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1. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: Enzymes

Author

Alexander, Stephen PH, Fabbro, Doriano, Kelly, Eamonn, Mathie, Alistair, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Sharman, Joanna L, Southan, Christopher, Davies, Jamie A, Beuve, Annie, Boison, Detlev, Brouckaert, Peter, Burnett, John C, Burns, Kathryn, Dessauer, Carmen, Friebe, Andreas, Garthwaite, John, Gertsch, Jürg, Helsby, Nuala, Izzo, Angelo A, Koesling, Doris, Kuhn, Michaela, Ostrom, Rennolds, Papapetropoulos, Andreas, Potter, Lincoln R, Pyne, Nigel J, Pyne, Susan, Russwurm, Michael, Schmidt, Harald HHW, Seifert, Roland, Stasch, Johannes‐Peter, Szabo, Csaba, van der Stelt, Mario, van der Vliet, Albert, and Watts, Val

Subjects
Pharmacology and Pharmaceutical Sciences, Biomedical and Clinical Sciences, Generic health relevance, Animals, Databases, Pharmaceutical, Enzyme Inhibitors, Humans, Hydrolases, Isomerases, Ligands, Ligases, Lyases, Oxidoreductases, Transferases, CGTP Collaborators, Pharmacology & Pharmacy, Pharmacology and pharmaceutical sciences
Abstract

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 views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14752. Enzymes are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, catalytic receptors and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Published
2019

4. Receptor guanylyl cyclase (RGC) family in GtoPdb v.2023.1

Author

Beuve, Annie, primary, Brouckaert, Peter, primary, Burnett, Jr., John C., primary, Friebe, Andreas, primary, Garthwaite, John, primary, Hobbs, Adrian J., primary, Koesling, Doris, primary, Kuhn, Michaela, primary, Potter, Lincoln R., primary, Russwurm, Michael, primary, Schmidt, Harald H.H.W., primary, Stasch, Johannes-Peter, primary, and Waldman, Scott A., primary

Published
2023
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5. The Concise Guide to PHARMACOLOGY 2023/24: Catalytic receptors.

Author

Alexander, Stephen P. H., Fabbro, Doriano, Kelly, Eamonn, Mathie, Alistair A., Peters, John A., Veale, Emma L., Armstrong, Jane F., Faccenda, Elena, Harding, Simon D., Davies, Jamie A., Beuve, Annie, Brouckaert, Peter, Bryant, Clare, Burnett, John C., Farndale, Richard W., Friebe, Andreas, Garthwaite, John, Hobbs, Adrian J., Jarvis, Gavin E., and Koesling, Doris

Subjects
NUCLEAR receptors (Biochemistry), G protein coupled receptors, PHARMACOLOGY, CLINICAL pharmacology, DRUG target, ION channels, DATABASES
Abstract

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 nearly 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 targets and their ligands (https://www.guidetopharmacology.org/), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes almost 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point‐in‐time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.16180. Catalytic receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein‐coupled receptors, ion channels, nuclear hormone receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid‐2023, and supersedes data presented in the 2021/22, 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC‐IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate. [ABSTRACT FROM AUTHOR]

Published
2023
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6. Supplementary Figures S1-S7 from Depleting MET-Expressing Tumor Cells by ADCC Provides a Therapeutic Advantage over Inhibiting HGF/MET Signaling

Author

Hultberg, Anna, primary, Morello, Virginia, primary, Huyghe, Leander, primary, De Jonge, Natalie, primary, Blanchetot, Christophe, primary, Hanssens, Valérie, primary, De Boeck, Gitte, primary, Silence, Karen, primary, Festjens, Els, primary, Heukers, Raimond, primary, Roux, Benjamin, primary, Lamballe, Fabienne, primary, Ginestier, Christophe, primary, Charafe-Jauffret, Emmanuelle, primary, Maina, Flavio, primary, Brouckaert, Peter, primary, Saunders, Michael, primary, Thibault, Alain, primary, Dreier, Torsten, primary, de Haard, Hans, primary, and Michieli, Paolo, primary

Published
2023
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7. Data from Depleting MET-Expressing Tumor Cells by ADCC Provides a Therapeutic Advantage over Inhibiting HGF/MET Signaling

Author

Hultberg, Anna, primary, Morello, Virginia, primary, Huyghe, Leander, primary, De Jonge, Natalie, primary, Blanchetot, Christophe, primary, Hanssens, Valérie, primary, De Boeck, Gitte, primary, Silence, Karen, primary, Festjens, Els, primary, Heukers, Raimond, primary, Roux, Benjamin, primary, Lamballe, Fabienne, primary, Ginestier, Christophe, primary, Charafe-Jauffret, Emmanuelle, primary, Maina, Flavio, primary, Brouckaert, Peter, primary, Saunders, Michael, primary, Thibault, Alain, primary, Dreier, Torsten, primary, de Haard, Hans, primary, and Michieli, Paolo, primary

Published
2023
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8. Supplementary Tables S1-S7 from Depleting MET-Expressing Tumor Cells by ADCC Provides a Therapeutic Advantage over Inhibiting HGF/MET Signaling

Author

Hultberg, Anna, primary, Morello, Virginia, primary, Huyghe, Leander, primary, De Jonge, Natalie, primary, Blanchetot, Christophe, primary, Hanssens, Valérie, primary, De Boeck, Gitte, primary, Silence, Karen, primary, Festjens, Els, primary, Heukers, Raimond, primary, Roux, Benjamin, primary, Lamballe, Fabienne, primary, Ginestier, Christophe, primary, Charafe-Jauffret, Emmanuelle, primary, Maina, Flavio, primary, Brouckaert, Peter, primary, Saunders, Michael, primary, Thibault, Alain, primary, Dreier, Torsten, primary, de Haard, Hans, primary, and Michieli, Paolo, primary

Published
2023
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9. Supplementary Methods and References from Depleting MET-Expressing Tumor Cells by ADCC Provides a Therapeutic Advantage over Inhibiting HGF/MET Signaling

Author

Hultberg, Anna, primary, Morello, Virginia, primary, Huyghe, Leander, primary, De Jonge, Natalie, primary, Blanchetot, Christophe, primary, Hanssens, Valérie, primary, De Boeck, Gitte, primary, Silence, Karen, primary, Festjens, Els, primary, Heukers, Raimond, primary, Roux, Benjamin, primary, Lamballe, Fabienne, primary, Ginestier, Christophe, primary, Charafe-Jauffret, Emmanuelle, primary, Maina, Flavio, primary, Brouckaert, Peter, primary, Saunders, Michael, primary, Thibault, Alain, primary, Dreier, Torsten, primary, de Haard, Hans, primary, and Michieli, Paolo, primary

Published
2023
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15. Microcirculatory Function during Endotoxemia—A Functional Citrulline-Arginine-NO Pathway and NOS3 Complex Is Essential to Maintain the Microcirculation

Author

Wijnands, Karolina A. P., primary, Meesters, Dennis M., additional, Vandendriessche, Benjamin, additional, Briedé, Jacob J., additional, van Eijk, Hans M. H., additional, Brouckaert, Peter, additional, Cauwels, Anje, additional, Lamers, Wouter H., additional, and Poeze, Martijn, additional

Published
2021
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18. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Catalytic receptors

Author

Alexander, Stephen P H, primary, Fabbro, Doriano, additional, Kelly, Eamonn, additional, Mathie, Alistair, additional, Peters, John A, additional, Veale, Emma L, additional, Armstrong, Jane F, additional, Faccenda, Elena, additional, Harding, Simon D, additional, Pawson, Adam J, additional, Southan, Christopher, additional, Davies, Jamie A, additional, Beuve, Annie, additional, Brouckaert, Peter, additional, Bryant, Clare, additional, Burnett, John C., additional, Farndale, Richard W., additional, Friebe, Andreas, additional, Garthwaite, John, additional, Hobbs, Adrian J., additional, Jarvis, Gavin E., additional, Kuhn, Michaela, additional, MacEwan, David, additional, Monie, Tom P., additional, Potter, Lincoln R., additional, Schmidt, Harald H.H.W., additional, and Waldman, Scott A., additional

Published
2021
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19. Receptor guanylyl cyclase (RGC) family in GtoPdb v.2021.3

Author

Beuve, Annie, primary, Brouckaert, Peter, primary, Burnett, Jr., John C., primary, Friebe, Andreas, primary, Garthwaite, John, primary, Hobbs, Adrian J., primary, Koesling, Doris, primary, Kuhn, Michaela, primary, Potter, Lincoln R., primary, Russwurm, Michael, primary, Schmidt, Harald H.H.W., primary, Stasch, Johannes-Peter, primary, and Waldman, Scott A., primary

Published
2021
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20. THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: Catalytic receptors

Author

Alexander, Stephen PH, Fabbro, Doriano, Kelly, Eamonn, Mathie, Alistair, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Southan, Christopher, Davies, Jamie A, Beuve, Annie, Brouckaert, Peter, Bryant, Clare, Burnett, John C, Farndale, Richard W, Friebe, Andreas, Garthwaite, John, Hobbs, Adrian J, Jarvis, Gavin E, Kuhn, Michaela, MacEwan, David, Monie, Tom P, Papapetropoulos, Andreas, Potter, Lincoln R, Schmidt, Harald H H W, Szabo, Csaba, Waldman, Scott A, Alexander, Stephen PH, Fabbro, Doriano, Kelly, Eamonn, Mathie, Alistair, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Southan, Christopher, Davies, Jamie A, Beuve, Annie, Brouckaert, Peter, Bryant, Clare, Burnett, John C, Farndale, Richard W, Friebe, Andreas, Garthwaite, John, Hobbs, Adrian J, Jarvis, Gavin E, Kuhn, Michaela, MacEwan, David, Monie, Tom P, Papapetropoulos, Andreas, Potter, Lincoln R, Schmidt, Harald H H W, Szabo, Csaba, and Waldman, Scott A

Abstract

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), which provides more detailed views of target and ligand properties. Although the Concise Guide constitutes over 500 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.15541. Catalytic receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: G protein-coupled receptors, ion channels, nuclear hormone receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2021, and supersedes data presented in the 2019/20, 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the Nomenclature and Standards Committee of the International Union of Basic and Clinical Pharmacology (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Published
2021

21. Genetic modifiers of hypertension in soluble guanylate cyclase α1-deficient mice

Author

Buys, Emmanuel S., Raher, Michael J., Kirby, Andrew, Mohd, Shahid, Baron, David M., Hayton, Sarah R., Tainsh, Laurel T., Sips, Patrick Y., Rauwerdink, Kristen M., Yan, Qingshang, Tainsh, Robert E.T., Shakartzi, Hannah R., Stevens, Christine, Decaluwe, Kelly, Rodrigues-Machado, Maria da Gloria, Malhotra, Rajeev, de Voorde, Johan Van, Wang, Tong, Brouckaert, Peter, Daly, Mark J., and Bloch, Kenneth D.

Subjects
Blood pressure -- Measurement, Guanylate cyclase -- Properties, Hypertension -- Diagnosis -- Care and treatment -- Genetic aspects, Health care industry
Abstract

Nitric oxide (NO) plays an essential role in regulating hypertension and blood flow by inducing relaxation of vascular smooth muscle. Male mice deficient in a NO receptor component, the α1 subunit of soluble guanylate cyclase (sGCα1), are prone to hypertension in some, but not all, mouse strains, suggesting that additional genetic factors contribute to the onset of hypertension. Using linkage analyses, we discovered a quantitative trait locus (QTL) on chromosome 1 that was linked to mean arterial pressure (MAP) in the context of sGCα1 deficiency. This region is syntenic with previously identified blood pressure-related QTLs in the human and rat genome and contains the genes coding for renin. Hypertension was associated with increased activity of the renin-angiotensin-aldosterone system (RAAS). Further, we found that RAAS inhibition normalized MAP and improved endothelium-dependent vasorelaxation in sGCα1-deficient mice. These data identify the RAAS as a blood pressure-modifying mechanism in a setting of impaired NO/cGMP signaling., Introduction Systemic arterial hypertension is one of the most widespread public health problems in the developed world and the most prevalent modifiable risk factor for cardiovascular disease (CVD) in both [...]

Published
2012
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30. sGC[[alpha].sub.1][[beta].sub.1] attenuates cardiac dysfunction and mortality in murine inflammatory shock models

Author

Buys, Emmanuel S., Cauwels, Anje, Raher, Michael J., Passeri, Jonathan J., Hobai, Ion, Cawley, Sharon M., Rauwerdink, Kristen M., Thibault, Helene, Sips, Patrick Y., Thoonen, Robrecht, Scherrer-Crosbie, Marielle, Ichinose, Fumito, Brouckaert, Peter, and Bloch, Kenneth D.

Subjects
Cyclic guanylic acid -- Physiological aspects, Cyclic guanylic acid -- Research, Guanylate cyclase -- Physiological aspects, Guanylate cyclase -- Research, Heart diseases -- Risk factors, Heart diseases -- Prevention, Heart diseases -- Research, Mortality -- Prevention, Mortality -- Research, Biological sciences
Abstract

Altered cGMP signaling has been implicated in myocardial depression, morbidity, and mortality associated with sepsis. Previous studies, using inhibitors of soluble guanylate cyclase (sGC), suggested that cGMP generated by sGC contributed to the cardiac dysfunction and mortality associated with sepsis. We used sGC[[alpha].sub.1]-deficient (sGC[[alpha].sub.1.sup.-/-]) mice to unequivocally determine the role of sGC[[alpha].sub.1][[beta].sub.1] in the development of cardiac dysfunction and death associated with two models of inflammatory shock: endotoxin- and TNF-induced shock. At baseline, echocardiographic assessment and invasive hemodynamic measurements of left ventricular (LV) dimensions and function did not differ between wild-type (WT) mice and sGC[[alpha].sub.1.sup.-/-] mice on the C57BL/6 background (sGC[[alpha].sub.1.sup.-/-B6] mice). At 14 h after endotoxin challenge, cardiac dysfunction was more pronounced in sGC[[alpha].sub.1.sup.-/-B6] than WT mice, as assessed using echocardiographic and hemodynamic indexes of LV function. Similarly, [Ca.sup.2+] handling and cell shortening were impaired to a greater extent in cardiomyocytes isolated from sGC[[alpha].sub.1.sup.-/-B6] than WT mice after endotoxin challenge. Importantly, morbidity and mortality associated with inflammatory shock induced by endotoxin or TNF were increased in sGC[[alpha].sub.1.sup.-/-B6] compared with WT mice. Together, these findings suggest that cGMP generated by sGC[[alpha].sub.1][[beta].sub.1] protects against cardiac dysfunction and mortality in murine inflammatory shock models. soluble guanylate cyclase; left ventricular function; sepsis; mice; nitric oxide

Published
2009

32. Anaphylactic shock depends on PI3K and eNOS-derived NO

Author

Cauwels, Anje, Janssen, Ben, Buys, Emmanuel, Sips, Patrick, and Brouckaert, Peter

Subjects
Anaphylaxis -- Causes of, Anaphylaxis -- Research, Nitric oxide -- Health aspects, Nitric oxide -- Research
Abstract

Anaphylactic shock is a sudden, life-threatening allergic reaction associated with severe hypotension. Platelet-activating factor (PAF) is implicated in the cardiovascular dysfunctions occurring in various shock syndromes, including anaphylaxis. Excessive production [...]

Published
2006

33. Rapid downregulation of adipose tissue lipoprotein lipase activity on food deprivation: evidence that TNF-[alpha] is involved

Author

Wu, Gengshu, Brouckaert, Peter, and Olivecrona, Thomas

Subjects
Proteolipids -- Research, Lipoproteins -- Research, Biological sciences
Abstract

When food was removed from young rats in the early morning, adipose tissue tumor necrosis factor (TNF)-[alpha] activity increased 50% and lipoprotein lipase (LPL) activity decreased 70% in 6 h. There was a strong negative correlation between the TNF-[alpha] and LPL activities. Exogenous TNF-[alpha] further decreased LPL activity. Pentoxifylline, known to decrease production of TNF-[alpha], had no effect on LPL activity in fed rats but almost abolished the rise of TNF-[alpha] and the decrease of LPL activity in rats deprived of food. The specific activity of LPL decreased from 0.92 mU/ng in fed rats to 0.35 and 0.24 mU/ng in rats deprived of food given saline or TNF-[alpha], indicating a shift in the LPL molecules toward an inactive state. Lipopolysaccharide increased adipose tissue TNF-[alpha] and decreased LPL activity. Both of these effects were strongly impeded by pretreatment of the rats with pentoxifylline, or dexamethasone. Pretreatment of the rats with actinomycin D virtually abolished the response of LPL activity to food deprivation or exogenous TNF-[alpha]. We conclude that food deprivation, like lipopolysaccharide, signals via TNF-[alpha] to a gene whose product causes a rapid shift of newly synthesized LPL molecules toward an inactive form and thereby shuts down extraction of lipoprotein triglycerides by the adipose tissue. adipocytes; cytokines; endothelium; lasting; heparin; lipopolysaccharide; rat; secretion; tumor necrosis factor-[alpha]

Published
2004

40. Receptor guanylyl cyclase (RGC) family (version 2020.3) in the IUPHAR/BPS Guide to Pharmacology Database

Author

Beuve, Annie, primary, Brouckaert, Peter, primary, Burnett, Jr., John C., primary, Friebe, Andreas, primary, Garthwaite, John, primary, Hobbs, Adrian J., primary, Koesling, Doris, primary, Kuhn, Michaela, primary, Potter, Lincoln R., primary, Russwurm, Michael, primary, Schmidt, Harald H.H.W., primary, Stasch, Johannes-Peter, primary, and Waldman, Scott A., primary

Published
2020
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45. The Role of EUTox in Uremic Toxin Research

Author

Vanholder, Raymond, Abou-Deif, Omar, Argiles, Angel, Baurmeister, Ulrich, Beige, Joachim, Brouckaert, Peter, Brunet, Philippe, Cohen, Gerald, De Deyn, Peter Paul, Drüeke, Tilman B., Fliser, Danilo, Glorieux, Griet, Herget-Rosenthal, Stefan, Hörl, Walter H, Jankowski, Joachim, Jörres, Achim, Massy, Ziad A., Mischak, Harald, Perna, Alessandra F., Rodriguez-Portillo, Juan Mariano, Spasovski, Goce, Stegmayr, Bernd G., Stenvinkel, Peter, Thornalley, Paul J., Wanner, Christoph, and Wiecek, Andrzej

Published
2009
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48. THE CONCISE GUIDE TO PHARMACOLOGY 2019/20: G protein-coupled receptors

Author

Alexander, Stephen PH, Christopoulos, Arthur, Davenport, Anthony P, Kelly, Eamonn, Mathie, Alistair, Peters, John A, Veale, Emma L, Armstrong, Jane F, Faccenda, Elena, Harding, Simon D, Pawson, Adam J, Sharman, Joanna L, Southan, Christopher, Davies, Jamie A, Arumugam, Thiruma V, Bennett, Andrew, Sjogren, Benita, Sobey, Christopher, Wong, Szu Shen, Abbracchio, Maria P, Alexander, Wayne, Al-hosaini, Khaled, Back, Magnus, Beaulieu, Jean-Martin, Bernstein, Kenneth E, Bettler, Bernhard, Birdsall, Nigel JM, Blaho, Victoria, Bousquet, Corinne, Brauner-Osborne, Hans, Burnstock, Geoffrey, Calo, Girolamo, Castano, Justo P, Catt, Kevin J, Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chun, Jerold, Cianciulli, Antonia, Clapp, Lucie H, Couture, Rejean, Csaba, Zsolt, Dent, Gordon, Singh, Khuraijam Dhanachandra, Douglas, Steven D, Dournaud, Pascal, Eguchi, Satoru, Escher, Emanuel, Filardo, Edward, Fong, Tung M, Fumagalli, Marta, Gainetdinov, Raul R, de Gasparo, Marc, Gershengorn, Marvin, Gobeil, Fernand, Goodfriend, Theodore L, Goudet, Cyril, Gregory, Karen J, Gundlach, Andrew L, Hamann, Jorg, Hanson, Julien, Hauger, Richard L, Hay, Debbie, Heinemann, Akos, Hollenberg, Morley D, Holliday, Nicholas D, Horiuchi, Mastgugu, Hoyer, Daniel, Hunyady, Laszlo, Husain, Ahsan, Ijzerman, Adriaan P, Inagami, Tadashi, Jacobson, Kenneth A, Jensen, Robert T, Jockers, Ralf, Jonnalagadda, Deepa, Karnik, Sadashiva, Kaupmann, Klemens, Kemp, Jacqueline, Kennedy, Charles, Kihara, Yasuyuki, Kozielewicz, Pawel, Kreienkamp, Hans-Juergen, Kukkonen, Jyrki P, Langenhan, Tobias, Leach, Katie, Lecca, Davide, Lee, John D, Leeman, Susan E, Leprince, Jerome, Lolait, Stephen J, Lupp, Amelie, Macrae, Robyn, Maguire, Janet, Mazella, Jean, McArdle, Craig A, Melmed, Shlomo, Michel, Martin C, Miller, Laurence, Mitolo, Vincenzo, Mouillac, Bernard, Murphy, Philip M, Nahon, Jean-Louis, Norel, Xavier, Nyimanu, Duuamene, O'Carroll, Anne-Marie, Offermanns, Stefan, Panaro, Maria A, Pertwee, Roger G, Pin, Jean-Philippe, Prossnitz, Eric, Ramachandran, Rithwik, Reinscheid, Rainer K, Rondard, Philippe, Rovati, G Enrico, Ruzza, Chiara, Sanger, Gareth, Schoeneberg, Torsten, Schulte, Gunnar, Schulz, Stefan, Segaloff, Deborah L, Serhan, Charles N, Stoddart, Leigh A, Sugimoto, Yukihiko, Summers, Roger, Tan, Valerie, Thomas, Walter, Timmermans, Pieter BMWM, Tirupula, Kalyan, Tulipano, Giovanni, Unal, Hamiyet, Unger, Thomas, Vanderheyden, Patrick, Vaudry, David, Vaudry, Hubert, Vilardaga, Jean-Pierre, Walker, Christopher S, Ward, Donald T, Wester, Hans-Juergen, Willars, Gary B, Williams, Tom Lloyd, Woodruff, Trent M, Yao, Chengcan, Aldrich, Richard W, Becirovic, Elvir, Biel, Martin, Catterall, William A, Conner, Alex C, Davies, Paul, Delling, Markus, Di Virgilio, Francesco, Falzoni, Simonetta, George, Chandy, Goldstein, Steve AN, Grissmer, Stephan, Ha, Kotdaji, Hammelmann, Verena, Hanukoglu, Israel, Jarvis, Mike, Jensen, Anders A, Kaczmarek, Leonard K, Kellenberger, Stephan, King, Brian, Lynch, Joseph W, Perez-Reyes, Edward, Plant, Leigh D, Rash, Lachlan D, Ren, Dejian, Sivilotti, Lucia G, Smart, Trevor G, Snutch, Terrance P, Tian, Jinbin, Van den Eynde, Charlotte, Vriens, Joris, Wei, Aguan D, Winn, Brenda T, Wulff, Heike, Xu, Haoxing, Yue, Lixia, Zhang, Xiaoli, Zhu, Michael, Coons, Laurel, Fuller, Peter, Korach, Kenneth S, Young, Morag, Bryant, Clare, Farndale, Richard W, Hobbs, Adrian, Jarvis, Gavin E, MacEwan, David, Monie, Tom P, Waldman, Scott, Beuve, Annie, Boison, Detlev, Brouckaert, Peter, Burnett, John C, Burns, Kathryn, Dessauer, Carmen, Friebe, Andreas, Garthwaite, John, Gertsch, Jurg, Helsby, Nuala, Izzo, Angelo A, Koesling, Doris, Kuhn, Michaela, Ostrom, Rennolds, Papapetropoulos, Andreas, Potter, Lincoln R, Pyne, Nigel J, Pyne, Susan, Russwurm, Michael, Schmidt, Harald HHW, Seifert, Roland, Stasch, Johannes-Peter, Szabo, Csaba, van der Stelt, Mario, van der Vliet, Albert, Watts, Val, Anderson, Catriona MH, Broer, Stefan, Dawson, Paul, Hagenbuch, Bruno, Hammond, James R, Hancox, Jules, Inui, Ken-ichi, Kanai, Yoshikatsu, Kemp, Stephan, Thwaites, David T, Verri, Tiziano, University of Nottingham, UK (UON), Monash university, University of Cambridge [UK] (CAM), University of Bristol [Bristol], University of Greenwich, Ninewells Hospital and Medical School [Dundee], University of Edinburgh, Institut de Génomique Fonctionnelle (IGF), Institut National de la Santé et de la Recherche Médicale (INSERM)-Université de Montpellier (UM)-Centre National de la Recherche Scientifique (CNRS), Centre Hospitalier Régional Universitaire [Montpellier] (CHRU Montpellier), Institut de médecine moléculaire de Rangueil (I2MR), Université Toulouse III - Paul Sabatier (UT3), Université Fédérale Toulouse Midi-Pyrénées-Université Fédérale Toulouse Midi-Pyrénées-IFR150-Institut National de la Santé et de la Recherche Médicale (INSERM), Department of Drug Design and Pharmacology [Copenhagen] (ILF), Faculty of Health and Medical Sciences, University of Copenhagen = Københavns Universitet (KU)-University of Copenhagen = Københavns Universitet (KU), University of Córdoba [Córdoba], Neuroprotection du Cerveau en Développement / Promoting Research Oriented Towards Early Cns Therapies (PROTECT), Assistance publique - Hôpitaux de Paris (AP-HP) (AP-HP)-Hôpital Robert Debré-Université Paris Diderot - Paris 7 (UPD7)-Institut National de la Santé et de la Recherche Médicale (INSERM), Novartis Institutes for BioMedical Research (NIBR), Institut Cochin (IC UM3 (UMR 8104 / U1016)), Université Paris Descartes - Paris 5 (UPD5)-Institut National de la Santé et de la Recherche Médicale (INSERM)-Centre National de la Recherche Scientifique (CNRS), Différenciation et communication neuronale et neuroendocrine (DC2N), Université de Rouen Normandie (UNIROUEN), Normandie Université (NU)-Normandie Université (NU)-Institut National de la Santé et de la Recherche Médicale (INSERM), Institut de pharmacologie moléculaire et cellulaire (IPMC), Université Nice Sophia Antipolis (1965 - 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Subjects
0301 basic medicine, RM, Databases, Pharmaceutical, Computer science, Drug classification, Pharmacology, Ligands, Receptors, G-Protein-Coupled, NO, law.invention, 03 medical and health sciences, Databases, G-Protein-Coupled, 0302 clinical medicine, law, Summary information, Receptors, Animals, Humans, Pharmacology & Pharmacy, The Concise Guide to Pharmacology 2019/20, ComputingMilieux_MISCELLANEOUS, G protein-coupled receptor, Clinical pharmacology, Science & Technology, Extramural, POTENT, Pharmaceutical Preparations, 3. Good health, 030104 developmental biology, Pharmaceutical, [SDV.SP.PHARMA]Life Sciences [q-bio]/Pharmaceutical sciences/Pharmacology, [SDV.NEU]Life Sciences [q-bio]/Neurons and Cognition [q-bio.NC], Catalytic receptors, Life Sciences & Biomedicine, 030217 neurology & neurosurgery
Abstract

© 2019 The Authors. British Journal of Pharmacology published by John Wiley & Sons Ltd on behalf of The British Pharmacological Society. 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 views of target and ligand properties. Although the Concise Guide represents approximately 400 pages, the material presented is substantially reduced compared to information and links presented on the website. It provides a permanent, citable, point-in-time record that will survive database updates. The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/10.1111/bph.14748. G protein-coupled receptors are one of the six major pharmacological targets into which the Guide is divided, with the others being: ion channels, nuclear hormone receptors, catalytic receptors, enzymes and transporters. These are presented with nomenclature guidance and summary information on the best available pharmacological tools, alongside key references and suggestions for further reading. The landscape format of the Concise Guide is designed to facilitate comparison of related targets from material contemporary to mid-2019, and supersedes data presented in the 2017/18, 2015/16 and 2013/14 Concise Guides and previous Guides to Receptors and Channels. It is produced in close conjunction with the International Union of Basic and Clinical Pharmacology Committee on Receptor Nomenclature and Drug Classification (NC-IUPHAR), therefore, providing official IUPHAR classification and nomenclature for human drug targets, where appropriate.

Published
2019
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50. Mechanism of tolerance to tumor necrosis factor: receptor-specific pathway and selectivity

Author

Takahashi, Nozomi, Brouckaert, Peter, and Fiers, Walter

Subjects
Tumor necrosis factor -- Analysis, Interleukin-1 -- Bioavailability, Interleukin-6 -- Analysis, Biological sciences
Abstract

A study to characterize the pathways active in generating a selective tolerance to some of the effects of low doses of tumor necrosis factor (TNF) initiated due to its multiple injection revealed that tolerance discreetly inhibits the TNF-R75-directed pathways, specifically the part copied by interlukin-1 and RU-38486. The introduction of tolerance was found to be controlled by the excitation of TNF-R55.

Published
1995

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