User: Guest  Login
Title:

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

Document type:
Journal Article; Research Support, Non-U.S. Gov't
Author(s):
Lier, Svenja; Sellmer, Andreas; Orben, Felix; Heinzlmeir, Stephanie; Krauß, Lukas; Schneeweis, Christian; Hassan, Zonera; Schneider, Carolin; Patricia Gloria Schäfer, Arlett; 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...     »
Journal title abbreviation:
Bioorg Chem
Year:
2022
Journal volume:
119
Fulltext / DOI:
doi:10.1016/j.bioorg.2021.105505
Pubmed ID:
http://view.ncbi.nlm.nih.gov/pubmed/34838332
Print-ISSN:
0045-2068
TUM Institution:
Klinik und Poliklinik für Innere Medizin II, Gastroenterologie; Klinik und Poliklinik für Innere Medizin III, Hämatologie und Onkologie; Lehrstuhl für Translationale Tumorforschung (DKTK) (Prof. Saur); Professur für Molekulare Onkologie und Funktionelle Genomik (Prof. Rad)
 BibTeX