DC Field | Value | Language |
---|---|---|
dc.contributor.author | Moon, H | - |
dc.contributor.author | Lee, WS | - |
dc.contributor.author | Oh, M | - |
dc.contributor.author | Lee, H | - |
dc.contributor.author | Lee, JH | - |
dc.contributor.author | Im, W | - |
dc.contributor.author | Lim, HS | - |
dc.date.accessioned | 2016-04-01T07:59:28Z | - |
dc.date.available | 2016-04-01T07:59:28Z | - |
dc.date.created | 2015-06-01 | - |
dc.date.issued | 2014-12 | - |
dc.identifier.issn | 2156-8952 | - |
dc.identifier.other | 2015-OAK-0000032662 | - |
dc.identifier.uri | https://oasis.postech.ac.kr/handle/2014.oak/27096 | - |
dc.description.abstract | alpha-Helices play a critical role in mediating many protein-protein interactions (PPIs) as recognition motifs. Therefore, there is a considerable interest in developing small molecules that can mimic helical peptide segments to modulate alpha-helix-mediated PPIs. Due to the relatively low aqueous solubility and synthetic difficulty of most current alpha-helix mimetic small molecules, one important goal in this area is to develop small molecules with favorable physicochemical properties and ease of synthesis. Here we designed phenyl-piperazine-triazine-based alpha-helix mimetics that possess improved water solubility and excellent synthetic accessibility. We developed a facile solid-phase synthetic route that allows for rapid creation of a large, diverse combinatorial library of alpha-helix mimetics. Further, we identified a selective inhibitor of the Mcl-1/BH3 interaction by screening a focused library of phenyl-piperazine-triazines, demonstrating that the scaffold is able to serve as functional mimetics of alpha-helical peptides. We believe that our phenyl-piperazine-triazine-based alpha-helix mimetics, along with the facile and divergent solid-phase synthetic method, have great potential as powerful tools for discovering potent inhibitors of given alpha-helix-mediated PPIs. | - |
dc.description.statementofresponsibility | ungraded | - |
dc.language | English | - |
dc.publisher | AMER CHEMICAL SOC | - |
dc.relation.isPartOf | ACS COMBINATORIAL SCIENCE | - |
dc.title | Design, Solid-Phase Synthesis, and Evaluation of a Phenyl-Piperazine-Triazine Scaffold as alpha-Helix Mimetics | - |
dc.type | Article | - |
dc.contributor.college | 화학과 | - |
dc.identifier.doi | 10.1021/CO500114F | - |
dc.author.google | Moon, H | - |
dc.author.google | Lee, WS | - |
dc.author.google | Oh, M | - |
dc.author.google | Lee, H | - |
dc.author.google | Lee, JH | - |
dc.author.google | Im, W | - |
dc.author.google | Lim, HS | - |
dc.relation.volume | 16 | - |
dc.relation.issue | 12 | - |
dc.relation.startpage | 695 | - |
dc.relation.lastpage | 701 | - |
dc.contributor.id | 10115917 | - |
dc.relation.journal | ACS COMBINATORIAL SCIENCE | - |
dc.relation.sci | SCI | - |
dc.collections.name | Journal Papers | - |
dc.type.rims | ART | - |
dc.identifier.bibliographicCitation | ACS COMBINATORIAL SCIENCE, v.16, no.12, pp.695 - 701 | - |
dc.identifier.wosid | 000346114600006 | - |
dc.date.tcdate | 2019-02-01 | - |
dc.citation.endPage | 701 | - |
dc.citation.number | 12 | - |
dc.citation.startPage | 695 | - |
dc.citation.title | ACS COMBINATORIAL SCIENCE | - |
dc.citation.volume | 16 | - |
dc.contributor.affiliatedAuthor | Lim, HS | - |
dc.identifier.scopusid | 2-s2.0-84909624147 | - |
dc.description.journalClass | 1 | - |
dc.description.journalClass | 1 | - |
dc.description.wostc | 11 | - |
dc.description.scptc | 13 | * |
dc.date.scptcdate | 2018-05-121 | * |
dc.type.docType | Article | - |
dc.subject.keywordPlus | PROTEIN-PROTEIN INTERACTIONS | - |
dc.subject.keywordPlus | SMALL-MOLECULE INHIBITORS | - |
dc.subject.keywordPlus | DRUG DISCOVERY | - |
dc.subject.keywordPlus | MCL-1 | - |
dc.subject.keywordPlus | DERIVATIVES | - |
dc.subject.keywordPlus | MIMICS | - |
dc.subject.keywordPlus | STRATEGIES | - |
dc.subject.keywordPlus | INTERFACES | - |
dc.subject.keywordPlus | PEPTIDES | - |
dc.subject.keywordPlus | AGENTS | - |
dc.subject.keywordAuthor | alpha-helix mimetics | - |
dc.subject.keywordAuthor | solid-phase synthesis | - |
dc.subject.keywordAuthor | combinatorial library | - |
dc.subject.keywordAuthor | protein-protein interaction inhibitor | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Applied | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Medicinal | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Multidisciplinary | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalResearchArea | Pharmacology & Pharmacy | - |
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