Targeted protein degradation: mechanisms, strategies and application
L Zhao, J Zhao, K Zhong, A Tong, D Jia - Signal transduction and …, 2022 - nature.com
Traditional drug discovery mainly focuses on direct regulation of protein activity. The
development and application of protein activity modulators, particularly inhibitors, has been …
development and application of protein activity modulators, particularly inhibitors, has been …
Payload diversification: a key step in the development of antibody–drug conjugates
L Conilh, L Sadilkova, W Viricel, C Dumontet - Journal of Hematology & …, 2023 - Springer
Antibody–drug conjugates (ADCs) is a fast moving class of targeted biotherapeutics that
currently combines the selectivity of monoclonal antibodies with the potency of a payload …
currently combines the selectivity of monoclonal antibodies with the potency of a payload …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
Molecular glues for targeted protein degradation: from serendipity to rational discovery
Targeted protein degradation is a promising area in the discovery and development of
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
innovative therapeutics. Molecular glues mediate proximity-induced protein degradation and …
The rise of molecular glues
SL Schreiber - Cell, 2021 - cell.com
2021 marks the 30th anniversary of the revelation that cyclosporin A and FK506 act in a way
previously not seen—as" molecular glues" that induce neo-protein–protein associations. As …
previously not seen—as" molecular glues" that induce neo-protein–protein associations. As …
Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K
Molecular glue compounds induce protein–protein interactions that, in the context of a
ubiquitin ligase, lead to protein degradation. Unlike traditional enzyme inhibitors, these …
ubiquitin ligase, lead to protein degradation. Unlike traditional enzyme inhibitors, these …
Microenvironment mapping via Dexter energy transfer on immune cells
Many disease pathologies can be understood through the elucidation of localized
biomolecular networks, or microenvironments. To this end, enzymatic proximity labeling …
biomolecular networks, or microenvironments. To this end, enzymatic proximity labeling …
Late-stage diversification of natural products
B Hong, T Luo, X Lei - ACS central science, 2020 - ACS Publications
Late-stage diversification of natural products is an efficient way to generate natural product
derivatives for drug discovery and chemical biology. Benefiting from the development of site …
derivatives for drug discovery and chemical biology. Benefiting from the development of site …
Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase
Abstract PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …