[HTML][HTML] Structure driven compound optimization in targeted protein degradation
TM Leissing, LM Luh, PM Cromm - Drug Discovery Today: Technologies, 2020 - Elsevier
… This review discusses target protein degradation from a structural perspective and
highlights the evolution of certain degraders based on the obtained structural insights. …
highlights the evolution of certain degraders based on the obtained structural insights. …
High-throughput quantitative assay technologies for accelerating the discovery and optimization of targeted protein degradation therapeutics
JR Simard, L Lee, E Vieux, R Improgo… - … the Science of Drug …, 2021 - journals.sagepub.com
… modifications and protein–protein interactions. The field of targeted protein degradation is
an … Cells expressing the tagged target protein are then treated with compound to induce …
an … Cells expressing the tagged target protein are then treated with compound to induce …
Targeted protein degradation: from chemical biology to drug discovery
PM Cromm, CM Crews - Cell chemical biology, 2017 - cell.com
… target effects can hamper compound efficacy. Nucleic acid-based strategies that control protein
… the cell's own protein destruction machinery for selective degradation of essential drivers …
… the cell's own protein destruction machinery for selective degradation of essential drivers …
The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation
… in complete target protein degradation unless they have been extensively optimized. The …
efficacy window of any targeted protein degradation compound. As levels of any given …
efficacy window of any targeted protein degradation compound. As levels of any given …
Development of targeted protein degradation therapeutics
PP Chamberlain, LG Hamann - Nature chemical biology, 2019 - nature.com
… Targeted protein degradation as a therapeutic modality has … : optimization of first-generation
peptidic proteolysis-targeted … advantageous and may allow compounds with only moderate …
peptidic proteolysis-targeted … advantageous and may allow compounds with only moderate …
Fundamental aspects of DMPK optimization of targeted protein degraders
C Cantrill, P Chaturvedi, C Rynn, JP Schaffland… - Drug discovery today, 2020 - Elsevier
… Targeted protein degradation requires several … optimization. Overall, the approaches and
assays described in this section are expected to work both for bRo5 and eRo5 compounds alike…
assays described in this section are expected to work both for bRo5 and eRo5 compounds alike…
Targeted protein degradation: advances, challenges, and prospects for computational methods
… We will start by examining the targeted protein degradation process and the range of …
When developing degrader compounds, it is important to optimize additional properties, …
When developing degrader compounds, it is important to optimize additional properties, …
Targeted protein degradation: Design considerations for PROTAC development
NL Tran, GA Leconte, FM Ferguson - Current protocols, 2022 - Wiley Online Library
… Therefore, evaluating degrader activity in the cellular context that phenotypic assays will be
performed in is advised if different to the workhorse cell lines of the compound optimization. …
performed in is advised if different to the workhorse cell lines of the compound optimization. …
From screening to targeted degradation: strategies for the discovery and optimization of small molecule ligands for PCSK9
WL Petrilli, GC Adam, RS Erdmann… - Cell chemical …, 2020 - cell.com
… Finally, ligand-induced protein degradation was shown with … of PCSK9 and compound 1
to enable the optimization of the … protein-templated in situ click chemistry as a kinetic target-…
to enable the optimization of the … protein-templated in situ click chemistry as a kinetic target-…
Targeted protein degradation: current and future challenges
… optimization [22]. Furthermore, as PROTACs are required to individually bind both the
target protein … to structure-informed lead optimization to identify a compound that can re-enhance …
target protein … to structure-informed lead optimization to identify a compound that can re-enhance …
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