Putative therapeutic agents for the learning and memory deficits of people with Down syndrome
A novel series of DYRK1A inhibitors were identified by combination of in silico screening, in vitro assay, and cell-based screenings. Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes sign...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-07, Vol.16 (14), p.3772-3776 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Kim, Nam Doo Yoon, Jeonghyeok Kim, Jung Ho Lee, Jung Tae Chon, Yong Sog Hwang, Mi-Kyung Ha, Ilho Song, Woo-Joo |
| description | A novel series of DYRK1A inhibitors were identified by combination of in silico screening, in vitro assay, and cell-based screenings.
Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits. |
| doi_str_mv | 10.1016/j.bmcl.2006.04.042 |
| format | Article |
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Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2006.04.042</identifier><identifier>PMID: 16698266</identifier><language>eng</language><publisher>Oxford: Elsevier Ltd</publisher><subject>Amino Acids - chemistry ; Animals ; Binding Sites ; Biological and medical sciences ; Disease Models, Animal ; Down syndrome ; Down Syndrome - drug therapy ; Down Syndrome - physiopathology ; Dyrk Kinases ; DYRK1A ; Enzyme Inhibitors - isolation & purification ; Enzyme Inhibitors - pharmacology ; Humans ; Hydrogen Bonding ; Inhibitor ; Learning and memory deficits ; Learning Disabilities - drug therapy ; Learning Disabilities - physiopathology ; Medical sciences ; Memory Disorders - drug therapy ; Memory Disorders - physiopathology ; Mice ; Miscellaneous ; Molecular Structure ; Neuropharmacology ; Pharmacology. Drug treatments ; Pharmacophore ; Protein Serine-Threonine Kinases - antagonists & inhibitors ; Protein-Tyrosine Kinases - antagonists & inhibitors</subject><ispartof>Bioorganic & medicinal chemistry letters, 2006-07, Vol.16 (14), p.3772-3776</ispartof><rights>2006 Elsevier Ltd</rights><rights>2006 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c415t-ee50619178adf5c697b199561a5ec90adac6adbb376965414d599184812db3123</citedby><cites>FETCH-LOGICAL-c415t-ee50619178adf5c697b199561a5ec90adac6adbb376965414d599184812db3123</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2006.04.042$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,778,782,3539,27913,27914,45984</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=17850744$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/16698266$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kim, Nam Doo</creatorcontrib><creatorcontrib>Yoon, Jeonghyeok</creatorcontrib><creatorcontrib>Kim, Jung Ho</creatorcontrib><creatorcontrib>Lee, Jung Tae</creatorcontrib><creatorcontrib>Chon, Yong Sog</creatorcontrib><creatorcontrib>Hwang, Mi-Kyung</creatorcontrib><creatorcontrib>Ha, Ilho</creatorcontrib><creatorcontrib>Song, Woo-Joo</creatorcontrib><title>Putative therapeutic agents for the learning and memory deficits of people with Down syndrome</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>A novel series of DYRK1A inhibitors were identified by combination of in silico screening, in vitro assay, and cell-based screenings.
Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits.</description><subject>Amino Acids - chemistry</subject><subject>Animals</subject><subject>Binding Sites</subject><subject>Biological and medical sciences</subject><subject>Disease Models, Animal</subject><subject>Down syndrome</subject><subject>Down Syndrome - drug therapy</subject><subject>Down Syndrome - physiopathology</subject><subject>Dyrk Kinases</subject><subject>DYRK1A</subject><subject>Enzyme Inhibitors - isolation & purification</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>Humans</subject><subject>Hydrogen Bonding</subject><subject>Inhibitor</subject><subject>Learning and memory deficits</subject><subject>Learning Disabilities - drug therapy</subject><subject>Learning Disabilities - physiopathology</subject><subject>Medical sciences</subject><subject>Memory Disorders - drug therapy</subject><subject>Memory Disorders - physiopathology</subject><subject>Mice</subject><subject>Miscellaneous</subject><subject>Molecular Structure</subject><subject>Neuropharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Pharmacophore</subject><subject>Protein Serine-Threonine Kinases - antagonists & inhibitors</subject><subject>Protein-Tyrosine Kinases - antagonists & inhibitors</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2006</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkM-L1TAQx4Mo7nP1H_Agueitz0mbpA14kfUnLOhBwYuENJnu5tEmNUl3ef-9Le_B3hQGBobPzHz5EPKSwZ4Bk28P-36y474GkHvga9WPyI5xyauGg3hMdqAkVJ3ivy7Is5wPAIwD50_JBZNSdbWUO_L7-1JM8XdIyy0mM-NSvKXmBkPJdIhpG9MRTQo-3FATHJ1wiulIHQ7e-hWKA50xziPSe19u6Yd4H2g-BpfihM_Jk8GMGV-c-yX5-enjj6sv1fW3z1-v3l9XljNRKkQBkinWdsYNwkrV9kwpIZkRaBUYZ6w0ru-bViopOONOKMU63rHa9Q2rm0vy5nR3TvHPgrnoyWeL42gCxiVr2QEHEPy_IGuZ4tBsYH0CbYo5Jxz0nPxk0lEz0Jt9fdCbfb3Z18DX2mK8Ol9f-gndw8pZ9wq8PgMmWzMOyQTr8wPXdgJavn1_d-JwlXbnMelsPQaLzie0Rbvo_5XjL58QowE</recordid><startdate>20060715</startdate><enddate>20060715</enddate><creator>Kim, Nam Doo</creator><creator>Yoon, Jeonghyeok</creator><creator>Kim, Jung Ho</creator><creator>Lee, Jung Tae</creator><creator>Chon, Yong Sog</creator><creator>Hwang, Mi-Kyung</creator><creator>Ha, Ilho</creator><creator>Song, Woo-Joo</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>7QO</scope><scope>7TK</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>7X8</scope></search><sort><creationdate>20060715</creationdate><title>Putative therapeutic agents for the learning and memory deficits of people with Down syndrome</title><author>Kim, Nam Doo ; Yoon, Jeonghyeok ; Kim, Jung Ho ; Lee, Jung Tae ; Chon, Yong Sog ; Hwang, Mi-Kyung ; Ha, Ilho ; Song, Woo-Joo</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-ee50619178adf5c697b199561a5ec90adac6adbb376965414d599184812db3123</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2006</creationdate><topic>Amino Acids - chemistry</topic><topic>Animals</topic><topic>Binding Sites</topic><topic>Biological and medical sciences</topic><topic>Disease Models, Animal</topic><topic>Down syndrome</topic><topic>Down Syndrome - drug therapy</topic><topic>Down Syndrome - physiopathology</topic><topic>Dyrk Kinases</topic><topic>DYRK1A</topic><topic>Enzyme Inhibitors - isolation & purification</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>Humans</topic><topic>Hydrogen Bonding</topic><topic>Inhibitor</topic><topic>Learning and memory deficits</topic><topic>Learning Disabilities - drug therapy</topic><topic>Learning Disabilities - physiopathology</topic><topic>Medical sciences</topic><topic>Memory Disorders - drug therapy</topic><topic>Memory Disorders - physiopathology</topic><topic>Mice</topic><topic>Miscellaneous</topic><topic>Molecular Structure</topic><topic>Neuropharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Pharmacophore</topic><topic>Protein Serine-Threonine Kinases - antagonists & inhibitors</topic><topic>Protein-Tyrosine Kinases - antagonists & inhibitors</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kim, Nam Doo</creatorcontrib><creatorcontrib>Yoon, Jeonghyeok</creatorcontrib><creatorcontrib>Kim, Jung Ho</creatorcontrib><creatorcontrib>Lee, Jung Tae</creatorcontrib><creatorcontrib>Chon, Yong Sog</creatorcontrib><creatorcontrib>Hwang, Mi-Kyung</creatorcontrib><creatorcontrib>Ha, Ilho</creatorcontrib><creatorcontrib>Song, Woo-Joo</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>Biotechnology Research Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kim, Nam Doo</au><au>Yoon, Jeonghyeok</au><au>Kim, Jung Ho</au><au>Lee, Jung Tae</au><au>Chon, Yong Sog</au><au>Hwang, Mi-Kyung</au><au>Ha, Ilho</au><au>Song, Woo-Joo</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Putative therapeutic agents for the learning and memory deficits of people with Down syndrome</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2006-07-15</date><risdate>2006</risdate><volume>16</volume><issue>14</issue><spage>3772</spage><epage>3776</epage><pages>3772-3776</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>A novel series of DYRK1A inhibitors were identified by combination of in silico screening, in vitro assay, and cell-based screenings.
Mental retardation is the most common and debilitating condition for individuals with Down syndrome (DS). The hyper-activation of DYRK1A by overexpression causes significant learning and memory deficits in DS-model mice. Thus far, no mechanism-based drug has been developed to address this. After a combination of in silico and in vitro screenings, two DYRK1A inhibitors were isolated that are active in a cell-based assay. Further optimization could lead to a novel drug discovery that could address DS learning and memory deficits.</abstract><cop>Oxford</cop><pub>Elsevier Ltd</pub><pmid>16698266</pmid><doi>10.1016/j.bmcl.2006.04.042</doi><tpages>5</tpages></addata></record> |
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| subjects | Amino Acids - chemistry Animals Binding Sites Biological and medical sciences Disease Models, Animal Down syndrome Down Syndrome - drug therapy Down Syndrome - physiopathology Dyrk Kinases DYRK1A Enzyme Inhibitors - isolation & purification Enzyme Inhibitors - pharmacology Humans Hydrogen Bonding Inhibitor Learning and memory deficits Learning Disabilities - drug therapy Learning Disabilities - physiopathology Medical sciences Memory Disorders - drug therapy Memory Disorders - physiopathology Mice Miscellaneous Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pharmacophore Protein Serine-Threonine Kinases - antagonists & inhibitors Protein-Tyrosine Kinases - antagonists & inhibitors |
| title | Putative therapeutic agents for the learning and memory deficits of people with Down syndrome |
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