The secretin receptor is a protein that in humans is encoded by the SCTR gene. This protein is a G protein-coupled receptor which binds secretin and is the leading member (i.e., first cloned) of the secretin receptor family, also called class B GPCR subfamily.[5] SCTR belongs to the glucagon-VIP-secretin receptor family; its locus is 2q14.2.[6]
Interactions
The secretin receptor has been shown to interact with pituitary adenylate cyclase activating peptide.[7]
Clinical significance
Breast Cancer
SCTR neither uniformly upregulated or downregulated in tumors, hence, it has the potential to promote or suppress tumor proliferation.[8] In a study investigating methylation of the SCTR genes in breast cancer tissue, hypermethylation and downregulation were observed; pathway analysis in MCF-10A cells determined these most likely effect the G2/M stage checkpoint.[8] However, SCTR was overexpressed in MCF-7 cells, leading to increased proliferation and migration.[8] The study concluded that SCTR downregulates proliferation in normal breast cells and upregulates proliferation in breast cancer cells that have their proliferation downregulated by promoter methylation.[8]
Colorectal cancer
SCTR has been observed to be hypermethylated in colorectal cancer.[9] Moreover, because of the high frequency of hypermethylation at CpG islands in colorectal cancer, SCTR hypermethylation is an effective diagnostic marker that has achieved high diagnostic performance; colorectal cancer and precursor legions were able to be distinguished using SCTR methylation as a diagnostic tool.[10] Additionally, SCTR genes were found to be hypermethylated in cell-free DNA samples of colorectal cancer patients, but not in cells from healthy patients.[10]
References
- 1 2 3 GRCh38: Ensembl release 89: ENSG00000080293 – Ensembl, May 2017
- 1 2 3 GRCm38: Ensembl release 89: ENSMUSG00000026387 – Ensembl, May 2017
- ↑ "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.
- ↑ Dong M, Miller LJ (2002). "Molecular pharmacology of the secretin receptor". Receptors & Channels. 8 (3–4): 189–200. doi:10.1080/10606820213686. PMID 12529936.
- ↑ "SCTR secretin receptor [Homo sapiens (human)] - Gene - NCBI". www.ncbi.nlm.nih.gov. Retrieved 2026-05-03.
- ↑ Felley CP, Qian JM, Mantey S, Pradhan T, Jensen RT (December 1992). "Chief cells possess a receptor with high affinity for PACAP and VIP that stimulates pepsinogen release". The American Journal of Physiology. 263 (6 Pt 1): G901–7. doi:10.1152/ajpgi.1992.263.6.G901. PMID 1335692.
- 1 2 3 4 Kang S, Kim B, Kang HS, Jeong G, Bae H, Lee H, et al. (November 2015). "SCTR regulates cell cycle-related genes toward anti-proliferation in normal breast cells while having pro-proliferation activity in breast cancer cells". International Journal of Oncology. 47 (5): 1923–1931. doi:10.3892/ijo.2015.3164. PMID 26397240.
- ↑ Frigola J, Song J, Stirzaker C, Hinshelwood RA, Peinado MA, Clark SJ (May 2006). "Epigenetic remodeling in colorectal cancer results in coordinate gene suppression across an entire chromosome band". Nature Genetics. 38 (5): 540–549. doi:10.1038/ng1781. PMID 16642018.
- 1 2 "User:YonathanBiochemRec/Secretin receptor/Outline", Wikipedia, 2026-05-03, retrieved 2026-05-03
Further reading
- Ulrich CD, Holtmann M, Miller LJ (February 1998). "Secretin and vasoactive intestinal peptide receptors: members of a unique family of G protein-coupled receptors". Gastroenterology. 114 (2): 382–397. doi:10.1016/S0016-5085(98)70491-3. PMID 9453500.
- Felley CP, Qian JM, Mantey S, Pradhan T, Jensen RT (December 1992). "Chief cells possess a receptor with high affinity for PACAP and VIP that stimulates pepsinogen release". The American Journal of Physiology. 263 (6 Pt 1): G901–7. doi:10.1152/ajpgi.1992.263.6.G901. PMID 1335692.
- Ishihara T, Nakamura S, Kaziro Y, Takahashi T, Takahashi K, Nagata S (July 1991). "Molecular cloning and expression of a cDNA encoding the secretin receptor". The EMBO Journal. 10 (7): 1635–1641. doi:10.1002/j.1460-2075.1991.tb07686.x. PMC 452832. PMID 1646711.
- Robberecht P, De Neef P, Waelbroeck M, Camus JC, Scemama JL, Fourmy D, et al. (1988). "Secretin receptors in human pancreatic membranes". Pancreas. 3 (5): 529–535. doi:10.1097/00006676-198810000-00004. PMID 3186683. S2CID 23220534.
- Chow BK (July 1995). "Molecular cloning and functional characterization of a human secretin receptor". Biochemical and Biophysical Research Communications. 212 (1): 204–211. doi:10.1006/bbrc.1995.1957. PMID 7612008.
- Patel DR, Kong Y, Sreedharan SP (March 1995). "Molecular cloning and expression of a human secretin receptor". Molecular Pharmacology. 47 (3): 467–473. doi:10.1016/S0026-895X(25)08566-9. PMID 7700244.
- Holtmann MH, Hadac EM, Miller LJ (June 1995). "Critical contributions of amino-terminal extracellular domains in agonist binding and activation of secretin and vasoactive intestinal polypeptide receptors. Studies of chimeric receptors". The Journal of Biological Chemistry. 270 (24): 14394–14398. doi:10.1074/jbc.270.24.14394. PMID 7782300.
- Jiang S, Ulrich C (February 1995). "Molecular cloning and functional expression of a human pancreatic secretin receptor". Biochemical and Biophysical Research Communications. 207 (3): 883–890. doi:10.1006/bbrc.1995.1268. PMID 7864894.
- Sreedharan SP, Patel DR, Huang JX, Goetzl EJ (June 1993). "Cloning and functional expression of a human neuroendocrine vasoactive intestinal peptide receptor". Biochemical and Biophysical Research Communications. 193 (2): 546–553. doi:10.1006/bbrc.1993.1658. PMID 8390245.
- Mark HF, Chow BK (October 1995). "Localization of the gene encoding the secretin receptor, SCTR, on human chromosome 2q14.1 by fluorescence in situ hybridization and chromosome morphometry". Genomics. 29 (3): 817–818. doi:10.1006/geno.1995.9922. PMID 8575789.
- Vilardaga JP, di Paolo E, de Neef P, Waelbroeck M, Bollen A, Robberecht P (January 1996). "Lysine 173 residue within the first exoloop of rat secretin receptor is involved in carboxylate moiety recognition of Asp 3 in secretin". Biochemical and Biophysical Research Communications. 218 (3): 842–846. doi:10.1006/bbrc.1996.0150. PMID 8579602.
- Chow BK (1998). "Functional antagonism of the human secretin receptor by a recombinant protein encoding the N-terminal ectodomain of the receptor". Receptors & Signal Transduction. 7 (3): 143–150. PMID 9440501.
- Shetzline MA, Premont RT, Walker JK, Vigna SR, Caron MG (March 1998). "A role for receptor kinases in the regulation of class II G protein-coupled receptors. Phosphorylation and desensitization of the secretin receptor". The Journal of Biological Chemistry. 273 (12): 6756–6762. doi:10.1074/jbc.273.12.6756. PMID 9506976.
- Ho PK, Fong RS, Kai HS, Lau EH, Ngan ES, Cotton CU, et al. (July 1999). "The human secretin receptor gene: genomic organization and promoter characterization". FEBS Letters. 455 (3): 209–214. doi:10.1016/S0014-5793(99)00864-9. PMID 10437774. S2CID 1197008.
- Pang RT, Ng SS, Cheng CH, Holtmann MH, Miller LJ, Chow BK (November 1999). "Role of N-linked glycosylation on the function and expression of the human secretin receptor". Endocrinology. 140 (11): 5102–5111. doi:10.1210/endo.140.11.7134. PMID 10537138.
- Chan KY, Pang RT, Chow BK (September 2001). "Functional segregation of the highly conserved basic motifs within the third endoloop of the human secretin receptor". Endocrinology. 142 (9): 3926–3934. doi:10.1210/endo.142.9.8389. PMID 11517171.
- Pang RT, Lee LT, Ng SS, Yung WH, Chow BK (February 2004). "CpG methylation and transcription factors Sp1 and Sp3 regulate the expression of the human secretin receptor gene". Molecular Endocrinology. 18 (2): 471–483. doi:10.1210/me.2003-0245. PMID 14645499.
External links
- IUPHAR GPCR Database - Secretin receptor Archived 2016-03-03 at the Wayback Machine
- secretin+receptor at the U.S. National Library of Medicine Medical Subject Headings (MeSH)
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