[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 …
dysfunction in disease. Approaches to therapeutically target RNA structures with small …
[HTML][HTML] Programming inactive RNA-binding small molecules into bioactive degraders
Target occupancy is often insufficient to elicit biological activity, particularly for RNA,
compounded by the longstanding challenges surrounding the molecular recognition of 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 …
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 …
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
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 …
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 …
(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
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 …
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 …
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 …
earliest genomic aberrations occurring during cancer development and are closely related …