[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 …
Advancing targeted protein degradation for cancer therapy
The human proteome contains approximately 20,000 proteins, and it is estimated that more
than 600 of them are functionally important for various types of cancers, including nearly 400 …
than 600 of them are functionally important for various types of cancers, including nearly 400 …
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 …
Advances in targeting 'undruggable'transcription factors with small molecules
MJ Henley, AN Koehler - Nature Reviews Drug Discovery, 2021 - nature.com
Transcription factors (TFs) represent key biological players in diseases including cancer,
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
autoimmunity, diabetes and cardiovascular disease. However, outside nuclear receptors …
Cell cycle on the crossroad of tumorigenesis and cancer therapy
Aberrancy in cell cycle progression is one of the fundamental mechanisms underlying
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
tumorigenesis, making regulators of the cell cycle machinery rational anticancer therapeutic …
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 …
Semiconducting polymer nanoparticles with surface‐mimicking protein secondary structure as lysosome‐targeting chimaeras for self‐synergistic cancer …
Immunotherapy has received tremendous attention for tumor treatment, but the efficacy is
greatly hindered by insufficient tumor‐infiltration of immune cells and immunosuppressive …
greatly hindered by insufficient tumor‐infiltration of immune cells and immunosuppressive …
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 …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
[HTML][HTML] Emerging degrader technologies engaging lysosomal pathways
Targeted protein degradation (TPD) provides unprecedented opportunities for drug
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …
discovery. While the proteolysis-targeting chimera (PROTAC) technology has already …