[HTML][HTML] PROTAC targeted protein degraders: the past is prologue
Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to
tackle disease-causing proteins that have historically been highly challenging to target with …
tackle disease-causing proteins that have historically been highly challenging to target with …
[HTML][HTML] A selective and orally bioavailable VHL-recruiting PROTAC achieves SMARCA2 degradation in vivo
Targeted protein degradation offers an alternative modality to classical inhibition and holds
the promise of addressing previously undruggable targets to provide novel therapeutic …
the promise of addressing previously undruggable targets to provide novel therapeutic …
Recent developments in PROTAC‐mediated protein degradation: from bench to clinic
Abstract Proteolysis‐targeting chimeras (PROTACs), an emerging paradigm‐shifting
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
technology, hijacks the ubiquitin‐proteasome system for targeted protein degradation …
Degrader-antibody conjugates
PS Dragovich - Chemical Society Reviews, 2022 - pubs.rsc.org
Degrader-antibody conjugates (DACs) are novel entities that combine a proteolysis
targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical …
targeting chimera (PROTAC) payload with a monoclonal antibody via some type of chemical …
[HTML][HTML] From conception to development: investigating PROTACs features for improved cell permeability and successful protein degradation
C Cecchini, S Pannilunghi, S Tardy… - Frontiers in …, 2021 - frontiersin.org
Proteolysis Targeting Chimeras (PROTACs) are heterobifunctional degraders that
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
specifically eliminate targeted proteins by hijacking the ubiquitin-proteasome system (UPS) …
Direct-to-biology accelerates PROTAC synthesis and the evaluation of linker effects on permeability and degradation
CE Hendrick, JR Jorgensen, C Chaudhry… - ACS medicinal …, 2022 - ACS Publications
A platform to accelerate optimization of proteolysis targeting chimeras (PROTACs) has been
developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large …
developed using a direct-to-biology (D2B) approach with a focus on linker effects. A large …
PROTAC degraders as chemical probes for studying target biology and target validation
Small molecule degraders such as PROTACs (PROteolysis TArgeting Chimeras) have
emerged as new promising pharmacological modalities and the first PROTAC drug …
emerged as new promising pharmacological modalities and the first PROTAC drug …
Amide-to-ester substitution as a strategy for optimizing PROTAC permeability and cellular activity
VG Klein, AG Bond, C Craigon… - Journal of medicinal …, 2021 - ACS Publications
Criteria for predicting the druglike properties of “beyond Rule of 5” Proteolysis Targeting
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Chimeras (PROTAC) degraders are underdeveloped. PROTAC components are often …
Discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-helical peptide in clinical development
V Guerlavais, TK Sawyer, L Carvajal… - Journal of Medicinal …, 2023 - ACS Publications
We report the discovery of sulanemadlin (ALRN-6924), the first cell-permeating, stabilized α-
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …
helical peptide to enter clinical trials. ALRN-6924 is a “stapled peptide” that mimics the N …