Selective blockade of TRPA1 channel attenuates pathological pain without altering noxious cold sensation or body temperature regulation
Chen, Jun, Joshi, Shailen K., DiDomenico, Stanley, Perner, Richard J., Mikusa, Joe P., Gauvin, Donna M., Segreti, Jason A., Han, Ping, Zhang, Xu-Feng, Niforatos, Wende, Bianchi, Bruce R., Baker, Scott J., Zhong, Chengmin, Simler, Gricelda H., McDonald, Heath A., Schmidt, Robert G., McGaraughty, Steve P., Chu, Katharine L., Faltynek, Connie R., Kort, Michael E., Reilly, Regina M., Kym, Philip R.
Published in Pain (Amsterdam) (01.05.2011)
Published in Pain (Amsterdam) (01.05.2011)
Get full text
Journal Article
TRPA1 Modulation of Spontaneous and Mechanically Evoked Firing of Spinal Neurons in Uninjured, Osteoarthritic, and Inflamed Rats
McGaraughty, Steve, Chu, Katharine L, Perner, Richard J, DiDomenico, Stan, Kort, Michael E, Kym, Philip R
Published in Molecular pain (05.03.2010)
Published in Molecular pain (05.03.2010)
Get full text
Journal Article
Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists
Gomtsyan, Arthur, Schmidt, Robert G, Bayburt, Erol K, Gfesser, Gregory A, Voight, Eric A, Daanen, Jerome F, Schmidt, Diana L, Cowart, Marlon D, Liu, Huaqing, Altenbach, Robert J, Kort, Michael E, Clapham, Bruce, Cox, Phil B, Shrestha, Anurupa, Henry, Rodger, Whittern, David N, Reilly, Regina M, Puttfarcken, Pamela S, Brederson, Jill-Desiree, Song, Ping, Li, Bin, Huang, Susan M, McDonald, Heath A, Neelands, Torben R, McGaraughty, Steve P, Gauvin, Donna M, Joshi, Shailen K, Banfor, Patricia N, Segreti, Jason A, Shebley, Mohamad, Faltynek, Connie R, Dart, Michael J, Kym, Philip R
Published in Journal of medicinal chemistry (26.05.2016)
Published in Journal of medicinal chemistry (26.05.2016)
Get full text
Journal Article
Repeated dosing of ABT-102, a potent and selective TRPV1 antagonist, enhances TRPV1-mediated analgesic activity in rodents, but attenuates antagonist-induced hyperthermia
Honore, Prisca, Chandran, Prasant, Hernandez, Gricelda, Gauvin, Donna M., Mikusa, Joseph P., Zhong, Chengmin, Joshi, Shailen K., Ghilardi, Joseph R., Sevcik, Molly A., Fryer, Ryan M., Segreti, Jason A., Banfor, Patricia N., Marsh, Kennan, Neelands, Torben, Bayburt, Erol, Daanen, Jerome F., Gomtsyan, Arthur, Lee, Chih-Hung, Kort, Michael E., Reilly, Regina M., Surowy, Carol S., Kym, Philip R., Mantyh, Patrick W., Sullivan, James P., Jarvis, Michael F., Faltynek, Connie R.
Published in Pain (Amsterdam) (01.03.2009)
Published in Pain (Amsterdam) (01.03.2009)
Get full text
Journal Article
Mechanistic insights into a heterobifunctional degrader-induced PTPN2/N1 complex
Hao, Qi, Rathinaswamy, Manoj K., Klinge, Kelly L., Bratkowski, Matthew, Mafi, Amirhossein, Baumgartner, Christina K., Hamel, Keith M., Veits, Gesine K., Jain, Rinku, Catalano, Claudio, Fitzgerald, Mark, Hird, Alexander W., Park, Eunice, Vora, Harit U., Henderson, James A., Longenecker, Kenton, Hutchins, Charles W., Qiu, Wei, Scapin, Giovanna, Sun, Qi, Stoll, Vincent S., Sun, Chaohong, Li, Ping, Eaton, Dan, Stokoe, David, Fisher, Stewart L., Nasveschuk, Christopher G., Paddock, Marcia, Kort, Michael E.
Published in Communications chemistry (16.08.2024)
Published in Communications chemistry (16.08.2024)
Get full text
Journal Article
Molecular Determinants of Species-Specific Activation or Blockade of TRPA1 Channels
Chen, Jun, Zhang, Xu-Feng, Kort, Michael E, Huth, Jeffrey R, Sun, Chaohong, Miesbauer, Laura J, Cassar, Steven C, Neelands, Torben, Scott, Victoria E, Moreland, Robert B, Reilly, Regina M, Hajduk, Philip J, Kym, Philip R, Hutchins, Charles W, Faltynek, Connie R
Published in The Journal of neuroscience (07.05.2008)
Published in The Journal of neuroscience (07.05.2008)
Get full text
Journal Article
A Selective Nav1.8 Sodium Channel Blocker, A-803467 [5-(4-Chlorophenyl-N-(3,5-dimethoxyphenyl)furan-2-carboxamide], Attenuates Spinal Neuronal Activity in Neuropathic Rats
McGaraughty, Steve, Chu, Katharine L, Scanio, Marc J C, Kort, Michael E, Faltynek, Connie R, Jarvis, Michael F
Published in The Journal of pharmacology and experimental therapeutics (01.03.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.03.2008)
Get full text
Journal Article
Synthesis and biological evaluation of 5-substituted and 4,5-disubstituted-2-arylamino oxazole TRPV1 antagonists
Perner, Richard J., Koenig, John R., DiDomenico, Stanley, Gomtsyan, Arthur, Schmidt, Robert G., Lee, Chih-Hung, Hsu, Margaret C., McDonald, Heath A., Gauvin, Donna M., Joshi, Shailen, Turner, Teresa M., Reilly, Regina M., Kym, Philip R., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (01.07.2010)
Published in Bioorganic & medicinal chemistry (01.07.2010)
Get full text
Journal Article
IL-23 induces regulatory T cell plasticity with implications for inflammatory skin diseases
Kannan, Arun K., Su, Zhi, Gauvin, Donna M., Paulsboe, Stephanie E., Duggan, Ryan, Lasko, Loren M., Honore, Prisca, Kort, Michael E., McGaraughty, Steve P., Scott, Victoria E., Gauld, Stephen B.
Published in Scientific reports (27.11.2019)
Published in Scientific reports (27.11.2019)
Get full text
Journal Article
Discovery of a Potent Chloroacetamide GPX4 Inhibitor with Bioavailability to Enable Target Engagement in Mice, a Potential Tool Compound for Inducing Ferroptosis In Vivo
Randolph, John T., O’Connor, Matthew J., Han, Fei, Hutchins, Charles W., Siu, Y. Amy, Cho, Min, Zheng, Yunan, Hickson, Jonathan A., Markley, Jana L., Manaves, Vlasios, Algire, Mikkel, Baker, Kenton A., Chapman, Alex M., Gopalakrishnan, Sujatha M., Panchal, Sanjay C., Foster-Duke, Kelly, Stolarik, DeAnne F., Kempf-Grote, Anita, Dammeier, Darby, Fossey, Stacey, Sun, Qi, Sun, Chaohong, Shen, Yu, Dart, Michael J., Kati, Warren M., Lai, Albert, Firestone, Ari J., Kort, Michael E.
Published in Journal of medicinal chemistry (23.03.2023)
Published in Journal of medicinal chemistry (23.03.2023)
Get full text
Journal Article
Effects of Substitution on 9-(3-Bromo-4-fluorophenyl)-5,9-dihydro-3H,4H-2,6-dioxa-4- azacyclopenta[b]naphthalene-1,8-dione, a Dihydropyridine ATP-Sensitive Potassium Channel Opener
Altenbach, Robert J, Brune, Michael E, Buckner, Steven A, Coghlan, Michael J, Daza, Anthony V, Fabiyi, Adebola, Gopalakrishnan, Murali, Henry, Rodger F, Khilevich, Albert, Kort, Michael E, Milicic, Ivan, Scott, Victoria E, Smith, Jamie C, Whiteaker, Kristi L, Carroll, William A
Published in Journal of medicinal chemistry (16.11.2006)
Published in Journal of medicinal chemistry (16.11.2006)
Get full text
Journal Article
Transient receptor potential channel ankyrin-1 is not a cold sensor for autonomic thermoregulation in rodents
de Oliveira, Cristiane, Garami, Andras, Lehto, Sonya G, Pakai, Eszter, Tekus, Valeria, Pohoczky, Krisztina, Youngblood, Beth D, Wang, Weiya, Kort, Michael E, Kym, Philip R, Pinter, Erika, Gavva, Narender R, Romanovsky, Andrej A
Published in The Journal of neuroscience (26.03.2014)
Published in The Journal of neuroscience (26.03.2014)
Get full text
Journal Article
Discovery of potent furan piperazine sodium channel blockers for treatment of neuropathic pain
Drizin, Irene, Gregg, Robert J., Scanio, Marc J.C., Shi, Lei, Gross, Michael F., Atkinson, Robert N., Thomas, James B., Johnson, Matthew S., Carroll, William A., Marron, Brian E., Chapman, Mark L., Liu, Dong, Krambis, Michael J., Shieh, Char-Chang, Zhang, XuFeng, Hernandez, Gricelda, Gauvin, Donna M., Mikusa, Joseph P., Zhu, Chang Z., Joshi, Shailen, Honore, Prisca, Marsh, Kennan C., Roeloffs, Rosemarie, Werness, Stephen, Krafte, Douglas S., Jarvis, Michael F., Faltynek, Connie R., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (15.06.2008)
Published in Bioorganic & medicinal chemistry (15.06.2008)
Get full text
Journal Article
Inhibition of Interleukin-23-Mediated Inflammation with a Novel Small Molecule Inverse Agonist of ROR γ t
Gauld, Stephen B, Jacquet, Sebastien, Gauvin, Donna, Wallace, Craig, Wang, Yibing, McCarthy, Richard, Goess, Christian, Leys, Laura, Huang, Susan, Su, Zhi, Edelmayer, Rebecca, Wetter, Joseph, Salte, Katherine, McGaraughty, Steven P, Argiriadi, Maria A, Honore, Prisca, Luccarini, Jean-Michel, Bressac, Didier, Desino, Kelly, Breinlinger, Eric, Cusack, Kevin, Potin, Dominique, Kort, Michael E, Masson, Philippe J
Published in The Journal of pharmacology and experimental therapeutics (01.10.2019)
Published in The Journal of pharmacology and experimental therapeutics (01.10.2019)
Get full text
Journal Article
Analgesic potential of TRPV1 antagonists
Kym, Philip R., Kort, Michael E., Hutchins, Charles W.
Published in Biochemical pharmacology (01.08.2009)
Published in Biochemical pharmacology (01.08.2009)
Get full text
Journal Article
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Nav1.7/ Nav1.8 blockers for the treatment of pain
Patel, Meena V., Peltier, Hillary M., Matulenko, Mark A., Koenig, John R., C. Scanio, Marc J., Gum, Rebecca J., El-Kouhen, Odile F., Fricano, Meagan M., Lundgaard, Greta L., Neelands, Torben, Zhang, Xu-Feng, Zhan, Cenchen, Pai, Madhavi, Ghoreishi-Haack, Nayereh, Hudzik, Thomas, Gintant, Gary, Martin, Ruth, McGaraughty, Steve, Xu, Jun, Bow, Daniel, Kalvass, John C., Kym, Philip R., DeGoey, David A., Kort, Michael E.
Published in Bioorganic & medicinal chemistry (01.06.2022)
Published in Bioorganic & medicinal chemistry (01.06.2022)
Get full text
Journal Article
Discovery of novel quinoline sulphonamide derivatives as potent, selective and orally active RORγ inverse agonists
Amaudrut, Jérôme, Argiriadi, Maria A., Barth, Martine, Breinlinger, Eric C., Bressac, Didier, Broqua, Pierre, Calderwood, David J., Chatar, Mohamed, Cusack, Kevin P., Gauld, Stephen B., Jacquet, Sébastien, Kamath, Rajesh V., Kort, Michael E., Lepais, Valérie, Luccarini, Jean-Michel, Masson, Philippe, Montalbetti, Christian, Mounier, Laurent, Potin, Dominique, Poupardin, Olivia, Rouaud, Sylvie, Spitzer, Luc, Wallace, Craig D.
Published in Bioorganic & medicinal chemistry letters (15.07.2019)
Published in Bioorganic & medicinal chemistry letters (15.07.2019)
Get full text
Journal Article
Structure−Activity Relationship Studies on a Series of Novel, Substituted 1-Benzyl-5-phenyltetrazole P2X7 Antagonists
Nelson, Derek W, Gregg, Robert J, Kort, Michael E, Perez-Medrano, Arturo, Voight, Eric A, Wang, Ying, Grayson, George, Namovic, Marian T, Donnelly-Roberts, Diana L, Niforatos, Wende, Honore, Prisca, Jarvis, Michael F, Faltynek, Connie R, Carroll, William A
Published in Journal of medicinal chemistry (15.06.2006)
Published in Journal of medicinal chemistry (15.06.2006)
Get full text
Journal Article
Pharmacology of modality-specific transient receptor potential vanilloid-1 antagonists that do not alter body temperature
Reilly, Regina M, McDonald, Heath A, Puttfarcken, Pamela S, Joshi, Shailen K, Lewis, LaGeisha, Pai, Madhavi, Franklin, Pamela H, Segreti, Jason A, Neelands, Torben R, Han, Ping, Chen, Jun, Mantyh, Patrick W, Ghilardi, Joseph R, Turner, Teresa M, Voight, Eric A, Daanen, Jerome F, Schmidt, Robert G, Gomtsyan, Arthur, Kort, Michael E, Faltynek, Connie R, Kym, Philip R
Published in The Journal of pharmacology and experimental therapeutics (01.08.2012)
Published in The Journal of pharmacology and experimental therapeutics (01.08.2012)
Get full text
Journal Article