Characteristics of parathyroid hormone-1 receptor agonists and antagonists
Parathyroid hormone-1 receptor (PTH1R) is a member of B G protein-coupled receptors. The agonistic activation of the PTH1R results in the production and secretion of osteoclast-stimulating cytokines while antagonists may be used to treat bone metastases, hypercalcemia, cachexia and hyperparathyroidi...
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| Veröffentlicht in: | Future medicinal chemistry 2019-04, Vol.11 (8), p.817-831 |
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| container_title | Future medicinal chemistry |
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| creator | Zhong, Yanwen Li, Xuanyi Zhu, Dongji Zhao, Ningjing Yao, Hequan Lin, Kejiang |
| description | Parathyroid hormone-1 receptor (PTH1R) is a member of B G protein-coupled receptors. The agonistic activation of the PTH1R results in the production and secretion of osteoclast-stimulating cytokines while antagonists may be used to treat bone metastases, hypercalcemia, cachexia and hyperparathyroidism.
We built pharmacophore models and investigated the characteristics of PTH1R agonists and antagonists. The agonist model consists of three hydrophobic points, one hydrogen bond acceptor and one positive ionizable point. The antagonist model consists of one hydrogen bond donor and three hydrophobic points.
The features of the two models are similar, but the hydrogen bond acceptor, which is the main difference between PTH1R agonists and antagonists, suggests it may be essential for the agonist. |
| doi_str_mv | 10.4155/fmc-2018-0508 |
| format | Article |
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We built pharmacophore models and investigated the characteristics of PTH1R agonists and antagonists. The agonist model consists of three hydrophobic points, one hydrogen bond acceptor and one positive ionizable point. The antagonist model consists of one hydrogen bond donor and three hydrophobic points.
The features of the two models are similar, but the hydrogen bond acceptor, which is the main difference between PTH1R agonists and antagonists, suggests it may be essential for the agonist.</description><identifier>ISSN: 1756-8919</identifier><identifier>EISSN: 1756-8927</identifier><identifier>DOI: 10.4155/fmc-2018-0508</identifier><identifier>PMID: 30998079</identifier><language>eng</language><publisher>England: Future Science Ltd</publisher><subject>agonist ; Agonists ; Amino Acid Sequence ; Animals ; antagonist ; Biological activity ; Cachexia ; Cytokines ; Drug Design ; Enzymes ; G protein-coupled receptors ; Humans ; Hydrogen ; Hydrogen Bonding ; Hydrogen bonds ; Hydrophobic and Hydrophilic Interactions ; Hydrophobicity ; Hypercalcemia ; Hyperparathyroidism ; Hypotheses ; Metastases ; Molecular Docking Simulation ; Osteoporosis ; Parathyroid ; Parathyroid hormone ; parathyroid hormone-1 receptor (PTH1R) ; pharmacophore ; Polypeptides ; Receptor, Parathyroid Hormone, Type 1 - agonists ; Receptor, Parathyroid Hormone, Type 1 - antagonists & inhibitors ; Receptor, Parathyroid Hormone, Type 1 - chemistry ; Receptor, Parathyroid Hormone, Type 1 - metabolism</subject><ispartof>Future medicinal chemistry, 2019-04, Vol.11 (8), p.817-831</ispartof><rights>2019 Newlands Press</rights><rights>Copyright Newlands Press Apr 2019</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c371t-9a89be515410c19405090b4fbe3a8c36bbc2b9e19f764cb00d261da1240d44103</citedby><cites>FETCH-LOGICAL-c371t-9a89be515410c19405090b4fbe3a8c36bbc2b9e19f764cb00d261da1240d44103</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27903,27904</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/30998079$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Zhong, Yanwen</creatorcontrib><creatorcontrib>Li, Xuanyi</creatorcontrib><creatorcontrib>Zhu, Dongji</creatorcontrib><creatorcontrib>Zhao, Ningjing</creatorcontrib><creatorcontrib>Yao, Hequan</creatorcontrib><creatorcontrib>Lin, Kejiang</creatorcontrib><title>Characteristics of parathyroid hormone-1 receptor agonists and antagonists</title><title>Future medicinal chemistry</title><addtitle>Future Med Chem</addtitle><description>Parathyroid hormone-1 receptor (PTH1R) is a member of B G protein-coupled receptors. The agonistic activation of the PTH1R results in the production and secretion of osteoclast-stimulating cytokines while antagonists may be used to treat bone metastases, hypercalcemia, cachexia and hyperparathyroidism.
We built pharmacophore models and investigated the characteristics of PTH1R agonists and antagonists. The agonist model consists of three hydrophobic points, one hydrogen bond acceptor and one positive ionizable point. The antagonist model consists of one hydrogen bond donor and three hydrophobic points.
The features of the two models are similar, but the hydrogen bond acceptor, which is the main difference between PTH1R agonists and antagonists, suggests it may be essential for the agonist.</description><subject>agonist</subject><subject>Agonists</subject><subject>Amino Acid Sequence</subject><subject>Animals</subject><subject>antagonist</subject><subject>Biological activity</subject><subject>Cachexia</subject><subject>Cytokines</subject><subject>Drug Design</subject><subject>Enzymes</subject><subject>G protein-coupled receptors</subject><subject>Humans</subject><subject>Hydrogen</subject><subject>Hydrogen Bonding</subject><subject>Hydrogen bonds</subject><subject>Hydrophobic and Hydrophilic Interactions</subject><subject>Hydrophobicity</subject><subject>Hypercalcemia</subject><subject>Hyperparathyroidism</subject><subject>Hypotheses</subject><subject>Metastases</subject><subject>Molecular Docking Simulation</subject><subject>Osteoporosis</subject><subject>Parathyroid</subject><subject>Parathyroid hormone</subject><subject>parathyroid hormone-1 receptor (PTH1R)</subject><subject>pharmacophore</subject><subject>Polypeptides</subject><subject>Receptor, Parathyroid Hormone, Type 1 - agonists</subject><subject>Receptor, Parathyroid Hormone, Type 1 - antagonists & inhibitors</subject><subject>Receptor, Parathyroid Hormone, Type 1 - chemistry</subject><subject>Receptor, Parathyroid Hormone, Type 1 - metabolism</subject><issn>1756-8919</issn><issn>1756-8927</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>AZQEC</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><sourceid>DWQXO</sourceid><sourceid>GNUQQ</sourceid><recordid>eNp1kL1rwzAQxUVpaUKasWsxdOniVifLHxpL6CeBLu0sJPncOMSWK9lD_vvKOMlQqODQ3fG7x-MRcg30nkOaPlSNiRmFIqYpLc7IHPI0iwvB8vNTD2JGlt5vaXgJK0SWXpJZQoUoaC7m5H21UU6ZHl3t-9r4yFZRFzb9Zu9sXUYb6xrbYgyRQ4Ndb12kvm0bYB-ptgzVH-crclGpncfl4V-Qr-enz9VrvP54eVs9rmOT5NDHQhVCYwopB2pA8GBdUM0rjYkqTJJpbZgWCKLKM240pSXLoFTAOC15uEkW5G7S7Zz9GdD3sqm9wd1OtWgHLxkDSBijggf09g-6tYNrgzvJggOaF0BHKp4o46z3DivZubpRbi-ByjFnGXKWY85yzDnwNwfVQTdYnuhjqgEQE1AN_eDQmxpbg3KawkVt6hb_Ef8F2EeLHA</recordid><startdate>20190401</startdate><enddate>20190401</enddate><creator>Zhong, Yanwen</creator><creator>Li, Xuanyi</creator><creator>Zhu, Dongji</creator><creator>Zhao, Ningjing</creator><creator>Yao, Hequan</creator><creator>Lin, Kejiang</creator><general>Future Science Ltd</general><general>Newlands Press</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>3V.</scope><scope>7X7</scope><scope>7XB</scope><scope>8FE</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABUWG</scope><scope>AFKRA</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BHPHI</scope><scope>CCPQU</scope><scope>DWQXO</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>LK8</scope><scope>M0S</scope><scope>M7P</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>7X8</scope></search><sort><creationdate>20190401</creationdate><title>Characteristics of parathyroid hormone-1 receptor agonists and antagonists</title><author>Zhong, Yanwen ; Li, Xuanyi ; Zhu, Dongji ; Zhao, Ningjing ; Yao, Hequan ; Lin, Kejiang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c371t-9a89be515410c19405090b4fbe3a8c36bbc2b9e19f764cb00d261da1240d44103</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>agonist</topic><topic>Agonists</topic><topic>Amino Acid Sequence</topic><topic>Animals</topic><topic>antagonist</topic><topic>Biological activity</topic><topic>Cachexia</topic><topic>Cytokines</topic><topic>Drug Design</topic><topic>Enzymes</topic><topic>G protein-coupled receptors</topic><topic>Humans</topic><topic>Hydrogen</topic><topic>Hydrogen Bonding</topic><topic>Hydrogen bonds</topic><topic>Hydrophobic and Hydrophilic Interactions</topic><topic>Hydrophobicity</topic><topic>Hypercalcemia</topic><topic>Hyperparathyroidism</topic><topic>Hypotheses</topic><topic>Metastases</topic><topic>Molecular Docking Simulation</topic><topic>Osteoporosis</topic><topic>Parathyroid</topic><topic>Parathyroid hormone</topic><topic>parathyroid hormone-1 receptor (PTH1R)</topic><topic>pharmacophore</topic><topic>Polypeptides</topic><topic>Receptor, Parathyroid Hormone, Type 1 - agonists</topic><topic>Receptor, Parathyroid Hormone, Type 1 - antagonists & inhibitors</topic><topic>Receptor, Parathyroid Hormone, Type 1 - chemistry</topic><topic>Receptor, Parathyroid Hormone, Type 1 - metabolism</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zhong, Yanwen</creatorcontrib><creatorcontrib>Li, Xuanyi</creatorcontrib><creatorcontrib>Zhu, Dongji</creatorcontrib><creatorcontrib>Zhao, Ningjing</creatorcontrib><creatorcontrib>Yao, Hequan</creatorcontrib><creatorcontrib>Lin, Kejiang</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>ProQuest Central (Corporate)</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest Central UK/Ireland</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Natural Science Collection</collection><collection>ProQuest One Community College</collection><collection>ProQuest Central Korea</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>ProQuest Biological Science Collection</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Biological Science Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>MEDLINE - Academic</collection><jtitle>Future medicinal chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zhong, Yanwen</au><au>Li, Xuanyi</au><au>Zhu, Dongji</au><au>Zhao, Ningjing</au><au>Yao, Hequan</au><au>Lin, Kejiang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Characteristics of parathyroid hormone-1 receptor agonists and antagonists</atitle><jtitle>Future medicinal chemistry</jtitle><addtitle>Future Med Chem</addtitle><date>2019-04-01</date><risdate>2019</risdate><volume>11</volume><issue>8</issue><spage>817</spage><epage>831</epage><pages>817-831</pages><issn>1756-8919</issn><eissn>1756-8927</eissn><abstract>Parathyroid hormone-1 receptor (PTH1R) is a member of B G protein-coupled receptors. The agonistic activation of the PTH1R results in the production and secretion of osteoclast-stimulating cytokines while antagonists may be used to treat bone metastases, hypercalcemia, cachexia and hyperparathyroidism.
We built pharmacophore models and investigated the characteristics of PTH1R agonists and antagonists. The agonist model consists of three hydrophobic points, one hydrogen bond acceptor and one positive ionizable point. The antagonist model consists of one hydrogen bond donor and three hydrophobic points.
The features of the two models are similar, but the hydrogen bond acceptor, which is the main difference between PTH1R agonists and antagonists, suggests it may be essential for the agonist.</abstract><cop>England</cop><pub>Future Science Ltd</pub><pmid>30998079</pmid><doi>10.4155/fmc-2018-0508</doi><tpages>15</tpages></addata></record> |
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| subjects | agonist Agonists Amino Acid Sequence Animals antagonist Biological activity Cachexia Cytokines Drug Design Enzymes G protein-coupled receptors Humans Hydrogen Hydrogen Bonding Hydrogen bonds Hydrophobic and Hydrophilic Interactions Hydrophobicity Hypercalcemia Hyperparathyroidism Hypotheses Metastases Molecular Docking Simulation Osteoporosis Parathyroid Parathyroid hormone parathyroid hormone-1 receptor (PTH1R) pharmacophore Polypeptides Receptor, Parathyroid Hormone, Type 1 - agonists Receptor, Parathyroid Hormone, Type 1 - antagonists & inhibitors Receptor, Parathyroid Hormone, Type 1 - chemistry Receptor, Parathyroid Hormone, Type 1 - metabolism |
| title | Characteristics of parathyroid hormone-1 receptor agonists and antagonists |
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