Glucagon-like peptide 1 receptor

Details

Name
Glucagon-like peptide 1 receptor
Synonyms
  • GLP-1 receptor
Gene Name
GLP1R
Organism
Humans
Amino acid sequence
>lcl|BSEQ0010605|Glucagon-like peptide 1 receptor
MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDL
FCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPW
RDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIH
LNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAAN
YYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRN
SNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLL
GTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERW
RLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
Number of residues
463
Molecular Weight
53025.22
Theoretical pI
8.19
GO Classification
Functions
glucagon receptor activity / transmembrane signaling receptor activity
Processes
activation of adenylate cyclase activity / cAMP-mediated signaling / cell surface receptor signaling pathway / energy reserve metabolic process / learning or memory / positive regulation of blood pressure / positive regulation of cytosolic calcium ion concentration / regulation of heart contraction / regulation of insulin secretion / response to stress / small molecule metabolic process
Components
cytosol / integral component of membrane / intracellular / plasma membrane
General Function
Transmembrane signaling receptor activity
Specific Function
This is a receptor for glucagon-like peptide 1. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Pfam Domain Function
Transmembrane Regions
140-164 177-201 228-251 266-287 306-328 353-371 384-404
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0010606|Glucagon-like peptide 1 receptor (GLP1R)
ATGGCCGGCGCCCCCGGCCCGCTGCGCCTTGCGCTGCTGCTGCTCGGGATGGTGGGCAGG
GCCGGCCCCCGCCCCCAGGGTGCCACTGTGTCCCTCTGGGAGACGGTGCAGAAATGGCGA
GAATACCGACGCCAGTGCCAGCGCTCCCTGACTGAGGATCCACCTCCTGCCACAGACTTG
TTCTGCAACCGGACCTTCGATGAATACGCCTGCTGGCCAGATGGGGAGCCAGGCTCGTTC
GTGAATGTCAGCTGCCCCTGGTACCTGCCCTGGGCCAGCAGTGTGCCGCAGGGCCACGTG
TACCGGTTCTGCACAGCTGAAGGCCTCTGGCTGCAGAAGGACAACTCCAGCCTGCCCTGG
AGGGACTTGTCGGAGTGCGAGGAGTCCAAGCGAGGGGAAAGAAGCTCCCCGGAGGAGCAG
CTCCTGTTCCTCTACATCATCTACACGGTGGGCTACGCACTCTCCTTCTCTGCTCTGGTT
ATCGCCTCTGCGATCCTCCTCGGCTTCAGACACCTGCACTGCACCAGGAACTACATCCAC
CTGAACCTGTTTGCATCCTTCATCCTGCGAGCATTGTCCGTCTTCATCAAGGACGCAGCC
CTGAAGTGGATGTATAGCACAGCCGCCCAGCAGCACCAGTGGGATGGGCTCCTCTCCTAC
CAGGACTCTCTGAGCTGCCGCCTGGTGTTTCTGCTCATGCAGTACTGTGTGGCGGCCAAT
TACTACTGGCTCTTGGTGGAGGGCGTGTACCTGTACACACTGCTGGCCTTCTCGGTCTTA
TCTGAGCAATGGATCTTCAGGCTCTACGTGAGCATAGGCTGGGGTGTTCCCCTGCTGTTT
GTTGTCCCCTGGGGCATTGTCAAGTACCTCTATGAGGACGAGGGCTGCTGGACCAGGAAC
TCCAACATGAACTACTGGCTCATTATCCGGCTGCCCATTCTCTTTGCCATTGGGGTGAAC
TTCCTCATCTTTGTTCGGGTCATCTGCATCGTGGTATCCAAACTGAAGGCCAATCTCATG
TGCAAGACAGACATCAAATGCAGACTTGCCAAGTCCACGCTGACACTCATCCCCCTGCTG
GGGACTCATGAGGTCATCTTTGCCTTTGTGATGGACGAGCACGCCCGGGGGACCCTGCGC
TTCATCAAGCTGTTTACAGAGCTCTCCTTCACCTCCTTCCAGGGGCTGATGGTGGCCATA
TTATACTGCTTTGTCAACAATGAGGTCCAGCTGGAATTTCGGAAGAGCTGGGAGCGCTGG
CGGCTTGAGCACTTGCACATCCAGAGGGACAGCAGCATGAAGCCCCTCAAGTGTCCCACC
AGCAGCCTGAGCAGTGGAGCCACGGCGGGCAGCAGCATGTACACAGCCACTTGCCAGGCC
TCCTGCAGCTGA
Chromosome Location
6
Locus
6p21
External Identifiers
ResourceLink
UniProtKB IDP43220
UniProtKB Entry NameGLP1R_HUMAN
GenBank Protein ID405082
GenBank Gene IDU01104
GenAtlas IDGLP1R
HGNC IDHGNC:4324
General References
  1. Thorens B, Porret A, Buhler L, Deng SP, Morel P, Widmann C: Cloning and functional expression of the human islet GLP-1 receptor. Demonstration that exendin-4 is an agonist and exendin-(9-39) an antagonist of the receptor. Diabetes. 1993 Nov;42(11):1678-82. [PubMed:8405712]
  2. Dillon JS, Tanizawa Y, Wheeler MB, Leng XH, Ligon BB, Rabin DU, Yoo-Warren H, Permutt MA, Boyd AE 3rd: Cloning and functional expression of the human glucagon-like peptide-1 (GLP-1) receptor. Endocrinology. 1993 Oct;133(4):1907-10. [PubMed:8404634]
  3. Graziano MP, Hey PJ, Borkowski D, Chicchi GG, Strader CD: Cloning and functional expression of a human glucagon-like peptide-1 receptor. Biochem Biophys Res Commun. 1993 Oct 15;196(1):141-6. [PubMed:8216285]
  4. van Eyll B, Lankat-Buttgereit B, Bode HP, Goke R, Goke B: Signal transduction of the GLP-1-receptor cloned from a human insulinoma. FEBS Lett. 1994 Jul 4;348(1):7-13. [PubMed:7517895]
  5. Wei Y, Mojsov S: Tissue-specific expression of the human receptor for glucagon-like peptide-I: brain, heart and pancreatic forms have the same deduced amino acid sequences. FEBS Lett. 1995 Jan 30;358(3):219-24. [PubMed:7843404]
  6. Mungall AJ, Palmer SA, Sims SK, Edwards CA, Ashurst JL, Wilming L, Jones MC, Horton R, Hunt SE, Scott CE, Gilbert JG, Clamp ME, Bethel G, Milne S, Ainscough R, Almeida JP, Ambrose KD, Andrews TD, Ashwell RI, Babbage AK, Bagguley CL, Bailey J, Banerjee R, Barker DJ, Barlow KF, Bates K, Beare DM, Beasley H, Beasley O, Bird CP, Blakey S, Bray-Allen S, Brook J, Brown AJ, Brown JY, Burford DC, Burrill W, Burton J, Carder C, Carter NP, Chapman JC, Clark SY, Clark G, Clee CM, Clegg S, Cobley V, Collier RE, Collins JE, Colman LK, Corby NR, Coville GJ, Culley KM, Dhami P, Davies J, Dunn M, Earthrowl ME, Ellington AE, Evans KA, Faulkner L, Francis MD, Frankish A, Frankland J, French L, Garner P, Garnett J, Ghori MJ, Gilby LM, Gillson CJ, Glithero RJ, Grafham DV, Grant M, Gribble S, Griffiths C, Griffiths M, Hall R, Halls KS, Hammond S, Harley JL, Hart EA, Heath PD, Heathcott R, Holmes SJ, Howden PJ, Howe KL, Howell GR, Huckle E, Humphray SJ, Humphries MD, Hunt AR, Johnson CM, Joy AA, Kay M, Keenan SJ, Kimberley AM, King A, Laird GK, Langford C, Lawlor S, Leongamornlert DA, Leversha M, Lloyd CR, Lloyd DM, Loveland JE, Lovell J, Martin S, Mashreghi-Mohammadi M, Maslen GL, Matthews L, McCann OT, McLaren SJ, McLay K, McMurray A, Moore MJ, Mullikin JC, Niblett D, Nickerson T, Novik KL, Oliver K, Overton-Larty EK, Parker A, Patel R, Pearce AV, Peck AI, Phillimore B, Phillips S, Plumb RW, Porter KM, Ramsey Y, Ranby SA, Rice CM, Ross MT, Searle SM, Sehra HK, Sheridan E, Skuce CD, Smith S, Smith M, Spraggon L, Squares SL, Steward CA, Sycamore N, Tamlyn-Hall G, Tester J, Theaker AJ, Thomas DW, Thorpe A, Tracey A, Tromans A, Tubby B, Wall M, Wallis JM, West AP, White SS, Whitehead SL, Whittaker H, Wild A, Willey DJ, Wilmer TE, Wood JM, Wray PW, Wyatt JC, Young L, Younger RM, Bentley DR, Coulson A, Durbin R, Hubbard T, Sulston JE, Dunham I, Rogers J, Beck S: The DNA sequence and analysis of human chromosome 6. Nature. 2003 Oct 23;425(6960):805-11. [PubMed:14574404]
  7. Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [PubMed:15489334]
  8. Lankat-Buttgereit B, Goke B: Cloning and characterization of the 5' flanking sequences (promoter region) of the human GLP-1 receptor gene. Peptides. 1997;18(5):617-24. [PubMed:9213353]
  9. Mann RJ, Al-Sabah S, de Maturana RL, Sinfield JK, Donnelly D: Functional coupling of Cys-226 and Cys-296 in the glucagon-like peptide-1 (GLP-1) receptor indicates a disulfide bond that is close to the activation pocket. Peptides. 2010 Dec;31(12):2289-93. doi: 10.1016/j.peptides.2010.09.015. Epub 2010 Oct 1. [PubMed:20869417]
  10. Dezelak M, Bavec A: Glucagon like-peptide-1 receptor is covalently modified by endogenous mono-ADP-ribosyltransferase. Mol Biol Rep. 2012 Apr;39(4):4375-81. doi: 10.1007/s11033-011-1225-0. Epub 2011 Sep 8. [PubMed:21901419]
  11. Whitaker GM, Lynn FC, McIntosh CH, Accili EA: Regulation of GIP and GLP1 receptor cell surface expression by N-glycosylation and receptor heteromerization. PLoS One. 2012;7(3):e32675. doi: 10.1371/journal.pone.0032675. Epub 2012 Mar 7. [PubMed:22412906]
  12. Runge S, Thogersen H, Madsen K, Lau J, Rudolph R: Crystal structure of the ligand-bound glucagon-like peptide-1 receptor extracellular domain. J Biol Chem. 2008 Apr 25;283(17):11340-7. doi: 10.1074/jbc.M708740200. Epub 2008 Feb 20. [PubMed:18287102]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB01276Exenatideapproved, investigationalyesagonistDetails
DB00040GlucagonapprovedunknownagonistDetails
DB06655LiraglutideapprovedyesagonistDetails
DB09043AlbiglutideapprovedyesagonistDetails
DB09045Dulaglutideapproved, investigationalyesagonistDetails
DB09265LixisenatideapprovedyesagonistDetails
DB13928Semaglutideapproved, investigationalyesagonistDetails