Search Results - "Brust, Tarsis F"

Biased agonists of the kappa opioid receptor suppress pain and itch without causing sedation or dysphoria by Brust, Tarsis F, Morgenweck, Jenny, Kim, Susy A, Rose, Jamie H, Locke, Jason L, Schmid, Cullen L, Zhou, Lei, Stahl, Edward L, Cameron, Michael D, Scarry, Sarah M, Aubé, Jeffrey, Jones, Sara R, Martin, Thomas J, Bohn, Laura M

“…Agonists targeting the kappa opioid receptor (KOR) have been promising therapeutic candidates because of their efficacy for treating intractable itch and…”
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Editorial: Adenylyl cyclase isoforms as potential drug targets by Brust, Tarsis F, Ostrom, Rennolds S, Watts, Val J

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A Selective Adenylyl Cyclase 1 Inhibitor Relieves Pain Without Causing Tolerance by Giacoletti, Gianna, Price, Tatum, Hoelz, Lucas V B, Shremo Msdi, Abdulwhab, Cossin, Samantha, Vazquez-Falto, Katerina, Amorim Fernandes, Tácio V, Santos de Pontes, Vinícius, Wang, Hongbing, Boechat, Nubia, Nornoo, Adwoa, Brust, Tarsis F

“…Among the ten different adenylyl cyclase isoforms, studies with knockout animals indicate that inhibition of AC1 can relieve pain and reduce behaviors linked…”
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A “Genome-to-Lead” Approach for Insecticide Discovery: Pharmacological Characterization and Screening of Aedes aegypti D1-like Dopamine Receptors by Meyer, Jason M., Ejendal, Karin F. K., Avramova, Larisa V., Garland-Kuntz, Elisabeth E., Giraldo-Calderón, Gloria I., Brust, Tarsis F., Watts, Val J., Hill, Catherine A.

“…Background Many neglected tropical infectious diseases affecting humans are transmitted by arthropods such as mosquitoes and ticks. New mode-of-action…”
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Polydopamine-Based Simple and Versatile Surface Modification of Polymeric Nano Drug Carriers by Park, Joonyoung, Brust, Tarsis F, Lee, Hong Jae, Lee, Sang Cheon, Watts, Val J, Yeo, Yoon

“…The surface of a polymeric nanoparticle (NP) is often functionalized with cell-interactive ligands and/or additional polymeric layers to control NP interaction…”
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Physiological roles of mammalian transmembrane adenylyl cyclase isoforms by Ostrom, Katrina F, LaVigne, Justin E, Brust, Tarsis F, Seifert, Roland, Dessauer, Carmen W, Watts, Val J, Ostrom, Rennolds S

“…Adenylyl cyclases (ACs) catalyze the conversion of ATP to the ubiquitous second messenger cAMP. Mammals possess nine isoforms of transmembrane ACs, dubbed…”
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Repurposing of a Nucleoside Scaffold from Adenosine Receptor Agonists to Opioid Receptor Antagonists by Tosh, Dilip K, Ciancetta, Antonella, Mannes, Philip, Warnick, Eugene, Janowsky, Aaron, Eshleman, Amy J, Gizewski, Elizabeth, Brust, Tarsis F, Bohn, Laura M, Auchampach, John A, Gao, Zhan-Guo, Jacobson, Kenneth A

“…While screening off-target effects of rigid (N)-methanocarba-adenosine 5′-methylamides as A3 adenosine receptor (AR) agonists, we discovered μM binding hits at…”
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Adenylyl cyclase 7 and neuropsychiatric disorders: A new target for depression? by Price, Tatum, Brust, Tarsis F.

“…[Display omitted] Adenylyl cyclases (ACs) are enzymes that catalyze the production of cyclic adenosine monophosphate (cAMP) from adenosine triphosphate (ATP)…”
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Biased agonism: An emerging paradigm in GPCR drug discovery by Rankovic, Zoran, Brust, Tarsis F., Bohn, Laura M.

“…[Display omitted] G protein coupled receptors have historically been one of the most druggable classes of cellular proteins. The members of this large receptor…”
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Palladium-Catalyzed Regio- and Stereoselective γ‑Arylation of Tertiary Allylic Amines: Identification of Potent Adenylyl Cyclase Inhibitors by Ye, Zhishi, Brust, Tarsis F, Watts, Val J, Dai, Mingji

“…Substituted allylic amines and their derivatives are key structural motifs of many drug molecules and natural products. A general, mild, and practical…”
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O6C-20-nor-salvinorin A is a stable and potent KOR agonist by Hirasawa, Shun, Cho, Min, Brust, Tarsis F., Roach, Jeremy J., Bohn, Laura M., Shenvi, Ryan A.

“…[Display omitted] Salvinorin A (SalA) is a potent and selective agonist of the kappa-opioid receptor (KOR), but its instability has frustrated medicinal…”
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New functional activity of aripiprazole revealed: Robust antagonism of D2 dopamine receptor-stimulated Gβγ signaling by Brust, Tarsis F., Hayes, Michael P., Roman, David L., Watts, Val J.

“…The dopamine D2 receptor (DRD2) is a G protein-coupled receptor (GPCR) that is generally considered to be a primary target in the treatment of schizophrenia…”
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Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties by Brust, Tarsis F, Alongkronrusmee, Doungkamol, Soto-Velasquez, Monica, Baldwin, Tanya A, Ye, Zhishi, Dai, Mingji, Dessauer, Carmen W, van Rijn, Richard M, Watts, Val J

“…Adenylyl cyclase 1 (AC1) belongs to a group of adenylyl cyclases (ACs) that are stimulated by calcium in a calmodulin-dependent manner. Studies with AC1…”
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Bias analyses of preclinical and clinical D2 dopamine ligands: studies with immediate and complex signaling pathways by Brust, Tarsis F, Hayes, Michael P, Roman, David L, Burris, Kevin D, Watts, Val J

“…G protein-coupled receptors (GPCRs) often activate multiple signaling pathways, and ligands may evoke functional responses through individual pathways. These…”
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Bisamidate Prodrugs of 2-Substituted 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA, adefovir) as Selective Inhibitors of Adenylate Cyclase Toxin from Bordetella pertussis by Česnek, Michal, Jansa, Petr, Šmídková, Markéta, Mertlíková-Kaiserová, Helena, Dračínský, Martin, Brust, Tarsis F., Pávek, Petr, Trejtnar, František, Watts, Val J., Janeba, Zlatko

“…Novel small‐molecule agents to treat Bordetella pertussis infections are highly desirable, as pertussis (whooping cough) remains a serious health threat…”
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Drug-induced sensitization of adenylyl cyclase: assay streamlining and miniaturization for small molecule and siRNA screening applications by Conley, Jason M, Brust, Tarsis F, Xu, Ruqiang, Burris, Kevin D, Watts, Val J

“…Sensitization of adenylyl cyclase (AC) signaling has been implicated in a variety of neuropsychiatric and neurologic disorders including substance abuse and…”
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Discovery of antagonists of tick dopamine receptors via chemical library screening and comparative pharmacological analyses by Ejendal, Karin F.K., Meyer, Jason M., Brust, Tarsis F., Avramova, Larisa V., Hill, Catherine A., Watts, Val J.

“…Ticks transmit a wide variety of disease causing pathogens to humans and animals. Considering the global health impact of tick-borne diseases, there is a…”
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Cover Picture: Bisamidate Prodrugs of 2-Substituted 9-[2-(Phosphonomethoxy)ethyl]adenine (PMEA, adefovir) as Selective Inhibitors of Adenylate Cyclase Toxin from Bordetella pertussis (ChemMedChem 8/2015) by Česnek, Michal, Jansa, Petr, Šmídková, Markéta, Mertlíková-Kaiserová, Helena, Dračínský, Martin, Brust, Tarsis F., Pávek, Petr, Trejtnar, František, Watts, Val J., Janeba, Zlatko

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Gαi/o-coupled receptor-mediated sensitization of adenylyl cyclase: 40 years later by Brust, Tarsis F., Conley, Jason M., Watts, Val J.

“…Heterologous sensitization of adenylyl cyclase (also referred to as superactivation, sensitization, or supersensitization of adenylyl cyclase) is a cellular…”
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A "genome-to-lead" approach for insecticide discovery: pharmacological characterization and screening of Aedes aegypti D(1)-like dopamine receptors by Meyer, Jason M, Ejendal, Karin F K, Avramova, Larisa V, Garland-Kuntz, Elisabeth E, Giraldo-Calderón, Gloria I, Brust, Tarsis F, Watts, Val J, Hill, Catherine A

“…Many neglected tropical infectious diseases affecting humans are transmitted by arthropods such as mosquitoes and ticks. New mode-of-action chemistries are…”
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