Scanning protein surfaces with DNA-encoded libraries

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dc.contributor.authorKunig, Verena B. K.
dc.contributor.authorPotowski, Marco
dc.contributor.authorKlika Škopić, Mateja
dc.contributor.authorBrunschweiger, Andreas
dc.date.accessioned2022-04-27T11:37:27Z
dc.date.available2022-04-27T11:37:27Z
dc.date.issued2020-12-09
dc.description.abstractUnderstanding the ligandability of a target protein, defined as the capability of a protein to bind drug-like compounds on any site, can give important stimuli to drug-development projects. For instance, inhibition of protein–protein interactions usually depends on the identification of protein surface binders. DNA-encoded chemical libraries (DELs) allow scanning of protein surfaces with large chemical space. Encoded library selection screens uncovered several protein–protein interaction inhibitors and compounds binding to the surface of G protein-coupled receptors (GPCRs) and kinases. The protein surface-binding chemotypes from DELs are predominantly chemically modified and cyclized peptides, and functional small-molecule peptidomimetics. Peptoid libraries and structural peptidomimetics have been less studied in the DEL field, hinting at hitherto less populated chemical space and suggesting alternative library designs. Roughly a third of bioactive molecules evolved from smaller, target-focused libraries. They showcase the potential of encoded libraries to identify more potent molecules from weak, for example, fragment-like, starting points.en
dc.identifier.urihttp://hdl.handle.net/2003/40885
dc.identifier.urihttp://dx.doi.org/10.17877/DE290R-22742
dc.language.isoende
dc.relation.ispartofseriesChemMedChem;16(7)
dc.rights.urihttps://creativecommons.org/licenses/by/4.0/
dc.subjectDNA-encoded librariesen
dc.subjectDrug developmenten
dc.subjectPeptidomimeticsen
dc.subjectProtein-protein interactionsen
dc.subjectScreeningen
dc.subject.ddc570
dc.subject.ddc540
dc.titleScanning protein surfaces with DNA-encoded librariesen
dc.typeTextde
dc.type.publicationtypearticlede
dcterms.accessRightsopen access
eldorado.secondarypublicationtruede
eldorado.secondarypublication.primarycitationV. B. K. Kunig, M. Potowski, M. Klika Škopić, A. Brunschweiger, ChemMedChem 2021, 16, 1048.de
eldorado.secondarypublication.primaryidentifierhttps://doi.org/10.1002/cmdc.202000869de

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