Chemically Induced Degradation of Sirtuin 2 (Sirt2) by a Proteolysis Targeting Chimera (PROTAC) Based on Sirtuin Rearranging Ligands (SirReals)

Journal of Medicinal Chemistry

Volumn 61, Issue 2, 2018, Pages 482-491

  Schiedel, Matthias ^a,d   Herp, Daniel ^a   Hammelmann, Sören ^a   Swyter, Sören ^a   Lehotzky, Attila ^b   Robaa, Dina ^c   Oláh, Judit ^b   Ovádi, Judit ^b   Sippl, Wolfgang ^c   Jung, Manfred ^a  

^a UNIVERSITY OF FREIBURG   (Germany)

^b INSTITUTE OF EXPERIMENTAL MEDICINE   (Hungary)

^c MARTIN LUTHER UNIVERSITY HALLE WITTENBERG   (Germany)

^d UNIVERSITY OF OXFORD   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

2 [(4,6 DIMETHYLPYRIMIDIN 2 YL)THIO] N [5 [3 [[1 [4 [2 [[2 (2,6 DIOXOPIPERIDIN 3 YL) 1,3 DIOXOISOINDOLIN 4 YL]OXY]ACETAMIDO]BUTYL] 1H 1,2,3 TRIAZOL 4 YL]METHOXY]BENZYL]THIAZOL 2 YL]ACETAMIDE; 4 AZIDOBUTAN 1 AMINIUM CHLORIDE; BENZYLOXYCARBONYLLEUCYLLEUCYLLEUCINAL; COPPER; DIMETHYL 3 HYDROXYPHTHALATE; DIMETHYL 3 [2 [(4 AZIDOBUTYL)AMINO] 2 OXOETHOXY]PHTHALATE; DIMETHYL SULFOXIDE; LIGAND; N (4 AZIDOBUTYL) 2 CHLOROACETAMIDE; N (4 AZIDOBUTYL) 2 [[2 (2,6 DIOXOPIPERIDIN 3 YL) 1,3 DIOXOISOINDOLIN 4 YL]OXY]ACETAMIDE; PROTEIN INHIBITOR; SIRTUIN 2; SIRTUIN 2 INHIBITOR; THALIDOMIDE; UNCLASSIFIED DRUG; CRBN PROTEIN, HUMAN; PEPTIDE HYDROLASE; SIRT2 PROTEIN, HUMAN;

ALKYNYLATION; ARTICLE; CARBON NUCLEAR MAGNETIC RESONANCE; CATALYSIS; CELL ELONGATION; CHIMERA; CONTROLLED STUDY; CYCLOADDITION; DRUG STRUCTURE; FEMALE; HELA CELL LINE; HUMAN; HUMAN CELL; HYDROGEN BOND; IC50; IN VITRO STUDY; LIGAND BINDING; MICROTUBULE; MOLECULAR MODEL; PROTEIN ACETYLATION; PROTEIN DEGRADATION; PROTEIN TARGETING; PROTON NUCLEAR MAGNETIC RESONANCE; WESTERN BLOTTING; ACETYLATION; ANTAGONISTS AND INHIBITORS; CHEMISTRY; DRUG DESIGN; DRUG EFFECT; METABOLISM; MOLECULAR DOCKING; SYNTHESIS;

ACETYLATION; CHEMISTRY TECHNIQUES, SYNTHETIC; CYCLOADDITION REACTION; DRUG DESIGN; HELA CELLS; HUMANS; LIGANDS; MODELS, MOLECULAR; MOLECULAR DOCKING SIMULATION; PEPTIDE HYDROLASES; PROTEOLYSIS; SIRTUIN 2; THALIDOMIDE;

EID: 85041128346     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01872     Document Type: Article

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