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dc.creatorVan Zandt, Michael C.-
dc.creatorWhitehouse, Darren L.-
dc.creatorGolebiowski, Adam-
dc.creatorJi, Min Koo-
dc.creatorZhang, Mingbao-
dc.creatorBeckett, R. Paul-
dc.creatorJagdmann, G. Erik-
dc.creatorRyder, Todd R.-
dc.creatorSheeler, Ryan-
dc.creatorAndreoli, Monica-
dc.creatorConway, Bruce-
dc.creatorMahboubi, Keyvan-
dc.creatorD’Angelo, Gerard-
dc.creatorMitschler, Andre-
dc.creatorCousido Siah, Alexandra-
dc.creatorRuiz, Frances X.-
dc.creatorHoward, Eduardo Ignacio-
dc.creatorPodjarny, Alberto Daniel-
dc.creatorSchroeter, Hagen-
dc.date2017-09-05T13:52:03Z-
dc.date2017-09-05T13:52:03Z-
dc.date2013-03-
dc.date2017-09-01T17:44:32Z-
dc.date.accessioned2019-04-29T15:45:58Z-
dc.date.available2019-04-29T15:45:58Z-
dc.date.issued2013-03-
dc.identifierVan Zandt, Michael C.; Whitehouse, Darren L.; Golebiowski, Adam; Ji, Min Koo; Zhang, Mingbao; et al.; Discovery of (R)-2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury; American Chemical Society; Journal of Medicinal Chemistry; 56; 6; 3-2013; 2568-2580-
dc.identifier0022-2623-
dc.identifierhttp://hdl.handle.net/11336/23649-
dc.identifierCONICET Digital-
dc.identifierCONICET-
dc.identifier.urihttp://rodna.bn.gov.ar:8080/jspui/handle/bnmm/301465-
dc.descriptionRecent efforts to identify treatments for myocardial ischemia reperfusion injury have resulted in the discovery of a novel series of highly potent α,α-disubstituted amino acid-based arginase inhibitors. The lead candidate, (R)-2-amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic acid, compound 9, inhibits human arginases I and II with IC50s of 223 and 509 nM, respectively, and is active in a recombinant cellular assay overexpressing human arginase I (CHO cells). It is 28% orally bioavailable and significantly reduces the infarct size in a rat model of myocardial ischemia/reperfusion injury. Herein, we report the design, synthesis, and structure−activity relationships (SAR) for this novel series of inhibitors along with pharmacokinetic and in vivo efficacy data for compound 9 and X-ray crystallography data for selected lead compounds cocrystallized with arginases I and II.-
dc.descriptionFil: Van Zandt, Michael C.. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Whitehouse, Darren L.. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Golebiowski, Adam. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Ji, Min Koo. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Zhang, Mingbao. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Beckett, R. Paul. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Jagdmann, G. Erik. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Ryder, Todd R.. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Sheeler, Ryan. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Andreoli, Monica. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Conway, Bruce. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Mahboubi, Keyvan. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: D’Angelo, Gerard. Institutes for Pharmaceutical Discovery; Estados Unidos-
dc.descriptionFil: Mitschler, Andre. Université de Strasbourg; Francia-
dc.descriptionFil: Cousido Siah, Alexandra. Université de Strasbourg; Francia-
dc.descriptionFil: Ruiz, Frances X.. Université de Strasbourg; Francia-
dc.descriptionFil: Howard, Eduardo Ignacio. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - La Plata. Instituto de Física de Líquidos y Sistemas Biológicos. Universidad Nacional de La Plata. Facultad de Ciencias Exactas. Instituto de Física de Líquidos y Sistemas Biológicos; Argentina. Université de Strasbourg; Francia-
dc.descriptionFil: Podjarny, Alberto Daniel. Université de Strasbourg; Francia-
dc.descriptionFil: Schroeter, Hagen. Mars Incorporated; Estados Unidos-
dc.formatapplication/pdf-
dc.formatapplication/pdf-
dc.languageeng-
dc.publisherAmerican Chemical Society-
dc.relationinfo:eu-repo/semantics/altIdentifier/doi/http://dx.doi.org/10.1021/jm400014c-
dc.relationinfo:eu-repo/semantics/altIdentifier/url/http://pubs.acs.org/doi/abs/10.1021/jm400014c-
dc.rightsinfo:eu-repo/semantics/restrictedAccess-
dc.rightshttps://creativecommons.org/licenses/by-nc-sa/2.5/ar/-
dc.sourcereponame:CONICET Digital (CONICET)-
dc.sourceinstname:Consejo Nacional de Investigaciones Científicas y Técnicas-
dc.sourceinstacron:CONICET-
dc.subjectHuman Arginases I and II-
dc.subjectInhibitors-
dc.subjectStructure-activity relationships (SAR)-
dc.subjectBioquímica y Biología Molecular-
dc.subjectCiencias Biológicas-
dc.subjectCIENCIAS NATURALES Y EXACTAS-
dc.titleDiscovery of (R)-2-Amino-6-borono-2-(2-(piperidin-1-yl)ethyl)hexanoic Acid and Congeners As Highly Potent Inhibitors of Human Arginases I and II for Treatment of Myocardial Reperfusion Injury-
dc.typeinfo:eu-repo/semantics/article-
dc.typeinfo:eu-repo/semantics/publishedVersion-
dc.typeinfo:ar-repo/semantics/articulo-
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