Human malignant melanoma cells express high-affinity receptors for melatonin: antiproliferative effects of melatonin and 6-chloromelatonin
In order to explore the potential oncostatic properties of the pineal hormone, melatonin, we have investigated its binding characteristics and functional effects in a human malignant melanoma (M-6) cell line. Binding studies in M-6 membranes showed the coexistence of 2-[ 125I]iodomelatonin binding s...
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| Veröffentlicht in: | European journal of pharmacology 1993-07, Vol.246 (2), p.89-96 |
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| container_end_page | 96 |
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| container_title | European journal of pharmacology |
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| creator | Ying, Shui-Wang Niles, Lennard P. Crocker, Candice |
| description | In order to explore the potential oncostatic properties of the pineal hormone, melatonin, we have investigated its binding characteristics and functional effects in a human malignant melanoma (M-6) cell line. Binding studies in M-6 membranes showed the coexistence of 2-[
125I]iodomelatonin binding sites with picomolar and nanomolar affinities. Guanine nucleotides caused conversion of all high-affinity sites to a low-affinity state without a change in binding capacity. Melatonin induced a marked concentration-dependent reduction in forskolin-stimulated cAMP accumulation in intact M-6 cells, indicating that it binds to a functional receptor in this cell line. The in vitro proliferation of M-6 cells was significantly inhibited by melatonin and its analogues 6-chloromelatonin, and 2-iodomelatonin, at concentrations ranging from 10
−9 to 10
−4 M, as demonstrated by cell counts and measurements of DNA content. These findings indicate that M-6 cells express functional receptors for melatonin which may be involved in mediating the antiproliferative effects of this hormone. |
| doi_str_mv | 10.1016/0922-4106(93)90084-M |
| format | Article |
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125I]iodomelatonin binding sites with picomolar and nanomolar affinities. Guanine nucleotides caused conversion of all high-affinity sites to a low-affinity state without a change in binding capacity. Melatonin induced a marked concentration-dependent reduction in forskolin-stimulated cAMP accumulation in intact M-6 cells, indicating that it binds to a functional receptor in this cell line. The in vitro proliferation of M-6 cells was significantly inhibited by melatonin and its analogues 6-chloromelatonin, and 2-iodomelatonin, at concentrations ranging from 10
−9 to 10
−4 M, as demonstrated by cell counts and measurements of DNA content. These findings indicate that M-6 cells express functional receptors for melatonin which may be involved in mediating the antiproliferative effects of this hormone.</description><identifier>ISSN: 0922-4106</identifier><identifier>ISSN: 0014-2999</identifier><identifier>DOI: 10.1016/0922-4106(93)90084-M</identifier><identifier>PMID: 8397097</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>2-Iodomelatonin ; 6-Chloromelatonin ; Adenylyl Cyclase Inhibitors ; Antineoplastic agents ; Biological and medical sciences ; cAMP ; Cell Division - drug effects ; Cell Membrane - metabolism ; Chemotherapy ; Colforsin - pharmacology ; Cyclic AMP - metabolism ; Cytostatic activity ; DNA, Neoplasm - biosynthesis ; Humans ; Indoles - pharmacology ; Iodine Radioisotopes ; Kinetics ; Medical sciences ; Melanoma - metabolism ; Melatonin ; Melatonin - analogs & derivatives ; Melatonin - pharmacology ; Melatonin receptors, Melanoma cells (Human) ; Nucleotides - pharmacology ; Pharmacology. Drug treatments ; Receptors, Melatonin ; Receptors, Neurotransmitter - biosynthesis ; Receptors, Neurotransmitter - metabolism ; Tumor Cells, Cultured - drug effects ; Tumor Cells, Cultured - metabolism</subject><ispartof>European journal of pharmacology, 1993-07, Vol.246 (2), p.89-96</ispartof><rights>1993</rights><rights>1993 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-4c7ab0c5574b63df25284069b724e046b0da923cff8c1f24025c4269534914da3</citedby><cites>FETCH-LOGICAL-c386t-4c7ab0c5574b63df25284069b724e046b0da923cff8c1f24025c4269534914da3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=4869499$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8397097$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ying, Shui-Wang</creatorcontrib><creatorcontrib>Niles, Lennard P.</creatorcontrib><creatorcontrib>Crocker, Candice</creatorcontrib><title>Human malignant melanoma cells express high-affinity receptors for melatonin: antiproliferative effects of melatonin and 6-chloromelatonin</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>In order to explore the potential oncostatic properties of the pineal hormone, melatonin, we have investigated its binding characteristics and functional effects in a human malignant melanoma (M-6) cell line. Binding studies in M-6 membranes showed the coexistence of 2-[
125I]iodomelatonin binding sites with picomolar and nanomolar affinities. Guanine nucleotides caused conversion of all high-affinity sites to a low-affinity state without a change in binding capacity. Melatonin induced a marked concentration-dependent reduction in forskolin-stimulated cAMP accumulation in intact M-6 cells, indicating that it binds to a functional receptor in this cell line. The in vitro proliferation of M-6 cells was significantly inhibited by melatonin and its analogues 6-chloromelatonin, and 2-iodomelatonin, at concentrations ranging from 10
−9 to 10
−4 M, as demonstrated by cell counts and measurements of DNA content. These findings indicate that M-6 cells express functional receptors for melatonin which may be involved in mediating the antiproliferative effects of this hormone.</description><subject>2-Iodomelatonin</subject><subject>6-Chloromelatonin</subject><subject>Adenylyl Cyclase Inhibitors</subject><subject>Antineoplastic agents</subject><subject>Biological and medical sciences</subject><subject>cAMP</subject><subject>Cell Division - drug effects</subject><subject>Cell Membrane - metabolism</subject><subject>Chemotherapy</subject><subject>Colforsin - pharmacology</subject><subject>Cyclic AMP - metabolism</subject><subject>Cytostatic activity</subject><subject>DNA, Neoplasm - biosynthesis</subject><subject>Humans</subject><subject>Indoles - pharmacology</subject><subject>Iodine Radioisotopes</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Melanoma - metabolism</subject><subject>Melatonin</subject><subject>Melatonin - analogs & derivatives</subject><subject>Melatonin - pharmacology</subject><subject>Melatonin receptors, Melanoma cells (Human)</subject><subject>Nucleotides - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Receptors, Melatonin</subject><subject>Receptors, Neurotransmitter - biosynthesis</subject><subject>Receptors, Neurotransmitter - metabolism</subject><subject>Tumor Cells, Cultured - drug effects</subject><subject>Tumor Cells, Cultured - metabolism</subject><issn>0922-4106</issn><issn>0014-2999</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1993</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFu1DAQhn0AldLyBiD5gBA9pExsx4k5VEJVoUituMDZcpxx1yixF9tb0VfoU9fbXS03TpZmvv_X-CPkbQvnLbTyEyjGGtGC_Kj4mQIYRHP7ghwfxq_I65x_A4BqlTgiRwNXPaj-mDxebxYT6GJmfxdMKHTB2YS4GGpxnjPFv-uEOdOVv1s1xjkffHmgCS2uS0yZupieIyUGHz7T2uDXKc7eYTLF3yNF59CWTKP7x1VsorKxqzmmeJiekpfOzBnf7N8T8uvr1c_L6-bmx7fvl19uGssHWRphezOC7bpejJJPjnVsECDV2DOBIOQIk1GMW-cG2zomgHVWMKk6LlQrJsNPyIddbz30zwZz0YvP29-agHGTdd8pyYHxCoodaFPMOaHT6-QXkx50C3qrXW_96q1frbh-1q5va-zdvn8zLjgdQnvndf9-vzfZmtklE6zPB0wMUgmlKnaxw7C6uPeYdLYeg8XJV_1FT9H__44nh2qjRw</recordid><startdate>19930715</startdate><enddate>19930715</enddate><creator>Ying, Shui-Wang</creator><creator>Niles, Lennard P.</creator><creator>Crocker, Candice</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19930715</creationdate><title>Human malignant melanoma cells express high-affinity receptors for melatonin: antiproliferative effects of melatonin and 6-chloromelatonin</title><author>Ying, Shui-Wang ; Niles, Lennard P. ; Crocker, Candice</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-4c7ab0c5574b63df25284069b724e046b0da923cff8c1f24025c4269534914da3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1993</creationdate><topic>2-Iodomelatonin</topic><topic>6-Chloromelatonin</topic><topic>Adenylyl Cyclase Inhibitors</topic><topic>Antineoplastic agents</topic><topic>Biological and medical sciences</topic><topic>cAMP</topic><topic>Cell Division - drug effects</topic><topic>Cell Membrane - metabolism</topic><topic>Chemotherapy</topic><topic>Colforsin - pharmacology</topic><topic>Cyclic AMP - metabolism</topic><topic>Cytostatic activity</topic><topic>DNA, Neoplasm - biosynthesis</topic><topic>Humans</topic><topic>Indoles - pharmacology</topic><topic>Iodine Radioisotopes</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Melanoma - metabolism</topic><topic>Melatonin</topic><topic>Melatonin - analogs & derivatives</topic><topic>Melatonin - pharmacology</topic><topic>Melatonin receptors, Melanoma cells (Human)</topic><topic>Nucleotides - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Receptors, Melatonin</topic><topic>Receptors, Neurotransmitter - biosynthesis</topic><topic>Receptors, Neurotransmitter - metabolism</topic><topic>Tumor Cells, Cultured - drug effects</topic><topic>Tumor Cells, Cultured - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ying, Shui-Wang</creatorcontrib><creatorcontrib>Niles, Lennard P.</creatorcontrib><creatorcontrib>Crocker, Candice</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ying, Shui-Wang</au><au>Niles, Lennard P.</au><au>Crocker, Candice</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Human malignant melanoma cells express high-affinity receptors for melatonin: antiproliferative effects of melatonin and 6-chloromelatonin</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1993-07-15</date><risdate>1993</risdate><volume>246</volume><issue>2</issue><spage>89</spage><epage>96</epage><pages>89-96</pages><issn>0922-4106</issn><issn>0014-2999</issn><abstract>In order to explore the potential oncostatic properties of the pineal hormone, melatonin, we have investigated its binding characteristics and functional effects in a human malignant melanoma (M-6) cell line. Binding studies in M-6 membranes showed the coexistence of 2-[
125I]iodomelatonin binding sites with picomolar and nanomolar affinities. Guanine nucleotides caused conversion of all high-affinity sites to a low-affinity state without a change in binding capacity. Melatonin induced a marked concentration-dependent reduction in forskolin-stimulated cAMP accumulation in intact M-6 cells, indicating that it binds to a functional receptor in this cell line. The in vitro proliferation of M-6 cells was significantly inhibited by melatonin and its analogues 6-chloromelatonin, and 2-iodomelatonin, at concentrations ranging from 10
−9 to 10
−4 M, as demonstrated by cell counts and measurements of DNA content. These findings indicate that M-6 cells express functional receptors for melatonin which may be involved in mediating the antiproliferative effects of this hormone.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>8397097</pmid><doi>10.1016/0922-4106(93)90084-M</doi><tpages>8</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1993-07, Vol.246 (2), p.89-96 |
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| source | MEDLINE; Elsevier ScienceDirect Journals; Alma/SFX Local Collection |
| subjects | 2-Iodomelatonin 6-Chloromelatonin Adenylyl Cyclase Inhibitors Antineoplastic agents Biological and medical sciences cAMP Cell Division - drug effects Cell Membrane - metabolism Chemotherapy Colforsin - pharmacology Cyclic AMP - metabolism Cytostatic activity DNA, Neoplasm - biosynthesis Humans Indoles - pharmacology Iodine Radioisotopes Kinetics Medical sciences Melanoma - metabolism Melatonin Melatonin - analogs & derivatives Melatonin - pharmacology Melatonin receptors, Melanoma cells (Human) Nucleotides - pharmacology Pharmacology. Drug treatments Receptors, Melatonin Receptors, Neurotransmitter - biosynthesis Receptors, Neurotransmitter - metabolism Tumor Cells, Cultured - drug effects Tumor Cells, Cultured - metabolism |
| title | Human malignant melanoma cells express high-affinity receptors for melatonin: antiproliferative effects of melatonin and 6-chloromelatonin |
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