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1. The Concise Guide To Pharmacology 2021/22: G Protein-Coupled Receptors

Author

Nigel J. M. Birdsall, Stephen J Lolait, Hans-Jürgen Wester, Paul L. Chazot, Sadashiva S. Karnik, Simon D. Harding, Celine Valant, Stephen P.H. Alexander, Olivier Civelli, Zsolt Csaba, Mastgugu Horiuchi, Khuraijam Dhanachandra Singh, Theodore L. Goodfriend, Morley D. Hollenberg, Duuamene Nyimanu, Shlomo Melmed, G. Enrico Rovati, Xavier Norel, Leigh A. Stoddart, Klemens Kaupmann, Robyn Macrae, Nicholas D. Holliday, Deborah L. Segaloff, Justo P. Castaño, Tony Ngo, Gordon Dent, Jean-Martin Beaulieu, Thomas L Williams, Antonia Cianciulli, Paweł Kozielewicz, Xaria X. Li, Jyrki P. Kukkonen, Craig A. McArdle, John D. Lee, Philippe Rondard, Steven D. Douglas, Hubert Vaudry, Khaled A. Al-Hosaini, Nan Chiang, Bernhard Bettler, Giovanni Tulipano, Corinne Bousquet, Karen J. Gregory, Craig Gerard, Robert T. Jensen, Stefan Schulz, Rithwik Ramachandran, Ross A. D. Bathgate, Deepa Jonnalagadda, David M. Thal, Takio Kitazawa, Manisha Ray, Bice Chini, Thomas Unger, Marta Fumagalli, Jean-Pierre Vilardaga, Donald T. Ward, Roger G. Pertwee, Stefan Offermanns, Marvin C. Gershengorn, Marc Parmentier, Pieter Timmermans, Eamonn Kelly, Yukihiko Sugimoto, Hamiyet Unal, Vincenzo Mitolo, Alistair Mathie, Emma L. Veale, Andrew L. Gundlach, Anthony P. Davenport, Mark T. Quinn, Jérôme Leprince, Christa E. Müller, Geoffrey Burnstock, Akos Heinemann, Jacqueline R. Kemp, Richard D. Ye, Bernard Mouillac, Roger J. Summers, Raul R. Gainetdinov, Girolamo Calò, Philip N. Murphy, Amelie Lupp, Kalyan C. Tirupula, Walter G. Thomas, Julien Hanson, Ahsan Husain, Katie Leach, Lucie H. Clapp, Hans Bräuner-Osborne, Gunnar Schulte, Kenneth E. Bernstein, Jean Mazella, Torsten Schöneberg, Satoru Eguchi, Martin C. Michel, Maria Antonietta Panaro, Kevin J. Catt, Rainer K. Reinscheid, Hans-Jürgen Kreienkamp, Wayne R. Alexander, Emanuel Escher, Anne Marie O'Carroll, Magnus Bäck, Laurence J. Miller, Jane F. Armstrong, Chiara Ruzza, Trent M. Woodruff, Daniel Hoyer, Chengcan Yao, Maria P. Abbracchio, John A. Peters, Gary B. Willars, Jean-Philippe Pin, David Vaudry, Debbie L. Hay, François Boulay, Davide Lecca, Eric R. Prossnitz, Arthur Christopoulos, Victoria A. Blaho, Yasuyuki Kihara, Charles Kennedy, Christopher Southan, László Hunyady, Pascal Dournaud, Fernand Gobeil, Cyril Goudet, Charles N. Serhan, Claes Dahlgren, Jörg Hamann, Tobias Langenhan, Ralf Jockers, Nicholas M. Barnes, Jean-Louis Nahon, Richard L. Hauger, Adam J. Pawson, Gareth J. Sanger, Tung Fong, Susan E. Leeman, Elena Faccenda, Edward J. Filardo, Valerie P. Tan, Marc de Gasparo, Ji Ming Wang, Jamie A. Davies, Jerold Chun, Stefania Ceruti, Tadashi Inagami, Réjean Couture, Kenneth A. Jacobson, Patrick Vanderheyden, Adriaan P. IJzerman, Janet J. Maguire, Christopher S. Walker, RS: CARIM other, Alexander, Stephen Ph [0000-0003-4417-497X], Christopoulos, Arthur [0000-0003-4442-3294], Davenport, Anthony P [0000-0002-2096-3117], Mathie, Alistair [0000-0001-6094-2890], Peters, John A [0000-0002-4277-4245], Veale, Emma L [0000-0002-6778-9929], Armstrong, Jane F [0000-0002-0524-0260], Faccenda, Elena [0000-0001-9855-7103], Harding, Simon D [0000-0002-9262-8318], Pawson, Adam J [0000-0003-2280-845X], Southan, Christopher [0000-0001-9580-0446], Davies, Jamie A [0000-0001-6660-4032], Abbracchio, Maria Pia [0000-0002-7833-3388], Bäck, Magnus [0000-0003-0853-5141], Bathgate, Ross [0000-0001-6301-861X], Beaulieu, Jean-Martin [0000-0002-0446-7447], Bettler, Bernhard [0000-0003-0842-8207], Blaho, Victoria [0000-0001-8499-2278], Bousquet, Corinne [0000-0002-2501-0593], Bräuner-Osborne, Hans [0000-0001-9495-7388], Burnstock, Geoffrey [0000-0001-8152-7979], Ceruti, Stefania [0000-0003-1663-4211], Chazot, Paul [0000-0002-5453-0379], Chiang, Nan [0000-0003-1963-1585], Chini, Bice [0000-0002-1686-284X], Chun, Jerold [0000-0003-3964-0921], Clapp, Lucie H [0000-0001-7802-4481], Dent, Gordon [0000-0001-9419-2952], Singh, Khuraijam Dhanachandra [0000-0003-0506-6896], Fumagalli, Marta [0000-0002-0158-842X], Gainetdinov, Raul R [0000-0003-2951-6038], Goudet, Cyril [0000-0002-8255-3535], Gregory, Karen J [0000-0002-3833-2137], Gundlach, Andrew L [0000-0002-6066-9692], Hamann, Jörg [0000-0002-9448-1727], Hanson, Julien [0000-0001-7063-7590], Hay, Debbie L [0000-0002-9558-5122], Heinemann, Akos [0000-0002-8554-2372], Holliday, Nicholas D [0000-0002-2900-828X], Hoyer, Daniel [0000-0002-1405-7089], IJzerman, Adriaan P [0000-0002-1182-2259], Jacobson, Kenneth A [0000-0001-8104-1493], Jockers, Ralf [0000-0002-4354-1750], Jonnalagadda, Deepa [0000-0002-1511-8197], Karnik, Sadashiva [0000-0003-0746-2753], Kaupmann, Klemens [0000-0001-8903-2508], Kennedy, Charles [0000-0001-9661-5437], Kihara, Yasuyuki [0000-0001-7462-3006], Kozielewicz, Pawel [0000-0003-1414-3566], Kukkonen, Jyrki P [0000-0002-6989-1564], Langenhan, Tobias [0000-0002-9061-3809], Leach, Katie [0000-0002-9280-1803], Lecca, Davide [0000-0002-3258-363X], Lee, John D [0000-0002-9976-7396], Leprince, Jérôme [0000-0002-7814-9927], Li, Xaria X [0000-0001-5924-2977], Lolait, Stephen J [0000-0001-7228-8072], Maguire, Janet [0000-0002-9254-7040], Mazella, Jean [0000-0002-5627-0742], McArdle, Craig A [0000-0003-4836-5351], Michel, Martin C [0000-0003-4161-8467], Miller, Laurence J [0000-0002-4554-3872], Mouillac, Bernard [0000-0002-3906-8673], Müller, Christa E [0000-0002-0013-6624], Nahon, Jean-Louis [0000-0001-9572-7779], Ngo, Tony [0000-0002-6779-2546], Norel, Xavier [0000-0003-0734-3359], O'Carroll, Anne-Marie [0000-0001-5255-8506], Offermanns, Stefan [0000-0001-8676-6805], Pertwee, Roger G [0000-0003-3227-2783], Pin, Jean-Philippe [0000-0002-1423-345X], Prossnitz, Eric R [0000-0001-9190-8302], Ramachandran, Rithwik [0000-0001-9557-9905], Ray, Manisha [0000-0002-8844-6191], Rondard, Philippe [0000-0003-1134-2738], Rovati, G Enrico [0000-0002-8788-9783], Ruzza, Chiara [0000-0003-1360-202X], Sanger, Gareth J [0000-0002-4231-1945], Schöneberg, Torsten [0000-0001-5313-0237], Schulte, Gunnar [0000-0002-2700-7013], Stoddart, Leigh A [0000-0002-4469-0600], Sugimoto, Yukihiko [0000-0001-6973-932X], Summers, Roger [0000-0002-8367-4056], Tan, Valerie P [0000-0002-7308-1601], Thal, David [0000-0002-0325-2524], Valant, Celine [0000-0002-2509-7465], Walker, Christopher S [0000-0001-8151-4123], Ward, Donald T [0000-0003-1342-9458], Woodruff, Trent M [0000-0003-1382-911X], Yao, Chengcan [0000-0003-3754-2842], Apollo - University of Cambridge Repository, Department of Pharmacology, and Experimental Immunology

Subjects
RM, Cytoplasmic and Nuclear, Computer science, Databases, Pharmaceutical, Humans, Ion Channels, Ligands, Receptors, Cytoplasmic and Nuclear, Receptors, G-Protein-Coupled, Pharmacology, IN-VITRO CHARACTERIZATION, NO, RS, law.invention, G-Protein-Coupled, Databases, 03 medical and health sciences, CALCIUM-SENSING RECEPTOR, 0302 clinical medicine, DELTA-OPIOID RECEPTOR, law, Summary information, Receptors, HISTAMINE H-3 RECEPTOR, FATTY-ACID RECEPTOR, METABOTROPIC GLUTAMATE-RECEPTOR, 030304 developmental biology, G protein-coupled receptor, GONADOTROPIN-RELEASING-HORMONE, 0303 health sciences, Clinical pharmacology, FORMYL PEPTIDE RECEPTOR, MUSCARINIC ACETYLCHOLINE-RECEPTOR, 3. Good health, 317 Pharmacy, 030220 oncology & carcinogenesis, Pharmaceutical, NEGATIVE ALLOSTERIC MODULATOR, Catalytic receptors
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.15538. 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-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

2. Natriuretic Peptide Expression and Function in GH3 Somatolactotropes and Feline Somatotrope Pituitary Tumours

Author

Patrick J. Kenny, Márta Korbonits, Jordan E. Read, Stijn J. M. Niessen, Victoria J Crossley, Samantha M. Mirczuk, Christopher J Scudder, Jacob T. Regan, Robert C. Fowkes, Imelda M. McGonnell, Craig A. McArdle, Holger A. Volk, Caroline P.D. Wheeler-Jones, David B. Church, Bigboy H. Simbi, Joe Fenn, Karen M. Richardson, McArdle, Craig A [0000-0003-4836-5351], Fenn, Joseph [0000-0001-7851-670X], Volk, Holger A [0000-0002-7312-638X], Wheeler-Jones, Caroline P [0000-0002-6542-7713], Fowkes, Robert C [0000-0002-2222-2056], and Apollo - University of Cambridge Repository

Subjects
0301 basic medicine, Male, Growth hormone receptor, pituitary, lcsh:Chemistry, chemistry.chemical_compound, 0302 clinical medicine, Natriuretic peptide, Cyclic AMP, feline, Receptor, lcsh:QH301-705.5, Cyclic GMP, Thyrotropin-Releasing Hormone, Spectroscopy, Forskolin, General Medicine, NPR1, NPR2, Computer Science Applications, medicine.anatomical_structure, Phenotype, Pituitary Gland, CNP, Female, medicine.medical_specialty, Somatotropic cell, medicine.drug_class, 030209 endocrinology & metabolism, Biology, Catalysis, Article, Cell Line, Inorganic Chemistry, 03 medical and health sciences, Anterior pituitary, Internal medicine, medicine, Animals, Pituitary Neoplasms, Physical and Theoretical Chemistry, Rats, Wistar, Molecular Biology, multiplex RT-qPCR, Organic Chemistry, somatotrope, Colforsin, Estrogens, Natriuretic Peptide, C-Type, Rats, 030104 developmental biology, Endocrinology, chemistry, lcsh:Biology (General), lcsh:QD1-999, Acromegaly, Mutation, Cats, Receptors, Atrial Natriuretic Factor
Abstract

Patients harbouring mutations in genes encoding C-type natriuretic peptide (CNP, NPPC) or its receptor guanylyl cyclase B (GC-B, NPR2) suffer from severe growth phenotypes, loss-of-function mutations cause achondroplasia, whereas gain-of-function mutations cause skeletal overgrowth. Although most of the effects of CNP/GC-B on growth are mediated directly on bone, evidence suggests the natriuretic peptides may also affect anterior pituitary control of growth. Our previous studies described the expression of NPPC and NPR2 in a range of human pituitary tumours, normal human pituitary, and normal fetal human pituitary. However, the natriuretic peptide system in somatotropes has not been extensively explored. Here, we examine the expression and function of the CNP/GC-B system in rat GH3 somatolactotrope cell line and pituitary tumours from a cohort of feline hypersomatotropism (HST, acromegaly) patients. Using multiplex RT-qPCR, all three natriuretic peptides and their receptors were detected in GH3 cells. The expression of Nppc was significantly enhanced following treatment with either 100 nM TRH or 10 &micro, M forskolin, yet only Npr1 expression was sensitive to forskolin stimulation, the effects of forskolin and TRH on Nppc expression were PKA- and MAPK-dependent, respectively. CNP stimulation of GH3 somatolactotropes significantly inhibited Esr1, Insr and Lepr expression, but dramatically enhanced cFos expression at the same time point. Oestrogen treatment significantly enhanced expression of Nppa, Nppc, Npr1, and Npr2 in GH3 somatolactotropes, but inhibited CNP-stimulated cGMP accumulation. Finally, transcripts for all three natriuretic peptides and receptors were expressed in feline pituitary tumours from patients with HST. NPPC expression was negatively correlated with pituitary tumour volume and SSTR5 expression, but positively correlated with D2R and GHR expression. Collectively, these data provide mechanisms that control expression and function of CNP in somatolactotrope cells, and identify putative transcriptional targets for CNP action in somatotropes.

Published
2021
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