Synthesis and characterization of a bidirectional photoswitchable antagonist toolbox for real-time GPCR photopharmacology

NJ Hauwert, TAM Mocking… - Journal of the …, 2018 - ACS Publications
Noninvasive methods to modulate G protein-coupled receptors (GPCRs) with temporal and
spatial precision are in great demand. Photopharmacology uses photons to control in situ …

A Photoswitchable Agonist for the Histamine H3 Receptor, a Prototypic Family AG‐Protein‐Coupled Receptor

NJ Hauwert, TAM Mocking… - Angewandte …, 2019 - Wiley Online Library
Spatiotemporal control over biochemical signaling processes involving G protein‐coupled
receptors (GPCRs) is highly desired for dissecting their complex intracellular signaling. We …

Selective photoswitchable allosteric agonist of a G protein-coupled receptor

P Donthamsetti, DB Konrad, B Hetzler… - Journal of the …, 2021 - ACS Publications
G protein-coupled receptors (GPCRs) are the most common targets of drug discovery.
However, the similarity between related GPCRs combined with the complex spatiotemporal …

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 …

Fluorination of photoswitchable muscarinic agonists tunes receptor pharmacology and photochromic properties

L Agnetta, M Bermudez, F Riefolo… - Journal of Medicinal …, 2019 - ACS Publications
Red-shifted azobenzene scaffolds have emerged as useful molecular photoswitches to
expand potential applications of photopharmacological tool compounds. As one of them …

[PDF][PDF] A fine-tuned azobenzene for enhanced photopharmacology in vivo

VA Gutzeit, A Acosta-Ruiz, H Munguba, S Häfner… - Cell chemical …, 2021 - cell.com
Despite the power of photopharmacology for interrogating signaling proteins, many
photopharmacological systems are limited by their efficiency, speed, or spectral properties …

Photoswitchable Affinity Reagents: Computational Design and Efficient Red‐Light Switching

N Yasuike, KM Blacklock, H Lu, ASI Jaikaran… - …, 2019 - Wiley Online Library
Photo‐controlled affinity reagents seek to provide modular spatiotemporal control of
bioactivity by conferring photo‐switchability of function on an affinity reagent scaffold. Herein …

Rational remodeling of atypical scaffolds for the design of photoswitchable cannabinoid receptor tools

T Hu, G Zheng, D Xue, S Zhao, F Li… - Journal of Medicinal …, 2021 - ACS Publications
Azobenzene-embedded photoswitchable ligands are the widely used chemical tools in
photopharmacological studies. Current approaches to azobenzene introduction rely mainly …

[PDF][PDF] Branched photoswitchable tethered ligands enable ultra-efficient optical control and detection of G protein-coupled receptors in vivo

A Acosta-Ruiz, VA Gutzeit, MJ Skelly, S Meadows… - Neuron, 2020 - cell.com
The limitations of classical drugs have spurred the development of covalently tethered
photoswitchable ligands to control neuromodulatory receptors. However, a major …

Mechanistic insights into light-driven allosteric control of GPCR biological activity

M Ricart-Ortega, AE Berizzi, V Pereira… - ACS Pharmacology & …, 2020 - ACS Publications
G protein-coupled receptors (GPCR), including the metabotrobic glutamate 5 receptor
(mGlu5), are important therapeutic targets and the development of allosteric ligands for …