G protein-coupled receptors: structure-and function-based drug discovery

D Yang, Q Zhou, V Labroska, S Qin… - Signal transduction and …, 2021 - nature.com
As one of the most successful therapeutic target families, G protein-coupled receptors
(GPCRs) have experienced a transformation from random ligand screening to knowledge …

DNA-encoded chemical libraries

AL Satz, A Brunschweiger, ME Flanagan… - Nature Reviews …, 2022 - nature.com
DNA-encoded chemical library (DECL) technology is used by the pharmaceutical industry to
discover small molecules capable of modulating biologically relevant targets. DECL …

Ultra-large library docking for discovering new chemotypes

J Lyu, S Wang, TE Balius, I Singh, A Levit, YS Moroz… - Nature, 2019 - nature.com
Despite intense interest in expanding chemical space, libraries containing hundreds-of-
millions to billions of diverse molecules have remained inaccessible. Here we investigate …

Trends in GPCR drug discovery: new agents, targets and indications

AS Hauser, MM Attwood, M Rask-Andersen… - Nature reviews Drug …, 2017 - nature.com
G protein-coupled receptors (GPCRs) are the most intensively studied drug targets, mostly
due to their substantial involvement in human pathophysiology and their pharmacological …

Strategies for developing DNA-encoded libraries beyond binding assays

Y Huang, Y Li, X Li - Nature Chemistry, 2022 - nature.com
DNA-encoded chemical libraries (DELs) have emerged as a powerful technology in drug
discovery. The wide adoption of DELs in the pharmaceutical industry and the rapid …

Open-air alkylation reactions in photoredox-catalyzed DNA-encoded library synthesis

JP Phelan, SB Lang, J Sim, S Berritt… - Journal of the …, 2019 - ACS Publications
DNA-encoded library (DEL) technology is a powerful tool commonly used by the
pharmaceutical industry for the identification of compounds with affinity to biomolecular …

Small-molecule discovery through DNA-encoded libraries

AA Peterson, DR Liu - Nature Reviews Drug Discovery, 2023 - nature.com
The development of bioactive small molecules as probes or drug candidates requires
discovery platforms that enable access to chemical diversity and can quickly reveal new …

A µ-opioid receptor modulator that works cooperatively with naloxone

ES O'Brien, VA Rangari, A El Daibani, SO Eans… - Nature, 2024 - nature.com
The µ-opioid receptor (µOR) is a well-established target for analgesia, yet conventional
opioid receptor agonists cause serious adverse effects, notably addiction and respiratory …

Selection of DNA-encoded chemical libraries against endogenous membrane proteins on live cells

Y Huang, L Meng, Q Nie, Y Zhou, L Chen, S Yang… - Nature Chemistry, 2021 - nature.com
Membrane proteins on the cell surface perform a myriad of biological functions; however,
ligand discovery for membrane proteins is highly challenging, because a natural cellular …

The symbiotic relationship between drug discovery and organic chemistry

OO Grygorenko, DM Volochnyuk… - … A European Journal, 2020 - Wiley Online Library
All pharmaceutical products contain organic molecules; the source may be a natural product
or a fully synthetic molecule, or a combination of both. Thus, it follows that organic chemistry …