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 …

Noncoding RNA therapeutics—challenges and potential solutions

M Winkle, SM El-Daly, M Fabbri, GA Calin - Nature reviews Drug …, 2021 - nature.com
Therapeutic targeting of noncoding RNAs (ncRNAs), such as microRNAs (miRNAs) and
long noncoding RNAs (lncRNAs), represents an attractive approach for the treatment of …

Proximity-based modalities for biology and medicine

X Liu, A Ciulli - ACS Central Science, 2023 - ACS Publications
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …

Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets

Y Xiong, Y Zhong, H Yim, X Yang, KS Park… - Journal of the …, 2022 - ACS Publications
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed for …

Targeting the SARS-CoV-2 RNA genome with small molecule binders and ribonuclease targeting chimera (RIBOTAC) degraders

HS Haniff, Y Tong, X Liu, JL Chen, BM Suresh… - ACS Central …, 2020 - ACS Publications
COVID-19 is a global pandemic, thus requiring multiple strategies to develop modalities
against it. Herein, we designed multiple bioactive small molecules that target a functional …

Identification of RNA structures and their roles in RNA functions

X Cao, Y Zhang, Y Ding, Y Wan - Nature Reviews Molecular Cell …, 2024 - nature.com
The development of high-throughput RNA structure profiling methods in the past decade has
greatly facilitated our ability to map and characterize different aspects of RNA structures …

SPR-measured dissociation kinetics of PROTAC ternary complexes influence target degradation rate

MJ Roy, S Winkler, SJ Hughes, C Whitworth… - ACS chemical …, 2019 - ACS Publications
Bifunctional degrader molecules, known as proteolysis-targeting chimeras (PROTACs),
function by recruiting a target to an E3 ligase, forming a target/PROTAC/ligase ternary …

Small molecule recognition of disease-relevant RNA structures

SM Meyer, CC Williams, Y Akahori, T Tanaka… - Chemical Society …, 2020 - pubs.rsc.org
Targeting RNAs with small molecules represents a new frontier in drug discovery and
development. The rich structural diversity of folded RNAs offers a nearly unlimited reservoir …

Progress and challenges in targeted protein degradation for neurodegenerative disease therapy

Y Fang, J Wang, M Zhao, Q Zheng, C Ren… - Journal of Medicinal …, 2022 - ACS Publications
Neurodegenerative diseases (NDs) are currently incurable diseases that cause progressive
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …

Proximity-inducing modalities: the past, present, and future

S Singh, W Tian, ZC Severance… - Chemical Society …, 2023 - pubs.rsc.org
Living systems use proximity to regulate biochemical processes. Inspired by this
phenomenon, bifunctional modalities that induce proximity have been developed to redirect …