Abstract |
The somatostatin receptor subtype 2 (SSTR2) was detected in a wide range of human and rat tumors using in vitro receptor binding ([125I] MK-678), receptor gene expression analysis, and immunoblotting techniques. The highest receptor concentrations were observed in the rat AR42J pancreatic and human small cell lung cancer (SCLC) cell lines, NCI-H69 and NCI-H345, with much lower levels detected in breast, prostate, melanoma, and hepatic tumors. Several human pancreas tumors were devoid of SSTR2. For all tumors showing detectable [125I] MK-678 binding, SSTR2 receptor mRNA was expressed. Furthermore, a mRNA transcript corresponding to a truncated isoform of SSTR2 was detected at low levels in the human SCLC NCI-H69 cell line, and likely represents a human homologue of rodent SSTR2B. Immunoblotting analysis using the SSTR2-specific antibody, 2e3, detected multiple immunoreactive protein species, including a predominant 150-kDa molecule, which could be blocked by the SSTR2-derived 2e3 peptide. Somatostatin (SRIF) peptides with high SSTR2 affinity and antiproliferative properties were potent inhibitors of [125I] MK-678 binding to several tumor types, suggesting that they may exert antitumor effects via the SSTR2 receptor.
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Authors | J E Taylor, M A Theveniau, R Bashirzadeh, T Reisine, P A Eden |
Journal | Peptides
(Peptides)
Vol. 15
Issue 7
Pg. 1229-36
( 1994)
ISSN: 0196-9781 [Print] United States |
PMID | 7854974
(Publication Type: Journal Article)
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Chemical References |
- DNA Primers
- DNA, Neoplasm
- RNA, Messenger
- Receptors, Somatostatin
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Topics |
- Animals
- Base Sequence
- Breast Neoplasms
(genetics, metabolism)
- DNA Primers
(genetics)
- DNA, Neoplasm
(genetics)
- Female
- Gastrointestinal Neoplasms
(genetics, metabolism)
- Gene Expression
- Humans
- In Vitro Techniques
- Kinetics
- Lung Neoplasms
(genetics, metabolism)
- Male
- Melanoma
(genetics, metabolism)
- Mice
- Molecular Sequence Data
- Neoplasms
(genetics, metabolism)
- Polymerase Chain Reaction
- Prostatic Neoplasms
(genetics, metabolism)
- RNA, Messenger
(genetics, metabolism)
- Rats
- Receptors, Somatostatin
(classification, genetics, metabolism)
- Tumor Cells, Cultured
(metabolism)
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