[HTML][HTML] G Protein-Coupled Receptor Kinase 2 Selectively Enhances β-Arrestin Recruitment to the D2 Dopamine Receptor through Mechanisms That Are …
M Sánchez-Soto, NM Boldizsar, KA Schardien… - Biomolecules, 2023 - mdpi.com
The D2 dopamine receptor (D2R) signals through both G proteins and β-arrestins to regulate
important physiological processes, such as movement, reward circuitry, emotion, and …
important physiological processes, such as movement, reward circuitry, emotion, and …
Identification and Characterization of ML321: A Novel and Highly Selective D2 Dopamine Receptor Antagonist with Efficacy in Animal Models That Predict Atypical …
RB Free, AN Nilson, NM Boldizsar… - ACS Pharmacology & …, 2022 - ACS Publications
We have developed and characterized a novel D2R antagonist with exceptional GPCR
selectivity – ML321. In functional profiling screens of 168 different GPCRs, ML321 showed little …
selectivity – ML321. In functional profiling screens of 168 different GPCRs, ML321 showed little …
G protein‐coupled receptor kinases regulate & [beta]‐arrestin interactions with the D2 dopamine receptor in an isoform‐specific manner and in the absence of direct …
NM Boldizsar, M Sanchez‐Soto, K Schardien… - The FASEB …, 2022 - Wiley Online Library
The D2 dopamine receptor (D2R) regulates numerous CNS functions including movement,
cognition, emotion, and reward circuitry. Agonist binding to the D2R promotes the activation …
cognition, emotion, and reward circuitry. Agonist binding to the D2R promotes the activation …
Phosphorylation barcodes direct biased chemokine signaling at CXCR3
G protein-coupled receptor (GPCR)-biased agonism, selective activation of certain signaling
pathways relative to others, is thought to be directed by differential GPCR phosphorylation "…
pathways relative to others, is thought to be directed by differential GPCR phosphorylation "…
Biased agonists of the chemokine receptor CXCR3 differentially signal through Gαi:β-arrestin complexes
…, A Warman, I Choi, CC Honeycutt, N Boldizsar… - Science …, 2022 - science.org
G protein–coupled receptors (GPCRs) are the largest family of cell surface receptors and
signal through the proximal effectors, G proteins and β-arrestins, to influence nearly every …
signal through the proximal effectors, G proteins and β-arrestins, to influence nearly every …
[HTML][HTML] Location bias contributes to functionally selective responses of biased CXCR3 agonists
DS Eiger, N Boldizsar, CC Honeycutt, J Gardner… - Nature …, 2022 - nature.com
… 10 μL of 2.5 M calcium chloride was added to the plasmid constructs and mixed. 100 μL
of 2× HEPES-buffered saline solution (10 mM D-Glucose, 40 mM HEPES, 10 mM potassium …
of 2× HEPES-buffered saline solution (10 mM D-Glucose, 40 mM HEPES, 10 mM potassium …
Biased agonism at chemokine receptors
DS Eiger, N Boldizsar, CC Honeycutt, J Gardner… - Cellular signalling, 2021 - Elsevier
In the human chemokine system, interactions between the approximately 50 known endogenous
chemokine ligands and 20 known chemokine receptors (CKRs) regulate a wide range …
chemokine ligands and 20 known chemokine receptors (CKRs) regulate a wide range …
GRK2 Enhances ß-arrestin Recruitment to the D2 Dopamine Receptor Through a Mechanism that is Independent From Receptor Phosphorylation or G Protein …
N Boldizsar, M Sanchez-Soto, J Drube, R Haider… - 2023 - ASPET
ID 19401 Poster Board 148 The D2 dopamine receptor (D2R) interacts with and signals
through both G proteins and ss-arrestins to regulate important physiological processes, such as …
through both G proteins and ss-arrestins to regulate important physiological processes, such as …
Pharmacology and Therapeutic Potential of Dopamine D4 Receptor Antagonists for Cocaine Use Disorder
…, R Placide, ML Pham, FM Jakobs, N Boldizsar… - 2022 - chemrxiv.org
The dopamine D4 receptor (D4R), a G protein-coupled receptor, is predominantly expressed
in the prefrontal cortex in which it plays an important role in cognition, attention, and …
in the prefrontal cortex in which it plays an important role in cognition, attention, and …
Characterization and Chemical Optimization of the D2 Dopamine Receptor‐Selective Antagonist, ML321, Identifies Lead Compounds for the Clinical Treatment of …
…, A Dulcey Garcia, RB Free, N Boldizsar… - The FASEB …, 2022 - Wiley Online Library
Schizophrenia is a devastating illness characterized by both positive (hallucinations,
delusions) and negative (flat affect, decreased motivation) symptoms coupled with cognitive …
delusions) and negative (flat affect, decreased motivation) symptoms coupled with cognitive …