Discovery and the structural basis of a novel p21-activated kinase 4 inhibitor
DC Field | Value | Language |
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dc.contributor.author | Ryu, Byung Jun | - |
dc.contributor.author | Kim, Sunmin | - |
dc.contributor.author | Min, Bora | - |
dc.contributor.author | Kim, Keon Young | - |
dc.contributor.author | Lee, Jin Soo | - |
dc.contributor.author | Park, Whui Jung | - |
dc.contributor.author | Lee, Hyuk | - |
dc.contributor.author | Kim, Seong Hwan | - |
dc.contributor.author | Park, SangYoun | - |
dc.date.available | 2018-05-09T11:05:16Z | - |
dc.date.created | 2018-04-17 | - |
dc.date.issued | 2014-07-10 | - |
dc.identifier.issn | 0304-3835 | - |
dc.identifier.uri | http://scholarworks.bwise.kr/ssu/handle/2018.sw.ssu/9995 | - |
dc.description.abstract | Functional versatility and elevated expression in cancers have endowed p21-activated kinase 4 (PAK4) as one of the first-in-class anti-cancer drug target. In this study, a novel PAK4 inhibitor, KY-04031 (N-2-(2-(1H-indol-3-yflethyl)-N-4-(1H-indazol-5-yl)-6-methoxy-1,3,5-triazine-2,4-diamine), was discovered using a high-throughput screening. Analysis of the complex crystal structure illustrated that both indole and indazole of KY-04031 are responsible for PAK4 hinge interaction. Moreover, the molecule's triazine core was found to mimic the ribose of the natural ATP substrate. The cell-based anti-cancer potency of KY-04031 was less effective than the pyrroloaminopyrazoles; however, the unique molecular feature of KY-04031 can be exploited in designing new PAK4 inhibitors. (C) 2014 Elsevier Ireland Ltd. All rights reserved. | - |
dc.publisher | ELSEVIER IRELAND LTD | - |
dc.relation.isPartOf | CANCER LETTERS | - |
dc.subject | ANCHORAGE-INDEPENDENT GROWTH | - |
dc.subject | SERINE/THREONINE KINASE | - |
dc.subject | PAK4 KINASE | - |
dc.subject | CELLS | - |
dc.title | Discovery and the structural basis of a novel p21-activated kinase 4 inhibitor | - |
dc.type | Article | - |
dc.identifier.doi | 10.1016/j.canlet.2014.03.024 | - |
dc.type.rims | ART | - |
dc.identifier.bibliographicCitation | CANCER LETTERS, v.349, no.1, pp.45 - 50 | - |
dc.description.journalClass | 1 | - |
dc.identifier.wosid | 000337213900006 | - |
dc.identifier.scopusid | 2-s2.0-84901041726 | - |
dc.citation.endPage | 50 | - |
dc.citation.number | 1 | - |
dc.citation.startPage | 45 | - |
dc.citation.title | CANCER LETTERS | - |
dc.citation.volume | 349 | - |
dc.contributor.affiliatedAuthor | Park, SangYoun | - |
dc.type.docType | Article | - |
dc.subject.keywordAuthor | PAK4 | - |
dc.subject.keywordAuthor | HTS | - |
dc.subject.keywordAuthor | Protein kinase | - |
dc.subject.keywordAuthor | Cancer | - |
dc.subject.keywordAuthor | Drug discovery | - |
dc.subject.keywordAuthor | X-ray crystallography | - |
dc.subject.keywordPlus | ANCHORAGE-INDEPENDENT GROWTH | - |
dc.subject.keywordPlus | SERINE/THREONINE KINASE | - |
dc.subject.keywordPlus | PAK4 KINASE | - |
dc.subject.keywordPlus | CELLS | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
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