Fundamental aspects of DMPK optimization of targeted protein degraders.
Sign Up to like & getrecommendations! Published in 2020 at "Drug discovery today"
DOI: 10.1016/j.drudis.2020.03.012
Abstract: Targeted protein degraders are an emerging modality. Their properties fall outside the traditional small-molecule property space and are in the 'beyond rule of 5' space. Consequently, drug discovery programs focused on developing orally available degraders… read more here.
Keywords: aspects dmpk; protein degraders; optimization; targeted protein ... See more keywords
A Versatile and Sustainable Multicomponent Platform for the Synthesis of Protein Degraders: Proof-of-Concept Application to BRD4-Degrading PROTACs
Sign Up to like & getrecommendations! Published in 2022 at "Journal of Medicinal Chemistry"
DOI: 10.1021/acs.jmedchem.2c01218
Abstract: The use of small molecules to induce targeted protein degradation is increasingly growing in the drug discovery landscape, and protein degraders have progressed rapidly through the pipelines. Despite the advances made so far, their synthesis… read more here.
Keywords: protacs; synthesis; protein degraders; degrading protacs ... See more keywords
Discovery of CRBN as a target of thalidomide: a breakthrough for progress in the development of protein degraders.
Sign Up to like & getrecommendations! Published in 2022 at "Chemical Society reviews"
DOI: 10.1039/d2cs00116k
Abstract: Progress in strategies aimed at breaking down therapeutic target proteins has led to a paradigm shift in drug discovery. Thalidomide and its derivatives are the only protein degraders currently used in clinical practice. Our understanding… read more here.
Keywords: thalidomide derivatives; crbn; progress; protein degraders ... See more keywords