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: a comprehensive review with succesful stories and future challenges

A Gironda-Martínez, EJ Donckele… - ACS Pharmacology & …, 2021 - ACS Publications
DNA-encoded chemical libraries (DELs) represent a versatile and powerful technology
platform for the discovery of small-molecule ligands to protein targets of biological and …

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 …

G-protein–coupled receptors in heart disease

J Wang, C Gareri, HA Rockman - Circulation research, 2018 - Am Heart Assoc
GPCRs (G-protein [guanine nucleotide-binding protein]–coupled receptors) play a central
physiological role in the regulation of cardiac function in both health and disease and thus …

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 …

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 …

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 …

Widespread receptor-driven modulation in peripheral olfactory coding

L Xu, W Li, V Voleti, DJ Zou, EMC Hillman, S Firestein - Science, 2020 - science.org
INTRODUCTION The mammalian nose is arguably the best chemical sensor on the planet,
able to detect and discriminate among a large and diverse repertoire of mostly small …

α1-Adrenergic Receptors in Neurotransmission, Synaptic Plasticity, and Cognition

DM Perez - Frontiers in pharmacology, 2020 - frontiersin.org
α1-adrenergic receptors are G-Protein Coupled Receptors that are involved in
neurotransmission and regulate the sympathetic nervous system through binding and …

A data science roadmap for open science organizations engaged in early-stage drug discovery

K Edfeldt, AM Edwards, O Engkvist, J Günther… - Nature …, 2024 - nature.com
Abstract The Structural Genomics Consortium is an international open science research
organization with a focus on accelerating early-stage drug discovery, namely hit discovery …