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 …
Molecular glues: The adhesive connecting targeted protein degradation to the clinic
JM Sasso, R Tenchov, DS Wang, LS Johnson… - Biochemistry, 2022 - ACS Publications
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 …
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 …
[HTML][HTML] 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 …
Prey for the proteasome: targeted protein degradation—a medicinal chemist's perspective
LM Luh, U Scheib, K Juenemann… - Angewandte Chemie …, 2020 - Wiley Online Library
Targeted protein degradation (TPD), the ability to control a proteins fate by triggering its
degradation in a highly selective and effective manner, has created tremendous excitement …
degradation in a highly selective and effective manner, has created tremendous excitement …
Critical assessment of targeted protein degradation as a research tool and pharmacological modality
Small molecules continue to dominate drug discovery because of their ease of use, lower
cost of manufacturing, and access to intracellular targets. However, despite these …
cost of manufacturing, and access to intracellular targets. However, despite these …
Chemical-mediated targeted protein degradation in neurodegenerative diseases
S Hyun, D Shin - Life, 2021 - mdpi.com
Neurodegenerative diseases, including Alzheimer's disease, Huntington's disease, and
Parkinson's disease, are a class of diseases that lead to dysfunction of cognition and …
Parkinson's disease, are a class of diseases that lead to dysfunction of cognition and …
Rational discovery of molecular glue degraders via scalable chemical profiling
C Mayor-Ruiz, S Bauer, M Brand, Z Kozicka… - Nature chemical …, 2020 - nature.com
Targeted protein degradation is a new therapeutic modality based on drugs that destabilize
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
proteins by inducing their proximity to E3 ubiquitin ligases. Of particular interest are …
[PDF][PDF] 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 …
[HTML][HTML] Proteolysis targeting chimeras (PROTACs) come of age: entering the third decade of targeted protein degradation
MJ Bond, CM Crews - RSC chemical biology, 2021 - pubs.rsc.org
With the discovery of PROteolysis TArgeting Chimeras (PROTACs) twenty years ago,
targeted protein degradation (TPD) has changed the landscape of drug development …
targeted protein degradation (TPD) has changed the landscape of drug development …