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 …
Small-molecule discovery through DNA-encoded libraries
AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …
discovery platforms that enable access to chemical diversity and can quickly reveal new …
[HTML][HTML] Affinity and cooperativity modulate ternary complex formation to drive targeted protein degradation
RP Wurz, H Rui, K Dellamaggiore… - Nature …, 2023 - nature.com
Targeted protein degradation via “hijacking” of the ubiquitin-proteasome system using
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
proteolysis targeting chimeras (PROTACs) has evolved into a novel therapeutic modality …
[HTML][HTML] 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 …
[HTML][HTML] Predicting the structural basis of targeted protein degradation by integrating molecular dynamics simulations with structural mass spectrometry
T Dixon, D MacPherson, B Mostofian… - Nature …, 2022 - nature.com
Targeted protein degradation (TPD) is a promising approach in drug discovery for degrading
proteins implicated in diseases. A key step in this process is the formation of a ternary …
proteins implicated in diseases. A key step in this process is the formation of a ternary …
Ligation to Scavenging Strategy Enables On-Demand Termination of Targeted Protein Degradation
Y Jin, J Fan, R Wang, X Wang, N Li… - Journal of the …, 2023 - ACS Publications
Event-driven bifunctional molecules, typified by proteolysis targeting chimera (PROTAC)
technology, have been successfully applied in degrading many proteins of interest (POI) …
technology, have been successfully applied in degrading many proteins of interest (POI) …
E3 ligase autoinhibition by C-degron mimicry maintains C-degron substrate fidelity
DC Scott, MT King, K Baek, CT Gee, R Kalathur, J Li… - Molecular Cell, 2023 - cell.com
E3 ligase recruitment of proteins containing terminal destabilizing motifs (degrons) is
emerging as a major form of regulation. How those E3s discriminate bona fide substrates …
emerging as a major form of regulation. How those E3s discriminate bona fide substrates …
Proteome-scale discovery of protein degradation and stabilization effectors
J Poirson, H Cho, A Dhillon, S Haider, AZ Imrit… - Nature, 2024 - nature.com
Targeted protein degradation and stabilization are promising therapeutic modalities
because of their potency, versatility and their potential to expand the druggable target …
because of their potency, versatility and their potential to expand the druggable target …
Small molecule inhibitors targeting the cancers
Compared with traditional therapies, targeted therapy has merits in selectivity, efficacy, and
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …
tolerability. Small molecule inhibitors are one of the primary targeted therapies for cancer …
[HTML][HTML] Protein degradation: expanding the toolbox to restrain cancer drug resistance
Despite significant progress in clinical management, drug resistance remains a major
obstacle. Recent research based on protein degradation to restrain drug resistance has …
obstacle. Recent research based on protein degradation to restrain drug resistance has …