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 …
Noncoding RNA therapeutics—challenges and potential solutions
Therapeutic targeting of noncoding RNAs (ncRNAs), such as microRNAs (miRNAs) and
long noncoding RNAs (lncRNAs), represents an attractive approach for the treatment of …
long noncoding RNAs (lncRNAs), represents an attractive approach for the treatment of …
Proximity-based modalities for biology and medicine
Molecular proximity orchestrates biological function, and blocking existing proximities is an
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
established therapeutic strategy. By contrast, strengthening or creating neoproximity with …
Bridged proteolysis targeting chimera (PROTAC) enables degradation of undruggable targets
Proteolysis Targeting Chimeras (PROTACs) are attractive therapeutic modalities for
degrading disease-causing proteins. While many PROTACs have been developed 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
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 …
against it. Herein, we designed multiple bioactive small molecules that target a functional …
Identification of RNA structures and their roles in RNA functions
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 …
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 …
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 …
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” …
degeneration of nerve cells. Many of the disease-causing proteins of NDs are “undruggable” …
Proximity-inducing modalities: the past, present, and future
Living systems use proximity to regulate biochemical processes. Inspired by this
phenomenon, bifunctional modalities that induce proximity have been developed to redirect …
phenomenon, bifunctional modalities that induce proximity have been developed to redirect …