Cloning, Functional Expression and Pharmacological Characterization of a Fourth (hSSTR4) and a Fifth (hSSTR5) Human Somatostatin Receptor Subtype

Yamada, Yoshio; Kagimoto, Shinji; Kubota, Akira; Yasuda, Kaori; Masuda, Kimio; Someya, Yuichi; Ihara, Yu; Li, Qing; Imura, Hiroo; Seino, Susumu; Seino, Yutaka

doi:10.1006/bbrc.1993.2122

Cited by 237 publications

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“…After sst 2 , it was the second most often expressed subtype in the present group of tumors; sst 5 mRNA is often expressed in tumors exhibiting sst 2 as well. It was, however, also found in those tumors lacking sst 2 mRNA but with measurable amounts of octreotide binding sites; this finding suggests that, despite the lower octreotide affinity of sst 5 compared with sst 2 (Kubota et al, 1994;Yamada et al, 1993), 125 I-[Tyr 3 ]-octreotide is able to label these sst 5 -expressing human tumors sufficiently well. It is not clear whether a particularly high density of the sst 5 receptor subtype is necessary to be identified by 125 I-[Tyr 3 ]-octreotide.…”

Section: Discussionmentioning

confidence: 93%

“…The protocol followed was essentially that described in detail by Reubi et al (1994). Fortyeight-base-long oligonucleotides complementary to the bases coding for amino acids 2-17 and 252-267 of the human sst 1 mRNA sequence (Yamada et al, 1992b), 31-46 and 237-252 of the human sst 2 mRNA sequence (Yamada et al, 1992b), 228-243 and 366-381 of the human sst 3 mRNA sequence (Yamada et al, 1992a) and 2-17, 327-342 and 349-364 of the human sst 5 mRNA sequence (Yamada et al, 1993) were synthesized and purified on a 20% polyacrylamide-8 M urea sequencing gel (Microsynth, Balgach, Switzerland).…”

Section: In Situ Hybridization Histochemistrymentioning

confidence: 99%

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Somatostatin receptor subtypes sst1, sst2, sst3 and sst5expression in human pituitary, gastroentero-pancreatic and mammary tumors

et al. 1997

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Using in situ hybridization techniques with selective oligoprobes, the gene expression of sst 1 , sst 2 , sst 3 and sst 5 was studied in a series of 32 human pituitary adenomas, 28 breast tumors and 21 endocrine gastroentero-pancreatic tumors, shown to express somatostatin receptors to variable extents. In most of these tumors the sst 2 receptor subtype was abundantly expressed, even though a significant number of pituitary adenomas, breast and gastroentero-pancreatic tumors expressed sst 1 and/or sst 3 as well. A very high incidence of the sst 5 subtype was found in growth hormone-producing pituitary adenomas and, to a lesser extent, in inactive pituitary adenomas, whereas breast tumors seldom expressed sst 5 ; gastroentero-pancreatic tumors showed all possible combinations of sst expression, with, however, a predominance of sst 2 and sst 1 . Overall, the presence of sst 2 mRNA and/or sst 5 mRNA generally correlated with the presence of octreotide binding sites. A lack of octreotide binding sites corresponded with a lack of sst 2 mRNA. Several tumors exhibiting a low number of octreotide binding sites had no measurable sst 2 mRNA, despite abundance of b-actin mRNA, suggesting in these cases a very low abundance of sst mRNAs or a too low sensitivity of the in situ hybridization methodology. In all other cases, the method allowed precise localization of the respective mRNAs on the tumor tissue, notably in breast tumors with non-homogeneous receptor distribution. Tumors without measurable amounts of somatostatin receptors had no detectable sst mRNA. Our results indicate a highly variable abundance of the various sst mRNAs in individual somatostatin receptor-containing tumors.

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Section: Discussionmentioning

confidence: 93%

Section: In Situ Hybridization Histochemistrymentioning

confidence: 99%

Somatostatin receptor subtypes sst1, sst2, sst3 and sst5expression in human pituitary, gastroentero-pancreatic and mammary tumors

et al. 1997

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“…In situ studies also show that its expression is homogeneous. However, these and other studies show that most cell types express the hSSTR2 Yamada et al, 1993), hence selectivity of action is not possible.…”

Section: Discussionmentioning

confidence: 77%

“…Previous studies on somatostatin receptor expression have detected subtypes 1,2 and 5 in gastrointestinal tissue and cell lines (Yamada et al, 1992a, b;Eden and Taylor, 1993;O'Carroll et al, 1993) and hSSTR3 in the pancreas (Yamada et al, 1993). However, studies of colonic tissues have yielded different results with diverse methodologies (Miller et al, 1992;Reubi et al, 1994), and none of the methods used allow discrimination between the five receptor subtypes.…”

mentioning

confidence: 99%

Somatostatin receptor subtype mRNA expression in human colorectal cancer and normal colonic mucosae

Laws

Gough²,

Evans³

et al. 1997

Br J Cancer

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Summary Somatostatin analogues may be useful novel agents in the systemic treatment of advanced colorectal cancer, as somatostatin inhibits proliferation in a wide variety of cell types. Here, we report the expression profiles of somatostatin receptor mRNAs in 32 pairs of malignant and normal colonic epithelia. Receptor subtype 2 (hSSTR2) mRNA was detected throughout nearly 90% of both malignant and normal tissue by reverse transcription-polymerase chain reaction (RT-PCR) and in situ hybridization. Subtype 5 (hSSTR5) mRNA was detected in 46% and 45% of tumour and mucosal samples respectively, but in 75% (9/12) of early-stage tumours (tubulovillous adenomas, Dukes' A and B) compared with 31% (5/16) of late-stage tumours (Dukes' C and 'D' tumours), 0.05>P>0.025 (X2 with Yates' correction). There was also reduced expression of hSSTR5 in samples of metastatic tumour (11%, 1/9) compared with all tumour samples (56%, 18/32) 0.025>P>0.01 (X2 with Yates' correction). Other hSSTRs (1, 3 and 4) were expressed infrequently. Thus, hSSTR2 expression is retained after malignant transformation in colonic epithelium and, although it may potentially be a target for antiproliferative therapy, its ubiquitous expression militates against this. hSSTR5 warrants investigation as a tumour suppressor.

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“…Molecular cloning of human SSTR and VIPR has recently provided new insights into the biology and interactions of VIP and SST/OCT. So far, five different human SSTRs and two different VIPRs have been characterized in detail and have been cloned [37][38][39][40][41][42][43][44][45][46][47][48][49][50]. More recent data have demonstrated that SSTR3 is responsible for binding both SST/OCT and VIP and the observed cross-competition between these peptides in primary human tumours as well as human immortalized tumours [21].…”

Section: Vip and Sst Cross-compete For Cellular Binding Sitesmentioning

confidence: 99%

Mack Forster Award Lecture Receptor nuclear medicine: vasointestinal peptide and somatostatin receptor scintigraphy for diagnosis and treatment of tumour patients

Virgolini

1997

Eur J Clin Investigation

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Cloning, Functional Expression and Pharmacological Characterization of a Fourth (hSSTR4) and a Fifth (hSSTR5) Human Somatostatin Receptor Subtype

Cited by 237 publications

References 0 publications

Somatostatin receptor subtypes sst1, sst2, sst3 and sst5expression in human pituitary, gastroentero-pancreatic and mammary tumors

Somatostatin receptor subtypes sst1, sst2, sst3 and sst5expression in human pituitary, gastroentero-pancreatic and mammary tumors

Somatostatin receptor subtype mRNA expression in human colorectal cancer and normal colonic mucosae

Mack Forster Award Lecture Receptor nuclear medicine: vasointestinal peptide and somatostatin receptor scintigraphy for diagnosis and treatment of tumour patients

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