Search Results - "McDermott, Jeff S"

Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement by Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M

“…Human genetic evidence has identified the voltage-gated sodium channel NaV1.7 as an attractive target for the treatment of pain. We initially identified…”
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Pharmacological effects of nonselective and subtype-selective nicotinic acetylcholine receptor agonists in animal models of persistent pain by Gao, BaoXi, Hierl, Markus, Clarkin, Kristie, Juan, Todd, Nguyen, Hung, Valk, Marissa van der, Deng, Hong, Guo, Wenhong, Lehto, Sonya G., Matson, David, McDermott, Jeff S., Knop, Johannes, Gaida, Kevin, Cao, Lei, Waldon, Dan, Albrecht, Brian K., Boezio, Alessandro A., Copeland, Katrina W., Harmange, Jean-Christophe, Springer, Stephanie K., Malmberg, Annika B., McDonough, Stefan I.

“…Nicotinic acetylcholine receptors (nAChRs) are longstanding targets for a next generation of pain therapeutics, but the nAChR subtypes that govern analgesia…”
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Targeting the Nerve Growth Factor (NGF) Pathway in Drug Discovery. Potential Applications to New Therapies for Chronic Pain by Norman, Bryan H, McDermott, Jeff S

“…The neurotrophin nerve growth factor (NGF) has been implicated as a key mediator of chronic pain. NGF binds the tropomysin receptor kinase A (TrkA) and p75,…”
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The Utility of hERG and Repolarization Assays in Evaluating Delayed Cardiac Repolarization: Influence of Multi-Channel Block by Martin, Ruth L, McDermott, Jeff S, Salmen, Heinz J, Palmatier, Jason, Cox, Bryan F, Gintant, Gary A

“…Drug-induced delayed cardiac repolarization is a recognized risk factor for proarrhythmia and is associated with block of IKr (the potassium current encoded by…”
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Heterogeneity of synaptic NMDA receptor responses within individual lamina I pain‐processing neurons across sex in rats and humans by Dedek, Annemarie, Topcu, Emine, Dedek, Christopher, McDermott, Jeff S., Krajewski, Jeffrey L., Tsai, Eve C., Hildebrand, Michael E.

“…Excitatory glutamatergic NMDA receptors (NMDARs) are key regulators of spinal pain processing, and yet the biophysical properties of NMDARs in dorsal horn…”
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Cardiac ion channels by Priest, Birgit T, McDermott, Jeff S

“…Ion channels are critical for all aspects of cardiac function, including rhythmicity and contractility. Consequently, ion channels are key targets for…”
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Antitussive effects of NaV 1.7 blockade in Guinea pigs by Yu, Li, Tsuji, Kojun, Ujihara, Izumi, Liu, Qi, Pavelkova, Nikoleta, Tsujimura, Takanori, Inoue, Makoto, Meeker, Sonya, Nisenbaum, Eric, McDermott, Jeff S., Krajewski, Jeff, Undem, Bradley J., Kollarik, Marian, Canning, Brendan J.

“…Our previous studies implicated the voltage-gated sodium channel subtype NaV 1.7 in the transmission of action potentials by the vagal afferent nerves…”
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Antitussive effects of Na V 1.7 blockade in Guinea pigs by Yu, Li, Tsuji, Kojun, Ujihara, Izumi, Liu, Qi, Pavelkova, Nikoleta, Tsujimura, Takanori, Inoue, Makoto, Meeker, Sonya, Nisenbaum, Eric, McDermott, Jeff S, Krajewski, Jeff, Undem, Bradley J, Kollarik, Marian, Canning, Brendan J

“…Our previous studies implicated the voltage-gated sodium channel subtype Na 1.7 in the transmission of action potentials by the vagal afferent nerves…”
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Stimulus intensity-dependent recruitment of Na V 1 subunits in action potential initiation in nerve terminals of vagal C-fibers innervating the esophagus by Ru, Fei, Pavelkova, Nikoleta, Krajewski, Jeffrey L, McDermott, Jeff S, Undem, Bradley J, Kollarik, Marian

“…We investigated voltage-gated sodium channel (Na 1) subunits that regulate action potential initiation in the nerve terminals of vagal nodose C-fibers…”
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Tetrodotoxin-resistant sodium channels in sensory neurons generate slow resurgent currents that are enhanced by inflammatory mediators by Tan, Zhi-Yong, Piekarz, Andrew D, Priest, Birgit T, Knopp, Kelly L, Krajewski, Jeffrey L, McDermott, Jeff S, Nisenbaum, Eric S, Cummins, Theodore R

“…Resurgent sodium currents contribute to the regeneration of action potentials and enhanced neuronal excitability. Tetrodotoxin-sensitive (TTX-S) resurgent…”
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The discovery of benzoxazine sulfonamide inhibitors of NaV1.7: Tools that bridge efficacy and target engagement by La, Daniel S., Peterson, Emily A., Bode, Christiane, Boezio, Alessandro A., Bregman, Howard, Chu-Moyer, Margaret Y., Coats, James, DiMauro, Erin F., Dineen, Thomas A., Du, Bingfan, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Fremeau, Robert, Huang, Xin, Ilch, Christopher, Kornecook, Thomas J., Kreiman, Charles, Ligutti, Joseph, Jasmine Lin, Min-Hwa, McDermott, Jeff S., Marx, Isaac, Matson, David J., McDonough, Stefan I., Moyer, Bryan D., Nho Nguyen, Hanh, Taborn, Kristin, Yu, Violeta, Weiss, Matthew M.

“…[Display omitted] The voltage-gated sodium channel NaV1.7 has received much attention from the scientific community due to compelling human genetic data…”
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Extracellular signal-regulated kinases mediate the enhancing effects of inflammatory mediators on resurgent currents in dorsal root ganglion neurons by Wu, Bin, McDermott, Jeff S, Krajewski, Jeffrey L, Knopp, Kelly L, Nisenbaum, Eric S, Cummins, Theodore R, Tan, Zhi-Yong

“…Previously we reported that a group of inflammatory mediators significantly enhanced resurgent currents in dorsal root ganglion neurons. To understand the…”
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Discovery and hit-to-lead optimization of pyrrolopyrimidines as potent, state-dependent Na(v)1.7 antagonists by Chakka, Nagasree, Bregman, Howie, Du, Bingfan, Nguyen, Hanh Nho, Buchanan, John L, Feric, Elma, Ligutti, Joseph, Liu, Dong, McDermott, Jeff S, Zou, Anruo, McDonough, Stefan I, Dimauro, Erin F

“…Herein we describe the discovery, optimization, and structure-activity relationships of novel potent pyrrolopyrimidine Na(v)1.7 antagonists. Hit-to-lead SAR…”
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The discovery of benzoxazine sulfonamide inhibitors of Na V 1.7: Tools that bridge efficacy and target engagement by La, Daniel S, Peterson, Emily A, Bode, Christiane, Boezio, Alessandro A, Bregman, Howard, Chu-Moyer, Margaret Y, Coats, James, DiMauro, Erin F, Dineen, Thomas A, Du, Bingfan, Gao, Hua, Graceffa, Russell, Gunaydin, Hakan, Guzman-Perez, Angel, Fremeau, Jr, Robert, Huang, Xin, Ilch, Christopher, Kornecook, Thomas J, Kreiman, Charles, Ligutti, Joseph, Jasmine Lin, Min-Hwa, McDermott, Jeff S, Marx, Isaac, Matson, David J, McDonough, Stefan I, Moyer, Bryan D, Nho Nguyen, Hanh, Taborn, Kristin, Yu, Violeta, Weiss, Matthew M

“…The voltage-gated sodium channel Na 1.7 has received much attention from the scientific community due to compelling human genetic data linking gain- and…”
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The discovery of aminopyrazines as novel, potent Na(v)1.7 antagonists: hit-to-lead identification and SAR by Bregman, Howard, Nguyen, Hanh Nho, Feric, Elma, Ligutti, Joseph, Liu, Dong, McDermott, Jeff S, Wilenkin, Ben, Zou, Anruo, Huang, Liyue, Li, Xingwen, McDonough, Stefan I, Dimauro, Erin F

“…Herein the discovery of a novel class of aminoheterocyclic Na(v)1.7 antagonists is reported. Hit compound 1 was potent but suffered from poor pharmacokinetics…”
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Discovery and optimization of aminopyrimidinones as potent and state-dependent Nav1.7 antagonists by Nguyen, Hanh Nho, Bregman, Howie, Buchanan, John L., Du, Bingfan, Feric, Elma, Huang, Liyue, Li, Xingwen, Ligutti, Joseph, Liu, Dong, Malmberg, Annika B., Matson, David J., McDermott, Jeff S., Patel, Vinod F., Wilenkin, Ben, Zou, Anruo, McDonough, Stefan I., DiMauro, Erin F.

“…Clinical genetic data have shown that the product of the SCN9A gene, voltage-gated sodium ion channel Nav1.7, is a key control point for pain perception and a…”
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The Canine Purkinje Fiber: An In Vitro Model System for Acquired Long QT Syndrome and Drug-Induced Arrhythmogenesis by Gintant, Gary A, Limberis, James T, McDermott, Jeff S, Wegner, Craig D, Cox, Bryan F

“…Torsade de pointes is a rare but potentially fatal ventricular arrhythmia associated with drug-induced delayed repolarization and prolongation of the QT…”
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Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha 4 beta 2 nicotinic acetylcholine receptor potentiators by Albrecht, Brian K, Berry, Virginia, Boezio, Alessandro A, Cao, Lei, Clarkin, Kristie, Guo, Wenhong, Harmange, Jean-Christophe, Hierl, Markus, Huang, Liyue, Janosky, Brett, Knop, Johannes, Malmberg, Annika, McDermott, Jeff S, Nguyen, Hung Q, Springer, Stephanie K, Waldon, Daniel, Woodin, Katrina, McDonough, Stefan I

“…The discovery of a series of small molecule alpha 4 beta 2 nAChR potentiators is reported. The structure-activity relationship leads to potent compounds…”
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Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement by Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M

“…Human genetic evidence has identified the voltage-gated sodium channel Na 1.7 as an attractive target for the treatment of pain. We initially identified…”
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Correction to "Sulfonamides as Selective Na V 1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement" by Marx, Isaac E, Dineen, Thomas A, Able, Jessica, Bode, Christiane, Bregman, Howard, Chu-Moyer, Margaret, DiMauro, Erin F, Du, Bingfan, Foti, Robert S, Fremeau, Jr, Robert T, Gao, Hua, Gunaydin, Hakan, Hall, Brian E, Huang, Liyue, Kornecook, Thomas, Kreiman, Charles R, La, Daniel S, Ligutti, Joseph, Lin, Min-Hwa Jasmine, Liu, Dong, McDermott, Jeff S, Moyer, Bryan D, Nguyen, Hanh N, Peterson, Emily A, Roberts, Jonathan T, Rose, Paul, Wang, Jean, Youngblood, Beth D, Yu, Violeta, Weiss, Matthew M

“…[This corrects the article DOI: 10.1021/acsmedchemlett.6b00243.]…”
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