Novel mechanisms of molecular glue-induced protein degradation
S Alabi - Biochemistry, 2021 - ACS Publications
Molecular glues, as defined thus far in the targeted protein degradation (TPD) field, are
monovalent small molecules (< 500 Da) that reshape the surface of an E3 ligase receptor …
monovalent small molecules (< 500 Da) that reshape the surface of an E3 ligase receptor …
Molecular glues: the adhesive connecting targeted protein degradation to the clinic
Targeted protein degradation is a rapidly exploding drug discovery strategy that uses small
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
molecules to recruit disease-causing proteins for rapid destruction mainly via the ubiquitin …
Discovery of a molecular glue promoting CDK12-DDB1 interaction to trigger cyclin K degradation
L Lv, P Chen, L Cao, Y Li, Z Zeng, Y Cui, Q Wu, J Li… - Elife, 2020 - elifesciences.org
Molecular-glue degraders mediate interactions between target proteins and components of
the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a …
the ubiquitin-proteasome system to cause selective protein degradation. Here, we report a …
Emerging mechanisms of targeted protein degradation by molecular glues
Targeted protein degradation has emerged as a transformative therapeutic modality for the
treatment of human diseases. The clinical successes of approved protein degraders like …
treatment of human diseases. The clinical successes of approved protein degraders like …
Design principles for cyclin K molecular glue degraders
Z Kozicka, DJ Suchyta, V Focht, G Kempf… - Nature chemical …, 2024 - nature.com
Molecular glue degraders are an effective therapeutic modality, but their design principles
are not well understood. Recently, several unexpectedly diverse compounds were reported …
are not well understood. Recently, several unexpectedly diverse compounds were reported …
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 …
Targeted protein degradation: from mechanisms to clinic
Targeted protein degradation refers to the use of small molecules to induce the selective
degradation of proteins. In its most common form, this degradation is achieved through …
degradation of proteins. In its most common form, this degradation is achieved through …
Haven't got a glue: protein surface variation for the design of molecular glue degraders
Molecular glue degraders are small, drug-like compounds that induce interactions between
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
an E3 ubiquitin ligase and a target, which result in ubiquitination and subsequent …
Molecular glue-mediated targeted protein degradation: A novel strategy in small-molecule drug development
X Tan, Z Huang, H Pei, Z Jia, J Zheng - iScience, 2024 - cell.com
Small-molecule drugs are effective and thus most widely used. However, their applications
are limited by their reliance on active high-affinity binding sites, restricting their target …
are limited by their reliance on active high-affinity binding sites, restricting their target …
The importance of cellular degradation kinetics for understanding mechanisms in targeted protein degradation
Targeted protein degradation has exploded over the past several years due to preclinical
and early clinical therapeutic success of numerous compounds, and the emergence of new …
and early clinical therapeutic success of numerous compounds, and the emergence of new …