Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators
[Display omitted] Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregula...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2016-11, Vol.26 (21), p.5139-5148 |
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container_title | Bioorganic & medicinal chemistry letters |
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creator | Cameron, Kimberly O. Kurumbail, Ravi G. |
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Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature. |
doi_str_mv | 10.1016/j.bmcl.2016.09.065 |
format | Article |
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Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2016.09.065</identifier><identifier>PMID: 27727125</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Allostery ; AMP-Activated Protein Kinases - chemistry ; AMP-Activated Protein Kinases - metabolism ; AMPK ; Animals ; CBM ; CBS ; Crystallography ; Enzyme Activation ; Enzyme activators ; Enzyme Activators - pharmacology ; Humans ; Phosphorylation ; Protein Conformation</subject><ispartof>Bioorganic & medicinal chemistry letters, 2016-11, Vol.26 (21), p.5139-5148</ispartof><rights>2016 Elsevier Ltd</rights><rights>Copyright © 2016 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c492t-c52f785c56fe609a5a888b097122c17100170f62ffe7f5c7c718faf4649526be3</citedby><cites>FETCH-LOGICAL-c492t-c52f785c56fe609a5a888b097122c17100170f62ffe7f5c7c718faf4649526be3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X16310149$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27727125$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cameron, Kimberly O.</creatorcontrib><creatorcontrib>Kurumbail, Ravi G.</creatorcontrib><title>Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature.</description><subject>Allostery</subject><subject>AMP-Activated Protein Kinases - chemistry</subject><subject>AMP-Activated Protein Kinases - metabolism</subject><subject>AMPK</subject><subject>Animals</subject><subject>CBM</subject><subject>CBS</subject><subject>Crystallography</subject><subject>Enzyme Activation</subject><subject>Enzyme activators</subject><subject>Enzyme Activators - pharmacology</subject><subject>Humans</subject><subject>Phosphorylation</subject><subject>Protein Conformation</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kEtrGzEUhUVpqJ2kf6CLomWymIkkj17QTQjNgySklBS6E7LmqpbjGbmSbMi_j4zdLrPS5eqcwz0fQl8oaSmh4mLZzge3almdW6JbIvgHNKWd6JpZR_hHNCVakEbp7vcEHee8JIR2pOs-oQmTkknK-BS9_AQHY8HrFP8kyBmHEZcF4NDXbfDB2RLiiKPHtm5iDiPgIY5xvYh5vbAFGutK2Nah32UUqP6XMNoM-Ozy8cf9OT78x5RP0ZG3qwyfD-8J-nX9_fnqtnl4urm7unxoXKdZaRxnXiruuPAgiLbcKqXmRNeDmaOS1hqSeMG8B-m5k05S5a2vvTVnYg6zE3S2z60H_d1ALmYI2cFqZUeIm2yomvGZVkKRKmV7qUsx5wTerFMYbHo1lJgdZLM0O8hmB9kQbSrkavp6yN_MB-j_W_5RrYJvewHUltsAyWQXYHTQhwSumD6G9_LfALx0jro</recordid><startdate>20161101</startdate><enddate>20161101</enddate><creator>Cameron, Kimberly O.</creator><creator>Kurumbail, Ravi G.</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></search><sort><creationdate>20161101</creationdate><title>Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators</title><author>Cameron, Kimberly O. ; Kurumbail, Ravi G.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c492t-c52f785c56fe609a5a888b097122c17100170f62ffe7f5c7c718faf4649526be3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Allostery</topic><topic>AMP-Activated Protein Kinases - chemistry</topic><topic>AMP-Activated Protein Kinases - metabolism</topic><topic>AMPK</topic><topic>Animals</topic><topic>CBM</topic><topic>CBS</topic><topic>Crystallography</topic><topic>Enzyme Activation</topic><topic>Enzyme activators</topic><topic>Enzyme Activators - pharmacology</topic><topic>Humans</topic><topic>Phosphorylation</topic><topic>Protein Conformation</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cameron, Kimberly O.</creatorcontrib><creatorcontrib>Kurumbail, Ravi G.</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><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cameron, Kimberly O.</au><au>Kurumbail, Ravi G.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2016-11-01</date><risdate>2016</risdate><volume>26</volume><issue>21</issue><spage>5139</spage><epage>5148</epage><pages>5139-5148</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Adenosine monophosphate-activated protein kinase (AMPK), a serine/threonine heterotrimeric protein kinase, is a critical regulator of cellular and whole body energy homeostasis. There are twelve known AMPK isoforms that are differentially expressed in tissues and species. Dysregulation of AMPK signaling is associated with a multitude of human pathologies. Hence isoform-selective activators of AMPK are actively being sought for the treatment of cardiovascular and metabolic diseases. The present review summarizes the status of direct AMPK activators from the patent and published literature.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>27727125</pmid><doi>10.1016/j.bmcl.2016.09.065</doi><tpages>10</tpages></addata></record> |
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subjects | Allostery AMP-Activated Protein Kinases - chemistry AMP-Activated Protein Kinases - metabolism AMPK Animals CBM CBS Crystallography Enzyme Activation Enzyme activators Enzyme Activators - pharmacology Humans Phosphorylation Protein Conformation |
title | Recent progress in the identification of adenosine monophosphate-activated protein kinase (AMPK) activators |
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