Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor
Using a genomics-based reverse pharmacological approach for screening orphan G-protein coupled receptors, we have identified and cloned a novel high-affinity histamine receptor. This receptor, termed AXOR35, is most closely related to the H3 histamine receptor, sharing 37% protein sequence identity....
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| Veröffentlicht in: | Molecular pharmacology 2001-03, Vol.59 (3), p.434-441 |
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| container_title | Molecular pharmacology |
| container_volume | 59 |
| creator | Zhu, Y Michalovich, D Wu, H Tan, K B Dytko, G M Mannan, I J Boyce, R Alston, J Tierney, L A Li, X Herrity, N C Vawter, L Sarau, H M Ames, R S Davenport, C M Hieble, J P Wilson, S Bergsma, D J Fitzgerald, L R |
| description | Using a genomics-based reverse pharmacological approach for screening orphan G-protein coupled receptors, we have identified
and cloned a novel high-affinity histamine receptor. This receptor, termed AXOR35, is most closely related to the H3 histamine
receptor, sharing 37% protein sequence identity. A multiple responsive element/cyclic AMP-responsive element-luciferase reporter
assay was used to identify histamine as a ligand for AXOR35. When transfected into human embryonic kidney 293 cells, the AXOR35
receptor showed a strong, dose-dependent calcium mobilization response to histamine and H3 receptor agonists including imetit
and immepip. Radioligand binding confirmed that the AXOR35 receptor was a high-affinity histamine receptor. The pharmacology
of the AXOR35 receptor was found to closely resemble that of the H3 receptor; the major difference was that ( R )-α-methylhistamine was a low potency agonist of the AXOR35 receptor. Thioperamide is an antagonist at AXOR 35. Expression
of AXOR35 mRNA in human tissues is highest in peripheral blood mononuclear cells and in tissues likely to contain high concentrations
of blood cells, such as bone marrow and lung. In situ hybridization analysis of a wide survey of mouse tissues showed that
mouse AXOR35 mRNA is selectively expressed in hippocampus. The identification and localization of this new histamine receptor
will expand our understanding of the physiological and pathological roles of histamine and may provide additional opportunities
for pharmacological modification of these actions. |
| doi_str_mv | 10.1124/mol.59.3.434 |
| format | Article |
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and cloned a novel high-affinity histamine receptor. This receptor, termed AXOR35, is most closely related to the H3 histamine
receptor, sharing 37% protein sequence identity. A multiple responsive element/cyclic AMP-responsive element-luciferase reporter
assay was used to identify histamine as a ligand for AXOR35. When transfected into human embryonic kidney 293 cells, the AXOR35
receptor showed a strong, dose-dependent calcium mobilization response to histamine and H3 receptor agonists including imetit
and immepip. Radioligand binding confirmed that the AXOR35 receptor was a high-affinity histamine receptor. The pharmacology
of the AXOR35 receptor was found to closely resemble that of the H3 receptor; the major difference was that ( R )-α-methylhistamine was a low potency agonist of the AXOR35 receptor. Thioperamide is an antagonist at AXOR 35. Expression
of AXOR35 mRNA in human tissues is highest in peripheral blood mononuclear cells and in tissues likely to contain high concentrations
of blood cells, such as bone marrow and lung. In situ hybridization analysis of a wide survey of mouse tissues showed that
mouse AXOR35 mRNA is selectively expressed in hippocampus. The identification and localization of this new histamine receptor
will expand our understanding of the physiological and pathological roles of histamine and may provide additional opportunities
for pharmacological modification of these actions.</description><identifier>ISSN: 0026-895X</identifier><identifier>EISSN: 1521-0111</identifier><identifier>DOI: 10.1124/mol.59.3.434</identifier><identifier>PMID: 11179436</identifier><language>eng</language><publisher>United States: American Society for Pharmacology and Experimental Therapeutics</publisher><subject>Amino Acid Sequence ; Animals ; Calcium - metabolism ; Cloning, Molecular ; Dose-Response Relationship, Drug ; Gene Expression ; Genes, Reporter ; Histamine - metabolism ; Humans ; Luciferases ; Mice ; Molecular Sequence Data ; Radioligand Assay ; Receptors, Histamine - genetics ; Receptors, Histamine - metabolism ; Receptors, Histamine H3 - chemistry ; Receptors, Histamine H3 - metabolism ; Sequence Homology, Amino Acid ; Tissue Distribution ; Tritium</subject><ispartof>Molecular pharmacology, 2001-03, Vol.59 (3), p.434-441</ispartof><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c383t-c6fb28a73ca68cbf6fa5ac81218ac1a25110e76501ece5970616bbe1b8c99b643</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11179436$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Zhu, Y</creatorcontrib><creatorcontrib>Michalovich, D</creatorcontrib><creatorcontrib>Wu, H</creatorcontrib><creatorcontrib>Tan, K B</creatorcontrib><creatorcontrib>Dytko, G M</creatorcontrib><creatorcontrib>Mannan, I J</creatorcontrib><creatorcontrib>Boyce, R</creatorcontrib><creatorcontrib>Alston, J</creatorcontrib><creatorcontrib>Tierney, L A</creatorcontrib><creatorcontrib>Li, X</creatorcontrib><creatorcontrib>Herrity, N C</creatorcontrib><creatorcontrib>Vawter, L</creatorcontrib><creatorcontrib>Sarau, H M</creatorcontrib><creatorcontrib>Ames, R S</creatorcontrib><creatorcontrib>Davenport, C M</creatorcontrib><creatorcontrib>Hieble, J P</creatorcontrib><creatorcontrib>Wilson, S</creatorcontrib><creatorcontrib>Bergsma, D J</creatorcontrib><creatorcontrib>Fitzgerald, L R</creatorcontrib><title>Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor</title><title>Molecular pharmacology</title><addtitle>Mol Pharmacol</addtitle><description>Using a genomics-based reverse pharmacological approach for screening orphan G-protein coupled receptors, we have identified
and cloned a novel high-affinity histamine receptor. This receptor, termed AXOR35, is most closely related to the H3 histamine
receptor, sharing 37% protein sequence identity. A multiple responsive element/cyclic AMP-responsive element-luciferase reporter
assay was used to identify histamine as a ligand for AXOR35. When transfected into human embryonic kidney 293 cells, the AXOR35
receptor showed a strong, dose-dependent calcium mobilization response to histamine and H3 receptor agonists including imetit
and immepip. Radioligand binding confirmed that the AXOR35 receptor was a high-affinity histamine receptor. The pharmacology
of the AXOR35 receptor was found to closely resemble that of the H3 receptor; the major difference was that ( R )-α-methylhistamine was a low potency agonist of the AXOR35 receptor. Thioperamide is an antagonist at AXOR 35. Expression
of AXOR35 mRNA in human tissues is highest in peripheral blood mononuclear cells and in tissues likely to contain high concentrations
of blood cells, such as bone marrow and lung. In situ hybridization analysis of a wide survey of mouse tissues showed that
mouse AXOR35 mRNA is selectively expressed in hippocampus. The identification and localization of this new histamine receptor
will expand our understanding of the physiological and pathological roles of histamine and may provide additional opportunities
for pharmacological modification of these actions.</description><subject>Amino Acid Sequence</subject><subject>Animals</subject><subject>Calcium - metabolism</subject><subject>Cloning, Molecular</subject><subject>Dose-Response Relationship, Drug</subject><subject>Gene Expression</subject><subject>Genes, Reporter</subject><subject>Histamine - metabolism</subject><subject>Humans</subject><subject>Luciferases</subject><subject>Mice</subject><subject>Molecular Sequence Data</subject><subject>Radioligand Assay</subject><subject>Receptors, Histamine - genetics</subject><subject>Receptors, Histamine - metabolism</subject><subject>Receptors, Histamine H3 - chemistry</subject><subject>Receptors, Histamine H3 - metabolism</subject><subject>Sequence Homology, Amino Acid</subject><subject>Tissue Distribution</subject><subject>Tritium</subject><issn>0026-895X</issn><issn>1521-0111</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpFkM9r2zAUgMVoWbN2t52HLu0pzvQsS5aPw6TNILRltLDLEM-qnGjYlic5_fXXTyOBnB6P973v8BHyBdgCIC--9b5biGrBFwUvPpAZiBwyBgAnZMZYLjNViV9n5FOMfxiDQij2kZylc1kVXM7I77rzgxs2c7p8HYON0flhTnF4ovdbDD0a3_mNM9jROu1oJhvcO06Jor6lSG_9s-3oatfjQFcuTti7wdKf1thx8uGCnLbYRfv5MM_J4_XyoV5l67ubH_X3dWa44lNmZNvkCktuUCrTtLJFgUZBDgoNYC4AmC2lYJC8oiqZBNk0FhplqqqRBT8nV3vvGPzfnY2T7l00tutwsH4XdfrIVZnzBM73oAk-xmBbPQbXY3jTwPT_nDrl1KLSXKecCf968O6a3j4d4UO_BFzuga3bbF9csHo8Zns7iv4B35Z-oA</recordid><startdate>20010301</startdate><enddate>20010301</enddate><creator>Zhu, Y</creator><creator>Michalovich, D</creator><creator>Wu, H</creator><creator>Tan, K B</creator><creator>Dytko, G M</creator><creator>Mannan, I J</creator><creator>Boyce, R</creator><creator>Alston, J</creator><creator>Tierney, L A</creator><creator>Li, X</creator><creator>Herrity, N C</creator><creator>Vawter, L</creator><creator>Sarau, H M</creator><creator>Ames, R S</creator><creator>Davenport, C M</creator><creator>Hieble, J P</creator><creator>Wilson, S</creator><creator>Bergsma, D J</creator><creator>Fitzgerald, L R</creator><general>American Society for Pharmacology and Experimental Therapeutics</general><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>20010301</creationdate><title>Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor</title><author>Zhu, Y ; Michalovich, D ; Wu, H ; Tan, K B ; Dytko, G M ; Mannan, I J ; Boyce, R ; Alston, J ; Tierney, L A ; Li, X ; Herrity, N C ; Vawter, L ; Sarau, H M ; Ames, R S ; Davenport, C M ; Hieble, J P ; Wilson, S ; Bergsma, D J ; Fitzgerald, L R</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c383t-c6fb28a73ca68cbf6fa5ac81218ac1a25110e76501ece5970616bbe1b8c99b643</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Amino Acid Sequence</topic><topic>Animals</topic><topic>Calcium - metabolism</topic><topic>Cloning, Molecular</topic><topic>Dose-Response Relationship, Drug</topic><topic>Gene Expression</topic><topic>Genes, Reporter</topic><topic>Histamine - metabolism</topic><topic>Humans</topic><topic>Luciferases</topic><topic>Mice</topic><topic>Molecular Sequence Data</topic><topic>Radioligand Assay</topic><topic>Receptors, Histamine - genetics</topic><topic>Receptors, Histamine - metabolism</topic><topic>Receptors, Histamine H3 - chemistry</topic><topic>Receptors, Histamine H3 - metabolism</topic><topic>Sequence Homology, Amino Acid</topic><topic>Tissue Distribution</topic><topic>Tritium</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhu, Y</creatorcontrib><creatorcontrib>Michalovich, D</creatorcontrib><creatorcontrib>Wu, H</creatorcontrib><creatorcontrib>Tan, K B</creatorcontrib><creatorcontrib>Dytko, G M</creatorcontrib><creatorcontrib>Mannan, I J</creatorcontrib><creatorcontrib>Boyce, R</creatorcontrib><creatorcontrib>Alston, J</creatorcontrib><creatorcontrib>Tierney, L A</creatorcontrib><creatorcontrib>Li, X</creatorcontrib><creatorcontrib>Herrity, N C</creatorcontrib><creatorcontrib>Vawter, L</creatorcontrib><creatorcontrib>Sarau, H M</creatorcontrib><creatorcontrib>Ames, R S</creatorcontrib><creatorcontrib>Davenport, C M</creatorcontrib><creatorcontrib>Hieble, J P</creatorcontrib><creatorcontrib>Wilson, S</creatorcontrib><creatorcontrib>Bergsma, D J</creatorcontrib><creatorcontrib>Fitzgerald, L R</creatorcontrib><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>Molecular pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhu, Y</au><au>Michalovich, D</au><au>Wu, H</au><au>Tan, K B</au><au>Dytko, G M</au><au>Mannan, I J</au><au>Boyce, R</au><au>Alston, J</au><au>Tierney, L A</au><au>Li, X</au><au>Herrity, N C</au><au>Vawter, L</au><au>Sarau, H M</au><au>Ames, R S</au><au>Davenport, C M</au><au>Hieble, J P</au><au>Wilson, S</au><au>Bergsma, D J</au><au>Fitzgerald, L R</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor</atitle><jtitle>Molecular pharmacology</jtitle><addtitle>Mol Pharmacol</addtitle><date>2001-03-01</date><risdate>2001</risdate><volume>59</volume><issue>3</issue><spage>434</spage><epage>441</epage><pages>434-441</pages><issn>0026-895X</issn><eissn>1521-0111</eissn><abstract>Using a genomics-based reverse pharmacological approach for screening orphan G-protein coupled receptors, we have identified
and cloned a novel high-affinity histamine receptor. This receptor, termed AXOR35, is most closely related to the H3 histamine
receptor, sharing 37% protein sequence identity. A multiple responsive element/cyclic AMP-responsive element-luciferase reporter
assay was used to identify histamine as a ligand for AXOR35. When transfected into human embryonic kidney 293 cells, the AXOR35
receptor showed a strong, dose-dependent calcium mobilization response to histamine and H3 receptor agonists including imetit
and immepip. Radioligand binding confirmed that the AXOR35 receptor was a high-affinity histamine receptor. The pharmacology
of the AXOR35 receptor was found to closely resemble that of the H3 receptor; the major difference was that ( R )-α-methylhistamine was a low potency agonist of the AXOR35 receptor. Thioperamide is an antagonist at AXOR 35. Expression
of AXOR35 mRNA in human tissues is highest in peripheral blood mononuclear cells and in tissues likely to contain high concentrations
of blood cells, such as bone marrow and lung. In situ hybridization analysis of a wide survey of mouse tissues showed that
mouse AXOR35 mRNA is selectively expressed in hippocampus. The identification and localization of this new histamine receptor
will expand our understanding of the physiological and pathological roles of histamine and may provide additional opportunities
for pharmacological modification of these actions.</abstract><cop>United States</cop><pub>American Society for Pharmacology and Experimental Therapeutics</pub><pmid>11179436</pmid><doi>10.1124/mol.59.3.434</doi><tpages>8</tpages></addata></record> |
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| ispartof | Molecular pharmacology, 2001-03, Vol.59 (3), p.434-441 |
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| source | MEDLINE; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; Free Full-Text Journals in Chemistry |
| subjects | Amino Acid Sequence Animals Calcium - metabolism Cloning, Molecular Dose-Response Relationship, Drug Gene Expression Genes, Reporter Histamine - metabolism Humans Luciferases Mice Molecular Sequence Data Radioligand Assay Receptors, Histamine - genetics Receptors, Histamine - metabolism Receptors, Histamine H3 - chemistry Receptors, Histamine H3 - metabolism Sequence Homology, Amino Acid Tissue Distribution Tritium |
| title | Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor |
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