Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics
Peptidomimetic motilin antagonists ( 17c and 17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs. We successfully discovered peptidomimetic motilin antagonists ( 17c and 17d) through the improvement of physicochemical proper...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2009-07, Vol.19 (13), p.3426-3429 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Taka, Naoki Matsuoka, Hiroharu Sato, Tsutomu Yoshino, Hitoshi Imaoka, Ikuhiro Sato, Haruhiko Kotake, Ken-ichiro Kumagai, Yoshikazu Kamei, Kenshi Ozaki, Ken-ichi Higashida, Atsuko Kuroki, Toshio |
| description | Peptidomimetic motilin antagonists (
17c and
17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.
We successfully discovered peptidomimetic motilin antagonists (
17c and
17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (
2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs. |
| doi_str_mv | 10.1016/j.bmcl.2009.05.059 |
| format | Article |
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17c and
17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.
We successfully discovered peptidomimetic motilin antagonists (
17c and
17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (
2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2009.05.059</identifier><identifier>PMID: 19481451</identifier><language>eng</language><publisher>Amsterdam: Elsevier Ltd</publisher><subject>Animals ; Biological and medical sciences ; Caco-2 Cells ; Cell Line ; Digestive system ; Drug Discovery ; Gastrointestinal Agents - antagonists & inhibitors ; Gastrointestinal Agents - metabolism ; GM-109 ; Humans ; Medical sciences ; Motilin ; Motilin - antagonists & inhibitors ; Motilin - metabolism ; Motilin receptor antagonist ; Oligopeptides - chemical synthesis ; Oligopeptides - chemistry ; Oligopeptides - pharmacology ; Peptides - chemical synthesis ; Peptides - chemistry ; Peptidomimetics ; Permeability ; Pharmacology. Drug treatments ; Rabbits ; Rats</subject><ispartof>Bioorganic & medicinal chemistry letters, 2009-07, Vol.19 (13), p.3426-3429</ispartof><rights>2009</rights><rights>2009 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c384t-46cc5aff56528194c5ac09b27b8a4da83c7679105bde94932bad57a5eb704e843</citedby><cites>FETCH-LOGICAL-c384t-46cc5aff56528194c5ac09b27b8a4da83c7679105bde94932bad57a5eb704e843</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0960894X09007070$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=21650094$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19481451$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Taka, Naoki</creatorcontrib><creatorcontrib>Matsuoka, Hiroharu</creatorcontrib><creatorcontrib>Sato, Tsutomu</creatorcontrib><creatorcontrib>Yoshino, Hitoshi</creatorcontrib><creatorcontrib>Imaoka, Ikuhiro</creatorcontrib><creatorcontrib>Sato, Haruhiko</creatorcontrib><creatorcontrib>Kotake, Ken-ichiro</creatorcontrib><creatorcontrib>Kumagai, Yoshikazu</creatorcontrib><creatorcontrib>Kamei, Kenshi</creatorcontrib><creatorcontrib>Ozaki, Ken-ichi</creatorcontrib><creatorcontrib>Higashida, Atsuko</creatorcontrib><creatorcontrib>Kuroki, Toshio</creatorcontrib><title>Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>Peptidomimetic motilin antagonists (
17c and
17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.
We successfully discovered peptidomimetic motilin antagonists (
17c and
17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (
2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.</description><subject>Animals</subject><subject>Biological and medical sciences</subject><subject>Caco-2 Cells</subject><subject>Cell Line</subject><subject>Digestive system</subject><subject>Drug Discovery</subject><subject>Gastrointestinal Agents - antagonists & inhibitors</subject><subject>Gastrointestinal Agents - metabolism</subject><subject>GM-109</subject><subject>Humans</subject><subject>Medical sciences</subject><subject>Motilin</subject><subject>Motilin - antagonists & inhibitors</subject><subject>Motilin - metabolism</subject><subject>Motilin receptor antagonist</subject><subject>Oligopeptides - chemical synthesis</subject><subject>Oligopeptides - chemistry</subject><subject>Oligopeptides - pharmacology</subject><subject>Peptides - chemical synthesis</subject><subject>Peptides - chemistry</subject><subject>Peptidomimetics</subject><subject>Permeability</subject><subject>Pharmacology. Drug treatments</subject><subject>Rabbits</subject><subject>Rats</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE1r3DAQhkVpaTZp_0APQZf25q1kS7YVegmbjxYCvbTQmxjL46JFljaSdmH_fWV2SW-BAUnwzDujh5BPnK054-3X7XqYjVvXjKk1k6XUG7LiohVVI5h8S1ZMtazqlfhzQS5T2jLGBRPiPbngSvRcSL4i7s4mEw4YjzRM1Jebo3PI1llPwWf4G7xNOd3QTfCFSjb4BcyYI-xwl-2I1CGMieZAQwTnjhQOYB0MDumJCLOdMVuTPpB3E7iEH8_nFfn9cP9r8716-vn4Y3P7VJmmF7kSrTESpkm2su7LquVhmBrqbuhBjNA3pms7xZkcRlRCNfUAo-xA4tAxgb1orsiXU-4uhuc9pqzn8kt0DjyGfdJt1zSyqChgfQJNDClFnPQu2hniUXOmF8d6qxfHenGsmSylStP1OX0_zDj-bzlLLcDnMwDJgJsieGPTC1fzVpa4Zfq3E4fFxcFi1MlY9AZHG9FkPQb72h7_AG8NnMc</recordid><startdate>20090701</startdate><enddate>20090701</enddate><creator>Taka, Naoki</creator><creator>Matsuoka, Hiroharu</creator><creator>Sato, Tsutomu</creator><creator>Yoshino, Hitoshi</creator><creator>Imaoka, Ikuhiro</creator><creator>Sato, Haruhiko</creator><creator>Kotake, Ken-ichiro</creator><creator>Kumagai, Yoshikazu</creator><creator>Kamei, Kenshi</creator><creator>Ozaki, Ken-ichi</creator><creator>Higashida, Atsuko</creator><creator>Kuroki, Toshio</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>20090701</creationdate><title>Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics</title><author>Taka, Naoki ; Matsuoka, Hiroharu ; Sato, Tsutomu ; Yoshino, Hitoshi ; Imaoka, Ikuhiro ; Sato, Haruhiko ; Kotake, Ken-ichiro ; Kumagai, Yoshikazu ; Kamei, Kenshi ; Ozaki, Ken-ichi ; Higashida, Atsuko ; Kuroki, Toshio</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c384t-46cc5aff56528194c5ac09b27b8a4da83c7679105bde94932bad57a5eb704e843</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Biological and medical sciences</topic><topic>Caco-2 Cells</topic><topic>Cell Line</topic><topic>Digestive system</topic><topic>Drug Discovery</topic><topic>Gastrointestinal Agents - antagonists & inhibitors</topic><topic>Gastrointestinal Agents - metabolism</topic><topic>GM-109</topic><topic>Humans</topic><topic>Medical sciences</topic><topic>Motilin</topic><topic>Motilin - antagonists & inhibitors</topic><topic>Motilin - metabolism</topic><topic>Motilin receptor antagonist</topic><topic>Oligopeptides - chemical synthesis</topic><topic>Oligopeptides - chemistry</topic><topic>Oligopeptides - pharmacology</topic><topic>Peptides - chemical synthesis</topic><topic>Peptides - chemistry</topic><topic>Peptidomimetics</topic><topic>Permeability</topic><topic>Pharmacology. Drug treatments</topic><topic>Rabbits</topic><topic>Rats</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Taka, Naoki</creatorcontrib><creatorcontrib>Matsuoka, Hiroharu</creatorcontrib><creatorcontrib>Sato, Tsutomu</creatorcontrib><creatorcontrib>Yoshino, Hitoshi</creatorcontrib><creatorcontrib>Imaoka, Ikuhiro</creatorcontrib><creatorcontrib>Sato, Haruhiko</creatorcontrib><creatorcontrib>Kotake, Ken-ichiro</creatorcontrib><creatorcontrib>Kumagai, Yoshikazu</creatorcontrib><creatorcontrib>Kamei, Kenshi</creatorcontrib><creatorcontrib>Ozaki, Ken-ichi</creatorcontrib><creatorcontrib>Higashida, Atsuko</creatorcontrib><creatorcontrib>Kuroki, Toshio</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 & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Taka, Naoki</au><au>Matsuoka, Hiroharu</au><au>Sato, Tsutomu</au><au>Yoshino, Hitoshi</au><au>Imaoka, Ikuhiro</au><au>Sato, Haruhiko</au><au>Kotake, Ken-ichiro</au><au>Kumagai, Yoshikazu</au><au>Kamei, Kenshi</au><au>Ozaki, Ken-ichi</au><au>Higashida, Atsuko</au><au>Kuroki, Toshio</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2009-07-01</date><risdate>2009</risdate><volume>19</volume><issue>13</issue><spage>3426</spage><epage>3429</epage><pages>3426-3429</pages><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>Peptidomimetic motilin antagonists (
17c and
17d) were identified. Both compounds dose-dependently suppressed motilin-induced colonic and gastric motility in conscious dogs.
We successfully discovered peptidomimetic motilin antagonists (
17c and
17d) through the improvement of physicochemical properties of a tetrapeptide antagonist (
2). Furthermore, with oral administration and based on motilin antagonistic activity, both compounds suppressed motilin-induced colonic and gastric motility in conscious dogs.</abstract><cop>Amsterdam</cop><pub>Elsevier Ltd</pub><pmid>19481451</pmid><doi>10.1016/j.bmcl.2009.05.059</doi><tpages>4</tpages></addata></record> |
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| ispartof | Bioorganic & medicinal chemistry letters, 2009-07, Vol.19 (13), p.3426-3429 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Biological and medical sciences Caco-2 Cells Cell Line Digestive system Drug Discovery Gastrointestinal Agents - antagonists & inhibitors Gastrointestinal Agents - metabolism GM-109 Humans Medical sciences Motilin Motilin - antagonists & inhibitors Motilin - metabolism Motilin receptor antagonist Oligopeptides - chemical synthesis Oligopeptides - chemistry Oligopeptides - pharmacology Peptides - chemical synthesis Peptides - chemistry Peptidomimetics Permeability Pharmacology. Drug treatments Rabbits Rats |
| title | Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics |
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