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 …
Chasing molecular glue degraders: screening approaches
A Domostegui, L Nieto-Barrado… - Chemical Society …, 2022 - pubs.rsc.org
Protein–protein interactions (PPIs) govern all biological processes. Some small molecules
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
modulate PPIs through induced protein proximity. In particular, molecular glue degraders …
An open-source drug discovery platform enables ultra-large virtual screens
On average, an approved drug currently costs US $2–3 billion and takes more than 10 years
to develop. In part, this is due to expensive and time-consuming wet-laboratory experiments …
to develop. In part, this is due to expensive and time-consuming wet-laboratory experiments …
Application of fragment-based drug discovery to versatile targets
Q Li - Frontiers in molecular biosciences, 2020 - frontiersin.org
Fragment-based drug discovery (FBDD) is a powerful method to develop potent small-
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …
molecule compounds starting from fragments binding weakly to targets. As FBDD exhibits …
Molecular glue discovery: current and future approaches
JA Dewey, C Delalande, SA Azizi, V Lu… - Journal of medicinal …, 2023 - ACS Publications
The intracellular interactions of biomolecules can be maneuvered to redirect signaling,
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …
reprogram the cell cycle, or decrease infectivity using only a few dozen atoms. Such …
Structure‐based design of a macrocyclic PROTAC
Constraining a molecule in its bioactive conformation via macrocyclization represents an
attractive strategy to rationally design functional chemical probes. While this approach has …
attractive strategy to rationally design functional chemical probes. While this approach has …
Restriction of HIV-1 and other retroviruses by TRIM5
BK Ganser-Pornillos, O Pornillos - Nature Reviews Microbiology, 2019 - nature.com
Mammalian cells express a variety of innate immune proteins—known as restriction factors—
which defend against invading retroviruses such as HIV-1. Two members of the tripartite …
which defend against invading retroviruses such as HIV-1. Two members of the tripartite …
Overview of recent strategic advances in medicinal chemistry
G Wu, T Zhao, D Kang, J Zhang, Y Song… - Journal of medicinal …, 2019 - ACS Publications
Introducing novel strategies, concepts, and technologies that speed up drug discovery and
the drug development cycle is of great importance both in the highly competitive …
the drug development cycle is of great importance both in the highly competitive …
Prospective discovery of small molecule enhancers of an E3 ligase-substrate interaction
KR Simonetta, J Taygerly, K Boyle, SE Basham… - Nature …, 2019 - nature.com
Protein–protein interactions (PPIs) governing the recognition of substrates by E3 ubiquitin
ligases are critical to cellular function. There is significant therapeutic potential in the …
ligases are critical to cellular function. There is significant therapeutic potential in the …
Quantifying protein–protein interactions by molecular counting with mass photometry
F Soltermann, EDB Foley, V Pagnoni… - Angewandte Chemie …, 2020 - Wiley Online Library
Interactions between biomolecules control the processes of life in health and their
malfunction in disease, making their characterization and quantification essential …
malfunction in disease, making their characterization and quantification essential …