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 …
Current advances of small molecule E3 ligands for proteolysis-targeting chimeras design
D Mi, Y Li, H Gu, Y Li, Y Chen - European Journal of Medicinal Chemistry, 2023 - Elsevier
Proteolysis-targeting chimeras (PROTACs) as an emerging drug discovery modality has
been extensively concerned in recent years. Over 20 years development, accumulated …
been extensively concerned in recent years. Over 20 years development, accumulated …
Discovery of potent and selective WDR5 proteolysis targeting chimeras as potential therapeutics for pancreatic cancer
As a core chromatin-regulatory scaffolding protein, WDR5 mediates numerous protein–
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
protein interactions (PPIs) with other partner oncoproteins. However, small-molecule …
Luciferase-and HaloTag-based reporter assays to measure small-molecule-induced degradation pathway in living cells
The rational development of small-molecule degraders (eg, proteolysis targeting chimeras)
remains a challenge as the rate-limiting steps that determine degrader efficiency are largely …
remains a challenge as the rate-limiting steps that determine degrader efficiency are largely …
Recent advances in developing degraders & inhibitors of lysine methyltransferases
Over the last several decades, there has been continued interest in developing novel
therapeutic approaches targeting protein lysine methyltransferases (PKMTs). Along with …
therapeutic approaches targeting protein lysine methyltransferases (PKMTs). Along with …
Discovery of novel BTK PROTACs with improved metabolic stability via linker rigidification strategy
S Chen, Z Chen, L Lu, Y Zhao, R Zhou, Q Xie… - European Journal of …, 2023 - Elsevier
Abstract Bruton's Tyrosine Kinase (BTK) functions as a key regulator of B-cell receptor (BCR)
signaling pathway, which is frequently hyperactivated in a variety of lymphoma cancers …
signaling pathway, which is frequently hyperactivated in a variety of lymphoma cancers …
Chemically induced degradation of epigenetic targets
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional small molecules that
induce the ternary complex formation between a protein-of-interest (POI) and an E3 ligase …
induce the ternary complex formation between a protein-of-interest (POI) and an E3 ligase …
PROTAC-Based Protein Degradation as a Promising Strategy for Targeted Therapy in Sarcomas
C Mancarella, A Morrione, K Scotlandi - International Journal of …, 2023 - mdpi.com
Sarcomas are heterogeneous bone and soft tissue cancers representing the second most
common tumor type in children and adolescents. Histology and genetic profiling discovered …
common tumor type in children and adolescents. Histology and genetic profiling discovered …
Chemical inhibitors targeting histone methylation readers
X Huang, Y Chen, Q Xiao, X Shang, Y Liu - Pharmacology & Therapeutics, 2024 - Elsevier
Histone methylation reader domains are protein modules that recognize specific histone
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
methylation marks, such as methylated or unmethylated lysine or arginine residues on …
Recent Progress in Modulation of WD40-Repeat Domain 5 Protein (WDR5): Inhibitors and Degraders
Simple Summary WD40-repeat (WDR) domain proteins play a crucial role in mediating
protein–protein interactions that sustain oncogenesis in human cancers. WDR5 has two …
protein–protein interactions that sustain oncogenesis in human cancers. WDR5 has two …