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 …
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 …
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
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 …
Emerging new concepts of degrader technologies
Traditional drug discovery focuses on identifying direct inhibitors of target proteins. This
typically relies on a measurable biochemical readout and accessible binding sites whose …
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 …
lead medicines. Many RNAs fold into structures that can be selectively targeted with small …
PROteolysis TArgeting Chimeras (PROTACs) as emerging anticancer therapeutics
Abstract Using PROteolysis TArgeting Chimeras (PROTACs) to degrade proteins that are
important for tumorigenesis has emerged as a potential therapeutic strategy for cancer …
important for tumorigenesis has emerged as a potential therapeutic strategy for cancer …
Proteolysis targeting chimeras (PROTACs) are emerging therapeutics for hematologic malignancies
Proteolysis targeting chimeras (PROTACs) are heterobifunctional small molecules that
utilize the ubiquitin proteasome system (UPS) to degrade proteins of interest (POI) …
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
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 …
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 …
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 …
number of druggable protein families. A new paradigm is emerging, however, in which small …