Stimuli-activatable PROTACs for precise protein degradation and cancer therapy

J Gao, L Yang, S Lei, F Zhou, H Nie, B Peng, T Xu… - Science bulletin, 2023 - Elsevier
The proteolysis targeting chimeras (PROTACs) approach has attracted extensive attention in
the past decade, which represents an emerging therapeutic modality with the potential to …

[HTML][HTML] Application of photopharmacology in agrochemicals

W Fu, Z Li, X Shao - Advanced Agrochem, 2023 - Elsevier
Photopharmacology is a novel technology in drug design that aims at solving poor drug
selectivity. This technology is currently in the proof-of-concept phase and relies on the …

Distinct beta-arrestin coupling and intracellular trafficking of metabotropic glutamate receptor homo-and heterodimers

J Lee, AJ Gonzalez-Hernandez, M Kristt, N Abreu… - Science …, 2023 - science.org
The metabotropic glutamate receptors (mGluRs) are family C, dimeric G protein–coupled
receptors (GPCRs), which play critical roles in synaptic transmission. Despite an increasing …

Control of Gαq signaling dynamics and GPCR cross-talk by GRKs

G Xiang, A Acosta-Ruiz, A Radoux-Mergault… - Science …, 2022 - science.org
Numerous processes contribute to the regulation of G protein–coupled receptors (GPCRs),
but relatively little is known about rapid mechanisms that control signaling on the seconds …

Thermal half-lives of azobenzene derivatives: Virtual screening based on intersystem crossing using a machine learning potential

S Axelrod, E Shakhnovich… - ACS Central …, 2023 - ACS Publications
Molecular photoswitches are the foundation of light-activated drugs. A key photoswitch is
azobenzene, which exhibits trans–cis isomerism in response to light. The thermal half-life of …

Photoswitchable Pseudoirreversible Butyrylcholinesterase Inhibitors Allow Optical Control of Inhibition in Vitro and Enable Restoration of Cognition in an Alzheimer's …

M Scheiner, A Sink, M Hoffmann… - Journal of the …, 2022 - ACS Publications
To develop tools to investigate the biological functions of butyrylcholinesterase (BChE) and
the mechanisms by which BChE affects Alzheimer's disease (AD), we synthesized several …

[HTML][HTML] In vivo photopharmacology with light-activated opioid drugs

SP McClain, X Ma, DA Johnson, CA Johnson… - Neuron, 2023 - cell.com
Traditional methods for site-specific drug delivery in the brain are slow, invasive, and difficult
to interface with recordings of neural activity. Here, we demonstrate the feasibility and …

Photoswitchable Serotonins for Optical Control of the 5‐HT2A Receptor**

J Morstein, G Romano, BE Hetzler… - Angewandte Chemie …, 2022 - Wiley Online Library
Serotonin receptors play central roles in neuromodulation and are critical drug targets for
psychiatric disorders. Optical control of serotonin receptor subtypes has the potential to …

Optical Approaches for Investigating Neuromodulation and G Protein–Coupled Receptor Signaling

DJ Marcus, MR Bruchas - Pharmacological Reviews, 2023 - ASPET
Despite the fact that roughly 40% of all US Food and Drug Administration (FDA)-approved
pharmacological therapeutics target G protein–coupled receptors (GPCRs), there remains a …

[HTML][HTML] Optical control of Class AG protein-coupled receptors with photoswitchable ligands

M Wijtmans, I Josimovic, HF Vischer, R Leurs - Current Opinion in …, 2022 - Elsevier
The field of photopharmacology of Class A GPCR ligands has recently attracted attention. In
this review we analyze 31 papers on currently available photoswitchable ligands for Class A …