Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders

A Newman-Tancredi, RY Depoortère… - Pharmacology & …, 2022 - Elsevier
Biased agonism (or “functional selectivity”) at G-protein-coupled receptors has attracted
rapidly increasing interest as a means to improve discovery of more efficacious and safer …

The signaling and pharmacology of the dopamine D1 receptor

J Jones-Tabah, H Mohammad, EG Paulus… - Frontiers in Cellular …, 2022 - frontiersin.org
The dopamine D1 receptor (D1R) is a Gαs/olf-coupled GPCR that is expressed in the
midbrain and forebrain, regulating motor behavior, reward, motivational states, and cognitive …

Ligand recognition and biased agonism of the D1 dopamine receptor

X Teng, S Chen, Y Nie, P Xiao, X Yu, Z Shao… - Nature …, 2022 - nature.com
Dopamine receptors are widely distributed in the central nervous system and are important
therapeutic targets for treatment of various psychiatric and neurological diseases. Here, we …

Crystal structure of dopamine D1 receptor in complex with G protein and a non-catechol agonist

B Sun, D Feng, MLH Chu, I Fish, S Lovera… - Nature …, 2021 - nature.com
Abstract Dopamine D1 receptor (D1R) is an important drug target implicated in many
psychiatric and neurological disorders. Selective agonism of D1R are sought to be the …

Computational insights into ligand–induced G protein and β-arrestin signaling of the dopamine D1 receptor

H Li, NM Urs, N Horenstein - Journal of Computer-Aided Molecular …, 2023 - Springer
The dopamine D1 receptor (D1R), is a class AG protein coupled-receptor (GPCR) which has
been a promising drug target for psychiatric and neurological disorders such as Parkinson's …

Advances in dopamine D1 receptor ligands for neurotherapeutics

DE Felsing, MK Jain, JA Allen - Current topics in medicinal …, 2019 - ingentaconnect.com
The dopamine D1 receptor (D1R) is essential for neurotransmission in various brain
pathways where it modulates key functions including voluntary movement, memory …

Designing Functionally Selective Noncatechol Dopamine D1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity

ML Martini, C Ray, X Yu, J Liu… - ACS chemical …, 2019 - ACS Publications
Dopamine receptors are important G protein-coupled receptors (GPCRs) with therapeutic
opportunities for treating Parkinson's Disease (PD) motor and cognitive deficits. Biased D1 …

Targeting β-arrestins in the treatment of psychiatric and neurological disorders

SS Harris, NM Urs - CNS drugs, 2021 - Springer
Therapies for psychiatric and neurological disorders have been in the development and
refinement process for the past 5 decades. Yet, most of these therapies lack optimal …

SpaceGrow: efficient shape-based virtual screening of billion-sized combinatorial fragment spaces

SMN Hönig, F Flachsenberg, C Ehrt… - Journal of Computer …, 2024 - Springer
The growing size of make-on-demand chemical libraries is posing new challenges to
cheminformatics. These ultra-large chemical libraries became too large for exhaustive …

Structure–Functional Selectivity Relationship Studies on A-86929 Analogs and Small Aryl Fragments toward the Discovery of Biased Dopamine D1 Receptor Agonists

H Li, R Mirabel, J Zimmerman, I Ghiviriga… - ACS Chemical …, 2022 - ACS Publications
Dopamine regulates normal functions such as movement, reinforcement learning, and
cognition, and its dysfunction has been implicated in multiple psychiatric and neurological …