PROTACs: past, present and future

K Li, CM Crews - Chemical Society Reviews, 2022 - pubs.rsc.org
Proteolysis-targeting chimeras (PROTACs) are heterobifunctional molecules consisting of
one ligand that binds to a protein of interest (POI) and another that can recruit an E3 …

[HTML][HTML] Targeting RNA structures with small molecules

JL Childs-Disney, X Yang, QMR Gibaut… - Nature Reviews Drug …, 2022 - nature.com
RNA adopts 3D structures that confer varied functional roles in human biology and
dysfunction in disease. Approaches to therapeutically target RNA structures with small …

[HTML][HTML] Programming inactive RNA-binding small molecules into bioactive degraders

Y Tong, Y Lee, X Liu, JL Childs-Disney, BM Suresh… - Nature, 2023 - nature.com
Target occupancy is often insufficient to elicit biological activity, particularly for RNA,
compounded by the longstanding challenges surrounding the molecular recognition of RNA …

[HTML][HTML] Amplifying gene expression with RNA-targeted therapeutics

O Khorkova, J Stahl, A Joji, CH Volmar… - Nature Reviews Drug …, 2023 - nature.com
Many diseases are caused by insufficient expression of mutated genes and would benefit
from increased expression of the corresponding protein. However, in drug development, it …

DNA-encoded library screening to inform design of a ribonuclease targeting chimera (RiboTAC)

SM Meyer, T Tanaka, PRA Zanon… - Journal of the …, 2022 - ACS Publications
Ribonuclease targeting chimeras (RiboTACs) induce degradation of an RNA target by
facilitating an interaction between an RNA and a ribonuclease (RNase). We describe the …

Proximity-Induced Nucleic Acid Degrader (PINAD) approach to targeted RNA degradation using small molecules

S Mikutis, M Rebelo, E Yankova, M Gu… - ACS Central …, 2023 - ACS Publications
Nature has evolved intricate machinery to target and degrade RNA, and some of these
molecular mechanisms can be adapted for therapeutic use. Small interfering RNAs and …

Nucleic-acid-based targeted degradation in drug discovery

W Wang, S He, G Dong, C Sheng - Journal of Medicinal Chemistry, 2022 - ACS Publications
Targeted protein degradation (TPD), represented by proteolysis-targeting chimera
(PROTAC), has emerged as a novel therapeutic modality in drug discovery. However, the …

Transcriptome-Wide Mapping of Small-Molecule RNA-Binding Sites in Cells Informs an Isoform-Specific Degrader of QSOX1 mRNA

Y Tong, QMR Gibaut, W Rouse… - Journal of the …, 2022 - ACS Publications
The interactions between cellular RNAs in MDA-MB-231 triple negative breast cancer cells
and a panel of small molecules appended with a diazirine cross-linking moiety and an …

Emerging targeted protein degradation tools for innovative drug discovery: From classical PROTACs to the novel and beyond

Y Zhong, F Chi, H Wu, Y Liu, Z Xie, W Huang… - European journal of …, 2022 - Elsevier
Targeted protein degradation technology has evolved a brand-new therapeutic modality
from an innovative drug discovery perspective. Though the classical PROTACs has …

[HTML][HTML] Modulating epigenetic modifications for cancer therapy

LJ Castro-Muñoz, EV Ulloa, C Sahlgren… - Oncology …, 2023 - spandidos-publications.com
Cancer is a global public health concern. Alterations in epigenetic processes are among the
earliest genomic aberrations occurring during cancer development and are closely related …