Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)

[Display omitted] A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2005-03, Vol.15 (6), p.1587-1590
Main Authors: Anderson, David R., Hegde, Shridhar, Reinhard, Emily, Gomez, Leslie, Vernier, William F., Lee, Len, Liu, Shuang, Sambandam, Aruna, Snider, Patricia A., Masih, Liaqat
Format: Article
Language:English
Subjects:
Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Gene Expression
Humans
Kinase inhibitor
MAP Kinase Kinase 2 - antagonists & inhibitors
Medical sciences
MK-2
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Pyridines - chemistry
Pyridines - pharmacology
Rats
Structure-Activity Relationship
TNFα
Tumor Necrosis Factor-alpha - metabolism
U937 Cells
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-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33
cites cdi_FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33
container_end_page 1590
container_issue 6
container_start_page 1587
container_title Bioorganic & medicinal chemistry letters
container_volume 15
creator Anderson, David R.
Hegde, Shridhar
Reinhard, Emily
Gomez, Leslie
Vernier, William F.
Lee, Len
Liu, Shuang
Sambandam, Aruna
Snider, Patricia A.
Masih, Liaqat
description [Display omitted] A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.
doi_str_mv 10.1016/j.bmcl.2005.01.067
format article
fullrecord <record><control><sourceid>proquest_cross</sourceid><recordid>TN_cdi_proquest_miscellaneous_67481207</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0960894X05001344</els_id><sourcerecordid>67481207</sourcerecordid><originalsourceid>FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33</originalsourceid><addsrcrecordid>eNp9kMFq3DAQhkVoSLZJXiCH4ktLerA7kiXLgl6WJW1CEnppITchS-NUW1veSN7Avn1sdiGn5jQD8_0_w0fIJYWCAq2-rYumt13BAEQBtIBKHpEF5RXPSw7iA1mAqiCvFX88JR9TWgNQDpyfkFMqJBc1sAWxy96Hwe5MGDa76J0PmPnw1zd-HGLKhjbrp-0JQ2bs6F_MiC7bxGFEH7J_PpiE-f8OGcuuHu5y9vWcHLemS3hxmGfkz4_r36ub_P7Xz9vV8j63Zc3HnDZOloI3TkmnrFIMRYu1ktxRhRwbYZgsTUW5QkQBiJIhKjCmLA1nTVmekS_73umP5y2mUfc-Wew6E3DYJl1JXlMGcgLZHrRxSCliqzfR9ybuNAU9q9VrPavVs1oNVE9qp9CnQ_u26dG9RQ4uJ-DzATDJmq6NJlif3rhK1ELJmfu-53By8eIx6mQ9BovOR7SjdoN_749XrSeYUQ</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>67481207</pqid></control><display><type>article</type><title>Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)</title><source>ScienceDirect Journals</source><creator>Anderson, David R. ; Hegde, Shridhar ; Reinhard, Emily ; Gomez, Leslie ; Vernier, William F. ; Lee, Len ; Liu, Shuang ; Sambandam, Aruna ; Snider, Patricia A. ; Masih, Liaqat</creator><creatorcontrib>Anderson, David R. ; Hegde, Shridhar ; Reinhard, Emily ; Gomez, Leslie ; Vernier, William F. ; Lee, Len ; Liu, Shuang ; Sambandam, Aruna ; Snider, Patricia A. ; Masih, Liaqat</creatorcontrib><description>[Display omitted] A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2005.01.067</identifier><identifier>PMID: 15745802</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Animals ; Biological and medical sciences ; Bones, joints and connective tissue. Antiinflammatory agents ; Gene Expression ; Humans ; Kinase inhibitor ; MAP Kinase Kinase 2 - antagonists &amp; inhibitors ; Medical sciences ; MK-2 ; Models, Chemical ; Molecular Structure ; Pharmacology. Drug treatments ; Pyridines - chemistry ; Pyridines - pharmacology ; Rats ; Structure-Activity Relationship ; TNFα ; Tumor Necrosis Factor-alpha - metabolism ; U937 Cells</subject><ispartof>Bioorganic &amp; medicinal chemistry letters, 2005-03, Vol.15 (6), p.1587-1590</ispartof><rights>2005 Elsevier Ltd</rights><rights>2005 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33</citedby><cites>FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&amp;idt=16585972$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/15745802$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Anderson, David R.</creatorcontrib><creatorcontrib>Hegde, Shridhar</creatorcontrib><creatorcontrib>Reinhard, Emily</creatorcontrib><creatorcontrib>Gomez, Leslie</creatorcontrib><creatorcontrib>Vernier, William F.</creatorcontrib><creatorcontrib>Lee, Len</creatorcontrib><creatorcontrib>Liu, Shuang</creatorcontrib><creatorcontrib>Sambandam, Aruna</creatorcontrib><creatorcontrib>Snider, Patricia A.</creatorcontrib><creatorcontrib>Masih, Liaqat</creatorcontrib><title>Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)</title><title>Bioorganic &amp; medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted] A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Gene Expression</subject><subject>Humans</subject><subject>Kinase inhibitor</subject><subject>MAP Kinase Kinase 2 - antagonists &amp; inhibitors</subject><subject>Medical sciences</subject><subject>MK-2</subject><subject>Models, Chemical</subject><subject>Molecular Structure</subject><subject>Pharmacology. Drug treatments</subject><subject>Pyridines - chemistry</subject><subject>Pyridines - pharmacology</subject><subject>Rats</subject><subject>Structure-Activity Relationship</subject><subject>TNFα</subject><subject>Tumor Necrosis Factor-alpha - metabolism</subject><subject>U937 Cells</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2005</creationdate><recordtype>article</recordtype><recordid>eNp9kMFq3DAQhkVoSLZJXiCH4ktLerA7kiXLgl6WJW1CEnppITchS-NUW1veSN7Avn1sdiGn5jQD8_0_w0fIJYWCAq2-rYumt13BAEQBtIBKHpEF5RXPSw7iA1mAqiCvFX88JR9TWgNQDpyfkFMqJBc1sAWxy96Hwe5MGDa76J0PmPnw1zd-HGLKhjbrp-0JQ2bs6F_MiC7bxGFEH7J_PpiE-f8OGcuuHu5y9vWcHLemS3hxmGfkz4_r36ub_P7Xz9vV8j63Zc3HnDZOloI3TkmnrFIMRYu1ktxRhRwbYZgsTUW5QkQBiJIhKjCmLA1nTVmekS_73umP5y2mUfc-Wew6E3DYJl1JXlMGcgLZHrRxSCliqzfR9ybuNAU9q9VrPavVs1oNVE9qp9CnQ_u26dG9RQ4uJ-DzATDJmq6NJlif3rhK1ELJmfu-53By8eIx6mQ9BovOR7SjdoN_749XrSeYUQ</recordid><startdate>20050315</startdate><enddate>20050315</enddate><creator>Anderson, David R.</creator><creator>Hegde, Shridhar</creator><creator>Reinhard, Emily</creator><creator>Gomez, Leslie</creator><creator>Vernier, William F.</creator><creator>Lee, Len</creator><creator>Liu, Shuang</creator><creator>Sambandam, Aruna</creator><creator>Snider, Patricia A.</creator><creator>Masih, Liaqat</creator><general>Elsevier Ltd</general><general>Elsevier</general><scope>IQODW</scope><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>20050315</creationdate><title>Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)</title><author>Anderson, David R. ; Hegde, Shridhar ; Reinhard, Emily ; Gomez, Leslie ; Vernier, William F. ; Lee, Len ; Liu, Shuang ; Sambandam, Aruna ; Snider, Patricia A. ; Masih, Liaqat</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2005</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Gene Expression</topic><topic>Humans</topic><topic>Kinase inhibitor</topic><topic>MAP Kinase Kinase 2 - antagonists &amp; inhibitors</topic><topic>Medical sciences</topic><topic>MK-2</topic><topic>Models, Chemical</topic><topic>Molecular Structure</topic><topic>Pharmacology. Drug treatments</topic><topic>Pyridines - chemistry</topic><topic>Pyridines - pharmacology</topic><topic>Rats</topic><topic>Structure-Activity Relationship</topic><topic>TNFα</topic><topic>Tumor Necrosis Factor-alpha - metabolism</topic><topic>U937 Cells</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Anderson, David R.</creatorcontrib><creatorcontrib>Hegde, Shridhar</creatorcontrib><creatorcontrib>Reinhard, Emily</creatorcontrib><creatorcontrib>Gomez, Leslie</creatorcontrib><creatorcontrib>Vernier, William F.</creatorcontrib><creatorcontrib>Lee, Len</creatorcontrib><creatorcontrib>Liu, Shuang</creatorcontrib><creatorcontrib>Sambandam, Aruna</creatorcontrib><creatorcontrib>Snider, Patricia A.</creatorcontrib><creatorcontrib>Masih, Liaqat</creatorcontrib><collection>Pascal-Francis</collection><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>Bioorganic &amp; medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Anderson, David R.</au><au>Hegde, Shridhar</au><au>Reinhard, Emily</au><au>Gomez, Leslie</au><au>Vernier, William F.</au><au>Lee, Len</au><au>Liu, Shuang</au><au>Sambandam, Aruna</au><au>Snider, Patricia A.</au><au>Masih, Liaqat</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)</atitle><jtitle>Bioorganic &amp; medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2005-03-15</date><risdate>2005</risdate><volume>15</volume><issue>6</issue><spage>1587</spage><epage>1590</epage><pages>1587-1590</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted] A class of inhibitors of mitogen-activated protein kinase-activated protein kinase 2 (MK-2) was discovered. These compounds have demonstrated activity against the enzyme with IC 50 values as low as 130 nM and suppress the expression of TNFα in U937 cells. These represent the first small molecule inhibitors of MK-2 to be reported.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>15745802</pmid><doi>10.1016/j.bmcl.2005.01.067</doi><tpages>4</tpages></addata></record>
fulltext fulltext
identifier ISSN: 0960-894X
ispartof Bioorganic & medicinal chemistry letters, 2005-03, Vol.15 (6), p.1587-1590
issn 0960-894X
1464-3405
language eng
recordid cdi_proquest_miscellaneous_67481207
source ScienceDirect Journals
subjects Animals
Biological and medical sciences
Bones, joints and connective tissue. Antiinflammatory agents
Gene Expression
Humans
Kinase inhibitor
MAP Kinase Kinase 2 - antagonists & inhibitors
Medical sciences
MK-2
Models, Chemical
Molecular Structure
Pharmacology. Drug treatments
Pyridines - chemistry
Pyridines - pharmacology
Rats
Structure-Activity Relationship
TNFα
Tumor Necrosis Factor-alpha - metabolism
U937 Cells
title Aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase 2 (MK-2)
url http://sfxeu10.hosted.exlibrisgroup.com/loughborough?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2024-12-27T06%3A39%3A07IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_cross&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Aminocyanopyridine%20inhibitors%20of%20mitogen%20activated%20protein%20kinase-activated%20protein%20kinase%202%20(MK-2)&rft.jtitle=Bioorganic%20&%20medicinal%20chemistry%20letters&rft.au=Anderson,%20David%20R.&rft.date=2005-03-15&rft.volume=15&rft.issue=6&rft.spage=1587&rft.epage=1590&rft.pages=1587-1590&rft.issn=0960-894X&rft.eissn=1464-3405&rft_id=info:doi/10.1016/j.bmcl.2005.01.067&rft_dat=%3Cproquest_cross%3E67481207%3C/proquest_cross%3E%3Cgrp_id%3Ecdi_FETCH-LOGICAL-c384t-1bd7354bd97d9c992e5fe8974d19e4eb5a273a6149eee50ee72ee90aa33a42b33%3C/grp_id%3E%3Coa%3E%3C/oa%3E%3Curl%3E%3C/url%3E&rft_id=info:oai/&rft_pqid=67481207&rft_id=info:pmid/15745802&rfr_iscdi=true