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Article ; Online: Optical Control of G-Actin with a Photoswitchable Latrunculin.

Vepřek, Nynke A / Cooper, Madeline H / Laprell, Laura / Yang, Emily Jie-Ning / Folkerts, Sander / Bao, Ruiyang / Boczkowska, Malgorzata / Palmer, Nicholas J / Dominguez, Roberto / Oertner, Thomas G / Pon, Liza A / Zuchero, J Bradley / Trauner, Dirk H

Journal of the American Chemical Society

2024 Volume 146, Issue 13, Page(s) 8895–8903

Abstract: ... to polymeric F-actin or monomeric G-actin to stabilize or destabilize filaments or prevent their formation and ... growth, respectively. Among these, the latrunculins, which bind to G-actin and affect polymerization, are ...

Abstract	Actin is one of the most abundant proteins in eukaryotic cells and is a key component of the cytoskeleton. A range of small molecules has emerged that interfere with actin dynamics by either binding to polymeric F-actin or monomeric G-actin to stabilize or destabilize filaments or prevent their formation and growth, respectively. Among these, the latrunculins, which bind to G-actin and affect polymerization, are widely used as tools to investigate actin-dependent cellular processes. Here, we report a photoswitchable version of latrunculin, termed opto-latrunculin (
MeSH term(s)	Animals ; Mice ; Humans ; Actins/chemistry ; Actin Cytoskeleton/metabolism ; Cytoskeleton/metabolism ; Cell Line ; Microtubules/metabolism
Chemical Substances	Actins
Language	English
Publishing date	2024-03-21
Publishing country	United States
Document type	Journal Article
ZDB-ID	3155-0
ISSN	1520-5126 ; 0002-7863
ISSN (online)	1520-5126
ISSN	0002-7863
DOI	10.1021/jacs.3c10776
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Article ; Online: BCR-ABL is enriched in S- and G

Nicholas, Bradley A / Purohit, Reshma / Woods, Andrew D / Kannan, Kavya / Srinivasa, Ganapati / Bridge, Julia A / Kim, Jin-Ah / Keller, Charles

Leukemia research

2023 Volume 126, Page(s) 107036

MeSH term(s)	Humans ; Fusion Proteins, bcr-abl ; Cell Cycle
Chemical Substances	Fusion Proteins, bcr-abl (EC 2.7.10.2)
Language	English
Publishing date	2023-02-08
Publishing country	England
Document type	Letter ; Research Support, Non-U.S. Gov't
ZDB-ID	752396-8
ISSN	1873-5835 ; 0145-2126
ISSN (online)	1873-5835
ISSN	0145-2126
DOI	10.1016/j.leukres.2023.107036
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Article: The G-alpha Gpa1 directs septin localization in the mating projection of

Johnson, Cory P / Hart, Andrew / Jarvis, Katherine F / Latario, Sarah G / Shrestha, Sudati / Leclerc, Nicholas / Khalil, André / Kelley, Joshua B

bioRxiv : the preprint server for biology

2023

Abstract: The yeast mating response uses a G-protein coupled receptor (GPCR), Ste2, to detect mating ... of the Gα, Gpa1, by the Regulator of G-protein Signaling (RGS), Sst2, is required for proper septin ...

Abstract	The yeast mating response uses a G-protein coupled receptor (GPCR), Ste2, to detect mating pheromone and initiate mating projection morphogenesis. The septin cytoskeleton plays a key role in the formation of the mating projection, forming structures at the base of the projection. Desensitization of the Gα, Gpa1, by the Regulator of G-protein Signaling (RGS), Sst2, is required for proper septin organization and morphogenesis. In cells where the Gα is hyperactive, septins are mislocalized to the site of polarity, and the cells are unable to track a pheromone gradient. We set out to identify the proteins that mediate Gα control of septins during the
Language	English
Publishing date	2023-06-16
Publishing country	United States
Document type	Preprint
DOI	10.1101/2023.06.16.545321
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Article ; Online: The Concise Guide to PHARMACOLOGY 2023/24: G protein-coupled receptors.

Alexander, Stephen P H / Christopoulos, Arthur / Davenport, Anthony P / Kelly, Eamonn / Mathie, Alistair A / Peters, John A / Veale, Emma L / Armstrong, Jane F / Faccenda, Elena / Harding, Simon D / Davies, Jamie A / Abbracchio, Maria Pia / Abraham, George / Agoulnik, Alexander / Alexander, Wayne / Al-Hosaini, Khaled / Bäck, Magnus / Baker, Jillian G / Barnes, Nicholas M /

Bathgate, Ross / Beaulieu, Jean-Martin / Beck-Sickinger, Annette G / Behrens, Maik / Bernstein, Kenneth E / Bettler, Bernhard / Birdsall, Nigel J M / Blaho, Victoria / Boulay, Francois / Bousquet, Corinne / Bräuner-Osborne, Hans / Burnstock, Geoffrey / Caló, Girolamo / Castaño, Justo P / Catt, Kevin J / Ceruti, Stefania / Chazot, Paul / Chiang, Nan / Chini, Bice / Chun, Jerold / Cianciulli, Antonia / Civelli, Olivier / Clapp, Lucie H / Couture, Réjean / Cox, Helen M / Csaba, Zsolt / Dahlgren, Claes / Dent, Gordon / Douglas, Steven D / Dournaud, Pascal / Eguchi, Satoru / Escher, Emanuel / Filardo, Edward J / Fong, Tung / Fumagalli, Marta / Gainetdinov, Raul R / Garelja, Michael L / de Gasparo, Marc / Gerard, Craig / Gershengorn, Marvin / Gobeil, Fernand / Goodfriend, Theodore L / Goudet, Cyril / Grätz, Lukas / Gregory, Karen J / Gundlach, Andrew L / Hamann, Jörg / Hanson, Julien / Hauger, Richard L / Hay, Debbie L / Heinemann, Akos / Herr, Deron / Hollenberg, Morley D / Holliday, Nicholas D / Horiuchi, Mastgugu / Hoyer, Daniel / Hunyady, László / 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 / Kitazawa, Takio / Kozielewicz, Pawel / Kreienkamp, Hans-Jürgen / Kukkonen, Jyrki P / Langenhan, Tobias / Larhammar, Dan / Leach, Katie / Lecca, Davide / Lee, John D / Leeman, Susan E / Leprince, Jérôme / Li, Xaria X / Lolait, Stephen J / Lupp, Amelie / Macrae, Robyn / Maguire, Janet / Malfacini, Davide / Mazella, Jean / McArdle, Craig A / Melmed, Shlomo / Michel, Martin C / Miller, Laurence J / Mitolo, Vincenzo / Mouillac, Bernard / Müller, Christa E / Murphy, Philip M / Nahon, Jean-Louis / Ngo, Tony / Norel, Xavier / Nyimanu, Duuamene / O'Carroll, Anne-Marie / Offermanns, Stefan / Panaro, Maria Antonietta / Parmentier, Marc / Pertwee, Roger G / Pin, Jean-Philippe / Prossnitz, Eric R / Quinn, Mark / Ramachandran, Rithwik / Ray, Manisha / Reinscheid, Rainer K / Rondard, Philippe / Rovati, G Enrico / Ruzza, Chiara / Sanger, Gareth J / Schöneberg, Torsten / Schulte, Gunnar / Schulz, Stefan / Segaloff, Deborah L / Serhan, Charles N / Singh, Khuraijam Dhanachandra / Smith, Craig M / Stoddart, Leigh A / Sugimoto, Yukihiko / Summers, Roger / Tan, Valerie P / Thal, David / Thomas, Walter Wally / Timmermans, Pieter B M W M / Tirupula, Kalyan / Toll, Lawrence / Tulipano, Giovanni / Unal, Hamiyet / Unger, Thomas / Valant, Celine / Vanderheyden, Patrick / Vaudry, David / Vaudry, Hubert / Vilardaga, Jean-Pierre / Walker, Christopher S / Wang, Ji Ming / Ward, Donald T / Wester, Hans-Jürgen / Willars, Gary B / Williams, Tom Lloyd / Woodruff, Trent M / Yao, Chengcan / Ye, Richard D

British journal of pharmacology

2023 Volume 180 Suppl 2, Page(s) S23–S144

Abstract: ... of this section can be found at http://onlinelibrary.wiley.com/doi/bph.16177. G protein-coupled receptors are one ...

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 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 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/bph.16177. 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-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.
MeSH term(s)	Humans ; Databases, Pharmaceutical ; Receptors, G-Protein-Coupled ; Ligands ; Ion Channels/chemistry ; Receptors, Cytoplasmic and Nuclear
Chemical Substances	Receptors, G-Protein-Coupled ; Ligands ; Ion Channels ; Receptors, Cytoplasmic and Nuclear
Language	English
Publishing date	2023-12-18
Publishing country	England
Document type	Journal Article
ZDB-ID	80081-8
ISSN	1476-5381 ; 0007-1188
ISSN (online)	1476-5381
ISSN	0007-1188
DOI	10.1111/bph.16177
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Article ; Online: Cerebral oxygenation and perfusion kinetics monitoring of military aircrew at high G using novel fNIRS wearable system.

Roumengous, Thibault / Boutwell, R Casey / Strohmaier, Jason / Allen, Jared / Goldbach, Brett / Marotta, Nicholas / Songkakul, Tanner / Critcher, Shelby / Morse, Bria G / Beer, Jeremy M A / Sherman, Paul M

Frontiers in neuroergonomics

2024 Volume 5, Page(s) 1357905

Abstract: ... challenges posed by high acceleration (G-force) in HPA aircrew and explores the potential of a novel wearable ... oxygenation during high G-force exposure.: Methods: The NIRSense Aerie system is a flight-optimized ... concentration changes. A human evaluation of the NIRSense Aerie was conducted on six subjects exposed to G ...

Abstract	Introduction: Real-time physiological episode (PE) detection and management in aircrew operating high-performance aircraft (HPA) is crucial for the US Military. This paper addresses the unique challenges posed by high acceleration (G-force) in HPA aircrew and explores the potential of a novel wearable functional near-infrared spectroscopy (fNIRS) system, named NIRSense Aerie, to continuously monitor cerebral oxygenation during high G-force exposure. Methods: The NIRSense Aerie system is a flight-optimized, wearable fNIRS device designed to monitor tissue oxygenation 13-20 mm below the skin's surface. The system includes an optical frontend adhered to the forehead, an electronics module behind the earcup of aircrew helmets, and a custom adhesive for secure attachment. The fNIRS optical layout incorporates near-distance, middle-distance, and far-distance infrared emitters, a photodetector, and an accelerometer for motion measurements. Data processing involves the modified Beer-Lambert law for computing relative chromophore concentration changes. A human evaluation of the NIRSense Aerie was conducted on six subjects exposed to G-forces up to +9 Gz in an Aerospace Environmental Protection Laboratory centrifuge. fNIRS data, pulse oximetry, and electrocardiography (HR) were collected to analyze cerebral and superficial tissue oxygenation kinetics during G-loading and recovery. Results: The NIRSense Aerie successfully captured cerebral deoxygenation responses during high G-force exposure, demonstrating its potential for continuous monitoring in challenging operational environments. Pulse oximetry was compromised during G-loading, emphasizing the system's advantage in uninterrupted cerebrovascular monitoring. Significant changes in oxygenation metrics were observed across G-loading levels, with distinct responses in Deoxy-Hb and Oxy-Hb concentrations. HR increased during G-loading, reflecting physiological stress and the anti-G straining maneuver. Discussion: The NIRSense Aerie shows promise for real-time monitoring of aircrew physiological responses during high G-force exposure. Despite challenges, the system provides valuable insights into cerebral oxygenation kinetics. Future developments aim for miniaturization and optimization for enhanced aircrew comfort and wearability. This technology has potential for improving anti-G straining maneuver learning and retention through real-time cerebral oxygenation feedback during centrifuge training.
Language	English
Publishing date	2024-02-23
Publishing country	Switzerland
Document type	Journal Article
ISSN	2673-6195
ISSN (online)	2673-6195
DOI	10.3389/fnrgo.2024.1357905
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Article ; Online: Reply to G. Escalante and D. St. Mart.

Askow, Andrew T / Burd, Nicholas A

International journal of sport nutrition and exercise metabolism

2023 Volume 33, Issue 3, Page(s) 173

MeSH term(s)	Humans ; Cholecalciferol ; Vitamin D
Chemical Substances	Cholecalciferol (1C6V77QF41) ; Vitamin D (1406-16-2)
Language	English
Publishing date	2023-02-22
Publishing country	United States
Document type	Journal Article ; Comment
ZDB-ID	1101115-4
ISSN	1543-2742 ; 1050-1606 ; 1526-484X
ISSN (online)	1543-2742
ISSN	1050-1606 ; 1526-484X
DOI	10.1123/ijsnem.2023-0010
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Article ; Online: Role of G protein-coupled receptor kinases (GRKs) in β

Ham, Seungmin / Mukaida, Saori / Sato, Masaaki / Keov, Peter / Bengtsson, Tore / Furness, Sebastian / Holliday, Nicholas D / Evans, Bronwyn A / Summers, Roger J / Hutchinson, Dana S

Pharmacology research & perspectives

2024 Volume 12, Issue 1, Page(s) e1176

Abstract: Truncation of the C-terminal tail of the ... ...

Abstract	Truncation of the C-terminal tail of the β
MeSH term(s)	Rats ; Animals ; G-Protein-Coupled Receptor Kinases ; Isoproterenol/pharmacology ; Glucose/metabolism ; Receptors, G-Protein-Coupled ; Receptors, Adrenergic
Chemical Substances	G-Protein-Coupled Receptor Kinases (EC 2.7.11.16) ; Isoproterenol (L628TT009W) ; Glucose (IY9XDZ35W2) ; Receptors, G-Protein-Coupled ; Receptors, Adrenergic
Language	English
Publishing date	2024-02-09
Publishing country	United States
Document type	Journal Article
ZDB-ID	2740389-0
ISSN	2052-1707 ; 2052-1707
ISSN (online)	2052-1707
ISSN	2052-1707
DOI	10.1002/prp2.1176
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Article: Molecular basis of proton-sensing by G protein-coupled receptors.

Howard, Matthew K / Hoppe, Nicholas / Huang, Xi-Ping / Macdonald, Christian B / Mehrota, Eshan / Grimes, Patrick Rockefeller / Zahm, Adam / Trinidad, Donovan D / English, Justin / Coyote-Maestas, Willow / Manglik, Aashish

bioRxiv : the preprint server for biology

2024

Abstract: Three proton-sensing G protein-coupled receptors (GPCRs), GPR4, GPR65, and GPR68, respond ...

Abstract	Three proton-sensing G protein-coupled receptors (GPCRs), GPR4, GPR65, and GPR68, respond to changes in extracellular pH to regulate diverse physiology and are implicated in a wide range of diseases. A central challenge in determining how protons activate these receptors is identifying the set of residues that bind protons. Here, we determine structures of each receptor to understand the spatial arrangement of putative proton sensing residues in the active state. With a newly developed deep mutational scanning approach, we determined the functional importance of every residue in proton activation for GPR68 by generating ~9,500 mutants and measuring effects on signaling and surface expression. This unbiased screen revealed that, unlike other proton-sensitive cell surface channels and receptors, no single site is critical for proton recognition in GPR68. Instead, a network of titratable residues extend from the extracellular surface to the transmembrane region and converge on canonical class A GPCR activation motifs to activate proton-sensing GPCRs. More broadly, our approach integrating structure and unbiased functional interrogation defines a new framework for understanding the rich complexity of GPCR signaling.
Language	English
Publishing date	2024-04-18
Publishing country	United States
Document type	Preprint
DOI	10.1101/2024.04.17.590000
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Article ; Online: Exploring water, sanitation, and hygiene coverage targets for reaching and sustaining trachoma elimination: G-computation analysis.

Sullivan, Kristin M / Harding-Esch, Emma M / Keil, Alexander P / Freeman, Matthew C / Batcho, Wilfrid E / Bio Issifou, Amadou A / Bucumi, Victor / Bella, Assumpta L / Epee, Emilienne / Bobo Barkesa, Segni / Seife Gebretsadik, Fikre / Sanha, Salimato / Kalua, Khumbo M / Masika, Michael P / Minnih, Abdallahi O / Abdala, Mariamo / Massangaie, Marília E / Amza, Abdou / Kadri, Boubacar /

Nassirou, Beido / Mpyet, Caleb D / Olobio, Nicholas / Badiane, Mouctar D / Elshafie, Balgesa E / Baayenda, Gilbert / Kabona, George E / Kaitaba, Oscar / Simon, Alistidia / Al-Khateeb, Tawfik Q / Mwale, Consity / Bakhtiari, Ana / Westreich, Daniel / Solomon, Anthony W / Gower, Emily W

PLoS neglected tropical diseases

2023 Volume 17, Issue 2, Page(s) e0011103

Abstract: ... coverages are needed to effectively reduce transmission.: Methods/findings: We used g-computation ...

Abstract	Background: Trachoma is the leading infectious cause of blindness. To reduce transmission, water, sanitation, and hygiene (WaSH) improvements are promoted through a comprehensive public health strategy. Evidence supporting the role of WaSH in trachoma elimination is mixed and it remains unknown what WaSH coverages are needed to effectively reduce transmission. Methods/findings: We used g-computation to estimate the impact on the prevalence of trachomatous inflammation-follicular among children aged 1-9 years (TF1-9) when hypothetical WaSH interventions raised the minimum coverages from 5% to 100% for "nearby" face-washing water (<30 minutes roundtrip collection time) and adult latrine use in an evaluation unit (EU). For each scenario, we estimated the generalized prevalence difference as the TF1-9 prevalence under the intervention scenarios minus the observed prevalence. Data from 574 cross-sectional surveys conducted in 16 African and Eastern Mediterranean countries were included. Surveys were conducted from 2015-2019 with support from the Global Trachoma Mapping Project and Tropical Data. When modeling interventions among EUs that had not yet met the TF1-9 elimination target, increasing nearby face-washing water and latrine use coverages above 30% was generally associated with consistent decreases in TF1-9. For nearby face-washing water, we estimated a ≥25% decrease in TF1-9 at 65% coverage, with a plateau upon reaching 85% coverage. For latrine use, the estimated decrease in TF1-9 accelerated from 80% coverage upward, with a ≥25% decrease in TF1-9 by 85% coverage. Among EUs that had previously met the elimination target, results were inconclusive. Conclusions: Our results support Sustainable Development Goal 6 and provide insight into potential WaSH-related coverage targets for trachoma elimination. Targets can be tested in future trials to improve evidence-based WaSH guidance for trachoma.
MeSH term(s)	Child ; Adult ; Humans ; Infant ; Trachoma/epidemiology ; Trachoma/prevention & control ; Sanitation/methods ; Water ; Cross-Sectional Studies ; Hygiene ; Prevalence
Chemical Substances	Water (059QF0KO0R)
Language	English
Publishing date	2023-02-13
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2429704-5
ISSN	1935-2735 ; 1935-2735
ISSN (online)	1935-2735
ISSN	1935-2735
DOI	10.1371/journal.pntd.0011103
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Article ; Online: THE CONCISE GUIDE TO PHARMACOLOGY 2021/22: G protein-coupled receptors.

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 / Southan, Christopher / Davies, Jamie A / Abbracchio, Maria Pia / Alexander, Wayne / Al-Hosaini, Khaled / Bäck, Magnus / Barnes, Nicholas M / Bathgate, Ross /

Beaulieu, Jean-Martin / Bernstein, Kenneth E / Bettler, Bernhard / Birdsall, Nigel J M / Blaho, Victoria / Boulay, Francois / Bousquet, Corinne / Bräuner-Osborne, Hans / Burnstock, Geoffrey / Caló, Girolamo / Castaño, Justo P / Catt, Kevin J / Ceruti, Stefania / Chazot, Paul / Chiang, Nan / Chini, Bice / Chun, Jerold / Cianciulli, Antonia / Civelli, Olivier / Clapp, Lucie H / Couture, Réjean / Csaba, Zsolt / Dahlgren, Claes / Dent, Gordon / Singh, Khuraijam Dhanachandra / Douglas, Steven D / Dournaud, Pascal / Eguchi, Satoru / Escher, Emanuel / Filardo, Edward J / Fong, Tung / Fumagalli, Marta / Gainetdinov, Raul R / Gasparo, Marc de / Gerard, Craig / Gershengorn, Marvin / Gobeil, Fernand / Goodfriend, Theodore L / Goudet, Cyril / Gregory, Karen J / Gundlach, Andrew L / Hamann, Jörg / Hanson, Julien / Hauger, Richard L / Hay, Debbie L / Heinemann, Akos / Hollenberg, Morley D / Holliday, Nicholas D / Horiuchi, Mastgugu / Hoyer, Daniel / Hunyady, László / 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 / Kitazawa, Takio / Kozielewicz, Pawel / Kreienkamp, Hans-Jürgen / Kukkonen, Jyrki P / Langenhan, Tobias / Leach, Katie / Lecca, Davide / Lee, John D / Leeman, Susan E / Leprince, Jérôme / Li, Xaria X / Williams, Tom Lloyd / Lolait, Stephen J / Lupp, Amelie / Macrae, Robyn / Maguire, Janet / Mazella, Jean / McArdle, Craig A / Melmed, Shlomo / Michel, Martin C / Miller, Laurence J / Mitolo, Vincenzo / Mouillac, Bernard / Müller, Christa E / Murphy, Philip / Nahon, Jean-Louis / Ngo, Tony / Norel, Xavier / Nyimanu, Duuamene / O'Carroll, Anne-Marie / Offermanns, Stefan / Panaro, Maria Antonietta / Parmentier, Marc / Pertwee, Roger G / Pin, Jean-Philippe / Prossnitz, Eric R / Quinn, Mark / Ramachandran, Rithwik / Ray, Manisha / Reinscheid, Rainer K / Rondard, Philippe / Rovati, G Enrico / Ruzza, Chiara / Sanger, Gareth J / Schöneberg, Torsten / Schulte, Gunnar / Schulz, Stefan / Segaloff, Deborah L / Serhan, Charles N / Stoddart, Leigh A / Sugimoto, Yukihiko / Summers, Roger / Tan, Valerie P / Thal, David / Thomas, Walter Wally / Timmermans, Pieter B M W M / Tirupula, Kalyan / Tulipano, Giovanni / Unal, Hamiyet / Unger, Thomas / Valant, Celine / Vanderheyden, Patrick / Vaudry, David / Vaudry, Hubert / Vilardaga, Jean-Pierre / Walker, Christopher S / Wang, Ji Ming / Ward, Donald T / Wester, Hans-Jürgen / Willars, Gary B / Woodruff, Trent M / Yao, Chengcan / Ye, Richard D

British journal of pharmacology

2021 Volume 178 Suppl 1, Page(s) S27–S156

Abstract: ... The full contents of this section can be found at http://onlinelibrary.wiley.com/doi/bph.15538. G protein ...

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.
MeSH term(s)	Databases, Pharmaceutical ; Humans ; Ion Channels ; Ligands ; Pharmacology ; Receptors, Cytoplasmic and Nuclear ; Receptors, G-Protein-Coupled
Chemical Substances	Ion Channels ; Ligands ; Receptors, Cytoplasmic and Nuclear ; Receptors, G-Protein-Coupled
Language	English
Publishing date	2021-09-22
Publishing country	England
Document type	Journal Article
ZDB-ID	80081-8
ISSN	1476-5381 ; 0007-1188
ISSN (online)	1476-5381
ISSN	0007-1188
DOI	10.1111/bph.15538
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