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 …

[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 …

Recent molecular insights into canonical pre-mRNA 3'-end processing

Y Sun, K Hamilton, L Tong - Transcription, 2020 - Taylor & Francis
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 …

[HTML][HTML] Template-assisted covalent modification of DCAF16 underlies activity of BRD4 molecular glue degraders

YD Li, MW Ma, MM Hassan, M Hunkeler, M Teng… - BioRxiv, 2023 - ncbi.nlm.nih.gov
Small molecules that induce protein-protein interactions to exert proximity-driven
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 …

Oligomeric remodeling by molecular glues revealed using native mass spectrometry and mass photometry

X Huang, H Kamadurai, P Siuti, E Ahmed… - Journal of the …, 2023 - ACS Publications
Molecular glues stabilize interactions between E3 ligases and novel substrates to promote
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 …

RNA‐binding motif protein 39 (RBM39): An emerging cancer target

Y Xu, A Nijhuis, HC Keun - British journal of pharmacology, 2022 - Wiley Online Library
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 …

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 …

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 …