Innovative, combinatorial and high-throughput approaches to degrader synthesis
R Stevens, JDF Thompson, JCL Fournier… - Chemical Society …, 2024 - pubs.rsc.org
Targeted protein degraders such as PROTACs and molecular glues are a rapidly emerging
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
therapeutic modality within industry and academia. Degraders possess unique mechanisms …
The expanding repertoire of covalent warheads for drug discovery
The reactive functionalities of drugs that engage in covalent interactions with the
enzyme/receptor residue in either a reversible or an irreversible manner are …
enzyme/receptor residue in either a reversible or an irreversible manner are …
Discovery of molecular glue degraders via isogenic morphological profiling
A Ng, F Offensperger, JA Cisneros… - ACS Chemical …, 2023 - ACS Publications
Molecular glue degraders (MGDs) are small molecules that degrade proteins of interest via
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
the ubiquitin–proteasome system. While MGDs were historically discovered serendipitously …
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 …
Confounding factors in targeted degradation of short-lived proteins
Targeted protein degradation has recently emerged as a novel option in drug discovery.
Natural protein half-life is expected to affect the efficacy of degrading agents, but to what …
Natural protein half-life is expected to affect the efficacy of degrading agents, but to what …
Integrated direct-to-biology platform for the nanoscale synthesis and biological evaluation of PROTACs
R Stevens, E Bendito-Moll, DJ Battersby… - Journal of Medicinal …, 2023 - ACS Publications
Proteolysis targeting chimeras (PROTACs) are heterobifunctional molecules that co-opt the
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …
cell's natural proteasomal degradation mechanisms to degrade undesired proteins. A …
Click chemistry and targeted degradation: a winning combination for medicinal chemists?
A Pasieka, E Diamanti, E Uliassi… - …, 2023 - Wiley Online Library
Click chemistry is universally recognized as a powerful strategy for the fast and precise
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new …
[HTML][HTML] Harnessing UBR5 for targeted protein degradation of key transcriptional regulators
AM Taherbhoy, DL Daniels - Trends in Pharmacological Sciences, 2023 - cell.com
Targeted protein degradation (TPD) has opened the door for drugging transcriptional
regulators, yet the number of proteins targeted and E3 ligases utilized remain limited. Here …
regulators, yet the number of proteins targeted and E3 ligases utilized remain limited. Here …
[HTML][HTML] Exploring the chemical space of orally bioavailable PROTACs
A principal challenge in the discovery of proteolysis targeting chimeras (PROTACs) as oral
medications is their bioavailability. To facilitate drug design, it is therefore essential to …
medications is their bioavailability. To facilitate drug design, it is therefore essential to …
RIPTACs: a groundbreaking approach to drug discovery
Regulated induced proximity targeting chimeras (RIPTACs), a new class of
heterobifunctional molecules, show promise in specifically targeting and eliminating cancer …
heterobifunctional molecules, show promise in specifically targeting and eliminating cancer …