Search Results - "Stahl, Edward L"

Crystal Structure of the Human Cannabinoid Receptor CB1 by Hua, Tian, Vemuri, Kiran, Pu, Mengchen, Qu, Lu, Han, Gye Won, Wu, Yiran, Zhao, Suwen, Shui, Wenqing, Li, Shanshan, Korde, Anisha, Laprairie, Robert B., Stahl, Edward L., Ho, Jo-Hao, Zvonok, Nikolai, Zhou, Han, Kufareva, Irina, Wu, Beili, Zhao, Qiang, Hanson, Michael A., Bohn, Laura M., Makriyannis, Alexandros, Stevens, Raymond C., Liu, Zhi-Jie

“…Cannabinoid receptor 1 (CB1) is the principal target of Δ9-tetrahydrocannabinol (THC), a psychoactive chemical from Cannabis sativa with a wide range of…”
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Activation and Signaling Mechanism Revealed by Cannabinoid Receptor-Gi Complex Structures by Hua, Tian, Li, Xiaoting, Wu, Lijie, Iliopoulos-Tsoutsouvas, Christos, Wang, Yuxia, Wu, Meng, Shen, Ling, Brust, Christina A., Nikas, Spyros P., Song, Feng, Song, Xiyong, Yuan, Shuguang, Sun, Qianqian, Wu, Yiran, Jiang, Shan, Grim, Travis W., Benchama, Othman, Stahl, Edward L., Zvonok, Nikolai, Zhao, Suwen, Bohn, Laura M., Makriyannis, Alexandros, Liu, Zhi-Jie

“…Human endocannabinoid systems modulate multiple physiological processes mainly through the activation of cannabinoid receptors CB1 and CB2. Their high sequence…”
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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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A Route to Potent, Selective, and Biased Salvinorin Chemical Space by Hill, Sarah J., Dao, Nathan, Dang, Vuong Q., Stahl, Edward L., Bohn, Laura M., Shenvi, Ryan A.

“…The salvinorins serve as templates for next generation analgesics, antipruritics, and dissociative hallucinogens via selective and potent agonism of the…”
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Hyperactivity in Mice Induced by Opioid Agonists with Partial Intrinsic Efficacy and Biased Agonism Administered Alone and in Combination with Morphine by Acevedo-Canabal, Agnes, Grim, Travis W, Schmid, Cullen L, McFague, Nina, Stahl, Edward L, Kennedy, Nicole M, Bannister, Thomas D, Bohn, Laura M

“…Opioid analgesics such as morphine and fentanyl induce mu-opioid receptor (MOR)-mediated hyperactivity in mice. Herein, we show that morphine, fentanyl,…”
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Low Intrinsic Efficacy Alone Cannot Explain the Improved Side Effect Profiles of New Opioid Agonists by Stahl, Edward L., Bohn, Laura M.

“…In a recent report in Science Signaling ( Gillis, A. , et al. Low intrinsic efficacy for G protein activation can explain the improved side effect profiles of…”
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A novel method for analyzing extremely biased agonism at G protein-coupled receptors by Stahl, Edward L, Zhou, Lei, Ehlert, Frederick J, Bohn, Laura M

“…Seven transmembrane receptors were originally named and characterized based on their ability to couple to heterotrimeric G proteins. The assortment of coupling…”
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Decaf or regular? Energizing the caffeine receptor by Stahl, Edward L., Bohn, Laura M.

“…Partial agonism describes the relative efficacy of a drug compared to one that produces a greater response in a particular system; the designation is dependent…”
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G protein signaling–biased mu opioid receptor agonists that produce sustained G protein activation are noncompetitive agonists by Stahl, Edward L., Schmid, Cullen L., Acevedo-Canabal, Agnes, Read, Cai, Grim, Travis W., Kennedy, Nicole M., Bannister, Thomas D., Bohn, Laura M.

“…The ability of a ligand to preferentially promote engagement of one signaling pathway over another downstream of GPCR activation has been referred to as…”
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A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal by Grim, Travis W, Schmid, Cullen L, Stahl, Edward L, Pantouli, Fani, Ho, Jo-Hao, Acevedo-Canabal, Agnes, Kennedy, Nicole M, Cameron, Michael D, Bannister, Thomas D, Bohn, Laura M

“…It has been demonstrated that opioid agonists that preferentially act at μ-opioid receptors to activate G protein signaling over βarrestin2 recruitment produce…”
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Arrestin recruitment to dopamine D2 receptor mediates locomotion but not incentive motivation by Donthamsetti, Prashant, Gallo, Eduardo F., Buck, David C., Stahl, Edward L., Zhu, Ying, Lane, J. Robert, Bohn, Laura M., Neve, Kim A., Kellendonk, Christoph, Javitch, Jonathan A.

“…The dopamine (DA) D2 receptor (D2R) is an important target for the treatment of neuropsychiatric disorders such as schizophrenia and Parkinson’s disease…”
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Synthesis and evaluation of 3,4,5-trisubstituted triazoles as G protein-biased kappa opioid receptor agonists by Trojniak, Ashley E., Dang, Vuong Q., Czekner, Kerri M., Russo, Robin J., Mather, Lilyan M., Stahl, Edward L., Cameron, Michael D., Bohn, Laura M., Aubé, Jeffrey

“…Kappa opioid receptor (KOR) agonists represent promising therapeutics for pain relief due to their analgesic properties along with lower abuse potential than…”
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G protein signaling-biased agonism at the κ-opioid receptor is maintained in striatal neurons by Ho, Jo-Hao, Stahl, Edward L, Schmid, Cullen L, Scarry, Sarah M, Aubé, Jeffrey, Bohn, Laura M

“…Biased agonists of G protein-coupled receptors may present a means to refine receptor signaling in a way that separates side effects from therapeutic…”
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Characterization of structurally novel G protein biased CB1 agonists: Implications for drug development by Ford, Benjamin M., Franks, Lirit N., Tai, Sherrica, Fantegrossi, William E., Stahl, Edward L., Berquist, Michael D., Cabanlong, Christian V., Wilson, Catheryn D., Penthala, Narsimha R., Crooks, Peter A., Prather, Paul L.

“…[Display omitted] The human cannabinoid subtype 1 receptor (hCB1R) is highly expressed in the CNS and serves as a therapeutic target for endogenous ligands as…”
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Approaches to Assess Biased Signaling at the CB1R Receptor by Laprairie, Robert B, Stahl, Edward L, Bohn, Laura M

“…G protein-coupled receptors, such as the cannabinoid type 1 receptor (CB1R), have been shown to interact with multiple binding partners to transmit signals. In…”
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Characterization of kappa opioid receptor mediated, dynorphin-stimulated [35S]GTPγS binding in mouse striatum for the evaluation of selective KOR ligands in an endogenous setting by Zhou, Lei, Stahl, Edward L., Lovell, Kimberly M., Frankowski, Kevin J., Prisinzano, Thomas E., Aubé, Jeffrey, Bohn, Laura M.

“…Differential modulation of kappa opioid receptor (KOR) signaling has been a proposed strategy for developing therapies for drug addiction and depression by…”
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Probing the CB 1 Cannabinoid Receptor Binding Pocket with AM6538, a High-Affinity Irreversible Antagonist by Laprairie, Robert B, Vemuri, Kiran, Stahl, Edward L, Korde, Anisha, Ho, Jo-Hao, Grim, Travis W, Hua, Tian, Wu, Yiran, Stevens, Raymond C, Liu, Zhi-Jie, Makriyannis, Alexandros, Bohn, Laura M

“…Cannabinoid receptor 1 (CB ) is a potential therapeutic target for the treatment of pain, obesity and obesity-related metabolic disorders, and addiction. The…”
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Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias by Lovell, Kimberly M, Frankowski, Kevin J, Stahl, Edward L, Slauson, Stephen R, Yoo, Euna, Prisinzano, Thomas E, Aubé, Jeffrey, Bohn, Laura M

“…Kappa opioid receptor (KOR) modulation is a promising target for drug discovery efforts due to KOR involvement in pain, depression, and addiction behaviors. We…”
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Characterization of structurally novel G protein biased CB 1 agonists: Implications for drug development by Ford, Benjamin M, Franks, Lirit N, Tai, Sherrica, Fantegrossi, William E, Stahl, Edward L, Berquist, Michael D, Cabanlong, Christian V, Wilson, Catheryn D, Penthala, Narsimha R, Crooks, Peter A, Prather, Paul L

“…The human cannabinoid subtype 1 receptor (hCB R) is highly expressed in the CNS and serves as a therapeutic target for endogenous ligands as well as…”
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Correction to “Structure–Activity Relationship Studies of Functionally Selective Kappa Opioid Receptor Agonists that Modulate ERK 1/2 Phosphorylation While Preserving G Protein Over βArrestin2 Signaling Bias” by Lovell, Kimberly M, Frankowski, Kevin J, Stahl, Edward L, Slauson, Stephen R, Yoo, Euna, Prisinzano, Thomas E, Aubé, Jeffrey, Bohn, Laura M

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