DC Field | Value | Language |
---|---|---|
dc.contributor.author | F Lu | - |
dc.contributor.author | Seung-Wook Chi | - |
dc.contributor.author | Do-heyoung Kim | - |
dc.contributor.author | Kyou Hoon Han | - |
dc.contributor.author | I D Kuntz | - |
dc.contributor.author | R K Guy | - |
dc.date.accessioned | 2017-04-19T09:05:16Z | - |
dc.date.available | 2017-04-19T09:05:16Z | - |
dc.date.issued | 2006 | - |
dc.identifier.issn | 1520-4766 | - |
dc.identifier.uri | 10.1021/cc050142v | ko |
dc.identifier.uri | https://oak.kribb.re.kr/handle/201005/7585 | - |
dc.description.abstract | The p53-MDM2 interaction regulates p53-mediated cellular responses to DNA damage, and MDM2 is overexpressed in 7% of all cancers. Structure-based computational design was applied to this system to design libraries centered on a scaffold that projects side chain functionalities with distance and angular relationships equivalent to those seen in the MDM2 interacting motif of p53. A library of 173 such compounds was synthesized using solution phase parallel chemistry. The in vitro competitive ability of the compounds to block p53 peptide binding to MDM2 was determined using a fluorescence polarization competition assay. The most active compound bound with Kd = 12 μM, and its binding was characterized by 15N-1H HSQC NMR. | - |
dc.publisher | American Chemical Society | ko |
dc.title | Proteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors | - |
dc.title.alternative | Proteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors | - |
dc.type | Article | - |
dc.citation.title | Journal of Combinatorial Chemistry | - |
dc.citation.number | 3 | - |
dc.citation.endPage | 325 | - |
dc.citation.startPage | 315 | - |
dc.citation.volume | 8 | - |
dc.contributor.affiliatedAuthor | Seung-Wook Chi | - |
dc.contributor.affiliatedAuthor | Do-heyoung Kim | - |
dc.contributor.affiliatedAuthor | Kyou Hoon Han | - |
dc.contributor.alternativeName | Lu | - |
dc.contributor.alternativeName | 지승욱 | - |
dc.contributor.alternativeName | 김도형 | - |
dc.contributor.alternativeName | 한규훈 | - |
dc.contributor.alternativeName | Kuntz | - |
dc.contributor.alternativeName | Guy | - |
dc.identifier.bibliographicCitation | Journal of Combinatorial Chemistry, vol. 8, no. 3, pp. 315-325 | - |
dc.identifier.doi | 10.1021/cc050142v | - |
dc.description.journalClass | N | - |
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