Proteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors

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dc.contributor.authorF Lu-
dc.contributor.authorSeung-Wook Chi-
dc.contributor.authorDo-heyoung Kim-
dc.contributor.authorKyou Hoon Han-
dc.contributor.authorI D Kuntz-
dc.contributor.authorR K Guy-
dc.date.accessioned2017-04-19T09:05:16Z-
dc.date.available2017-04-19T09:05:16Z-
dc.date.issued2006-
dc.identifier.issn1520-4766-
dc.identifier.uri10.1021/cc050142vko
dc.identifier.urihttps://oak.kribb.re.kr/handle/201005/7585-
dc.description.abstractThe 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.publisherAmerican Chemical Societyko
dc.titleProteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors-
dc.title.alternativeProteomimetic libraries: design, synthesis, and evaluation of p53-MDM2 interaction inhibitors-
dc.typeArticle-
dc.citation.titleJournal of Combinatorial Chemistry-
dc.citation.number3-
dc.citation.endPage325-
dc.citation.startPage315-
dc.citation.volume8-
dc.contributor.affiliatedAuthorSeung-Wook Chi-
dc.contributor.affiliatedAuthorDo-heyoung Kim-
dc.contributor.affiliatedAuthorKyou Hoon Han-
dc.contributor.alternativeNameLu-
dc.contributor.alternativeName지승욱-
dc.contributor.alternativeName김도형-
dc.contributor.alternativeName한규훈-
dc.contributor.alternativeNameKuntz-
dc.contributor.alternativeNameGuy-
dc.identifier.bibliographicCitationJournal of Combinatorial Chemistry, vol. 8, no. 3, pp. 315-325-
dc.identifier.doi10.1021/cc050142v-
dc.description.journalClassN-
Appears in Collections:
Division of Biomedical Research > 1. Journal Articles
Division of Bio Technology Innovation > Core Research Facility & Analysis Center > 1. Journal Articles
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