Search Results - "Christopher A. Gabel"

Interleukin-36 (IL-36) Ligands Require Processing for Full Agonist (IL-36α, IL-36β, and IL-36γ) or Antagonist (IL-36Ra) Activity by Towne, Jennifer E., Renshaw, Blair R., Douangpanya, Jason, Lipsky, Brian P., Shen, Min, Gabel, Christopher A., Sims, John E.

“…IL-36α, IL-36β, and IL-36γ (formerly IL-1F6, IL-1F8, and IL-1F9) are IL-1 family members that signal through the IL-1 receptor family members IL-1Rrp2…”
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Species-specific NLRP3 regulation and its role in CNS autoinflammatory diseases by Koller, Beverly H., Nguyen, MyTrang, Snouwaert, John N., Gabel, Christopher A., Ting, Jenny P.-Y.

“…The NLRP3 inflammasome is essential for caspase-1 activation and the release of interleukin (IL)-1β, IL-18, and gasdermin-D in myeloid cells. However, research…”
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Absence of the P2X7 Receptor Alters Leukocyte Function and Attenuates an Inflammatory Response by Labasi, Jeffrey M, Petrushova, Nina, Donovan, Carol, McCurdy, Sandra, Lira, Paul, Payette, Mary M, Brissette, William, Wicks, Joan R, Audoly, Laurent, Gabel, Christopher A

“…When challenged with extracellular ATP, leukocytes respond and activate processes attributed to the P2X(7) receptor (P2X(7)R), an unusual ligand-gated ion…”
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Externalization of the Leaderless Cytokine IL-1F6 Occurs in Response to Lipopolysaccharide/ATP Activation of Transduced Bone Marrow Macrophages by Martin, Unja, Scholler, John, Gurgel, Jesse, Renshaw, Blair, Sims, John E, Gabel, Christopher A

“…An interesting trait shared by many members of the IL-1 cytokine family is the absence of a signal sequence that can direct the newly synthesized polypeptides…”
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Role of p38 MAPK in UVB-Induced Inflammatory Responses in the Skin of SKH-1 Hairless Mice by Kim, Arianna L., Labasi, Jeffrey M., Zhu, Yucui, Tang, Xiuwei, McClure, Kim, Gabel, Christopher A., Athar, Mohammad, Bickers, David R.

“…The p38 mitogen-activated protein kinase (MAPK) signaling pathway is activated by numerous inflammatory mediators and environmental stresses. We assessed the…”
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Discovery of Clinical Candidate NT-0796, a Brain-Penetrant and Highly Potent NLRP3 Inflammasome Inhibitor for Neuroinflammatory Disorders by Harrison, David, Billinton, Andy, Bock, Mark G., Doedens, John R., Gabel, Christopher A., Holloway, M. Katharine, Porter, Roderick A., Reader, Valérie, Scanlon, Jane, Schooley, Kenneth, Watt, Alan P.

“…The NLRP3 inflammasome is a component of the innate immune system involved in the production of proinflammatory cytokines. Neurodegenerative disorders,…”
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The ester-containing prodrug NT-0796 enhances delivery of the NLRP3 inflammasome inhibitor NDT-19795 to monocytic cells expressing carboxylesterase-1 by Doedens, John R., Diamond, Christine, Harrison, David, Bock, Mark G., Clarke, Nicholas, Watt, Alan P., Gabel, Christopher A.

“…[Display omitted] NT-0796 is an ester prodrug which is metabolized by carboxylesterase-1 (CES1) to yield the carboxylic acid NDT-19795, an inhibitor of the NLR…”
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Discovery of a series of ester-substituted NLRP3 inflammasome inhibitors by Harrison, David, Boutard, Nicolas, Brzozka, Krzysztof, Bugaj, Marta, Chmielewski, Stefan, Cierpich, Anna, Doedens, John R., Fabritius, Charles-Henry R.Y., Gabel, Christopher A., Galezowski, Michal, Kowalczyk, Piotr, Levenets, Oleksandr, Mroczkowska, Magdalena, Palica, Katarzyna, Porter, Roderick A., Schultz, David, Sowinska, Marta, Topolnicki, Grzegorz, Urbanski, Piotr, Woyciechowski, Jakub, Watt, Alan P.

“…[Display omitted] The NLRP3 inflammasome is a component of the innate immune system involved in the production of proinflammatory cytokines. Aberrant…”
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Discovery and Optimization of Triazolopyrimidinone Derivatives as Selective NLRP3 Inflammasome Inhibitors by Harrison, David, Bock, Mark G., Doedens, John R., Gabel, Christopher A., Holloway, M. Katharine, Lewis, Arwel, Scanlon, Jane, Sharpe, Andrew, Simpson, Iain D., Smolak, Pamela, Wishart, Grant, Watt, Alan P.

“…The NLRP3 inflammasome is a multiprotein complex that facilitates activation and release of the proinflammatory cytokines interleukin-1β (IL-1β) and IL-18 in…”
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Pharmacological Analysis of NLRP3 Inflammasome Inhibitor Sodium [(1,2,3,5,6,7-Hexahydro-s-indacen-4-yl)carbamoyl][(1-methyl‑1H‑pyrazol-4-yl)({[(2S)‑oxolan-2-yl]methyl})sulfamoyl]azanide in Cellular and Mouse Models of Inflammation Provides a Translational Framework by Doedens, John R., Smolak, Pamela, Nguyen, MyTrang, Wescott, Heather, Diamond, Christine, Schooley, Ken, Billinton, Andy, Harrison, David, Koller, Beverly H., Watt, Alan P., Gabel, Christopher A.

“…Interleukin (IL)-1β is an apex proinflammatory cytokine produced in response to tissue injury and infection. The output of IL-1β from monocytes and macrophages…”
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Novel protein therapeutic joint retention strategy based on collagen‐binding Avimers by Hulme, Joanne T., D'Souza, Warren N., McBride, Helen J., Yoon, Bo‐Rin Park, Willee, Angela M., Duguay, Amy, Thomas, Melissa, Fan, Bin, Dayao, Maria Rosalyn, Rottman, James B., Merriam, Kim, Xie, Jiansong, Smith, Richard, Alba, Benjamin M., Case, Ryan B., Dang, Khue, Montalvan, Anielka, Grinberg, Natalia, Sun, Hong, Black, Roy A., Gabel, Christopher A., Sims, John E., Moore, Kevin, Bakker, Alice, Li, Peng

“…ABSTRACT Designing drugs to treat diseases associated with articular joints, particularly those targeting chondrocytes, is challenging due to unique local…”
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P2 purinergic receptor modulation of cytokine production by Gabel, Christopher A

“…Cytokines serve important functions in controlling host immunity. Cells involved in the synthesis of these polypeptide mediators have evolved highly regulated…”
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Deletion of the P2X7 Nucleotide Receptor Reveals Its Regulatory Roles in Bone Formation and Resorption by Ke, Hua Zhu, Qi, Hong, Weidema, A. Frederik, Zhang, Qing, Panupinthu, Nattapon, Crawford, D. Todd, Grasser, William A, Paralkar, Vishwas M, Li, Mei, Audoly, Laurent P, Gabel, Christopher A, Jee, Webster S. S, Dixon, S. Jeffrey, Sims, Stephen M, Thompson, David D

“…The P2X7 nucleotide receptor is an ATP-gated ion channel expressed widely in cells of hematopoietic origin. Our purpose was to explore the involvement of the…”
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Identification, Characterization, and Crystal Structure of the Omega Class Glutathione Transferases by Board, Philip G., Coggan, Marjorie, Chelvanayagam, Gareth, Easteal, Simon, Jermiin, Lars S., Schulte, Gayle K., Danley, Dennis E., Hoth, Lise R., Griffor, Matthew C., Kamath, Ajith V., Rosner, Michele H., Chrunyk, Boris A., Perregaux, David E., Gabel, Christopher A., Geoghegan, Kieran F., Pandit, Jayvardhan

“…A new class of glutathione transferases has been discovered by analysis of the expressed sequence tag data base and sequence alignment. Glutathione…”
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Identification and characterization of a novel class of interleukin-1 post-translational processing inhibitors by Perregaux, D G, McNiff, P, Laliberte, R, Hawryluk, N, Peurano, H, Stam, E, Eggler, J, Griffiths, R, Dombroski, M A, Gabel, C A

“…Lipopolysaccharide (LPS)-activated monocytes and macrophages produce large quantities of pro-interleukin (IL)-1beta but externalize little mature cytokine…”
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Theoretical and Experimental Design of Atypical Kinase Inhibitors:  Application to p38 MAP Kinase by McClure, Kim F, Abramov, Yuriy A, Laird, Ellen R, Barberia, John T, Cai, Weiling, Carty, Thomas J, Cortina, Santo R, Danley, Dennis E, Dipesa, Alan J, Donahue, Kathleen M, Dombroski, Mark A, Elliott, Nancy C, Gabel, Christopher A, Han, Seungil, Hynes, Thomas R, LeMotte, Peter K, Mansour, Mahmoud N, Marr, Eric S, Letavic, Michael A, Pandit, Jayvardhan, Ripin, David B, Sweeney, Francis J, Tan, Douglas, Tao, Yong

“…Mimics of the benzimidazolone nucleus found in inhibitors of p38 kinase are proposed, and their theoretical potential as bioisosteres is described. A set of…”
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ATP Treatment of Human Monocytes Promotes Caspase-1 Maturation and Externalization by Laliberte, R E, Eggler, J, Gabel, C A

“…Mechanisms that regulate conversion of prointerleukin-1β (pro-IL-1β) to its mature form by the cysteine protease caspase-1 are not well understood. In this…”
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Antimicrobial peptides initiate IL-1 beta posttranslational processing: a novel role beyond innate immunity by Perregaux, David G, Bhavsar, Kanan, Contillo, Len, Shi, Jishu, Gabel, Christopher A

“…Human monocytes stimulated with LPS produce large quantities of prointerleukin-1beta, but little of this cytokine product is released extracellularly as the…”
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Discovery, synthesis and SAR of azinyl- and azolylbenzamides antagonists of the P2X7 receptor by Subramanyam, Chakrapani, Duplantier, Allen J., Dombroski, Mark A., Chang, Shang-Poa, Gabel, Christopher A., Whitney-Pickett, Carrie, Perregaux, David G., Labasi, Jeff M., Yoon, Kwansik, Shepard, Richard M., Fisher, Michael

“…The discovery, of a series of 2-Cl-5-heteroaryl-benzamide antagonists of the P2X7 receptor via parallel medicinal chemistry is described. Initial analogs…”
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Optimization of the physicochemical and pharmacokinetic attributes in a 6-azauracil series of P2X₇ receptor antagonists leading to the discovery of the clinical candidate CE-224,535 by Duplantier, Allen J, Dombroski, Mark A, Subramanyam, Chakrapani, Beaulieu, Aimee M, Chang, Shang-Poa, Gabel, Christopher A, Jordan, Crystal, Kalgutkar, Amit S, Kraus, Kenneth G, Labasi, Jeff M, Mussari, Christopher, Perregaux, David G, Shepard, Rick, Taylor, Timothy J, Trevena, Kristen A, Whitney-Pickett, Carrie, Yoon, Kwansik

“…High throughput screening (HTS) of our compound file provided an attractive lead compound with modest P2X₇ receptor antagonist potency and high selectivity…”
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