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2. Bitter taste receptors

Author

Wooding, Stephen P, Ramirez, Vicente A, and Behrens, Maik

Subjects
Public Health, Evolutionary Biology, Health Sciences, Biological Sciences, Behavioral and Social Science, Neurosciences, Nutrition, Dental/Oral and Craniofacial Disease, Oral and gastrointestinal, Good Health and Well Being, bitter, molecular evolution, senses, taste, genetics, diet, Evolutionary biology, Public health
Abstract

Bitter taste perception plays vital roles in animal behavior and fitness. By signaling the presence of toxins in foods, particularly noxious defense compounds found in plants, it enables animals to avoid exposure. In vertebrates, bitter perception is initiated by TAS2Rs, a family of G protein-coupled receptors expressed on the surface of taste buds. There, oriented toward the interior of the mouth, they monitor the contents of foods, drinks and other substances as they are ingested. When bitter compounds are encountered, TAS2Rs respond by triggering neural pathways leading to sensation. The importance of this role placed TAS2Rs under selective pressures in the course of their evolution, leaving signatures in patterns of gene gain and loss, sequence polymorphism, and population structure consistent with vertebrates' diverse feeding ecologies. The protective value of bitter taste is reduced in modern humans because contemporary food supplies are safe and abundant. However, this is not always the case. Some crops, particularly in the developing world, retain surprisingly high toxicity and bitterness remains an important measure of safety. Bitter perception also shapes health through its influence on preference driven behaviors such as diet choice, alcohol intake and tobacco use. Further, allelic variation in TAS2Rs is extensive, leading to individual differences in taste sensitivity that drive these behaviors, shaping susceptibility to disease. Thus, bitter taste perception occupies a critical intersection between ancient evolutionary processes and modern human health.

Published
2021

3. Pharmacology of TAS1R2/TAS1R3 Receptors and Sweet Taste

Author

Behrens, Maik, Barrett, James E., Editor-in-Chief, Flockerzi, Veit, Editorial Board Member, Frohman, Michael A., Editorial Board Member, Geppetti, Pierangelo, Editorial Board Member, Hofmann, Franz B., Editorial Board Member, Kuner, Rohini, Editorial Board Member, Michel, Martin C., Editorial Board Member, Page, Clive P., Editorial Board Member, Wang, KeWei, Editorial Board Member, Palmer, R. Kyle, editor, and Servant, Guy, editor

Published
2022
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8. Differential Activation of TAS2R4 May Recover Ability to Taste Propylthiouracil for Some TAS2R38 AVI Homozygotes.

Author

Nolden, Alissa A., Behrens, Maik, McGeary, John E., Meyerhof, Wolfgang, and Hayes, John E.

Abstract

Bitterness from phenylthiocarbamide and 6-n-propylthiouracil (PROP) varies with polymorphisms in the TAS2R38 gene. Three SNPs form two common (AVI, PAV) and four rare haplotypes (AAI, AAV, PVI, and PAI). AVI homozygotes exhibit higher detection thresholds and lower suprathreshold bitterness for PROP compared to PAV homozygotes and heterozygotes, and these differences may influence alcohol and vegetable intake. Within a diplotype, substantial variation in suprathreshold bitterness persists, and some AVI homozygotes report moderate bitterness at high concentrations. A second receptor encoded by a gene containing a functional polymorphism may explain this. Early work has suggested that PROP might activate TAS2R4 in vitro, but later work did not replicate this. Here, we identify three TAS2R4 SNPs that result in three diplotypes—SLN/SLN, FVS/SLN, and FVS/FVS—which make up 25.1%, 44.9%, and 23.9% of our sample. These TAS2R4 haplotypes show minimal linkage disequilibrium with TAS2R38, so we examined the suprathreshold bitterness as a function of both. The participants (n = 243) rated five PROP concentrations in duplicate, interleaved with other stimuli. As expected, the TAS2R38 haplotypes explained ~29% (p < 0.0001) of the variation in the bitterness ratings, with substantial variation within the haplotypes (AVI/AVI, PAV/AVI, and PAV/PAV). Notably, the TAS2R4 diplotypes (independent of the TAS2R38 haplotypes) explained ~7–8% of the variation in the bitterness ratings (p = 0.0001). Given this, we revisited if PROP could activate heterologously expressed TAS2R4 in HEK293T cells, and calcium imaging indicated 3 mM PROP is a weak TAS2R4 agonist. In sum, our data are consistent with the second receptor hypothesis and may explain the recovery of the PROP tasting phenotype in some AVI homozygotes; further, this finding may potentially help explain the conflicting results on the TAS2R38 diplotype and food intake. [ABSTRACT FROM AUTHOR]

Published
2024
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9. Copy Number Variation in TAS2R Bitter Taste Receptor Genes: Structure, Origin, and Population Genetics.

Author

Roudnitzky, Natacha, Risso, Davide, Drayna, Dennis, Behrens, Maik, Meyerhof, Wolfgang, and Wooding, Stephen P

Subjects
Biological Sciences, Ecology, Genetics, Biotechnology, Nutrition, Human Genome, Alleles, Amino Acid Sequence, DNA Copy Number Variations, Genetics, Population, Humans, Receptors, G-Protein-Coupled, Sequence Alignment, Taste, Taste Perception, bitter, evolution, genetic, genomic, natural selection, taste receptor, Neurology & Neurosurgery, Biological sciences
Abstract

Bitter taste receptor genes (TAS2Rs) harbor extensive diversity, which is broadly distributed across human populations and strongly associated with taste response phenotypes. The majority of TAS2R variation is composed of single-nucleotide polymorphisms. However, 2 closely positioned loci at 12p13, TAS2R43 and -45, harbor high-frequency deletion (Δ) alleles in which genomic segments are absent, resulting in copy number variation (CNV). To resolve their chromosomal structure and organization, we generated maps using long-range contig alignments and local sequencing across the TAS2R43-45 region. These revealed that the deletion alleles (43Δ and 45Δ) are 37.8 and 32.2kb in length, respectively and span the complete coding region of each gene (~1kb) along with extensive up- and downstream flanking sequence, producing separate CNVs at the 2 loci. Comparisons with a chimpanzee genome, which contained intact homologs of TAS2R43, -45, and nearby TAS2Rs, indicated that the deletions evolved recently, through unequal recombination in a cluster of closely related loci. Population genetic analyses in 946 subjects from 52 worldwide populations revealed that copy number ranged from 0 to 2 at both TAS2R43 and TAS2R45, with 43Δ and 45Δ occurring at high global frequencies (0.33 and 0.18). Estimated recombination rates between the loci were low (ρ = 2.7×10(-4); r = 6.6×10(-9)) and linkage disequilibrium was high (D' = 1.0), consistent with their adjacent genomic positioning and recent origin. Geographic variation pointed to an African origin for the deletions. However, no signatures of natural selection were found in population structure or integrated haplotype scores spanning the region, suggesting that patterns of diversity at TAS2R43 and -45 are primarily due to genetic drift.

Published
2016

11. Sweet taste of heavy water

Author

Ben Abu, Natalie, Mason, Philip E., Klein, Hadar, Dubovski, Nitzan, Ben Shoshan-Galeczki, Yaron, Malach, Einav, Pražienková, Veronika, Maletínská, Lenka, Tempra, Carmelo, Chamorro, Victor Cruces, Cvačka, Josef, Behrens, Maik, Niv, Masha Y., and Jungwirth, Pavel

Published
2021
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13. Receptor Polymorphism and Genomic Structure Interact to Shape Bitter Taste Perception.

Author

Roudnitzky, Natacha, Behrens, Maik, Engel, Anika, Kohl, Susann, Thalmann, Sophie, Hübner, Sandra, Lossow, Kristina, Wooding, Stephen P, and Meyerhof, Wolfgang

Subjects
Taste Buds, Animals, Humans, Iridoids, Sesquiterpenes, Sesquiterpenes, Guaiane, Quassins, Phenylthiourea, Quinine, Receptors, G-Protein-Coupled, Genotype, Haplotypes, Polymorphism, Single Nucleotide, Alleles, European Continental Ancestry Group, Taste Perception, Genetic Association Studies, Developmental Biology, Genetics
Abstract

The ability to taste bitterness evolved to safeguard most animals, including humans, against potentially toxic substances, thereby leading to food rejection. Nonetheless, bitter perception is subject to individual variations due to the presence of genetic functional polymorphisms in bitter taste receptor (TAS2R) genes, such as the long-known association between genetic polymorphisms in TAS2R38 and bitter taste perception of phenylthiocarbamide. Yet, due to overlaps in specificities across receptors, such associations with a single TAS2R locus are uncommon. Therefore, to investigate more complex associations, we examined taste responses to six structurally diverse compounds (absinthin, amarogentin, cascarillin, grosheimin, quassin, and quinine) in a sample of the Caucasian population. By sequencing all bitter receptor loci, inferring long-range haplotypes, mapping their effects on phenotype variation, and characterizing functionally causal allelic variants, we deciphered at the molecular level how a subjects' genotype for the whole-family of TAS2R genes shapes variation in bitter taste perception. Within each haplotype block implicated in phenotypic variation, we provided evidence for at least one locus harboring functional polymorphic alleles, e.g. one locus for sensitivity to amarogentin, one of the most bitter natural compounds known, and two loci for sensitivity to grosheimin, one of the bitter compounds of artichoke. Our analyses revealed also, besides simple associations, complex associations of bitterness sensitivity across TAS2R loci. Indeed, even if several putative loci harbored both high- and low-sensitivity alleles, phenotypic variation depended on linkage between these alleles. When sensitive alleles for bitter compounds were maintained in the same linkage phase, genetically driven perceptual differences were obvious, e.g. for grosheimin. On the contrary, when sensitive alleles were in opposite phase, only weak genotype-phenotype associations were seen, e.g. for absinthin, the bitter principle of the beverage absinth. These findings illustrate the extent to which genetic influences on taste are complex, yet arise from both receptor activation patterns and linkage structure among receptor genes.

Published
2015

16. The Growing Complexity of Human Bitter Taste Perception

Author

Behrens, Maik

Abstract

Human bitter perception is important for the identification of potentially harmful substances in food. For quite some years, research focused on the identification of activators for ∼25 human bitter taste receptors. The discovery of antagonists as well as increasing knowledge about agonists of different efficacies has substantially added to the intricacy of bitter taste perception. This article seeks to raise awareness for an underestimated new level of complexity when compound mixtures or even whole food items are assessed for their bitter taste.

Published
2024
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19. Taste Receptor Gene Expression Outside the Gustatory System

Author

Behrens, Maik, Prandi, Simone, Meyerhof, Wolfgang, Bernstein, Peter R., Series editor, Buschauer, Armin, Series editor, Georg, Gunda I., Series editor, Lowe, John A., Series editor, Meanwell, Nicholas A., Series editor, Saxena, Anil Kumar, Series editor, Stilz, Ulrich, Series editor, Supuran, Claudiu T., Series editor, Zhang, Ao, Series editor, and Krautwurst, Dietmar, editor

Published
2017
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27. The Concise Guide to PHARMACOLOGY 2023/24 : G protein-coupled receptors

Author

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, Baeck, 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, Braeuner-Osborne, Hans, Burnstock, Geoffrey, Calo, Girolamo, Castano, Justo P., Catt, Kevin J., Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chini, Bice, Chun, Jerold, Cianciulli, Antonia, Civelli, Olivier, Clapp, Lucie H., Couture, Rejean, 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, Graetz, Lukas, Gregory, Karen J., Gundlach, Andrew L., Hamann, Joerg, Hanson, Julien, Hauger, Richard L., Hay, Debbie L., Heinemann, Akos, Herr, Deron, 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, Kitazawa, Takio, Kozielewicz, Pawel, Kreienkamp, Hans-Juergen, Kukkonen, Jyrki P., Langenhan, Tobias, Larhammar, Dan, Leach, Katie, Lecca, Davide, Lee, John D., Leeman, Susan E., Leprince, Jerome, 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, Mueller, 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., Schoeneberg, 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-Juergen, Willars, Gary B., Williams, Tom Lloyd, Woodruff, Trent M., Yao, Chengcan, Ye, Richard D., 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, Baeck, 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, Braeuner-Osborne, Hans, Burnstock, Geoffrey, Calo, Girolamo, Castano, Justo P., Catt, Kevin J., Ceruti, Stefania, Chazot, Paul, Chiang, Nan, Chini, Bice, Chun, Jerold, Cianciulli, Antonia, Civelli, Olivier, Clapp, Lucie H., Couture, Rejean, 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, Graetz, Lukas, Gregory, Karen J., Gundlach, Andrew L., Hamann, Joerg, Hanson, Julien, Hauger, Richard L., Hay, Debbie L., Heinemann, Akos, Herr, Deron, 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, Kitazawa, Takio, Kozielewicz, Pawel, Kreienkamp, Hans-Juergen, Kukkonen, Jyrki P., Langenhan, Tobias, Larhammar, Dan, Leach, Katie, Lecca, Davide, Lee, John D., Leeman, Susan E., Leprince, Jerome, 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, Mueller, 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., Schoeneberg, 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-Juergen, Willars, Gary B., Williams, Tom Lloyd, Woodruff, Trent M., Yao, Chengcan, and Ye, Richard D.

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 (), 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 . 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.

Published
2023
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28. Rebaudioside A from Stevia rebaudiana stimulates GLP-1 release by enteroendocrine cells via bitter taste signalling pathways

Author

Noya-Leal, Francisca, van der Wielen, Nikkie, Behrens, Maik, Rouschop, Sven, van Arkel, Jeroen, Jongsma, Maarten, Witkamp, Renger, Mes, Jurriaan J., Bastiaan-Net, Shanna, Meijerink, Jocelijn, Noya-Leal, Francisca, van der Wielen, Nikkie, Behrens, Maik, Rouschop, Sven, van Arkel, Jeroen, Jongsma, Maarten, Witkamp, Renger, Mes, Jurriaan J., Bastiaan-Net, Shanna, and Meijerink, Jocelijn

Abstract

Glucagon-like peptide 1 (GLP-1) is a multifaceted intestinal hormone with diverse physiological functions throughout the body. Previously, we demonstrated that the steviol glycoside rebaudioside A (rebA) from Stevia rebaudiana stimulates the release of GLP-1 from mouse intestinal organoids and pig intestinal segments. To further unravel the underlying mechanisms, we examined the involvement of sweet- and bitter taste receptors and their associated signal transduction pathways. Experiments with mouse and human intestinal enteroendocrine cell lines (STC-1 and HuTu-80, respectively) confirmed that rebA stimulates GLP-1 release in a concentration-dependent manner. Experiments with selective inhibitors of sweet signalling in both the murine as well as the human enteroendocrine cells showed that the GLP-1-induced release by rebA occurs independently of the sweet taste receptor. Functional screening of 34 murine bitter taste receptors (Tas2rs) revealed an activation response with Tas2r108, Tas2r123 and Tas2r134. Moreover, we found evidence in human HuTu-80 cells, that TAS2R4 and TRPM5 are involved in rebA-induced GLP-1 secretion, suggesting a role for bitter taste signaling in gut hormone release. Interestingly, the rebA-dependent GLP-1 release may be modulated by GABA and 6-methoxyflavanone present in the diet. Together, our findings warrant further characterization of the specific metabolic effects of rebA among the non-caloric sweeteners.

Published
2023

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

Author

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, 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, and Ye, Richard D

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.

Published
2023

40. Physiological activation of human and mouse bitter taste receptors by bile acids.

Author

Ziegler, Florian, Steuer, Alexandra, Di Pizio, Antonella, and Behrens, Maik

Abstract

Beside the oral cavity, bitter taste receptors are expressed in several non-gustatory tissues. Whether extra-oral bitter taste receptors function as sensors for endogenous agonists is unknown. To address this question, we devised functional experiments combined with molecular modeling approaches to investigate human and mouse receptors using a variety of bile acids as candidate agonists. We show that five human and six mouse receptors are responsive to an array of bile acids. Moreover, their activation threshold concentrations match published data of bile acid concentrations in human body fluids, suggesting a putative physiological activation of non-gustatory bitter receptors. We conclude that these receptors could serve as sensors for endogenous bile acid levels. These results also indicate that bitter receptor evolution may not be driven solely by foodstuff or xenobiotic stimuli, but also depend on endogenous ligands. The determined bitter receptor activation profiles of bile acids now enable detailed physiological model studies. Using a combined experimental-computational approach, the activation profiles of human and mouse bitter taste receptors, TAS2Rs and Tas2rs, by bile acids is described, suggesting a physiological role of bile acids for taste receptors in non-gustatory tissues. [ABSTRACT FROM AUTHOR]

Published
2023
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44. Contributors

Author

Ache, Barry W., primary, Amrein, Hubert, additional, Aoki, Mari, additional, Behrens, Maik, additional, Boehm, Ulrich, additional, Chamero, Pablo, additional, Corey, Elizabeth A., additional, Damak, Sami, additional, Ferguson, Christopher H., additional, Hansson, Bill, additional, Ihara, Sayoko, additional, Kinnamon, Sue C., additional, Korsching, Sigrun, additional, Kuo, Tsung-Han, additional, Leinders-Zufall, Trese, additional, Li, Qian, additional, Liberles, Stephen D., additional, Martens, Jeffrey R., additional, McIntyre, Jeremy C., additional, Meyerhof, Wolfgang, additional, Munger, Steven D., additional, Niimura, Yoshihito, additional, Ninomiya, Yuzo, additional, Pask, Gregory M., additional, Prabhakar, Nanduri R., additional, Ray, Anandasankar, additional, Rodriguez, Ivan, additional, Shigemura, Noriatsu, additional, Slack, Jay P., additional, Spehr, Marc, additional, Stowers, Lisa, additional, Takai, Shingo, additional, Touhara, Kazushige, additional, Wen, Shuping, additional, Wicher, Dieter, additional, Yoshida, Ryusuke, additional, and Zhao, Haiqing, additional

Published
2016
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47. Additional file 7 of BitterMatch: recommendation systems for matching molecules with bitter taste receptors

Author

Margulis, Eitan, Slavutsky, Yuli, Lang, Tatjana, Behrens, Maik, Benjamini, Yuval, and Niv, Masha Y.

Abstract

Additional file 7: Table S1. Substances used for experimental testing of prospective predictions and their maximal employed concentrations. Table S2. XGBoost hyper-parameters. To avoid overfitting 1000 trees were used accordingly the following hyper-parameters were adjusted. The rest of the parameters were set to their default values. Table S3. Prospective prediction results per ligand. 1–represents an activation of the receptor that was confirmed experimentally and blank space means no activation was detected. *-positive activation that was detected in another publication but not in our in-vitro experiment. green–TP, red-FN, blue-FP and white-TN

Published
2022
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