M. Beinfeld, Quan Chen, Fan Gao, R. Liddle, L. Miller, J. Rehfeld
{"title":"Cholecystokinin receptors in GtoPdb v.2023.1","authors":"M. Beinfeld, Quan Chen, Fan Gao, R. Liddle, L. Miller, J. Rehfeld","doi":"10.2218/gtopdb/f15/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f15/2023.1","url":null,"abstract":"Cholecystokinin receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on CCK receptors [90]) are activated by the endogenous peptides cholecystokinin-8 (CCK-8), CCK-33, CCK-58 and gastrin (gastrin-17). There are only two distinct subtypes of CCK receptors, CCK1 and CCK2 receptors [64, 124], with some alternatively spliced forms most often identified in neoplastic cells. The CCK receptor subtypes are distinguished by their peptide selectivity, with the CCK1 receptor requiring the carboxyl-terminal heptapeptide-amide that includes a sulfated tyrosine for high affinity and potency, while the CCK2 receptor requires only the carboxyl-terminal tetrapeptide shared by each CCK and gastrin peptides. These receptors have characteristic and distinct distributions, with both present in both the central nervous system and peripheral tissues.","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"8 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88750158","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
D. Bikle, H. Bräuner‐Osborne, E. Brown, Wenhan Chang, A. Conigrave, F. Hannan, K. Leach, D. Riccardi, D. Shoback, D. Ward, P. Yarova
{"title":"Calcium-sensing receptor in GtoPdb v.2023.1","authors":"D. Bikle, H. Bräuner‐Osborne, E. Brown, Wenhan Chang, A. Conigrave, F. Hannan, K. Leach, D. Riccardi, D. Shoback, D. Ward, P. Yarova","doi":"10.2218/gtopdb/f12/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f12/2023.1","url":null,"abstract":"The calcium-sensing receptor (CaS, provisional nomenclature as recommended by NC-IUPHAR [47] and subsequently updated [77]) responds to multiple endogenous ligands, including extracellular calcium and other divalent/trivalent cations, polyamines and polycationic peptides, L-amino acids (particularly L-Trp and L-Phe), glutathione and various peptide analogues, ionic strength and extracellular pH (reviewed in [78]). While divalent/trivalent cations, polyamines and polycations are CaS receptor agonists [14, 110], L-amino acids, glutamyl peptides, ionic strength and pH are allosteric modulators of agonist function [36, 47, 61, 108, 109]. Indeed, L-amino acids have been identified as \"co-agonists\", with both concomitant calcium and L-amino acid binding required for full receptor activation [149, 54]. The sensitivity of the CaS receptor to primary agonists is increased by elevated extracellular pH [18] or decreased extracellular ionic strength [109] while sensitivity is decreased by pathophysiological phosphate concentrations [20]. This receptor bears no sequence or structural relation to the plant calcium receptor, also called CaS.","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"28 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84897802","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"ABCD subfamily of peroxisomal ABC transporters in GtoPdb v.2023.1","authors":"S. Kemp","doi":"10.2218/gtopdb/f154/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f154/2023.1","url":null,"abstract":"Peroxisomes are indispensable organelles in higher eukaryotes. They are essential for the oxidation of a wide variety of metabolites, which include: saturated, monounsaturated and polyunsaturated fatty acids, branched-chain fatty acids, bile acids and dicarboxylic acids [5]. However, the peroxisomal membrane forms an impermeable barrier to these metabolites. The mammalian peroxisomal membrane harbours three ATP-binding cassette (ABC) half-transporters, named ABCD1, -2 and -3. The ABCD transporters predominantly act as homodimers to transport different acyl-CoAs.","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"35 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85078711","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
T. Billiar, G. Cirino, David Fulton, R. Motterlini, A. Papapetropoulos, Csaba Szabo
{"title":"Hydrogen sulphide synthesis in GtoPdb v.2023.1","authors":"T. Billiar, G. Cirino, David Fulton, R. Motterlini, A. Papapetropoulos, Csaba Szabo","doi":"10.2218/gtopdb/f279/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f279/2023.1","url":null,"abstract":"Hydrogen sulfide is a gasotransmitter, with similarities to nitric oxide and carbon monoxide. Although the enzymes indicated below have multiple enzymatic activities, the focus here is the generation of hydrogen sulphide (H2S) and the enzymatic characteristics are described accordingly. Cystathionine β-synthase (CBS) and cystathionine γ-lyase (CSE) are pyridoxal phosphate (PLP)-dependent enzymes. 3-mercaptopyruvate sulfurtransferase (3-MPST) functions to generate H2S; only CAT is PLP-dependent, while 3-MPST is not. Thus, this third pathway is sometimes referred to as PLP-independent. CBS and CSE are predominantly cytosolic enzymes, while 3-MPST is found both in the cytosol and the mitochondria. For an authoritative review on the pharmacological modulation of H2S levels, see Szabo and Papapetropoulos, 2017 [8].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"150 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"76456104","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
D. Bichet, Michel Bouvier, B. Chini, G. Gimpl, G. Guillon, Tadashi Kimura, M. Knepper, S. Lolait, M. Manning, B. Mouillac, A. O'Carroll, C. Serradeil‐Le Gal, M. Soloff, J. Verbalis, M. Wheatley, H. Zingg
{"title":"Vasopressin and oxytocin receptors in GtoPdb v.2023.1","authors":"D. Bichet, Michel Bouvier, B. Chini, G. Gimpl, G. Guillon, Tadashi Kimura, M. Knepper, S. Lolait, M. Manning, B. Mouillac, A. O'Carroll, C. Serradeil‐Le Gal, M. Soloff, J. Verbalis, M. Wheatley, H. Zingg","doi":"10.2218/gtopdb/f66/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f66/2023.1","url":null,"abstract":"Vasopressin (AVP) and oxytocin (OT) receptors (nomenclature as recommended by NC-IUPHAR [94]) are activated by the endogenous cyclic nonapeptides vasopressin and oxytocin. These peptides are derived from precursors which also produce neurophysins (neurophysin I for oxytocin; neurophysin II for vasopressin). Vasopressin and oxytocin differ at only 2 amino acids (positions 3 and 8). There are metabolites of these neuropeptides that may be biologically active [69].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"24 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79517132","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
{"title":"P1B P-type ATPases: Cu+-ATPases in GtoPdb v.2023.1","authors":"S. Lutsenko","doi":"10.2218/gtopdb/f161/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f161/2023.1","url":null,"abstract":"Copper-transporting ATPases convey copper ions across cell-surface and intracellular membranes. They consist of eight TM domains and associate with multiple copper chaperone proteins (e.g. ATOX1, O00244).","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"315 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"77572448","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Stephen P.H. Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner, Anthony P. Davenport, Khuraijam Dhanachandra Singh, Satoru Eguchi, Anthony Harmar, Nick Holliday, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Wen Chiy Liew, Amy E. Monaghan, Chido Mpamhanga, Richard Neubig, Adam J Pawson, Jean-Philippe Pin, Joanna L. Sharman, Michael Spedding, Eliot Spindel, Leigh Stoddart, Laura Storjohann, Walter G. Thomas, Kalyan Tirupula, Patrick Vanderheyden
{"title":"Class A Orphans in GtoPdb v.2023.1","authors":"Stephen P.H. Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner, Anthony P. Davenport, Khuraijam Dhanachandra Singh, Satoru Eguchi, Anthony Harmar, Nick Holliday, Robert T. Jensen, Sadashiva Karnik, Evi Kostenis, Wen Chiy Liew, Amy E. Monaghan, Chido Mpamhanga, Richard Neubig, Adam J Pawson, Jean-Philippe Pin, Joanna L. Sharman, Michael Spedding, Eliot Spindel, Leigh Stoddart, Laura Storjohann, Walter G. Thomas, Kalyan Tirupula, Patrick Vanderheyden","doi":"10.2218/gtopdb/f16/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f16/2023.1","url":null,"abstract":"Table 1 lists a number of putative GPCRs identified by NC-IUPHAR [161], for which preliminary evidence for an endogenous ligand has been published, or for which there exists a potential link to a disease, or disorder. These GPCRs have recently been reviewed in detail [121]. The GPCRs in Table 1 are all Class A, rhodopsin-like GPCRs. Class A orphan GPCRs not listed in Table 1 are putative GPCRs with as-yet unidentified endogenous ligands.Table 1: Class A orphan GPCRs with putative endogenous ligands GPR3GPR4GPR6GPR12GPR15GPR17GPR20 GPR22GPR26GPR31GPR34GPR35GPR37GPR39 GPR50GPR63GPR65GPR68GPR75GPR84GPR87 GPR88GPR132GPR149GPR161GPR183LGR4LGR5 LGR6MAS1MRGPRDMRGPRX1MRGPRX2P2RY10TAAR2 In addition the orphan receptors GPR18, GPR55 and GPR119 which are reported to respond to endogenous agents analogous to the endogenous cannabinoid ligands have been grouped together (GPR18, GPR55 and GPR119).","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"155 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135017137","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Demet Arac-Ozkan, Gabriela Aust, Tom I. Bonner, Heike Cappallo-Obermann, Caroline Formstone, Jörg Hamann, Breanne Harty, Henrike Heyne, Christiane Kirchhoff, Barbara Knapp, Arunkumar Krishnan, Tobias Langenhan, Diana Le Duc, Hsi-Hsien Lin, David C. Martinelli, Kelly Monk, Xianhua Piao, Simone Prömel, Torsten Schöneberg, Helgi Schiöth, Kathleen Singer, Martin Stacey, Yuri Ushkaryov, Uwe Wolfrum, Lei Xu
{"title":"Adhesion Class GPCRs in GtoPdb v.2023.1","authors":"Demet Arac-Ozkan, Gabriela Aust, Tom I. Bonner, Heike Cappallo-Obermann, Caroline Formstone, Jörg Hamann, Breanne Harty, Henrike Heyne, Christiane Kirchhoff, Barbara Knapp, Arunkumar Krishnan, Tobias Langenhan, Diana Le Duc, Hsi-Hsien Lin, David C. Martinelli, Kelly Monk, Xianhua Piao, Simone Prömel, Torsten Schöneberg, Helgi Schiöth, Kathleen Singer, Martin Stacey, Yuri Ushkaryov, Uwe Wolfrum, Lei Xu","doi":"10.2218/gtopdb/f17/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f17/2023.1","url":null,"abstract":"Adhesion GPCRs are structurally identified on the basis of a large extracellular region, similar to the Class B GPCR, but which is linked to the 7TM region by a GPCR autoproteolysis-inducing (GAIN) domain [10] containing a GPCR proteolysis site (GPS). The N-terminal extracellular region often shares structural homology with adhesive domains (e.g. cadherins, immunolobulin, lectins) facilitating inter- and matricellular interactions and leading to the term adhesion GPCR [104, 418]. Several receptors have been suggested to function as mechanosensors [320, 288, 396, 38]. Cryo-EM structures of the 7-transmembrane domain of several adhesion GPCRs have been determined recently [292, 21, 403, 212, 300, 302, 431, 293]. The nomenclature of these receptors was revised in 2015 as recommended by NC-IUPHAR and the Adhesion GPCR Consortium [125].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"74 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135017415","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Paul Chazot, Marlon Cowart, Hiroyuki Fukui, C. Robin Ganellin, Ralf Gutzmer, Helmut L. Haas, Stephen J. Hill, Rebecca Hills, Rob Leurs, Roberto Levi, Steve Liu, Pertti Panula, Walter Schunack, Jean-Charles Schwartz, Roland Seifert, Nigel P. Shankley, Holger Stark, Robin Thurmond, Henk Timmerman, J. Michael Young
{"title":"Histamine receptors in GtoPdb v.2023.1","authors":"Paul Chazot, Marlon Cowart, Hiroyuki Fukui, C. Robin Ganellin, Ralf Gutzmer, Helmut L. Haas, Stephen J. Hill, Rebecca Hills, Rob Leurs, Roberto Levi, Steve Liu, Pertti Panula, Walter Schunack, Jean-Charles Schwartz, Roland Seifert, Nigel P. Shankley, Holger Stark, Robin Thurmond, Henk Timmerman, J. Michael Young","doi":"10.2218/gtopdb/f33/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f33/2023.1","url":null,"abstract":"Histamine receptors (nomenclature as agreed by the NC-IUPHAR Subcommittee on Histamine Receptors [80, 174]) are activated by the endogenous ligand histamine. Marked species differences exist between histamine receptor orthologues [80]. The human and rat H3 receptor genes are subject to significant splice variance [12]. The potency order of histamine at histamine receptor subtypes is H3 = H4 > H2 > H1 [174]. Some agonists at the human H3 receptor display significant ligand bias [183]. Antagonists of all 4 histamine receptors have clinical uses: H1 antagonists for allergies (e.g. cetirizine), H2 antagonists for acid-reflux diseases (e.g. ranitidine), H3 antagonists for narcolepsy (e.g. pitolisant/WAKIX; Registered) and H4 antagonists for atopic dermatitis (e.g. adriforant; Phase IIa) [174] and vestibular neuritis (AUV) (SENS-111 (Seliforant, previously UR-63325), entered and completed vestibular neuritis (AUV) Phase IIa efficacy and safety trials, respectively) [217, 8].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"74 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135017421","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Anthony P. Davenport, Julien Hanson, Wen Chiy Liew
{"title":"Succinate receptor in GtoPdb v.2023.1","authors":"Anthony P. Davenport, Julien Hanson, Wen Chiy Liew","doi":"10.2218/gtopdb/f446/2023.1","DOIUrl":"https://doi.org/10.2218/gtopdb/f446/2023.1","url":null,"abstract":"Nomenclature as recommended by NC-IUPHAR [8]. The succinate receptor (GPR91, SUCNR1) is activated by the tricarboxylic acid (or Krebs) cycle intermediate succinate and other dicarboxylic acids with less clear physiological relevance such as maleate [17]. Since its pairing with its endogenous ligand in 2004, intense research has focused on the receptor-ligand pair role in various (patho)physiological processes such as regulation of renin production [17, 39], ischemia injury [17], fibrosis [25], retinal angiogenesis [34], inflammation [25, 23], immune response [32], obesity [44, 26, 21], diabetes [42, 22, 39], platelet aggregation [38, 36] or cancer [28, 46]. The succinate receptor is coupled to Gi/o [11, 17] and Gq/11 protein families [31, 17, 40]. Although the receptor is, upon ligand addition, rapidly desensitized [19, 31], and in some cells internalized [17], it seems to recruit arrestins weakly [10]. The cellular activation of the succinate receptor triggers various signalling pathways such as decrease of cAMP levels, [Ca2+]i mobilization and activation of kinases (ERK, c-Jun, Akt, Src, p38, PI3Kβ, etc.) [12]. The receptor is broadly expressed but is notably abundant in immune cells (M2 macrophages [40, 21], monocytes [32], immature dendritic cells [32], adipocytes [44], platelets [38, 36], etc.) and in the kidney [17].","PeriodicalId":14617,"journal":{"name":"IUPHAR/BPS Guide to Pharmacology CITE","volume":"80 1","pages":"0"},"PeriodicalIF":0.0,"publicationDate":"2023-04-26","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135018173","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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