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dc.contributor.authorGrotli, M.
dc.contributor.authorKoenig, B.
dc.contributor.authorKuzmanovic, N.
dc.contributor.authorSippl, W.
dc.contributor.authorJung, M.
dc.contributor.authorFalenczyk, C.
dc.contributor.authorSchiedel, M.
dc.contributor.authorKaraman, B.
dc.contributor.authorRumpf, T.
dc.date.accessioned2022-02-18T11:17:12Z
dc.date.available2022-02-18T11:17:12Z
dc.date.issued2014
dc.identifier.citationFalenczyk C., Schiedel M., Karaman B., Rumpf T., Kuzmanovic N., Grotli M., Sippl W., Jung M., Koenig B., "Chromo-pharmacophores: photochromic diarylmaleimide inhibitors for sirtuins", CHEMICAL SCIENCE, cilt.5, sa.12, ss.4794-4799, 2014
dc.identifier.issn2041-6520
dc.identifier.otherav_e65b2ecf-73e1-4ca3-821c-3c2e247da8ad
dc.identifier.othervv_1032021
dc.identifier.urihttp://hdl.handle.net/20.500.12627/180842
dc.identifier.urihttps://doi.org/10.1039/c4sc01346h
dc.description.abstractControlling the activity of sirtuins is of high biomedical relevance as the enzymes are involved in cancer, neurodegeneration and other diseases. Therefore structural elements of 3,4-bisindoylmaleimides (BIMs), which are known NAD(+)-dependent histone deacetylase (sirtuin) inhibitors, were merged with photochromic diarylmaleimides to yield photoswitchable enzyme inhibitors. The new inhibitors show excellent photophysical properties, are switchable even in polar solvents, and subtype selective against hSirt2. The inhibitory activity changes up to a factor of 22 for the two photoisomers and physiological properties can therefore be effectively toggled by irradiation with light of different wavelengths. Docking experiments using the enzyme crystal structure explain the observed activity changes based on the steric demand of the thiophene substitution and the rigidity of the molecular structure.
dc.language.isoeng
dc.subjectPhysical Sciences
dc.subjectAlkoloidler
dc.subjectGeneral Chemistry
dc.subjectTemel Bilimler
dc.subjectChemistry (miscellaneous)
dc.subjectBiyokimya
dc.subjectTemel Bilimler (SCI)
dc.subjectKimya
dc.subjectKİMYA, MULTİDİSİPLİNER
dc.titleChromo-pharmacophores: photochromic diarylmaleimide inhibitors for sirtuins
dc.typeMakale
dc.relation.journalCHEMICAL SCIENCE
dc.contributor.departmentUniversity of Regensburg , ,
dc.identifier.volume5
dc.identifier.issue12
dc.identifier.startpage4794
dc.identifier.endpage4799
dc.contributor.firstauthorID3381700


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