Search Results - "Marron, Brian E"

Voltage sensor interaction site for selective small molecule inhibitors of voltage-gated sodium channels by McCormack, Ken, Santos, Sonia, Chapman, Mark L, Krafte, Douglas S, Marron, Brian E, West, Christopher W, Krambis, Michael J, Antonio, Brett M, Zellmer, Shannon G, Printzenhoff, David, Padilla, Karen M, Lin, Zhixin, Wagoner, P Kay, Swain, Nigel A, Stupple, Paul A, de Groot, Marcel, Butt, Richard P, Castle, Neil A

“…Voltage-gated sodium (Na ᵥ) channels play a fundamental role in the generation and propagation of electrical impulses in excitable cells. Here we describe two…”
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Recent progress in sodium channel modulators for pain by Bagal, Sharan K., Chapman, Mark L., Marron, Brian E., Prime, Rebecca, Storer, R. Ian, Swain, Nigel A.

“…Voltage-gated sodium channels (Navs) are an important family of transmembrane ion channel proteins and Nav drug discovery is an exciting field. Pharmaceutical…”
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Subtype-Selective Small Molecule Inhibitors Reveal a Fundamental Role for Nav1.7 in Nociceptor Electrogenesis, Axonal Conduction and Presynaptic Release by Alexandrou, Aristos J, Brown, Adam R, Chapman, Mark L, Estacion, Mark, Turner, Jamie, Mis, Malgorzata A, Wilbrey, Anna, Payne, Elizabeth C, Gutteridge, Alex, Cox, Peter J, Doyle, Rachel, Printzenhoff, David, Lin, Zhixin, Marron, Brian E, West, Christopher, Swain, Nigel A, Storer, R Ian, Stupple, Paul A, Castle, Neil A, Hounshell, James A, Rivara, Mirko, Randall, Andrew, Dib-Hajj, Sulayman D, Krafte, Douglas, Waxman, Stephen G, Patel, Manoj K, Butt, Richard P, Stevens, Edward B

“…Human genetic studies show that the voltage gated sodium channel 1.7 (Nav1.7) is a key molecular determinant of pain sensation. However, defining the Nav1.7…”
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Voltage gated sodium channels as drug discovery targets by Bagal, Sharan K, Marron, Brian E, Owen, Robert M, Storer, R Ian, Swain, Nigel A

“…Voltage-gated sodium (Na V ) channels are a family of transmembrane ion channel proteins. They function by forming a gated, water-filled pore to help establish…”
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Discovery of Clinical Candidate 4‑[2-(5-Amino‑1H‑pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro‑N‑1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of NaV1.7 by Swain, Nigel. A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R. G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R. Ian, Stupple, Paul A, West, Christopher W

“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective NaV1.7 inhibitors is described. Optimization of early lead…”
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Discovery of the First Orally Available, Selective KNa1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series by Griffin, Andrew M, Kahlig, Kristopher M, Hatch, Robert John, Hughes, Zoë A, Chapman, Mark L, Antonio, Brett, Marron, Brian E, Wittmann, Marion, Martinez-Botella, Gabriel

“…The gene KCNT1 encodes the sodium-activated potassium channel KNa1.1 (Slack, Slo2.2). Variants in the KCNT1 gene induce a gain-of-function (GoF) phenotype in…”
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Highly potent and selective NaV1.7 inhibitors for use as intravenous agents and chemical probes by Storer, R. Ian, Pike, Andy, Swain, Nigel A., Alexandrou, Aristos J., Bechle, Bruce M., Blakemore, David C., Brown, Alan D., Castle, Neil A., Corbett, Matthew S., Flanagan, Neil J., Fengas, David, Johnson, M. Scott, Jones, Lyn H., Marron, Brian E., Payne, C. Elizabeth, Printzenhoff, David, Rawson, David J., Rose, Colin R., Ryckmans, Thomas, Sun, Jianmin, Theile, Jonathan W., Torella, Rubben, Tseng, Elaine, Warmus, Joseph S.

“…[Display omitted] The discovery and selection of a highly potent and selective NaV1.7 inhibitor PF-06456384, designed specifically for intravenous infusion, is…”
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Discovery of the First Orally Available, Selective K Na 1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series by Griffin, Andrew M, Kahlig, Kristopher M, Hatch, Robert John, Hughes, Zoë A, Chapman, Mark L, Antonio, Brett, Marron, Brian E, Wittmann, Marion, Martinez-Botella, Gabriel

“…The gene encodes the sodium-activated potassium channel K 1.1 (Slack, Slo2.2). Variants in the gene induce a gain-of-function (GoF) phenotype in ionic currents…”
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Discovery, Radiolabeling, and Evaluation of Subtype-Selective Inhibitors for Positron Emission Tomography Imaging of Brain Phosphodiesterase-4D by Wakabayashi, Yuichi, Telu, Sanjay, Dick, Rachel M, Fujita, Masahiro, Ooms, Maarten, Morse, Cheryl L, Liow, Jeih-San, Hong, Jinsoo S, Gladding, Robert L, Manly, Lester S, Zoghbi, Sami S, Mo, Xuesheng, D’Amato, Emily C, Sindac, Janice A, Nugent, Richard A, Marron, Brian E, Gurney, Mark E, Innis, Robert B, Pike, Victor W

“…We aimed to develop radioligands for PET imaging of brain phosphodiesterase subtype 4D (PDE4D), a potential target for developing cognition enhancing or…”
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Discovery of a Series of Indazole TRPA1 Antagonists by Pryde, David C, Marron, Brian E, West, Christopher W, Reister, Steven, Amato, George, Yoger, Katrina, Antonio, Brett, Padilla, Karen, Cox, Peter J, Turner, Jamie, Warmus, Joseph S, Swain, Nigel A, Omoto, Kiyoyuki, Mahoney, John H, Gerlach, Aaron C

“…A series of TRPA1 antagonists is described which has as its core structure an indazole moiety. The physical properties and in vitro DMPK profiles are…”
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A-887826 is a structurally novel, potent and voltage-dependent Na(v)1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats by Zhang, Xu-Feng, Shieh, Char-Chang, Chapman, Mark L, Matulenko, Mark A, Hakeem, Ahmed H, Atkinson, Robert N, Kort, Michael E, Marron, Brian E, Joshi, Shailen, Honore, Prisca, Faltynek, Connie R, Krafte, Douglas S, Jarvis, Michael F

“…Activation of sodium channels is essential to action potential generation and propagation. Recent genetic and pharmacological evidence indicates that…”
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Discovery of Clinical Candidate 4-[2-(5-Amino-1H-pyrazol-4-yl)-4-chlorophenoxy]-5-chloro-2-fluoro-N-1,3-thiazol-4-ylbenzenesulfonamide (PF-05089771): Design and Optimization of Diaryl Ether Aryl Sulfonamides as Selective Inhibitors of Na V 1.7 by Swain, Nigel A, Batchelor, Dave, Beaudoin, Serge, Bechle, Bruce M, Bradley, Paul A, Brown, Alan D, Brown, Bruce, Butcher, Ken J, Butt, Richard P, Chapman, Mark L, Denton, Stephen, Ellis, David, Galan, Sebastien R G, Gaulier, Steven M, Greener, Ben S, de Groot, Marcel J, Glossop, Mel S, Gurrell, Ian K, Hannam, Jo, Johnson, Matthew S, Lin, Zhixin, Markworth, Christopher J, Marron, Brian E, Millan, David S, Nakagawa, Shoko, Pike, Andy, Printzenhoff, David, Rawson, David J, Ransley, Sarah J, Reister, Steven M, Sasaki, Kosuke, Storer, R Ian, Stupple, Paul A, West, Christopher W

“…A series of acidic diaryl ether heterocyclic sulfonamides that are potent and subtype selective Na 1.7 inhibitors is described. Optimization of early lead…”
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Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Na(v)1.8 sodium channel with efficacy in a model of neuropathic pain by Scanio, Marc J C, Shi, Lei, Drizin, Irene, Gregg, Robert J, Atkinson, Robert N, Thomas, James B, Johnson, Matthew S, Chapman, Mark L, Liu, Dong, Krambis, Michael J, Liu, Yi, Shieh, Char-Chang, Zhang, Xufeng, Simler, Gricelda H, Joshi, Shailen, Honore, Prisca, Marsh, Kennan C, Knox, Alison, Werness, Stephen, Antonio, Brett, Krafte, Douglas S, Jarvis, Michael F, Faltynek, Connie R, Marron, Brian E, Kort, Michael E

“…Na(v)1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory…”
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Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Nav1.8 sodium channel with efficacy in a model of neuropathic pain by SCANIO, Marc J. C, LEI SHI, YI LIU, SHIEH, Char-Chang, XUFENG ZHANG, SIMLER, Gricelda H, JOSHI, Shailen, HONORE, Prisca, MARSH, Kennan C, KNOX, Alison, WERNESS, Stephen, ANTONIO, Brett, DRIZIN, Irene, KRAFTE, Douglas S, JARVIS, Michael F, FALTYNEK, Connie R, MARRON, Brian E, KORT, Michael E, GREGG, Robert J, ATKINSON, Robert N, THOMAS, James B, JOHNSON, Matthew S, CHAPMAN, Mark L, DONG LIU, KRAMBIS, Michael J

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Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives by Kort, Michael E, Atkinson, Robert N, Thomas, James B, Drizin, Irene, Johnson, Matthew S, Secrest, Matthew A, Gregg, Robert J, Scanio, Marc J C, Shi, Lei, Hakeem, Ahmed H, Matulenko, Mark A, Chapman, Mark L, Krambis, Michael J, Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Simler, Gricelda, Mikusa, Joseph P, Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Werness, Stephen, Antonio, Brett, Marsh, Kennan C, Faltynek, Connie R, Krafte, Douglas S, Jarvis, Michael F, Marron, Brian E

“…A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Na(v)1.8 sodium channel is reported. Replacement of the…”
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Subtype-selective Nav1.8 sodium channel blockers: Identification of potent, orally active nicotinamide derivatives by Kort, Michael E., Atkinson, Robert N., Thomas, James B., Drizin, Irene, Johnson, Matthew S., Secrest, Matthew A., Gregg, Robert J., Scanio, Marc J.C., Shi, Lei, Hakeem, Ahmed H., Matulenko, Mark A., Chapman, Mark L., Krambis, Michael J., Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Simler, Gricelda, Mikusa, Joseph P., Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Werness, Stephen, Antonio, Brett, Marsh, Kennan C., Faltynek, Connie R., Krafte, Douglas S., Jarvis, Michael F., Marron, Brian E.

“…A series of aryl-substituted nicotinamide derivatives with selective inhibitory activity against the Nav1.8 sodium channel is reported. Replacement of the…”
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Going to the well no more: lawn format assays for ultra-high-throughput screening by Marron, Brian E, Jayawickreme, Channa K

“…Screening in a ‘well-less’ or lawn format provides a means to screen large compound collections against many targets in a fast, versatile and cost effective…”
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Phosphodiesterase Type IV Inhibition. Structure-Activity Relationships of 1,3-Disubstituted Pyrrolidines by Feldman, Paul L, Brackeen, Marcus F, Cowan, David J, Marron, Brian E, Schoenen, Frank J, Stafford, Jeffrey A, Suh, Edward M, Domanico, Paul L, Rose, Dudley

“…The synthesis of 1,3-disubstituted pyrrolidines 2 and their activities as type IV phosphodiesterase (PDE) inhibitors are described. Various groups were…”
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A-887826 is a structurally novel, potent and voltage-dependent Nav1.8 sodium channel blocker that attenuates neuropathic tactile allodynia in rats by Zhang, Xu-Feng, Shieh, Char-Chang, Chapman, Mark L., Matulenko, Mark A., Hakeem, Ahmed H., Atkinson, Robert N., Kort, Michael E., Marron, Brian E., Joshi, Shailen, Honore, Prisca, Faltynek, Connie R., Krafte, Douglas S., Jarvis, Michael F.

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Discovery and Biological Evaluation of 5-Aryl-2-furfuramides, Potent and Selective Blockers of the Nav1.8 Sodium Channel with Efficacy in Models of Neuropathic and Inflammatory Pain by Kort, Michael E, Drizin, Irene, Gregg, Robert J, Scanio, Marc J. C, Shi, Lei, Gross, Michael F, Atkinson, Robert N, Johnson, Matthew S, Pacofsky, Gregory J, Thomas, James B, Carroll, William A, Krambis, Michael J, Liu, Dong, Shieh, Char-Chang, Zhang, XuFeng, Hernandez, Gricelda, Mikusa, Joseph P, Zhong, Chengmin, Joshi, Shailen, Honore, Prisca, Roeloffs, Rosemarie, Marsh, Kennan C, Murray, Bernard P, Liu, Jinrong, Werness, Stephen, Faltynek, Connie R, Krafte, Douglas S, Jarvis, Michael F, Chapman, Mark L, Marron, Brian E

“…Nav1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons…”
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