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 …
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 …
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 …
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
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 …
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
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 …
been a promising drug target for psychiatric and neurological disorders such as Parkinson's …
Advances in dopamine D1 receptor ligands for neurotherapeutics
The dopamine D1 receptor (D1R) is essential for neurotransmission in various brain
pathways where it modulates key functions including voluntary movement, memory …
pathways where it modulates key functions including voluntary movement, memory …
Designing Functionally Selective Noncatechol Dopamine D1 Receptor Agonists with Potent In Vivo Antiparkinsonian Activity
Dopamine receptors are important G protein-coupled receptors (GPCRs) with therapeutic
opportunities for treating Parkinson's Disease (PD) motor and cognitive deficits. Biased D1 …
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 …
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 …
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 …
cognition, and its dysfunction has been implicated in multiple psychiatric and neurological …