Designing Safer Analgesics via μ-Opioid Receptor Pathways
Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μO...
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| Veröffentlicht in: | Trends in pharmacological sciences (Regular ed.) 2017-11, Vol.38 (11), p.1016-1037 |
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| container_title | Trends in pharmacological sciences (Regular ed.) |
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| creator | Chan, H.C. Stephen McCarthy, Dillon Li, Jianing Palczewski, Krzysztof Yuan, Shuguang |
| description | Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μOR) and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics.
Pain is a major clinical and economic problem. Owing to the serious side effects associated with current painkillers, the discovery of less toxic medications is an imperative in both academia and industry.
Owing to recent advances in computational and structural biology, several μOR-mediated painkillers with fewer side effects have been successfully designed. |
| doi_str_mv | 10.1016/j.tips.2017.08.004 |
| format | Article |
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Pain is a major clinical and economic problem. Owing to the serious side effects associated with current painkillers, the discovery of less toxic medications is an imperative in both academia and industry.
Owing to recent advances in computational and structural biology, several μOR-mediated painkillers with fewer side effects have been successfully designed.</description><identifier>ISSN: 0165-6147</identifier><identifier>EISSN: 1873-3735</identifier><identifier>DOI: 10.1016/j.tips.2017.08.004</identifier><identifier>PMID: 28935293</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Analgesics, Opioid - chemistry ; Analgesics, Opioid - pharmacology ; Animals ; computational biology ; Drug Design ; drug discovery ; GPCR ; Humans ; opioid receptor ; Receptors, Opioid, mu - antagonists & inhibitors ; Receptors, Opioid, mu - chemistry ; Receptors, Opioid, mu - metabolism ; safer painkiller</subject><ispartof>Trends in pharmacological sciences (Regular ed.), 2017-11, Vol.38 (11), p.1016-1037</ispartof><rights>2017 Elsevier Ltd</rights><rights>Copyright © 2017 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c455t-77dcd96cc3c862586dedc3040f3b743a434bba41389fb8a4d62e98bf3991f7513</citedby><cites>FETCH-LOGICAL-c455t-77dcd96cc3c862586dedc3040f3b743a434bba41389fb8a4d62e98bf3991f7513</cites><orcidid>0000-0001-9858-4742</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.tips.2017.08.004$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>230,314,780,784,885,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/28935293$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Chan, H.C. Stephen</creatorcontrib><creatorcontrib>McCarthy, Dillon</creatorcontrib><creatorcontrib>Li, Jianing</creatorcontrib><creatorcontrib>Palczewski, Krzysztof</creatorcontrib><creatorcontrib>Yuan, Shuguang</creatorcontrib><title>Designing Safer Analgesics via μ-Opioid Receptor Pathways</title><title>Trends in pharmacological sciences (Regular ed.)</title><addtitle>Trends Pharmacol Sci</addtitle><description>Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μOR) and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics.
Pain is a major clinical and economic problem. Owing to the serious side effects associated with current painkillers, the discovery of less toxic medications is an imperative in both academia and industry.
Owing to recent advances in computational and structural biology, several μOR-mediated painkillers with fewer side effects have been successfully designed.</description><subject>Analgesics, Opioid - chemistry</subject><subject>Analgesics, Opioid - pharmacology</subject><subject>Animals</subject><subject>computational biology</subject><subject>Drug Design</subject><subject>drug discovery</subject><subject>GPCR</subject><subject>Humans</subject><subject>opioid receptor</subject><subject>Receptors, Opioid, mu - antagonists & inhibitors</subject><subject>Receptors, Opioid, mu - chemistry</subject><subject>Receptors, Opioid, mu - metabolism</subject><subject>safer painkiller</subject><issn>0165-6147</issn><issn>1873-3735</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2017</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMtKxDAUhoMoOl5ewIV06aY1ae4igngHQfGyDml6OmbotDXpjPhuPoPPZIdR0Y2rwMn3_-fwIbRLcEYwEQeTrPddzHJMZIZVhjFbQSOiJE2ppHwVjQaIp4IwuYE2Y5xgjCnNyTrayJWmPNd0hA7PIPpx45tx8mArCMlJY-vxMHMxmXubfLynt51vfZncg4Oub0NyZ_vnV_sWt9FaZesIO1_vFnq6OH88vUpvbi-vT09uUsc471MpS1dq4Rx1SuRciRJKRzHDFS0ko5ZRVhSWEap0VSjLSpGDVkVFtSaV5IRuoeNlbzcrpkMWmj7Y2nTBT214M6315u9P45_NuJ0bLjTmjA0F-18FoX2ZQezN1EcHdW0baGfREM1yIYWgCzRfoi60MQaoftYQbBbSzcQspJuFdIOVGaQPob3fB_5Evi0PwNESgEHT3EMw0XloHJQ-gOtN2fr_-j8BMUGUkA</recordid><startdate>20171101</startdate><enddate>20171101</enddate><creator>Chan, H.C. Stephen</creator><creator>McCarthy, Dillon</creator><creator>Li, Jianing</creator><creator>Palczewski, Krzysztof</creator><creator>Yuan, Shuguang</creator><general>Elsevier Ltd</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><scope>5PM</scope><orcidid>https://orcid.org/0000-0001-9858-4742</orcidid></search><sort><creationdate>20171101</creationdate><title>Designing Safer Analgesics via μ-Opioid Receptor Pathways</title><author>Chan, H.C. Stephen ; McCarthy, Dillon ; Li, Jianing ; Palczewski, Krzysztof ; Yuan, Shuguang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c455t-77dcd96cc3c862586dedc3040f3b743a434bba41389fb8a4d62e98bf3991f7513</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2017</creationdate><topic>Analgesics, Opioid - chemistry</topic><topic>Analgesics, Opioid - pharmacology</topic><topic>Animals</topic><topic>computational biology</topic><topic>Drug Design</topic><topic>drug discovery</topic><topic>GPCR</topic><topic>Humans</topic><topic>opioid receptor</topic><topic>Receptors, Opioid, mu - antagonists & inhibitors</topic><topic>Receptors, Opioid, mu - chemistry</topic><topic>Receptors, Opioid, mu - metabolism</topic><topic>safer painkiller</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Chan, H.C. Stephen</creatorcontrib><creatorcontrib>McCarthy, Dillon</creatorcontrib><creatorcontrib>Li, Jianing</creatorcontrib><creatorcontrib>Palczewski, Krzysztof</creatorcontrib><creatorcontrib>Yuan, Shuguang</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><collection>PubMed Central (Full Participant titles)</collection><jtitle>Trends in pharmacological sciences (Regular ed.)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Chan, H.C. Stephen</au><au>McCarthy, Dillon</au><au>Li, Jianing</au><au>Palczewski, Krzysztof</au><au>Yuan, Shuguang</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Designing Safer Analgesics via μ-Opioid Receptor Pathways</atitle><jtitle>Trends in pharmacological sciences (Regular ed.)</jtitle><addtitle>Trends Pharmacol Sci</addtitle><date>2017-11-01</date><risdate>2017</risdate><volume>38</volume><issue>11</issue><spage>1016</spage><epage>1037</epage><pages>1016-1037</pages><issn>0165-6147</issn><eissn>1873-3735</eissn><abstract>Pain is both a major clinical and economic problem, affecting more people than diabetes, heart disease, and cancer combined. While a variety of prescribed or over-the-counter (OTC) medications are available for pain management, opioid medications, especially those acting on the μ-opioid receptor (μOR) and related pathways, have proven to be the most effective, despite some serious side effects including respiration depression, pruritus, dependence, and constipation. It is therefore imperative that both academia and industry develop novel μOR analgesics which retain their opioid analgesic properties but with fewer or no adverse effects. In this review we outline recent progress towards the discovery of safer opioid analgesics.
Pain is a major clinical and economic problem. Owing to the serious side effects associated with current painkillers, the discovery of less toxic medications is an imperative in both academia and industry.
Owing to recent advances in computational and structural biology, several μOR-mediated painkillers with fewer side effects have been successfully designed.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>28935293</pmid><doi>10.1016/j.tips.2017.08.004</doi><tpages>22</tpages><orcidid>https://orcid.org/0000-0001-9858-4742</orcidid><oa>free_for_read</oa></addata></record> |
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| source | MEDLINE; ScienceDirect Journals (5 years ago - present) |
| subjects | Analgesics, Opioid - chemistry Analgesics, Opioid - pharmacology Animals computational biology Drug Design drug discovery GPCR Humans opioid receptor Receptors, Opioid, mu - antagonists & inhibitors Receptors, Opioid, mu - chemistry Receptors, Opioid, mu - metabolism safer painkiller |
| title | Designing Safer Analgesics via μ-Opioid Receptor Pathways |
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