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1
E x p r e s s i o n a n d f u n c t i o n
T o g g l e E x p r e s s i o n a n d f u n c t i o n s u b s e c t i o n
1 . 1
E x t r a - o r a l r o l e s o f T A S 2 R s
1 . 2
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2
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T A S 2 R 1
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F r o m W i k i p e d i a , t h e f r e e e n c y c l o p e d i a
Member of the 25 known human bitter taste receptors
Taste receptor type 2 member 1 (TAS2R1/T2R1) is a protein that in humans is encoded by the TAS2R1 gene .[5] [6] [7] It belongs to the G protein-coupled receptor (GPCR) family and is related to class A -like GPCRs, they contain 7 transmembrane helix bundles and short N-terminus loop.[8] Furthermore, TAS2R1 is member of the 25 known human bitter taste receptors, which enable the perception of bitter taste in the mouth cavity. Increasing evidence indicates a functional role of TAS2Rs in extra-oral tissues.[9]
Expression and function [ edit ]
Bitter taste receptors are expressed in taste receptor cells , which organized into taste buds on the papillae of the tongue and palate epithelium.
In addition, TAS2Rs were found to be expressed in extra-oral tissues, e.g. brain, lungs, gastrointestinal tract, etc.[9] So far, less is known about their function however, for example it was shown that:
TAS2Rs mediate relaxation of airway smooth muscles.[10]
TAS2R43 is involved in secretion of gastric acid in the stomach.[11]
TAS2R1, TAS2R4, TAS2R10, TAS2R38 and TAS2R49 were found to be down-regulated in breast cancer cells[12] .
TAS2R1, causes vasoconstrictor responses in the pulmonary circuit and relaxation in the airways[13] .
Structure of TAS2R1 receptor [ edit ]
Based on a recent homology model from BitterDB [14] [15] several conserved motifs , which are counterparts to Class A GPCRs[8] were found:
Transmembrane helix 1: N1.50 xxI1.53
Transmembrane helix 2: L2.46 xxxR2.50
Transmembrane helix 3: F3.49 Y 3.50 xxK3.53
Transmembrane helix 5: P5.50
Transmembrane helix 6: F6.44 xxxY6.46
Transmembrane helix 7: H7.49 S 7.50 xxL7.53
Numbering is according to the Balleros-Weinstein [16] system.
Unlike in Class A GPCRs, in transmembrane helix 4 no DRY[17] motif was found as well as position 6.50 is not conserved.
TAS2R1 gene[ edit ]
This gene encodes a member of a family of candidate taste receptors that are members of the G protein-coupled receptor superfamily and that are specifically expressed by taste receptor cells of the tongue and palate epithelia. This intronless taste receptor gene encodes a 7-transmembrane receptor protein, functioning as a bitter taste receptor.
In T2R1 two SNPs are known in R111H and R206W (dbSNP ).
Transcription factors [ edit ]
So far, AML1a, AP-1, AREB6, FOXL1, IRF-7A, Lmo2, NF-E2, NF-E2 p45 were found as the top transcription factor binding sites by QIAGEN in the TAS2R1 gene promoter .
Several mutations have been shown to influence binding of a ligand to TAS2R1 (based on BitterDB ):
Receptor region
BW number
Residue
Reference
TM1
1.5
N24
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM1
1.53
I27
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM2
2.5
R55
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM2
2.56
F61
doi: 10.1074/jbc.M111.246983
TM2
2.61
N66
doi: 10.3389/fmolb.2017.00063 doi: 10.1021/acs.jctc.5b00472 doi: 10.1016/bs.mcb.2015.10.005 doi: 10.1074/jbc.M111.246983
ECL1
E74
doi: 10.3389/fmolb.2017.00063
TM3
3.32
L85
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.3109/10799893.2011.578141
TM3
3.33
L86
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.3109/10799893.2011.578141
TM3
3.36
N89
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.1074/jbc.M111.246983 doi: doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM3
3.37
E90
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.3109/10799893.2011.578141
TM3
3.41
W94
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM3
3.46
L99
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM5
5.46
E182
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.3109/10799893.2011.578141
TM5
5.61
L197
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM5
5.64
S200
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM5
5.65
L201
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM7
7.39
I263
doi: 10.1016/bs.mcb.2015.10.005 doi: 10.3109/10799893.2011.578141
TM7
7.49
H273
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM7
7.53
L277
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
TM7
7.54
I278
doi: 10.1021/acs.jctc.5b00472 doi: 10.1074/jbc.M111.246983
Ligands [ edit ]
Up to now, 39 ligands for T2R1 were identified in BitterDB , among them L-amino acids , peptides , humulones , small molecules etc.[18]
See also [ edit ]
References [ edit ]
^ "Human PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ "Mouse PubMed Reference:" . National Center for Biotechnology Information, U.S. National Library of Medicine .
^ Adler E, Hoon MA, Mueller KL, Chandrashekar J, Ryba NJ, Zuker CS (Apr 2000). "A novel family of mammalian taste receptors" . Cell . 100 (6 ): 693–702. doi :10.1016/S0092-8674(00 )80705-9 . PMID 10761934 . S2CID 14604586 .
^ Matsunami H, Montmayeur JP, Buck LB (Apr 2000). "A family of candidate taste receptors in human and mouse". Nature . 404 (6778): 601–4. Bibcode :2000Natur.404..601M . doi :10.1038/35007072 . PMID 10766242 . S2CID 4336913 .
^ "Entrez Gene: TAS2R1 taste receptor, type 2, member 1" .
^ a b Di Pizio A, Levit A, Slutzki M, Behrens M, Karaman R, Niv MY (2016), "Comparing Class a GPCRS to bitter taste receptors", G Protein-Coupled Receptors - Signaling, Trafficking and Regulation , Methods in Cell Biology, vol. 132, Elsevier, pp. 401–427, doi :10.1016/bs.mcb.2015.10.005 , ISBN 978-0-12-803595-5 , PMID 26928553
^ a b Lu P, Zhang CH, Lifshitz LM, ZhuGe R (2017-01-04). "Extraoral bitter taste receptors in health and disease" . The Journal of General Physiology . 149 (2 ): 181–197. doi :10.1085/jgp.201611637 . ISSN 0022-1295 . PMC 5299619 . PMID 28053191 .
^ Deshpande DA, Wang WC, McIlmoyle EL, Robinett KS, Schillinger RM, An SS, Sham JS, Liggett SB (2010-10-24). "Bitter taste receptors on airway smooth muscle bronchodilate by localized calcium signaling and reverse obstruction" . Nature Medicine . 16 (11 ): 1299–1304. doi :10.1038/nm.2237 . ISSN 1078-8956 . PMC 3066567 . PMID 20972434 .
^ Liszt KI, Ley JP, Lieder B, Behrens M, Stöger V, Reiner A, Hochkogler CM, Köck E, Marchiori A (2017-07-10). "Caffeine induces gastric acid secretion via bitter taste signaling in gastric parietal cells" . Proceedings of the National Academy of Sciences . 114 (30 ): E6260–E6269. Bibcode :2017PNAS..114E6260L . doi :10.1073/pnas.1703728114 . ISSN 0027-8424 . PMC 5544304 . PMID 28696284 .
^ Singh N, Chakraborty R, Bhullar RP, Chelikani P (April 2014). "Differential expression of bitter taste receptors in non-cancerous breast epithelial and breast cancer cells". Biochemical and Biophysical Research Communications . 446 (2 ): 499–503. doi :10.1016/j.bbrc.2014.02.140 . ISSN 0006-291X . PMID 24613843 .
^ Upadhyaya JD, Singh N, Sikarwar AS, Chakraborty R, Pydi SP, Bhullar RP, Dakshinamurti S, Chelikani P (2014-10-23). "Dextromethorphan Mediated Bitter Taste Receptor Activation in the Pulmonary Circuit Causes Vasoconstriction" . PLOS ONE . 9 (10 ): e110373. Bibcode :2014PLoSO...9k0373U . doi :10.1371/journal.pone.0110373 . ISSN 1932-6203 . PMC 4207743 . PMID 25340739 .
^ Wiener A, Shudler M, Levit A, Niv MY (2011-09-22). "BitterDB: a database of bitter compounds" . Nucleic Acids Research . 40 (D1): D413–D419. doi :10.1093/nar/gkr755 . ISSN 1362-4962 . PMC 3245057 . PMID 21940398 .
^ Dagan-Wiener A, Di Pizio A, Nissim I, Bahia MS, Dubovski N, Margulis E, Niv MY (2018-10-24). "BitterDB: taste ligands and receptors database in 2019" . Nucleic Acids Research . 47 (D1): D1179–D1185. doi :10.1093/nar/gky974 . ISSN 0305-1048 . PMC 6323989 . PMID 30357384 .
^ Ballesteros JA, Weinstein H (1995), "[19 ] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors", Methods in Neurosciences , Elsevier, pp. 366–428, doi :10.1016/s1043-9471(05 )80049-7 , ISBN 978-0-12-185295-5
^ Rovati GE, Capra V, Neubig RR (2007-01-12). "The Highly Conserved DRY Motif of Class A G Protein-Coupled Receptors: Beyond the Ground State". Molecular Pharmacology . 71 (4 ): 959–964. doi :10.1124/mol.106.029470 . ISSN 0026-895X . PMID 17192495 . S2CID 15536186 .
^ "hTAS2R1" . BitterDB . The Hebrew University of Jerusalem.
Further reading [ edit ]
Margolskee RF (2002). "Molecular mechanisms of bitter and sweet taste transduction" . J. Biol. Chem . 277 (1 ): 1–4. doi :10.1074/jbc.R100054200 . PMID 11696554 .
Montmayeur JP, Matsunami H (2002). "Receptors for bitter and sweet taste". Curr. Opin. Neurobiol . 12 (4 ): 366–71. doi :10.1016/S0959-4388(02 )00345-8 . PMID 12139982 . S2CID 37807140 .
Chandrashekar J, Mueller KL, Hoon MA, Adler E, Feng L, Guo W, Zuker CS, Ryba NJ (2000). "T2Rs function as bitter taste receptors" . Cell . 100 (6 ): 703–11. doi :10.1016/S0092-8674(00 )80706-0 . PMID 10761935 . S2CID 7293493 .
Firestein S (2000). "The good taste of genomics" . Nature . 404 (6778): 552–3. doi :10.1038/35007167 . PMID 10766221 . S2CID 35741332 .
Zhang Y, Hoon MA, Chandrashekar J, Mueller KL, Cook B, Wu D, Zuker CS, Ryba NJ (2003). "Coding of sweet, bitter, and umami tastes: different receptor cells sharing similar signaling pathways" . Cell . 112 (3 ): 293–301. doi :10.1016/S0092-8674(03 )00071-0 . PMID 12581520 . S2CID 718601 .
Fischer A, Gilad Y, Man O, Pääbo S (2005). "Evolution of bitter taste receptors in humans and apes" . Mol. Biol. Evol . 22 (3 ): 432–6. doi :10.1093/molbev/msi027 . PMID 15496549 .
Go Y, Satta Y, Takenaka O, Takahata N (2006). "Lineage-specific loss of function of bitter taste receptor genes in humans and nonhuman primates" . Genetics . 170 (1 ): 313–26. doi :10.1534/genetics.104.037523 . PMC 1449719 . PMID 15744053 .
This article incorporates text from the United States National Library of Medicine , which is in the public domain .
R e t r i e v e d f r o m " https://en.wikipedia.org/w/index.php?title=TAS2R1&oldid=1212872963 "
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● T h i s p a g e w a s l a s t e d i t e d o n 9 M a r c h 2 0 2 4 , a t 2 3 : 5 2 ( U T C ) .
● T e x t i s a v a i l a b l e u n d e r t h e C r e a t i v e C o m m o n s A t t r i b u t i o n - S h a r e A l i k e L i c e n s e 4 . 0 ;
a d d i t i o n a l t e r m s m a y a p p l y . B y u s i n g t h i s s i t e , y o u a g r e e t o t h e T e r m s o f U s e a n d P r i v a c y P o l i c y . W i k i p e d i a ® i s a r e g i s t e r e d t r a d e m a r k o f t h e W i k i m e d i a F o u n d a t i o n , I n c . , a n o n - p r o f i t o r g a n i z a t i o n .
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