Regulator of G protein signaling proteins: novel multifunctional drug targets

H Zhong, RR Neubig�- Journal of Pharmacology and Experimental�…, 2001 - ASPET
G protein-coupled receptors (GPCRs) play a major role in signal transduction and are
targets of many therapeutic drugs. The regulator of G protein signaling (RGS) proteins form a …

Discovery of 1-[2-(2, 4-dimethylphenylsulfanyl) phenyl] piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder

…, K Frederiksen, KG Jensen, H Zhong…�- Journal of medicinal�…, 2011 - ACS Publications
The synthesis and structure−activity relationship of a novel series of compounds with combined
effects on 5-HT 3A and 5-HT 1A receptors and on the serotonin (5-HT) transporter (SERT…

Pharmacological effects of Lu AA21004: a novel multimodal compound for the treatment of major depressive disorder

…, A Pehrson, LT Brennum, SM Nielsen, H Zhong…�- …�of Pharmacology and�…, 2012 - ASPET
1-[2-(2,4-Dimethylphenyl-sulfanyl)-phenyl]-piperazine (Lu AA21004) is a human (h) serotonin
(5-HT) 3A receptor antagonist (K i = 3.7 nM), h5-HT 7 receptor antagonist (K i = 19 nM), h5-…

[HTML][HTML] A spatial focusing model for G protein signals: regulator of G protein signaling (RGS) protein-mediated kinetic scaffolding

H Zhong, SM Wade, PJ Woolf, JJ Linderman…�- Journal of Biological�…, 2003 - ASBMB
Regulators of G protein signaling (RGS) are GTPase-accelerating proteins (GAPs), which
can inhibit heterotrimeric G protein pathways. In this study, we provide experimental and …

Anxiolytic- and antidepressant-like profiles of the galanin-3 receptor (Gal3) antagonists SNAP 37889 and SNAP 398299

…, MJ Konkel, H Chen, H Zhong…�- Proceedings of the�…, 2005 - National Acad Sciences
The neuropeptide galanin mediates its effects through the receptor subtypes Gal 1 , Gal 2 ,
and Gal 3 and has been implicated in anxiety- and depression-related behaviors. …

Cocaine induction of dopamine transporter trafficking to the plasma membrane

KY Little, LW Elmer, H Zhong, JO Scheys…�- Molecular pharmacology, 2002 - ASPET
Several previous human postmortem experiments have detected an increase in striatal [ 3 H]WIN
35428 binding to the dopamine transporter (DAT) in chronic cocaine users. However, …

Escitalopram, an antidepressant with an allosteric effect at the serotonin transporter—a review of current understanding of its mechanism of action

H Zhong, N Haddjeri, C S�nchez�- Psychopharmacology, 2012 - Springer
Rationale Escitalopram is a widely used antidepressant for the treatment of patients with
major depression. It is the pure S-enantiomer of racemic citalopram. Several clinical trials and …

[HTML][HTML] Endogenous RGS protein action modulates μ-opioid signaling through Gαo: Effects on adenylyl cyclase, extracellular signal-regulated kinases, and�…

MJ Clark, C Harrison, H Zhong, RR Neubig…�- Journal of Biological�…, 2003 - ASBMB
RGS (regulators of Gprotein signaling) proteins are GTPase-activating proteins for the Gα
subunits of heterotrimeric G proteins and act to regulate signaling by rapidly cycling G protein. …

Small-molecule antagonists of melanopsin-mediated phototransduction

…, SP Hong, M Marzabadi, H Zhong…�- Nature chemical�…, 2013 - nature.com
Melanopsin, expressed in a subset of retinal ganglion cells, mediates behavioral adaptation
to ambient light and other non-image-forming photic responses. This has raised the …

[HTML][HTML] Rapid kinetics of Regulator of G-protein Signaling (RGS)-mediated Gαi and Gαo deactivation: Gα specificity of RGS4 and RGS7

KL Lan, H Zhong, M Nanamori, RR Neubig�- Journal of Biological�…, 2000 - ASBMB
Regulator of G-protein signaling (RGS) proteins accelerate GTP hydrolysis by Gα subunits
speeding deactivation. Gα deactivation kinetics mediated by RGS are too fast to be directly …