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 …

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 …

Proximity-based modalities for biology and medicine

X Liu, A Ciulli - ACS Central Science, 2023 - ACS Publications
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …

Molecular glues for targeted protein degradation: from serendipity to rational discovery

G Dong, Y Ding, S He, C Sheng - Journal of medicinal chemistry, 2021 - ACS Publications
Targeted protein degradation is a promising area in the discovery and development of
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 …

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 …

The CDK inhibitor CR8 acts as a molecular glue degrader that depletes cyclin K

M Słabicki, Z Kozicka, G Petzold, YD Li, M Manojkumar… - Nature, 2020 - nature.com
Molecular glue compounds induce protein–protein interactions that, in the context of a
ubiquitin ligase, lead to protein degradation. Unlike traditional enzyme inhibitors, these …

Microenvironment mapping via Dexter energy transfer on immune cells

JB Geri, JV Oakley, T Reyes-Robles, T Wang… - Science, 2020 - science.org
Many disease pathologies can be understood through the elucidation of localized
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 …

Differential PROTAC substrate specificity dictated by orientation of recruited E3 ligase

BE Smith, SL Wang, S Jaime-Figueroa, A Harbin… - Nature …, 2019 - nature.com
Abstract PROteolysis-TArgeting Chimeras (PROTACs) are hetero-bifunctional molecules
that recruit an E3 ubiquitin ligase to a given substrate protein resulting in its targeted …