Loading…

Novel Potent Selective Orally Active S1P5 Receptor Antagonists

S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we de...

Full description

Saved in:
Bibliographic Details
Published in:ACS medicinal chemistry letters 2021-03, Vol.12 (3), p.351-355
Main Authors: Ma, Bin, Guckian, Kevin M, Liu, Xiao-gao, Yang, Chunhua, Li, Bing, Scannevin, Robert, Mingueneau, Michaël, Drouillard, Annabelle, Walzer, Thierry
Format: Article
Language:English
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
cited_by cdi_FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753
cites cdi_FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753
container_end_page 355
container_issue 3
container_start_page 351
container_title ACS medicinal chemistry letters
container_volume 12
creator Ma, Bin
Guckian, Kevin M
Liu, Xiao-gao
Yang, Chunhua
Li, Bing
Scannevin, Robert
Mingueneau, Michaël
Drouillard, Annabelle
Walzer, Thierry
description S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.
doi_str_mv 10.1021/acsmedchemlett.0c00631
format article
fullrecord <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_7957944</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>2503437385</sourcerecordid><originalsourceid>FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753</originalsourceid><addsrcrecordid>eNqFkM1uwjAQhK2qVaG0r4By7AVqJ3acXJAQ6p-ECirt2XKcDQQ5MY0dJN6-iUIRnHryWjs7O_shNCR4TLBPnqSyBaRqA4UG58ZYYRwG5Ar1SUyjEYs4uz6re-jO2m0jiTnHt6gXBDyIcEj6aPJh9qC9pXFQOm8FGpTL9-AtKqn1wZt2vxVZMu8TFOycqbxp6eTalLl19h7dZFJbeDi-A_T98vw1exvNF6_vs-l8JCnjbqTiOAOquO8HwCBRIWGJlIoREnIifcaymFBQjEMaZBQTlcaJkpGKlJQs5SwYoEnnu6uT9u4mbBNQ7Kq8kNVBGJmLy06Zb8Ta7AWPGY8pbQwejwaV-anBOlHkVoHWsgRTW-EzHNCWSrsr7KSqMtZWkJ3WECxa-OISvjjCbwaH5yFPY3-0G4HfCRoDsTV1VTbM_nP9Baqwl6Q</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>2503437385</pqid></control><display><type>article</type><title>Novel Potent Selective Orally Active S1P5 Receptor Antagonists</title><source>American Chemical Society:Jisc Collections:American Chemical Society Read &amp; Publish Agreement 2022-2024 (Reading list)</source><source>PubMed Central</source><creator>Ma, Bin ; Guckian, Kevin M ; Liu, Xiao-gao ; Yang, Chunhua ; Li, Bing ; Scannevin, Robert ; Mingueneau, Michaël ; Drouillard, Annabelle ; Walzer, Thierry</creator><creatorcontrib>Ma, Bin ; Guckian, Kevin M ; Liu, Xiao-gao ; Yang, Chunhua ; Li, Bing ; Scannevin, Robert ; Mingueneau, Michaël ; Drouillard, Annabelle ; Walzer, Thierry</creatorcontrib><description>S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.</description><identifier>ISSN: 1948-5875</identifier><identifier>EISSN: 1948-5875</identifier><identifier>DOI: 10.1021/acsmedchemlett.0c00631</identifier><identifier>PMID: 33738061</identifier><language>eng</language><publisher>United States: American Chemical Society</publisher><ispartof>ACS medicinal chemistry letters, 2021-03, Vol.12 (3), p.351-355</ispartof><rights>2021 American Chemical Society</rights><rights>2021 American Chemical Society.</rights><rights>2021 American Chemical Society 2021 American Chemical Society</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753</citedby><cites>FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753</cites><orcidid>0000-0002-3913-0545</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7957944/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC7957944/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27915,27916,53782,53784</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/33738061$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ma, Bin</creatorcontrib><creatorcontrib>Guckian, Kevin M</creatorcontrib><creatorcontrib>Liu, Xiao-gao</creatorcontrib><creatorcontrib>Yang, Chunhua</creatorcontrib><creatorcontrib>Li, Bing</creatorcontrib><creatorcontrib>Scannevin, Robert</creatorcontrib><creatorcontrib>Mingueneau, Michaël</creatorcontrib><creatorcontrib>Drouillard, Annabelle</creatorcontrib><creatorcontrib>Walzer, Thierry</creatorcontrib><title>Novel Potent Selective Orally Active S1P5 Receptor Antagonists</title><title>ACS medicinal chemistry letters</title><addtitle>ACS Med. Chem. Lett</addtitle><description>S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.</description><issn>1948-5875</issn><issn>1948-5875</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><recordid>eNqFkM1uwjAQhK2qVaG0r4By7AVqJ3acXJAQ6p-ECirt2XKcDQQ5MY0dJN6-iUIRnHryWjs7O_shNCR4TLBPnqSyBaRqA4UG58ZYYRwG5Ar1SUyjEYs4uz6re-jO2m0jiTnHt6gXBDyIcEj6aPJh9qC9pXFQOm8FGpTL9-AtKqn1wZt2vxVZMu8TFOycqbxp6eTalLl19h7dZFJbeDi-A_T98vw1exvNF6_vs-l8JCnjbqTiOAOquO8HwCBRIWGJlIoREnIifcaymFBQjEMaZBQTlcaJkpGKlJQs5SwYoEnnu6uT9u4mbBNQ7Kq8kNVBGJmLy06Zb8Ta7AWPGY8pbQwejwaV-anBOlHkVoHWsgRTW-EzHNCWSrsr7KSqMtZWkJ3WECxa-OISvjjCbwaH5yFPY3-0G4HfCRoDsTV1VTbM_nP9Baqwl6Q</recordid><startdate>20210311</startdate><enddate>20210311</enddate><creator>Ma, Bin</creator><creator>Guckian, Kevin M</creator><creator>Liu, Xiao-gao</creator><creator>Yang, Chunhua</creator><creator>Li, Bing</creator><creator>Scannevin, Robert</creator><creator>Mingueneau, Michaël</creator><creator>Drouillard, Annabelle</creator><creator>Walzer, Thierry</creator><general>American Chemical Society</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope><scope>5PM</scope><orcidid>https://orcid.org/0000-0002-3913-0545</orcidid></search><sort><creationdate>20210311</creationdate><title>Novel Potent Selective Orally Active S1P5 Receptor Antagonists</title><author>Ma, Bin ; Guckian, Kevin M ; Liu, Xiao-gao ; Yang, Chunhua ; Li, Bing ; Scannevin, Robert ; Mingueneau, Michaël ; Drouillard, Annabelle ; Walzer, Thierry</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ma, Bin</creatorcontrib><creatorcontrib>Guckian, Kevin M</creatorcontrib><creatorcontrib>Liu, Xiao-gao</creatorcontrib><creatorcontrib>Yang, Chunhua</creatorcontrib><creatorcontrib>Li, Bing</creatorcontrib><creatorcontrib>Scannevin, Robert</creatorcontrib><creatorcontrib>Mingueneau, Michaël</creatorcontrib><creatorcontrib>Drouillard, Annabelle</creatorcontrib><creatorcontrib>Walzer, Thierry</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>ACS medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ma, Bin</au><au>Guckian, Kevin M</au><au>Liu, Xiao-gao</au><au>Yang, Chunhua</au><au>Li, Bing</au><au>Scannevin, Robert</au><au>Mingueneau, Michaël</au><au>Drouillard, Annabelle</au><au>Walzer, Thierry</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel Potent Selective Orally Active S1P5 Receptor Antagonists</atitle><jtitle>ACS medicinal chemistry letters</jtitle><addtitle>ACS Med. Chem. Lett</addtitle><date>2021-03-11</date><risdate>2021</risdate><volume>12</volume><issue>3</issue><spage>351</spage><epage>355</epage><pages>351-355</pages><issn>1948-5875</issn><eissn>1948-5875</eissn><abstract>S1P5 is one of the five sphingosine-1-phosphate (S1P) receptors which play important roles in immune and CNS cell homeostasis, growth, and differentiation. Little is known about the effect of modulation of S1P5 due to the lack of S1P5 specific modulators with suitable druglike properties. Here we describe the discovery and optimization of a novel series of potent selective S1P5 antagonists and the identification of an orally active brain-penetrant tool compound 15.</abstract><cop>United States</cop><pub>American Chemical Society</pub><pmid>33738061</pmid><doi>10.1021/acsmedchemlett.0c00631</doi><tpages>5</tpages><orcidid>https://orcid.org/0000-0002-3913-0545</orcidid><oa>free_for_read</oa></addata></record>
fulltext fulltext
identifier ISSN: 1948-5875
ispartof ACS medicinal chemistry letters, 2021-03, Vol.12 (3), p.351-355
issn 1948-5875
1948-5875
language eng
recordid cdi_pubmedcentral_primary_oai_pubmedcentral_nih_gov_7957944
source American Chemical Society:Jisc Collections:American Chemical Society Read & Publish Agreement 2022-2024 (Reading list); PubMed Central
title Novel Potent Selective Orally Active S1P5 Receptor Antagonists
url http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-15T01%3A45%3A21IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_pubme&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Novel%20Potent%20Selective%20Orally%20Active%20S1P5%20Receptor%20Antagonists&rft.jtitle=ACS%20medicinal%20chemistry%20letters&rft.au=Ma,%20Bin&rft.date=2021-03-11&rft.volume=12&rft.issue=3&rft.spage=351&rft.epage=355&rft.pages=351-355&rft.issn=1948-5875&rft.eissn=1948-5875&rft_id=info:doi/10.1021/acsmedchemlett.0c00631&rft_dat=%3Cproquest_pubme%3E2503437385%3C/proquest_pubme%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-a457t-c99fe4c7223e5ebc615baac511671a255f914ec57ed3f401cd9bca8c8caa5d753%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=2503437385&rft_id=info:pmid/33738061&rfr_iscdi=true