Search results for: Kenneth A. Jacobson

Items from 1 to 20 out of 258 results

article

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors

Stephen P. H. Alexander, Arthur Christopoulos, Anthony P. Davenport, Eamonn Kelly, more

British Journal of Pharmacology > 180 > S2 > S23 - S144

The Concise Guide to PHARMACOLOGY 2023/24 is the sixth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of approximately 1800 drug targets, and about 6000 interactions with about 3900 ligands. There is an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug...

article

Adenosine A_2A receptor antagonists: from caffeine to selective non‐xanthines

Kenneth A. Jacobson, Zhan‐Guo Gao, Pierre Matricon, Matthew T. Eddy, more

British Journal of Pharmacology > 179 > 14 > 3496 - 3511

A long evolution of knowledge of the psychostimulant caffeine led in the 1960s to another purine natural product, adenosine and its A_2A receptor. Adenosine is a short‐lived autocrine/paracrine mediator that acts pharmacologically at four different adenosine receptors in a manner opposite to the pan‐antagonist caffeine and serves as an endogenous allostatic regulator. Although detrimental in the developing...

article

Spinal A₃ adenosine receptor activation acutely restores morphine antinociception in opioid tolerant male rats

Heather Leduc‐Pessah, Cynthia Xu, Churmy Y. Fan, Rebecca Dalgarno, more

Journal of Neuroscience Research > 100 > 1 > 251 - 264

Opioids are potent analgesics, but their pain‐relieving effects diminish with repeated use. The reduction in analgesic potency is a hallmark of opioid analgesic tolerance, which hampers opioid pain therapy. In the central nervous system, opioid analgesia is critically modulated by adenosine, a purine nucleoside implicated in the beneficial and detrimental actions of opioid medications. Here, we focus...

article

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors

Stephen P H Alexander, Arthur Christopoulos, Anthony P Davenport, Eamonn Kelly, more

British Journal of Pharmacology > 178 > S1 > S27 - S156

The Concise Guide to PHARMACOLOGY 2021/22 is the fifth in this series of biennial publications. The Concise Guide provides concise overviews, mostly in tabular format, of the key properties of nearly 1900 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org),...

article

Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

Peter Illes, Christa E. Müller, Kenneth A. Jacobson, Thomas Grutter, more

British Journal of Pharmacology > 178 > 3 > 489 - 514

The known seven mammalian receptor subunits (P2X1–7) form cationic channels gated by ATP. Three subunits compose a receptor channel. Each subunit is a polypeptide consisting of two transmembrane regions (TM1 and TM2), intracellular N‐ and C‐termini, and a bulky extracellular loop. Crystallization allowed the identification of the 3D structure and gating cycle of P2X receptors. The agonist‐binding...

article

Update of P2Y receptor pharmacology: IUPHAR Review 27

Kenneth A. Jacobson, Esmerilda G. Delicado, Christian Gachet, Charles Kennedy, more

British Journal of Pharmacology > 177 > 11 > 2413 - 2433

Eight G protein‐coupled P2Y receptor subtypes respond to extracellular adenine and uracil mononucleotides and dinucleotides. P2Y receptors belong to the δ group of rhodopsin‐like GPCRs and contain two structurally distinct subfamilies: P2Y₁, P2Y₂, P2Y₄, P2Y₆, and P2Y₁₁ (principally G_q protein‐coupled P2Y₁‐like) and P2Y_12–14 (principally G_i protein‐coupled P2Y₁₂‐like) receptors. Brain P2Y receptors...

article

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors

Stephen P H Alexander, Arthur Christopoulos, Anthony P Davenport, Eamonn Kelly, more

British Journal of Pharmacology > 176 > S1 > S21 - S141

The Concise Guide to PHARMACOLOGY 2019/20 is the fourth in this series of biennial publications. The Concise Guide provides concise overviews of the key properties of nearly 1800 human drug targets with an emphasis on selective pharmacology (where available), plus links to the open access knowledgebase source of drug targets and their ligands (www.guidetopharmacology.org), which provides more detailed...

article

Cover Image, Volume 38, Issue 4

Kenneth A. Jacobson, Stefania Merighi, Katia Varani, Pier Andrea Borea, more

Medicinal Research Reviews > 38 > 4 > i - i

On the cover: The cover image, by Kenneth A. Jacobson et al., is based on the Review Article A₃ Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy, https://doi.org/10.1002/med.21456.

article

A₃ Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

Kenneth A. Jacobson, Stefania Merighi, Katia Varani, Pier Andrea Borea, more

Medicinal Research Reviews > 38 > 4 > 1031 - 1072

The A₃ adenosine receptor (A₃AR) subtype is a novel, promising therapeutic target for inflammatory diseases, such as rheumatoid arthritis (RA) and psoriasis, as well as liver cancer. A₃AR is coupled to inhibition of adenylyl cyclase and regulation of mitogen‐activated protein kinase (MAPK) pathways, leading to modulation of transcription. Furthermore, A₃AR affects functions of almost all immune cells...

article

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor

Matthew T. Eddy, Ming-Yue Lee, Zhan-Guo Gao, Kate L. White, more

Cell > 2018 > 172 > 1-2 > 68-80.e12

Signaling across cellular membranes, the 826 human G protein-coupled receptors (GPCRs) govern a wide range of vital physiological processes, making GPCRs prominent drug targets. X-ray crystallography provided GPCR molecular architectures, which also revealed the need for additional structural dynamics data to support drug development. Here, nuclear magnetic resonance (NMR) spectroscopy with the wild-type-like...

article

Polypharmacology of conformationally locked methanocarba nucleosides

Kenneth A. Jacobson, Dilip K. Tosh, Kiran S. Toti, Antonella Ciancetta

Drug Discovery Today > 2017 > 22 > 12 > 1782-1791

A single molecular scaffold can be adapted to interact with diverse targets, either separately or simultaneously. Nucleosides and nucleotides in which ribose is substituted with bicyclo[3.1.0]hexane are an example of a versatile drug-like scaffold for increasing selectivity at their classical targets: kinases, polymerases, adenosine and P2 receptors. Also, by applying structure-based functional group...

article

Purinergic drug targets for gastrointestinal disorders

Geoffrey Burnstock, Kenneth A Jacobson, Fievos L Christofi

Current Opinion in Pharmacology > 2017 > 37 > C > 131-141

Purinergic receptors are implicated in the pathogenesis of gastrointestinal disorders and are being explored as potential therapeutic targets. Gut inflammation releases ATP that acts on neuronal, glial, epithelial and immune cells. Purinergic signalling in glia and neurons is implicated in enteric neuropathies. Inflammation activates glia to increase ATP release and alter purinergic signalling. ATP...

article

Species differences and mechanism of action of A₃ adenosine receptor allosteric modulators

Lili Du, Zhan-Guo Gao, Silvia Paoletta, Tina C. Wan, more

Purinergic Signalling > 2018 > 14 > 1 > 59-71

Activity of the A₃ adenosine receptor (AR) allosteric modulators LUF6000 (2-cyclohexyl-N-(3,4-dichlorophenyl)-1H-imidazo [4,5-c]quinolin-4-amine) and LUF6096 (N-{2-[(3,4-dichlorophenyl)amino]quinolin-4-yl}cyclohexanecarbox-amide) was compared at four A₃AR species homologs used in preclinical drug development. In guanosine 5′-[γ-[³⁵S]thio]triphosphate ([³⁵S]GTPγS) binding assays with cell membranes...

article

Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms

Jesse Lea Carlin, Shalini Jain, Elizabeth Gizewski, Tina C. Wan, more

Neuropharmacology > 2017 > 114 > C > 101-113

Small mammals have the ability to enter torpor, a hypothermic, hypometabolic state, allowing impressive energy conservation. Administration of adenosine or adenosine 5'-monophosphate (AMP) can trigger a hypothermic, torpor-like state. We investigated the mechanisms for hypothermia using telemetric monitoring of body temperature in wild type and receptor knock out (Adora1^−/−, Adora3^−/−) mice. Confirming...

article

UDP-glucose promotes neutrophil recruitment in the lung

Juliana I. Sesma, Clarissa D. Weitzer, Alessandra Livraghi-Butrico, Hong Dang, more

Purinergic Signalling > 2016 > 12 > 4 > 627-635

Abstract In addition to their role in glycosylation reactions, UDP-sugars are released from cells and activate widely distributed cell surface P2Y₁₄ receptors (P2Y₁₄R). However, the physiological/pathophysiological consequences of UDP-sugar release are incompletely defined. Here, we report that UDP-glucose levels are abnormally elevated in lung secretions from patients with cystic fibrosis (CF) as...

article

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin

Zhan-Guo Gao, Kenneth A. Jacobson

Biochemical Pharmacology > 2016 > 107 > C > 59-66

Gα_q inhibitor UBO-QIC (FR900359) is becoming an important pharmacological tool, but its selectivity against other G proteins and their subunits, especially βγ, has not been well characterized. We examined UBO-QIC’s effect on diverse signaling pathways mediated via various G protein-coupled receptors (GPCRs) and G protein subunits by comparison with known Gα_i inhibitor pertussis toxin. As expected,...

article

Medicinal chemistry of adenosine, P2Y and P2X receptors

Kenneth A. Jacobson, Christa E. Müller

Neuropharmacology > 2016 > 104 > C > 31-49

Pharmacological tool compounds are now available to define action at the adenosine (ARs), P2Y and P2X receptors. We present a selection of the most commonly used agents to study purines in the nervous system. Some of these compounds, including A₁ and A₃ AR agonists, P2Y₁R and P2Y₁₂R antagonists, and P2X3, P2X4 and P2X7 antagonists, are potentially of clinical use in treatment of disorders of the nervous...

chapter

Xanthines as Adenosine Receptor Antagonists

Christa E. Müller, Kenneth A. Jacobson

Handbook of Experimental Pharmacology > Methylxanthines > 151-199

The natural plant alkaloids caffeine and theophylline were the first adenosine receptor (AR) antagonists described in the literature. They exhibit micromolar affinities and are non-selective. A large number of derivatives and analogues were subsequently synthesized and evaluated as AR antagonists. Very potent antagonists have thus been developed with selectivity for each of the four AR subtypes.

chapter

Adenosine A₃ Receptors in Muscle Protection

Bruce T. Liang, Maria Urso, Edward Zambraski, Kenneth A. Jacobson

A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics > Effects on Tissues and Organs and Therapeutic Applications > 257-280

A growing body of evidence has accumulated to indicate an important cyto-protective role of the adenosine A₃ receptor. This protective function, originally discovered in ameliorating ischemia–reperfusion injury in the heart, is now also extended to the skeletal muscle. Understanding the pharmacology of various adenosine receptor subtypes allowed their selective activation and delineated the protective...

chapter

Introduction to Adenosine Receptors as Therapeutic Targets

Kenneth A. Jacobson

Handbook of Experimental Pharmacology > Adenosine Receptors in Health and Disease > 1-24

Adenosine acts as a cytoprotective modulator in response to stress to an organ or tissue. Although short-lived in the circulation, it can activate four subtypes of G protein-coupled adenosine receptors (ARs): A₁, A_2A, A_2B, and A₃. The alkylxanthines caffeine and theophylline are the prototypical antagonists of ARs, and their stimulant actions occur primarily through this mechanism. For each of the...

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INFONA - science communication portal

Search results for: Kenneth A. Jacobson

The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors

Adenosine A_2A receptor antagonists: from caffeine to selective non‐xanthines

Spinal A₃ adenosine receptor activation acutely restores morphine antinociception in opioid tolerant male rats

THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein‐coupled receptors

Update of P2X receptor properties and their pharmacology: IUPHAR Review 30

Update of P2Y receptor pharmacology: IUPHAR Review 27

THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein‐coupled receptors

Cover Image, Volume 38, Issue 4

A₃ Adenosine Receptors as Modulators of Inflammation: From Medicinal Chemistry to Therapy

Allosteric Coupling of Drug Binding and Intracellular Signaling in the A2A Adenosine Receptor

Polypharmacology of conformationally locked methanocarba nucleosides

Purinergic drug targets for gastrointestinal disorders

Species differences and mechanism of action of A₃ adenosine receptor allosteric modulators

Hypothermia in mouse is caused by adenosine A1 and A3 receptor agonists and AMP via three distinct mechanisms

UDP-glucose promotes neutrophil recruitment in the lung

On the selectivity of the Gαq inhibitor UBO-QIC: A comparison with the Gαi inhibitor pertussis toxin

Medicinal chemistry of adenosine, P2Y and P2X receptors

Xanthines as Adenosine Receptor Antagonists

Adenosine A₃ Receptors in Muscle Protection

Introduction to Adenosine Receptors as Therapeutic Targets

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