TEAD-YAP interaction inhibitors and MDM2 binders from DNA-encoded indole-focused Ugi-peptidomimetics

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dc.contributor.authorKunig, Verena B. K.
dc.contributor.authorPotowski, Marco
dc.contributor.authorAkbarzadeh, Mohammad
dc.contributor.authorŠkopić, Mateja Klika
dc.contributor.authorSantos Smith, Denise dos
dc.contributor.authorArendt, Lukas
dc.contributor.authorDormuth, Ina
dc.contributor.authorAdihou, Hélène
dc.contributor.authorAndlovic, Blaž
dc.contributor.authorKaratas, Hacer
dc.contributor.authorShaabani, Shabnam
dc.contributor.authorZarganes-Tzitzikas, Tryfon
dc.contributor.authorNeochoritis, Constantinos G.
dc.contributor.authorZhang, Ran
dc.contributor.authorGroves, Matthew
dc.contributor.authorGuéret, Stéphanie M.
dc.contributor.authorOttmann, Christian
dc.contributor.authorRahnenführer, Jörg
dc.contributor.authorFried, Roland
dc.contributor.authorDömling, Alexander
dc.contributor.authorBrunschweiger, Andreas
dc.date.accessioned2021-07-19T11:36:48Z
dc.date.available2021-07-19T11:36:48Z
dc.date.issued2020-06-14
dc.description.abstractDNA-encoded combinatorial synthesis provides efficient and dense coverage of chemical space around privileged molecular structures. The indole side chain of tryptophan plays a prominent role in key, or “hot spot”, regions of protein–protein interactions. A DNA-encoded combinatorial peptoid library was designed based on the Ugi four-component reaction by employing tryptophan-mimetic indole side chains to probe the surface of target proteins. Several peptoids were synthesized on a chemically stable hexathymidine adapter oligonucleotide “hexT”, encoded by DNA sequences, and substituted by azide-alkyne cycloaddition to yield a library of 8112 molecules. Selection experiments for the tumor-relevant proteins MDM2 and TEAD4 yielded MDM2 binders and a novel class of TEAD-YAP interaction inhibitors that perturbed the expression of a gene under the control of these Hippo pathway effectors.en
dc.identifier.urihttp://hdl.handle.net/2003/40334
dc.identifier.urihttp://dx.doi.org/10.17877/DE290R-22209
dc.language.isoende
dc.relation.ispartofseriesAngewandte chemie international edition;Vol. 59. 2020, Issue 46, pp 20338-20342
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectCombinatorial chemistryen
dc.subjectDNA-encoded libraryen
dc.subjectPeptidomimeticsen
dc.subjectProtein–protein interaction inhibitionen
dc.subjectUgi reactionen
dc.subject.ddc570
dc.subject.ddc540
dc.titleTEAD-YAP interaction inhibitors and MDM2 binders from DNA-encoded indole-focused Ugi-peptidomimeticsen
dc.typeTextde
dc.type.publicationtypearticlede
dcterms.accessRightsopen access
eldorado.secondarypublicationtruede
eldorado.secondarypublication.primarycitationAngewandte chemie international edition. Vol. 59. 2020, Issue 46, pp 20338-20342de
eldorado.secondarypublication.primaryidentifierhttps://doi.org/10.1002/anie.202006280de

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