A comprehensive review of BET-targeting PROTACs for cancer therapy
XL Zhou, F Zhao, YT Xu, YY Guan, T Yu… - Bioorganic & Medicinal …, 2022 - Elsevier
Targeted protein degradation using proteolysis-targeting chimeras (PROTACs) has
emerged as an effective strategy for drug discovery, given their unique advantages over …
emerged as an effective strategy for drug discovery, given their unique advantages over …
[HTML][HTML] Targeted protein degradation: clinical advances in the field of oncology
AKAA Salama, MV Trkulja, E Casanova… - International Journal of …, 2022 - mdpi.com
The field of targeted protein degradation (TPD) is a rapidly developing therapeutic modality
with the promise to tame disease-relevant proteins in ways that are difficult or impossible to …
with the promise to tame disease-relevant proteins in ways that are difficult or impossible to …
Recent molecular insights into canonical pre-mRNA 3'-end processing
The majority of eukaryotic messenger RNA precursors (pre-mRNAs) undergo cleavage and
polyadenylation at their 3′ end. This canonical 3′-end processing depends on sequence …
polyadenylation at their 3′ end. This canonical 3′-end processing depends on sequence …
[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders
Small molecules that induce protein-protein interactions to exert proximity-driven
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
pharmacology such as targeted protein degradation are a powerful class of therapeutics 1 …
Clinical translation of targeted protein degraders
NR Kong, LH Jones - Clinical Pharmacology & Therapeutics, 2023 - Wiley Online Library
Targeted protein degradation (TPD) has emerged as a potentially transformational
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
therapeutic modality with considerable promise. Molecular glue degraders remodel the …
Oligomeric remodeling by molecular glues revealed using native mass spectrometry and mass photometry
Molecular glues stabilize interactions between E3 ligases and novel substrates to promote
substrate degradation, thereby facilitating the inhibition of traditionally “undruggable” protein …
substrate degradation, thereby facilitating the inhibition of traditionally “undruggable” protein …
Biophysical and computational approaches to study ternary complexes: a 'cooperative relationship'to rationalize targeted protein degradation
JA Ward, C Perez‐Lopez, C Mayor‐Ruiz - ChemBioChem, 2023 - Wiley Online Library
Degraders have illustrated that compound‐induced proximity to E3 ubiquitin ligases can
prompt the ubiquitination and degradation of disease‐relevant proteins. Hence, this …
prompt the ubiquitination and degradation of disease‐relevant proteins. Hence, this …
RNA‐binding motif protein 39 (RBM39): An emerging cancer target
RNA‐binding motif protein 39 (RBM39) is an RNA‐binding protein involved in transcriptional
co‐regulation and alternative RNA splicing. Recent studies have revealed that RBM39 is the …
co‐regulation and alternative RNA splicing. Recent studies have revealed that RBM39 is the …
Small-molecule approaches to targeted protein degradation
TB Faust, KA Donovan, H Yue… - Annual Review of …, 2021 - annualreviews.org
Many essential biological processes are regulated through proximity, from membrane
receptor signaling to transcriptional activity. The ubiquitin-proteasome system controls …
receptor signaling to transcriptional activity. The ubiquitin-proteasome system controls …
Targeting the spliceosome machinery: A new therapeutic axis in cancer?
B Eymin - Biochemical Pharmacology, 2021 - Elsevier
Pre-mRNA splicing is the removal of introns and ligation of exons to form mature mRNAs,
and it provides a critical mechanism by which eukaryotic cells can regulate their gene …
and it provides a critical mechanism by which eukaryotic cells can regulate their gene …