Search Results - "Javitch, Jonathan A."

Synthetic and Receptor Signaling Explorations of the Mitragyna Alkaloids: Mitragynine as an Atypical Molecular Framework for Opioid Receptor Modulators by Kruegel, Andrew C, Gassaway, Madalee M, Kapoor, Abhijeet, Váradi, András, Majumdar, Susruta, Filizola, Marta, Javitch, Jonathan A, Sames, Dalibor

“…Mu-opioid receptor agonists represent mainstays of pain management. However, the therapeutic use of these agents is associated with serious side effects,…”
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Extrapyramidal side effects of antipsychotics are linked to their association kinetics at dopamine D2 receptors by Sykes, David A., Moore, Holly, Stott, Lisa, Holliday, Nicholas, Javitch, Jonathan A., Lane, J. Robert, Charlton, Steven J.

“…Atypical antipsychotic drugs (APDs) have been hypothesized to show reduced extrapyramidal side effects (EPS) due to their rapid dissociation from the dopamine…”
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Single-molecule analysis of ligand efficacy in β2AR–G-protein activation by Gregorio, G. Glenn, Masureel, Matthieu, Hilger, Daniel, Terry, Daniel S., Juette, Manuel, Zhao, Hong, Zhou, Zhou, Perez-Aguilar, Jose Manuel, Hauge, Maria, Mathiasen, Signe, Javitch, Jonathan A., Weinstein, Harel, Kobilka, Brian K., Blanchard, Scott C.

“…G-protein-coupled receptor (GPCR)-mediated signal transduction is central to human physiology and disease intervention, yet the molecular mechanisms…”
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Roles of the Akt/GSK-3 and Wnt Signaling Pathways in Schizophrenia and Antipsychotic Drug Action by Freyberg, Zachary, Ferrando, Stephen J, Javitch, Jonathan A

“…AbstractDopamine D2 receptor antagonism is a unifying property of all antipsychotic drugs in clinical use. Remarkably, the effector molecules through which…”
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The role of kinetic context in apparent biased agonism at GPCRs by Klein Herenbrink, Carmen, Sykes, David A., Donthamsetti, Prashant, Canals, Meritxell, Coudrat, Thomas, Shonberg, Jeremy, Scammells, Peter J., Capuano, Ben, Sexton, Patrick M., Charlton, Steven J., Javitch, Jonathan A., Christopoulos, Arthur, Lane, J. Robert

“…Biased agonism describes the ability of ligands to stabilize different conformations of a GPCR linked to distinct functional outcomes and offers the prospect…”
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CrossTalk opposing view: Weighing the evidence for class A GPCR dimers, the jury is still out by Lambert, Nevin A., Javitch, Jonathan A.

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Potentiating SLC transporter activity: Emerging drug discovery opportunities by Rives, Marie-Laure, Javitch, Jonathan A., Wickenden, Alan D.

“…[Display omitted] Maintaining the integrity of cellular membranes is critical to protecting metabolic activities and genetic information from the environment…”
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The Mechanism of a Neurotransmitter:Sodium Symporter—Inward Release of Na + and Substrate Is Triggered by Substrate in a Second Binding Site by Shi, Lei, Quick, Matthias, Zhao, Yongfang, Weinstein, Harel, Javitch, Jonathan A.

“…Eukaryotic neurotransmitter:sodium symporters (NSSs), targets for antidepressants and psychostimulants, terminate neurotransmission by sodium-driven reuptake…”
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Accumbens dopamine D2 receptors increase motivation by decreasing inhibitory transmission to the ventral pallidum by Gallo, Eduardo F., Meszaros, Jozsef, Sherman, Jeremy D., Chohan, Muhammad O., Teboul, Eric, Choi, Claire S., Moore, Holly, Javitch, Jonathan A., Kellendonk, Christoph

“…Dopamine D2 receptors (D2Rs) in the nucleus accumbens (NAc) regulate motivated behavior, but the underlying neurobiological mechanisms remain unresolved. Here,…”
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What can crystal structures of aminergic receptors tell us about designing subtype-selective ligands? by Michino, Mayako, Beuming, Thijs, Donthamsetti, Prashant, Newman, Amy Hauck, Javitch, Jonathan A, Shi, Lei

“…G protein-coupled receptors (GPCRs) are integral membrane proteins that represent an important class of drug targets. In particular, aminergic GPCRs interact…”
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Allosteric communication between protomers of dopamine class A GPCR dimers modulates activation by Javitch, Jonathan A, Han, Yang, Moreira, Irina S, Urizar, Eneko, Weinstein, Harel

“…A major obstacle to understanding the functional importance of dimerization between class A G protein–coupled receptors (GPCRs) has been the methodological…”
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Elucidating the molecular logic of a metabotropic glutamate receptor heterodimer by Lin, Xin, Provasi, Davide, Niswender, Colleen M., Asher, Wesley B., Javitch, Jonathan A.

“…Metabotropic glutamate (mGlu) receptor protomers can heterodimerize, leading to different pharmacology compared to their homodimeric counterparts. Here, we use…”
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Genetically Targeted Optical Control of an Endogenous G Protein-Coupled Receptor by Donthamsetti, Prashant C, Broichhagen, Johannes, Vyklicky, Vojtech, Stanley, Cherise, Fu, Zhu, Visel, Meike, Levitz, Joshua L, Javitch, Jonathan A, Trauner, Dirk, Isacoff, Ehud Y

“…G protein-coupled receptors (GPCRs) are membrane proteins that play important roles in biology. However, our understanding of their function in complex living…”
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Tianeptine promotes lasting antiallodynic effects in a mouse model of neuropathic pain by Serafini, Randal A, Estill, Molly, Pekarskaya, Elizabeth A, Sakloth, Farhana, Shen, Li, Javitch, Jonathan A, Zachariou, Venetia

“…Tricyclic antidepressants (TCAs), such as desipramine (DMI), are effective at managing neuropathic pain symptoms but often take several weeks to become…”
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Single-molecule dynamics of gating in a neurotransmitter transporter homologue by Blanchard, Scott C, Javitch, Jonathan A, Zhao, Yongfang, Terry, Daniel, Shi, Lei, Weinstein, Harel

“…Neurotransmitter:Na + symporters (NSS) remove neurotransmitters from the synapse in a reuptake process that is driven by the Na + gradient. Drugs that…”
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Optical Control of Dopamine Receptors Using a Photoswitchable Tethered Inverse Agonist by Donthamsetti, Prashant C, Winter, Nils, Schönberger, Matthias, Levitz, Joshua, Stanley, Cherise, Javitch, Jonathan A, Isacoff, Ehud Y, Trauner, Dirk

“…Family A G protein-coupled receptors (GPCRs) control diverse biological processes and are of great clinical relevance. Their archetype rhodopsin becomes…”
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Dopamine D2 receptors form higher order oligomers at physiological expression levels by Guo, Wen, Urizar, Eneko, Kralikova, Michaela, Mobarec, Juan Carlos, Shi, Lei, Filizola, Marta, Javitch, Jonathan A

“…G‐protein‐coupled receptors are generally thought to be organized as dimers; whether they form higher order oligomers is a topic of much controversy. We…”
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Monitoring the function of membrane transport proteins in detergent-solubilized form by Quick, Matthias, Javitch, Jonathan A

“…Transport proteins constitute [almost equal to]10% of most proteomes and play vital roles in the translocation of solutes across membranes of all organisms…”
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Conformational dynamics of ligand-dependent alternating access in LeuT by Kazmier, Kelli, Sharma, Shruti, Quick, Matthias, Islam, Shahidul M, Roux, Benoît, Weinstein, Harel, Javitch, Jonathan A, Mchaourab, Hassane S

“…LeuT is a Na + -coupled amino acid transporter that is similar in sequence and function to eukaryotic neurotransmitter/sodium symporters, which are active in…”
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Cortical overgrowth in a preclinical forebrain organoid model of CNTNAP2-associated autism spectrum disorder by de Jong, Job O., Llapashtica, Ceyda, Genestine, Matthieu, Strauss, Kevin, Provenzano, Frank, Sun, Yan, Zhu, Huixiang, Cortese, Giuseppe P., Brundu, Francesco, Brigatti, Karlla W., Corneo, Barbara, Migliori, Bianca, Tomer, Raju, Kushner, Steven A., Kellendonk, Christoph, Javitch, Jonathan A., Xu, Bin, Markx, Sander

“…We utilized forebrain organoids generated from induced pluripotent stem cells of patients with a syndromic form of Autism Spectrum Disorder (ASD) with a…”
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