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 …
E3 ligase ligands for PROTACs: how they were found and how to discover new ones
T Ishida, A Ciulli - … Advancing the Science of Drug Discovery, 2021 - journals.sagepub.com
Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are
a new modality of chemical tools and potential therapeutics to understand and treat human …
a new modality of chemical tools and potential therapeutics to understand and treat human …
Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity
S Imaide, KM Riching, N Makukhin, V Vetma… - Nature chemical …, 2021 - nature.com
Bivalent proteolysis-targeting chimeras (PROTACs) drive protein degradation by
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
simultaneously binding a target protein and an E3 ligase and forming a productive ternary …
Discovery of XL01126: a potent, fast, cooperative, selective, orally bioavailable, and blood–brain barrier penetrant PROTAC degrader of leucine-rich repeat kinase 2
X Liu, AF Kalogeropulou, S Domingos… - Journal of the …, 2022 - ACS Publications
Leucine-rich repeat kinase 2 (LRRK2) is one of the most promising targets for Parkinson's
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …
disease. LRRK2-targeting strategies have primarily focused on type 1 kinase inhibitors …
[HTML][HTML] Current strategies for the design of PROTAC linkers: a critical review
RI Troup, C Fallan, MGJ Baud - Exploration of Targeted Anti-tumor …, 2020 - ncbi.nlm.nih.gov
Abstract PROteolysis TArgeting Chimeras (PROTACs) are heterobifunctional molecules
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
consisting of two ligands; an “anchor” to bind to an E3 ubiquitin ligase and a “warhead” to …
Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders
Targeted protein degradation is a novel pharmacology established by drugs that recruit
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
target proteins to E3 ubiquitin ligases. Based on the structure of the degrader and the target …
Multispecific drugs herald a new era of biopharmaceutical innovation
RJ Deshaies - Nature, 2020 - nature.com
The modern biopharmaceutical industry traces its roots to the dawn of the twentieth century,
coincident with marketing of aspirin—a signature event in the history of modern drug …
coincident with marketing of aspirin—a signature event in the history of modern drug …
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges
S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …
Defining molecular glues with a dual-nanobody cannabidiol sensor
Abstract “Molecular glue”(MG) is a term coined to describe the mechanism of action of the
plant hormone auxin and subsequently used to characterize synthetic small molecule …
plant hormone auxin and subsequently used to characterize synthetic small molecule …
Structure‐based design of a macrocyclic PROTAC
Constraining a molecule in its bioactive conformation via macrocyclization represents an
attractive strategy to rationally design functional chemical probes. While this approach has …
attractive strategy to rationally design functional chemical probes. While this approach has …