Methods to characterize and discover molecular degraders in cells

Lin, Zhi; Woo, Christina M.

doi:10.1039/d2cs00261b

Cited by 3 publications

(3 citation statements)

References 153 publications

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“…These examples demonstrate the potential of CtD synthetic strategy to revolutionize the discovery of first‐in‐class MGs by enabling the generation of diverse libraries of compounds starting from complex natural products [5–6,75,117–119] . This approach is supported by the use of several screening technologies that enable the identification of new MGs including high‐throughput screening (HTS) [5–6,75,118,183] . Another important screening tool is the activity‐based protein profiling that employs LCMS/MS to identify protein degraders [183–185] .…”

Section: Protein Degradersmentioning

confidence: 98%

“…[5][6]75,[117][118][119] This approach is supported by the use of several screening technologies that enable the identification of new MGs including highthroughput screening (HTS). [5][6]75,118,183] Another important screening tool is the activity-based protein profiling that employs LCMS/MS to identify protein degraders. [183][184][185] These technologies, and others, can help enable the identification of new molecular glues by enabling the rapid screening and…”

Section: Chemmedchemmentioning

confidence: 99%

“…[5][6]75,118,183] Another important screening tool is the activity-based protein profiling that employs LCMS/MS to identify protein degraders. [183][184][185] These technologies, and others, can help enable the identification of new molecular glues by enabling the rapid screening and…”

Section: Chemmedchemmentioning

confidence: 99%

See 2 more Smart Citations

Complexity‐to‐Diversity and Pseudo‐Natural Product Strategies as Powerful Platforms for Deciphering Next‐Generation Therapeutics

et al. 2023

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Stereochemical and skeletal complexity are particularly important vis‐à‐vis the cross‐talks between a small molecule and a complementary active site of a biological target. This intricate harmony is known to increase selectivity, reduce toxicity, and increase the success rate in clinical trials. Therefore, the development of novel strategies for establishing underrepresented chemical space that is rich in stereochemical and skeletal diversity is an important milestone in a drug discovery campaign. In this review, we discuss the evolution of interdisciplinary synthetic methodologies utilized in chemical biology and drug discovery that has revolutionized the discovery of first‐in‐class molecules over the last decade with an emphasis on complexity‐to‐diversity and pseudo‐natural product strategies as a remarkable toolbox for deciphering next‐generation therapeutics. We also report how these approaches dramatically revolutionized the discovery of novel chemical probes that target underrepresented biological space. We also highlight selected applications and discuss key opportunities offered by these tools and important synthetic strategies used for the construction of chemical spaces that are rich in skeletal and stereochemical diversity. We also provide insight on how the integration of these protocols has the promise of changing the drug discovery landscape.

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Section: Protein Degradersmentioning

confidence: 98%