Calcitonin gene-related peptide type 1 receptor

Details

Name

Calcitonin gene-related peptide type 1 receptor

Synonyms

• Calcitonin receptor-like receptor
• CGRP type 1 receptor
• CGRPR

Gene Name

CALCRL

UniProtKB Entry

Q16602Swiss-Prot

Organism

Humans

NCBI Taxonomy ID

9606

Amino acid sequence

>lcl|BSEQ0058156|Calcitonin gene-related peptide type 1 receptor
MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN

Number of residues

461

Molecular Weight

52978.05

Theoretical pI

Not Available

GO Classification

Functions

adrenomedullin binding / G protein-coupled receptor activity

Processes

adenylate cyclase-activating G protein-coupled receptor signaling pathway / adrenomedullin receptor signaling pathway / calcitonin gene-related peptide receptor signaling pathway / G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger / positive regulation of vascular associated smooth muscle cell proliferation / vascular associated smooth muscle cell proliferation

Components

adrenomedullin receptor complex / CGRP receptor complex / cytoplasm

General Function

Receptor for calcitonin-gene-related peptide (CGRP) together with RAMP1 and receptor for adrenomedullin together with RAMP3 (By similarity). Receptor for adrenomedullin together with RAMP2 (PubMed:22102369, PubMed:30115739). The activity of this receptor is mediated by G proteins which activate adenylyl cyclase (PubMed:22102369, PubMed:30115739)

Specific Function

adrenomedullin binding

Pfam Domain Function

• 7tm_2 (PF00002)
• HRM (PF02793)

Signal Regions

1-22

Transmembrane Regions

147-166 174-193 214-236 254-273 290-313 337-354 367-388

Cellular Location

Cell membrane

Gene sequence

>lcl|BSEQ0049733|Calcitonin gene-related peptide type 1 receptor (CALCRL)
ATGGAGAAAAAGTGTACCCTGTATTTTCTGGTTCTCTTGCCTTTTTTTATGATTCTTGTT
ACAGCAGAATTAGAAGAGAGTCCTGAGGACTCAATTCAGTTGGGAGTTACTAGAAATAAA
ATCATGACAGCTCAATATGAATGTTACCAAAAGATTATGCAAGACCCCATTCAACAAGCA
GAAGGCGTTTACTGCAACAGAACCTGGGATGGATGGCTCTGCTGGAACGATGTTGCAGCA
GGAACTGAATCAATGCAGCTCTGCCCTGATTACTTTCAGGACTTTGATCCATCAGAAAAA
GTTACAAAGATCTGTGACCAAGATGGAAACTGGTTTAGACATCCAGCAAGCAACAGAACA
TGGACAAATTATACCCAGTGTAATGTTAACACCCACGAGAAAGTGAAGACTGCACTAAAT
TTGTTTTACCTGACCATAATTGGACACGGATTGTCTATTGCATCACTGCTTATCTCGCTT
GGCATATTCTTTTATTTCAAGAGCCTAAGTTGCCAAAGGATTACCTTACACAAAAATCTG
TTCTTCTCATTTGTTTGTAACTCTGTTGTAACAATCATTCACCTCACTGCAGTGGCCAAC
AACCAGGCCTTAGTAGCCACAAATCCTGTTAGTTGCAAAGTGTCCCAGTTCATTCATCTT
TACCTGATGGGCTGTAATTACTTTTGGATGCTCTGTGAAGGCATTTACCTACACACACTC
ATTGTGGTGGCCGTGTTTGCAGAGAAGCAACATTTAATGTGGTATTATTTTCTTGGCTGG
GGATTTCCACTGATTCCTGCTTGTATACATGCCATTGCTAGAAGCTTATATTACAATGAC
AATTGCTGGATCAGTTCTGATACCCATCTCCTCTACATTATCCATGGCCCAATTTGTGCT
GCTTTACTGGTGAATCTTTTTTTCTTGTTAAATATTGTACGCGTTCTCATCACCAAGTTA
AAAGTTACACACCAAGCGGAATCCAATCTGTACATGAAAGCTGTGAGAGCTACTCTTATC
TTGGTGCCATTGCTTGGCATTGAATTTGTGCTGATTCCATGGCGACCTGAAGGAAAGATT
GCAGAGGAGGTATATGACTACATCATGCACATCCTTATGCACTTCCAGGGTCTTTTGGTC
TCTACCATTTTCTGCTTCTTTAATGGAGAGGTTCAAGCAATTCTGAGAAGAAACTGGAAT
CAATACAAAATCCAATTTGGAAACAGCTTTTCCAACTCAGAAGCTCTTCGTAGTGCGTCT
TACACAGTGTCAACAATCAGTGATGGTCCAGGTTATAGTCATGACTGTCCTAGTGAACAC
TTAAATGGAAAAAGCATCCATGATATTGAAAATGTTCTCTTAAAACCAGAAAATTTATAT
AATTGA

Chromosome Location

2

Locus

2q32.1

External Identifiers

Resource	Link
UniProtKB ID	Q16602
UniProtKB Entry Name	CALRL_HUMAN
GeneCard ID	CALCRL
HGNC ID	HGNC:16709
PDB ID(s)	3AQF, 3N7P, 3N7R, 3N7S, 4RWF, 4RWG, 5V6Y, 6D1U, 6E3Y, 6UMG, 6UUN, 6UUS, 6UVA, 6V2E, 6ZHO, 6ZIS, 7KNT, 7KNU, 7P0F, 7P0I, 8AX5, 8AX6, 8AX7
KEGG ID	hsa:10203
IUPHAR/Guide To Pharmacology ID	47
NCBI Gene ID	10203

General References

1. Aiyar N, Rand K, Elshourbagy NA, Zeng Z, Adamou JE, Bergsma DJ, Li Y: A cDNA encoding the calcitonin gene-related peptide type 1 receptor. J Biol Chem. 1996 May 10;271(19):11325-9. [Article]
2. Fluhmann B, Muff R, Hunziker W, Fischer JA, Born W: A human orphan calcitonin receptor-like structure. Biochem Biophys Res Commun. 1995 Jan 5;206(1):341-7. [Article]
3. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [Article]
4. Hillier LW, Graves TA, Fulton RS, Fulton LA, Pepin KH, Minx P, Wagner-McPherson C, Layman D, Wylie K, Sekhon M, Becker MC, Fewell GA, Delehaunty KD, Miner TL, Nash WE, Kremitzki C, Oddy L, Du H, Sun H, Bradshaw-Cordum H, Ali J, Carter J, Cordes M, Harris A, Isak A, van Brunt A, Nguyen C, Du F, Courtney L, Kalicki J, Ozersky P, Abbott S, Armstrong J, Belter EA, Caruso L, Cedroni M, Cotton M, Davidson T, Desai A, Elliott G, Erb T, Fronick C, Gaige T, Haakenson W, Haglund K, Holmes A, Harkins R, Kim K, Kruchowski SS, Strong CM, Grewal N, Goyea E, Hou S, Levy A, Martinka S, Mead K, McLellan MD, Meyer R, Randall-Maher J, Tomlinson C, Dauphin-Kohlberg S, Kozlowicz-Reilly A, Shah N, Swearengen-Shahid S, Snider J, Strong JT, Thompson J, Yoakum M, Leonard S, Pearman C, Trani L, Radionenko M, Waligorski JE, Wang C, Rock SM, Tin-Wollam AM, Maupin R, Latreille P, Wendl MC, Yang SP, Pohl C, Wallis JW, Spieth J, Bieri TA, Berkowicz N, Nelson JO, Osborne J, Ding L, Meyer R, Sabo A, Shotland Y, Sinha P, Wohldmann PE, Cook LL, Hickenbotham MT, Eldred J, Williams D, Jones TA, She X, Ciccarelli FD, Izaurralde E, Taylor J, Schmutz J, Myers RM, Cox DR, Huang X, McPherson JD, Mardis ER, Clifton SW, Warren WC, Chinwalla AT, Eddy SR, Marra MA, Ovcharenko I, Furey TS, Miller W, Eichler EE, Bork P, Suyama M, Torrents D, Waterston RH, Wilson RK: Generation and annotation of the DNA sequences of human chromosomes 2 and 4. Nature. 2005 Apr 7;434(7034):724-31. [Article]
5. Zhang Z, Henzel WJ: Signal peptide prediction based on analysis of experimentally verified cleavage sites. Protein Sci. 2004 Oct;13(10):2819-24. Epub 2004 Aug 31. [Article]
6. ter Haar E, Koth CM, Abdul-Manan N, Swenson L, Coll JT, Lippke JA, Lepre CA, Garcia-Guzman M, Moore JM: Crystal structure of the ectodomain complex of the CGRP receptor, a class-B GPCR, reveals the site of drug antagonism. Structure. 2010 Sep 8;18(9):1083-93. doi: 10.1016/j.str.2010.05.014. [Article]
7. Kusano S, Kukimoto-Niino M, Hino N, Ohsawa N, Okuda K, Sakamoto K, Shirouzu M, Shindo T, Yokoyama S: Structural basis for extracellular interactions between calcitonin receptor-like receptor and receptor activity-modifying protein 2 for adrenomedullin-specific binding. Protein Sci. 2012 Feb;21(2):199-210. doi: 10.1002/pro.2003. Epub 2011 Dec 28. [Article]

Associated Data

Bio-Entities

Bio-Entity	Type
Calcitonin gene-related peptide type 1 receptor (Humans)	protein primary

Drug Relations

Drug	Drug group	Pharmacological action?	Type	Actions	Details
Olcegepant	investigational	unknown	target	antagonist	Details
Telcagepant	investigational	yes	target	antagonist	Details
Erenumab	approved, investigational	unknown	target		Details
Ubrogepant	approved, investigational	yes	target	antagonist	Details
Rimegepant	approved, investigational	yes	target	antagonist	Details
Zavegepant	approved, investigational	yes	target	antagonist	Details
Atogepant	approved, investigational	yes	target	antagonist	Details
MK-3207	investigational	yes	target	antagonist	Details