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Title:

A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer

Document type:
Zeitschriftenaufsatz
Author(s):
Lier, Svenja; Sellmer, Andreas; Orben, Felix; Heinzlmeir, Stephanie; Krauß, Lukas; Schneeweis, Christian; Hassan, Zonera; Schneider, Carolin; Schäfer, Arlette; Pongratz, Herwig; Engleitner, Thomas; Öllinger, Rupert; Kuisl, Anna; Bassermann, Florian; Schlag, Christoph; Kong, Bo; Dove, Stefan; Kuster, Bernhard; Rad, Roland; Reichert, Maximilian; Wirth, Matthias; Saur, Dieter; Mahboobi, Siavosh; Schneider, Günter
Abstract:
Targeted protein degradation offers new opportunities to inactivate cancer drivers and has successfully entered the clinic. Ways to induce selective protein degradation include proteolysis targeting chimera (PROTAC) technology and immunomodulatory (IMiDs) / next-generation Cereblon (CRBN) E3 ligase modulating drugs (CELMoDs). Here, we aimed to develop a MYC PROTAC based on the MYC-MAX dimerization inhibitor 10058-F4 derivative 28RH and Thalidomide, called MDEG-541. We show that a subgroup of gas...     »
Keywords:
BayBioMS; Cereblon; GSPT1; GSPT2; MYC; PLK1
Journal title:
Bioorganic Chemistry
Year:
2021
Pages contribution:
105505
Fulltext / DOI:
doi:10.1016/j.bioorg.2021.105505
Publisher:
Elsevier BV
E-ISSN:
0045-2068
Date of publication:
01.11.2021
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