus aureus is an opportunistic pathogen that can cause soft tissue infections but is also a frequent cause of foodborne illnesses. One contributing factor for this food association is its high salt tolerance allowing this organism to survive commonly used food preservation methods. How this resistance is mediated is poorly ... Read more >>

Mol Microbiol (Molecular microbiology)
[2020, 113(4):699-717]

Cited: 4 times

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Differential activation of G-protein-mediated signalling by synthetic cannabinoid receptor agonists

Shivani Sachdev, Samuel Banister, Marina Santiago, Chris Bladen, Michael Kassiou, Mark Connor,

Synthetic cannabinoid receptor agonists (SCRAs) are new psychoactive substances associated with acute intoxication and even death. However, the molecular mechanisms through which SCRAs may exert their toxic effects remain unclear - including the potential differential activation of G protein subtypes by CB1, a major target of SCRA. We measured CB1-mediated ... Read more >>

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Cannabichromene is a cannabinoid CB2 receptor agonist.

Michael Udoh, Marina Santiago, Steven Devenish, Iain S McGregor, Mark Connor,

<h4>Background and purpose</h4>Cannabichromene (CBC) is one of the most abundant phytocannabinoids in Cannabis spp. It has modest antinociceptive and anti-inflammatory effects and potentiates some effects of Δ<sup>9</sup> -tetrahydrocannabinol in vivo. How CBC exerts these effects is poorly defined and there is little information about its efficacy at cannabinoid receptors. We ... Read more >>

Br J Pharmacol (British journal of pharmacology)
[2019, 176(23):4537-4547]

Cited: 11 times

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Brodifacoum does not modulate human cannabinoid receptor-mediated hyperpolarization of AtT20 cells or inhibition of adenylyl cyclase in HEK 293 cells.

Shivani Sachdev, Rochelle Boyd, Natasha L Grimsey, Marina Santiago, Mark Connor,

Background:Synthetic cannabinoids are a commonly used class of recreational drugs that can have significant adverse effects. There have been sporadic reports of co-consumption of illicit drugs with rodenticides such as warfarin and brodifacoum (BFC) over the past 20 years but recently, hundreds of people have been reported to have been ... Read more >>

PeerJ (PeerJ)
[2019, 7:e7733]

Cited: 3 times

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Absence of Entourage: Terpenoids Commonly Found in Cannabis sativa Do Not Modulate the Functional Activity of Δ9-THC at Human CB1 and CB2 Receptors.

Marina Santiago, Shivani Sachdev, Jonathon C Arnold, Iain S McGregor, Mark Connor,

Introduction: Compounds present in Cannabis sativa such as phytocannabinoids and terpenoids may act in concert to elicit therapeutic effects. Cannabinoids such as Δ9-tetrahydrocannabinol (Δ9-THC) directly activate cannabinoid receptor 1 (CB1) and cannabinoid receptor 2 (CB2); however, it is not known if terpenoids present in Cannabis also affect cannabinoid receptor signaling. ... Read more >>

Cannabis Cannabinoid Res (Cannabis and cannabinoid research)
[2019, 4(3):165-176]

Cited: 18 times

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High-throughput transposon sequencing highlights the cell wall as an important barrier for osmotic stress in methicillin resistantStaphylococcus aureusand underlines a tailored response to different osmotic stressors

Christopher Schuster, David Wiedemann, Freja Kirsebom, Marina Santiago, Suzanne Walker, Angelika Gründling,

<h4>Summary</h4> Staphylococcus aureus is an opportunistic pathogen that can cause soft tissue infections but is also a frequent cause of foodborne illnesses. One contributing factor for this food association is its high salt tolerance allowing this organism to survive commonly used food preservation methods. How this resistance is mediated is ... Read more >>

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Microbiome predictors of dysbiosis and VRE decolonization in patients with recurrent C. difficile infections in a multi-center retrospective study.

Marina Santiago, Lindsay Eysenbach, Jessica Allegretti, Olga Aroniadis, Lawrence J Brandt, Monika Fischer, Ari Grinspan, Colleen Kelly, Casey Morrow, Martin Rodriguez, Majdi Osman, Zain Kassam, Mark B Smith, Sonia Timberlake,

The gastrointestinal microbiome is intrinsically linked to the spread of antibiotic resistance. Antibiotic treatment puts patients at risk for colonization by opportunistic pathogens like vancomycin resistant Enterococcus and <i>Clostridioides difficile</i> by destroying the colonization resistance provided by the commensal microbiota. Once colonized, the host is at a much higher risk ... Read more >>

AIMS Microbiol (AIMS microbiology)
[2019, 5(1):1-18]

Cited: 2 times

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Absence of entourage: Terpenoids commonly found in Cannabis sativa do not modulate the functional activity of Δ9-THC at human CB1and CB2 receptors

Marina Santiago, Shivani Sachdev, Jonathon Arnold, Iain McGregor, Mark Connor,

<h4>Introduction</h4> Compounds present in Cannabis sativa such as phytocannabinoids and terpenoids, may act in concert to elicit therapeutic effects. Cannabinoids such as Δ 9 -tetrahydrocannabinol (Δ 9 -THC) directly activate cannabinoid receptor 1 (CB 1 ) and cannabinoid receptor 2 (CB 2 ), however, it is not known if terpenoids ... Read more >>

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