Multispecific drugs herald a new era of biopharmaceutical innovation

RJ Deshaies - Nature, 2020 - nature.com
The modern biopharmaceutical industry traces its roots to the dawn of the twentieth century,
coincident with marketing of aspirin—a signature event in the history of modern drug …

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 …

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 …

Emerging new concepts of degrader technologies

Y Ding, Y Fei, B Lu - Trends in Pharmacological Sciences, 2020 - cell.com
Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This
typically relies on a measurable biochemical readout and accessible binding sites whose …

How we think about targeting RNA with small molecules

MG Costales, JL Childs-Disney, HS Haniff… - Journal of medicinal …, 2020 - ACS Publications
RNA offers nearly unlimited potential as a target for small molecule chemical probes and
lead medicines. Many RNAs fold into structures that can be selectively targeted with small …

PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics

S Khan, Y He, X Zhang, Y Yuan, S Pu, Q Kong… - Oncogene, 2020 - nature.com
Abstract Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are
important for tumorigenesis has emerged as a potential therapeutic strategy for cancer …

Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies

Y He, S Khan, Z Huo, D Lv, X Zhang, X Liu… - Journal of Hematology & …, 2020 - Springer
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …

A general fragment-based approach to identify and optimize bioactive ligands targeting RNA

BM Suresh, W Li, P Zhang, KW Wang… - Proceedings of the …, 2020 - National Acad Sciences
RNAs have important functions that are dictated by their structure. Indeed, small molecules
that interact with RNA structures can perturb function, serving as chemical probes and lead …

Targeted degradation of the oncogenic microRNA 17-92 cluster by structure-targeting ligands

X Liu, HS Haniff, JL Childs-Disney… - Journal of the …, 2020 - ACS Publications
Many RNAs are processed into biologically active transcripts, the aberrant expression of
which can contribute to disease phenotypes. For example, the primary microRNA-17-92 (pri …

Design of small molecules targeting RNA structure from sequence

A Ursu, JL Childs-Disney, RJ Andrews… - Chemical Society …, 2020 - pubs.rsc.org
The design and discovery of small molecule medicines has largely been focused on a small
number of druggable protein families. A new paradigm is emerging, however, in which small …