Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists

Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists

Abstract ID 54221 Poster Board 553 The therapeutic management of neuropathic pain (NP) targets opioid receptors to modulate their signal processes. Currently, the most effective therapeutic analgesia is opioids to manage the long-term treatment of NP, and these unfortunately have associated side eff...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:The Journal of pharmacology and experimental therapeutics 2023-06, Vol.385, p.553-553
Hauptverfasser: Olayide, Israel, Braden, Kathryn, Salvemini, Daniela, Arnatt, Christopher K.
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
container_end_page 553
container_issue
container_start_page 553
container_title The Journal of pharmacology and experimental therapeutics
container_volume 385
creator Olayide, Israel
Braden, Kathryn
Salvemini, Daniela
Arnatt, Christopher K.
description Abstract ID 54221 Poster Board 553 The therapeutic management of neuropathic pain (NP) targets opioid receptors to modulate their signal processes. Currently, the most effective therapeutic analgesia is opioids to manage the long-term treatment of NP, and these unfortunately have associated side effects including addiction and physical dependencies. GPR183 (Epstein-Barr induced gene 2, EBI2), a non-opioid G-protein coupled receptor (GPCR) revealed to be involved in the pathway of NP generation. SAE-14, a novel small molecule, is a lead compound that was shown to antagonize GPR183 and is active in vivo in a chronic constriction model of neuropathic pain. It is necessary to optimize the pharmacophores of SAE-14 to enhance its binding interactions with GPR183. Therefore, we investigated a structural activity relationship of SAE-14, to uncover improved functional groups that would augment its antagonistic activity.
doi_str_mv 10.1124/jpet.122.542210
format Article
fullrecord <record><control><sourceid>elsevier_cross</sourceid><recordid>TN_cdi_crossref_primary_10_1124_jpet_122_542210</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0022356524169893</els_id><sourcerecordid>S0022356524169893</sourcerecordid><originalsourceid>FETCH-LOGICAL-c1310-dc8219e48c0edc522dfd138b8c7bb73c26ec808ee18db66416350ffe680720ae3</originalsourceid><addsrcrecordid>eNp10LFuwjAQgGEPrVRKO3f1CwR8thPMGCFKKyG1Ku1sJfYFjEIc2QYpb98guna65b7T6SfkBdgMgMv5scc0A85nueQc2B2ZMMZ5JvIifyCPMR4ZAykLMSGn3dClA0YXadVZukvhbNI5YFaa5C4uDfQL2yo538WD66lv6K5cZyBp2VWt348q0k32GXxC19GVP_ct2tEY7JMPFJQYN1O1952LKT6R-6ZqIz7_zSn5eV1_r96y7cfmfVVuMwMCWGaN4rBEqQxDa3LObWNBqFqZRV0vhOEFGsUUIihbF4WEQuSsabBQbMFZhWJK5re7JvgYAza6D-5UhUED09dC-lpIj4X0rdAoljeB41sXh0FH47AzaF1Ak7T17l_7C6Tyb-E</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype></control><display><type>article</type><title>Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists</title><source>Alma/SFX Local Collection</source><creator>Olayide, Israel ; Braden, Kathryn ; Salvemini, Daniela ; Arnatt, Christopher K.</creator><creatorcontrib>Olayide, Israel ; Braden, Kathryn ; Salvemini, Daniela ; Arnatt, Christopher K.</creatorcontrib><description>Abstract ID 54221 Poster Board 553 The therapeutic management of neuropathic pain (NP) targets opioid receptors to modulate their signal processes. Currently, the most effective therapeutic analgesia is opioids to manage the long-term treatment of NP, and these unfortunately have associated side effects including addiction and physical dependencies. GPR183 (Epstein-Barr induced gene 2, EBI2), a non-opioid G-protein coupled receptor (GPCR) revealed to be involved in the pathway of NP generation. SAE-14, a novel small molecule, is a lead compound that was shown to antagonize GPR183 and is active in vivo in a chronic constriction model of neuropathic pain. It is necessary to optimize the pharmacophores of SAE-14 to enhance its binding interactions with GPR183. Therefore, we investigated a structural activity relationship of SAE-14, to uncover improved functional groups that would augment its antagonistic activity.</description><identifier>ISSN: 0022-3565</identifier><identifier>DOI: 10.1124/jpet.122.542210</identifier><language>eng</language><publisher>Elsevier Inc</publisher><ispartof>The Journal of pharmacology and experimental therapeutics, 2023-06, Vol.385, p.553-553</ispartof><rights>2023 American Society for Pharmacology and Experimental Therapeutics</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></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></links><search><creatorcontrib>Olayide, Israel</creatorcontrib><creatorcontrib>Braden, Kathryn</creatorcontrib><creatorcontrib>Salvemini, Daniela</creatorcontrib><creatorcontrib>Arnatt, Christopher K.</creatorcontrib><title>Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists</title><title>The Journal of pharmacology and experimental therapeutics</title><description>Abstract ID 54221 Poster Board 553 The therapeutic management of neuropathic pain (NP) targets opioid receptors to modulate their signal processes. Currently, the most effective therapeutic analgesia is opioids to manage the long-term treatment of NP, and these unfortunately have associated side effects including addiction and physical dependencies. GPR183 (Epstein-Barr induced gene 2, EBI2), a non-opioid G-protein coupled receptor (GPCR) revealed to be involved in the pathway of NP generation. SAE-14, a novel small molecule, is a lead compound that was shown to antagonize GPR183 and is active in vivo in a chronic constriction model of neuropathic pain. It is necessary to optimize the pharmacophores of SAE-14 to enhance its binding interactions with GPR183. Therefore, we investigated a structural activity relationship of SAE-14, to uncover improved functional groups that would augment its antagonistic activity.</description><issn>0022-3565</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2023</creationdate><recordtype>article</recordtype><recordid>eNp10LFuwjAQgGEPrVRKO3f1CwR8thPMGCFKKyG1Ku1sJfYFjEIc2QYpb98guna65b7T6SfkBdgMgMv5scc0A85nueQc2B2ZMMZ5JvIifyCPMR4ZAykLMSGn3dClA0YXadVZukvhbNI5YFaa5C4uDfQL2yo538WD66lv6K5cZyBp2VWt348q0k32GXxC19GVP_ct2tEY7JMPFJQYN1O1952LKT6R-6ZqIz7_zSn5eV1_r96y7cfmfVVuMwMCWGaN4rBEqQxDa3LObWNBqFqZRV0vhOEFGsUUIihbF4WEQuSsabBQbMFZhWJK5re7JvgYAza6D-5UhUED09dC-lpIj4X0rdAoljeB41sXh0FH47AzaF1Ak7T17l_7C6Tyb-E</recordid><startdate>202306</startdate><enddate>202306</enddate><creator>Olayide, Israel</creator><creator>Braden, Kathryn</creator><creator>Salvemini, Daniela</creator><creator>Arnatt, Christopher K.</creator><general>Elsevier Inc</general><scope>AAYXX</scope><scope>CITATION</scope></search><sort><creationdate>202306</creationdate><title>Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists</title><author>Olayide, Israel ; Braden, Kathryn ; Salvemini, Daniela ; Arnatt, Christopher K.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c1310-dc8219e48c0edc522dfd138b8c7bb73c26ec808ee18db66416350ffe680720ae3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2023</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Olayide, Israel</creatorcontrib><creatorcontrib>Braden, Kathryn</creatorcontrib><creatorcontrib>Salvemini, Daniela</creatorcontrib><creatorcontrib>Arnatt, Christopher K.</creatorcontrib><collection>CrossRef</collection><jtitle>The Journal of pharmacology and experimental therapeutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Olayide, Israel</au><au>Braden, Kathryn</au><au>Salvemini, Daniela</au><au>Arnatt, Christopher K.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists</atitle><jtitle>The Journal of pharmacology and experimental therapeutics</jtitle><date>2023-06</date><risdate>2023</risdate><volume>385</volume><spage>553</spage><epage>553</epage><pages>553-553</pages><issn>0022-3565</issn><abstract>Abstract ID 54221 Poster Board 553 The therapeutic management of neuropathic pain (NP) targets opioid receptors to modulate their signal processes. Currently, the most effective therapeutic analgesia is opioids to manage the long-term treatment of NP, and these unfortunately have associated side effects including addiction and physical dependencies. GPR183 (Epstein-Barr induced gene 2, EBI2), a non-opioid G-protein coupled receptor (GPCR) revealed to be involved in the pathway of NP generation. SAE-14, a novel small molecule, is a lead compound that was shown to antagonize GPR183 and is active in vivo in a chronic constriction model of neuropathic pain. It is necessary to optimize the pharmacophores of SAE-14 to enhance its binding interactions with GPR183. Therefore, we investigated a structural activity relationship of SAE-14, to uncover improved functional groups that would augment its antagonistic activity.</abstract><pub>Elsevier Inc</pub><doi>10.1124/jpet.122.542210</doi><tpages>1</tpages><oa>free_for_read</oa></addata></record>
fulltext fulltext
identifier ISSN: 0022-3565
ispartof The Journal of pharmacology and experimental therapeutics, 2023-06, Vol.385, p.553-553
issn 0022-3565
language eng
recordid cdi_crossref_primary_10_1124_jpet_122_542210
source Alma/SFX Local Collection
title Synthesis and Structure-Activity Relationship of SAE-14 Analogs as G-Protein Coupled Receptor 183 Antagonists
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-02-09T12%3A37%3A14IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-elsevier_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Synthesis%20and%20Structure-Activity%20Relationship%20of%20SAE-14%20Analogs%20as%20G-Protein%20Coupled%20Receptor%20183%20Antagonists&rft.jtitle=The%20Journal%20of%20pharmacology%20and%20experimental%20therapeutics&rft.au=Olayide,%20Israel&rft.date=2023-06&rft.volume=385&rft.spage=553&rft.epage=553&rft.pages=553-553&rft.issn=0022-3565&rft_id=info:doi/10.1124/jpet.122.542210&rft_dat=%3Celsevier_cross%3ES0022356524169893%3C/elsevier_cross%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rft_els_id=S0022356524169893&rfr_iscdi=true