Parsing the Interferon Transcriptional Network and Its Disease Associations
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Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1‑((2S,5R)‑5-((7H‑Pyrrolo[2,3‑d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli, Dowty, Martin E, Banker, Mary Ellen, Juba, Brian, Jussif, Jason, Lin, Tsung, Vincent, Fabien, Czerwinski, Robert M, Casimiro-Garcia, Agustin, Unwalla, Ray, Trujillo, John I, Liang, Sidney, Balbo, Paul, Che, Ye, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Leung, Louis, Yang, Xin, Soucy, Sarah, Hegen, Martin, Coe, Jotham, Langille, Jonathan, Vajdos, Felix, Chrencik, Jill, Telliez, Jean-Baptiste
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Studies with neutralizing antibodies suggest CXCL8-mediated neutrophil activation is independent of C-C motif chemokine receptor-like 2 (CCRL2) ligand binding function
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Janus kinase inhibitors for the treatment of rheumatoid arthritis demonstrate similar profiles of in vitro cytokine receptor inhibition
Dowty, Martin E., Lin, Tsung H., Jesson, Michael I., Hegen, Martin, Martin, David A., Katkade, Vaibhav, Menon, Sujatha, Telliez, Jean‐Baptiste
Published in Pharmacology research & perspectives (01.12.2019)
Published in Pharmacology research & perspectives (01.12.2019)
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MAPKAP Kinase 2-Deficient Mice Are Resistant to Collagen-Induced Arthritis
Hegen, Martin, Gaestel, Matthias, Nickerson-Nutter, Cheryl L, Lin, Lih-Ling, Telliez, Jean-Baptiste
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Published in Journal of Immunology (01.08.2006)
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Antibodies specific for carbamylated proteins precede the onset of clinical symptoms in mice with collagen induced arthritis
Stoop, Jeroen N, Liu, Bi-Sheng, Shi, Jing, Jansen, Diahann T S L, Hegen, Martin, Huizinga, Tom W J, Trouw, Leendert A, Toes, René E M
Published in PloS one (15.07.2014)
Published in PloS one (15.07.2014)
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Anti-IL-13Rα2 therapy promotes recovery in a murine model of inflammatory bowel disease
Karmele, Erik P., Pasricha, Trisha S., Ramalingam, Thirumalai R., Thompson, Robert W., Gieseck, Richard L., Knilans, Kayla J., Hegen, Martin, Farmer, Mark, Jin, Fang, Kleinman, Aaron, Hinds, David A., Almeida Pereira, Thiago, de Queiroz Prado, Rafael, Bing, Nan, Tchistiakova, Lioudmila, Kasaian, Marion T., Wynn, Thomas A., Vannella, Kevin M.
Published in Mucosal immunology (01.09.2019)
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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of (( S)-2,2-Difluorocyclopropyl)((1 R,5 S)-3-(2-((1-methyl-1 H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841)
Fensome, Andrew, Ambler, Catherine M, Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F, Chrencik, Jill, Clark, James D, Dowty, Martin E, Efremov, Ivan V, Flick, Andrew, Gerstenberger, Brian S, Gopalsamy, Ariamala, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Jussif, Jason, Knafels, John D, Limburg, David C, Lin, David, Lin, Tsung H, Pierce, Betsy S, Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T, Telliez, Jean-Baptiste, Trujillo, John I, Vajdos, Felix F, Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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Pharmacokinetic, Biodistribution, and Biophysical Profiles of TNF Nanobodies Conjugated to Linear or Branched Poly(ethylene glycol)
Vugmeyster, Yulia, Entrican, Clifford A, Joyce, Alison P, Lawrence-Henderson, Rosemary F, Leary, Beth A, Mahoney, Christopher S, Patel, Himakshi K, Raso, Stephen W, Olland, Stephane H, Hegen, Martin, Xu, Xin
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Published in Bioconjugate chemistry (18.07.2012)
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Design of a Janus Kinase 3 (JAK3) Specific Inhibitor 1-(2s,5R)-5-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-y1)prop-2-en-1-one (PF-06651600) Allowing for the Interrogation of JAK3 Signaling in Humans
Thorarensen, Atli, Dowty, Martin E., Banker, Mary Ellen, Juba, Brian, Jussif, Jason, Lin, Tsung, Vincent, Fabien, Czerwinski, Robert M., Casimiro-Garcia, Agustin, Unwalla, Ray, Trujillo, John I., Liang, Sidney, Balbo, Paul, Che, Ye, Gilbert, Adam M., Brown, Matthew F., Hayward, Matthew, Montgomery, Justin, Leung, Louis, Yang, Xin, Soucy, Sarah, Hegen, Martin, Coe, Jotham, Langille, Jonathan, Vajdos, Felix, Chrencik, Jill, Telliez, Jean-Baptiste
Published in Journal of medicinal chemistry (09.03.2017)
Published in Journal of medicinal chemistry (09.03.2017)
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Dual Inhibition of TYK2 and JAK1 for the Treatment of Autoimmune Diseases: Discovery of ((S)-2,2-Difluorocyclopropyl)((1R,5S)-3-(2-(1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]octan-8-yl)methanone (PF-06700841
Fensome, Andrew, Ambler, Catherine M., Arnold, Eric, Banker, Mary Ellen, Brown, Matthew F., Chrencik, Jill, Clark, James D., Dowty, Martin E., Efremov, Ivan V., Flick, Andrew, Gerstenberger, Brian S., Gopalsamy, Ariamala, Hayward, Matthew M., Hegen, Martin, Hollingshead, Brett D., Jussif, Jason, Knafels, John D., Limburg, David C., Lin, David, Lin, Tsung H., Pierce, Betsy S., Saiah, Eddine, Sharma, Raman, Symanowicz, Peter T., Telliez, Jean-Baptiste, Trujillo, John I., Vajdos, Felix F., Vincent, Fabien, Wan, Zhao-Kui, Xing, Li, Yang, Xiaojing, Yang, Xin, Zhang, Liying
Published in Journal of medicinal chemistry (11.10.2018)
Published in Journal of medicinal chemistry (11.10.2018)
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RORγt inhibition ameliorates IL-23 driven experimental psoriatic arthritis by predominantly modulating γδ-T cells
Mortier, Céline, Gracey, Eric, Coudenys, Julie, Manuello, Teddy, Decruy, Tine, Maelegheer, Margaux, Stappers, Flore, Gilis, Elisabeth, Gaublomme, Djoere, Van Hoorebeke, Luc, Van Welden, Sophie, Ambler, Catherine, Hegen, Martin, Symanowicz, Peter, Steyn, Stefan, Berstein, Gabriel, Elewaut, Dirk, Venken, Koen
Published in Rheumatology (Oxford, England) (01.09.2023)
Published in Rheumatology (Oxford, England) (01.09.2023)
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Studies with neutralizing antibodies suggest CXCL8-mediated neutrophil activation is independent of C-C motif chemokine receptor-like 2
Su, Zhenwei, Brooks, Jonathan, Pelker, Jeffrey, Andreyeva, Tatyana, Sobon, Hanna, Gifford, Roger, Powers, Matthew, Wang, Jing, Dower, Corey, Hegen, Martin, Messing, Dean, Sheehan, Alfredo Darmanin, Brennan, Joseph J
Published in PloS one (20.01.2023)
Published in PloS one (20.01.2023)
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Identification of N‑{cis-3-[Methyl(7H‑pyrrolo[2,3‑d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases
Vazquez, Michael L, Kaila, Neelu, Strohbach, Joseph W, Trzupek, John D, Brown, Matthew F, Flanagan, Mark E, Mitton-Fry, Mark J, Johnson, Timothy A, TenBrink, Ruth E, Arnold, Eric P, Basak, Arindrajit, Heasley, Steven E, Kwon, Soojin, Langille, Jonathan, Parikh, Mihir D, Griffin, Sarah H, Casavant, Jeffrey M, Duclos, Brian A, Fenwick, Ashley E, Harris, Thomas M, Han, Seungil, Caspers, Nicole, Dowty, Martin E, Yang, Xin, Banker, Mary Ellen, Hegen, Martin, Symanowicz, Peter T, Li, Li, Wang, Lu, Lin, Tsung H, Jussif, Jason, Clark, James D, Telliez, Jean-Baptiste, Robinson, Ralph P, Unwalla, Ray
Published in Journal of medicinal chemistry (08.02.2018)
Published in Journal of medicinal chemistry (08.02.2018)
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The Interleukin‐1 Receptor–Associated Kinase 4 Inhibitor PF‐06650833 Blocks Inflammation in Preclinical Models of Rheumatic Disease and in Humans Enrolled in a Randomized Clinical Trial
Winkler, Aaron, Sun, Weiyong, De, Saurav, Jiao, Aiping, Sharif, M. Nusrat, Symanowicz, Peter T., Athale, Shruti, Shin, Julia H., Wang, Ju, Jacobson, Bruce A., Ramsey, Simeon J., Dower, Ken, Andreyeva, Tatyana, Liu, Heng, Hegen, Martin, Homer, Bruce L., Brodfuehrer, Joanne, Tilley, Mera, Gilbert, Steven A., Danto, Spencer I., Beebe, Jean J., Barnes, Betsy J., Pascual, Virginia, Lin, Lih‐Ling, Kilty, Iain, Fleming, Margaret, Rao, Vikram R.
Published in Arthritis & rheumatology (Hoboken, N.J.) (01.12.2021)
Published in Arthritis & rheumatology (Hoboken, N.J.) (01.12.2021)
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Blockade of the interleukin‐21/interleukin‐21 receptor pathway ameliorates disease in animal models of rheumatoid arthritis
Young, Deborah A., Hegen, Martin, Ma, Hak Ling Margery, Whitters, Matthew J., Albert, Leo M., Lowe, Leslie, Senices, Mayra, Wu, Paul W., Sibley, Barbara, Leathurby, Yelena, Brown, Tom P., Nickerson‐Nutter, Cheryl, Keith, James C., Collins, Mary
Published in Arthritis and rheumatism (01.04.2007)
Published in Arthritis and rheumatism (01.04.2007)
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Discovery of Tyrosine Kinase 2 (TYK2) Inhibitor (PF-06826647) for the Treatment of Autoimmune Diseases
Gerstenberger, Brian S, Ambler, Catherine, Arnold, Eric P, Banker, Mary-Ellen, Brown, Matthew F, Clark, James D, Dermenci, Alpay, Dowty, Martin E, Fensome, Andrew, Fish, Susan, Hayward, Matthew M, Hegen, Martin, Hollingshead, Brett D, Knafels, John D, Lin, David W, Lin, Tsung H, Owen, Dafydd R, Saiah, Eddine, Sharma, Raman, Vajdos, Felix F, Xing, Li, Yang, Xiaojing, Yang, Xin, Wright, Stephen W
Published in Journal of medicinal chemistry (25.11.2020)
Published in Journal of medicinal chemistry (25.11.2020)
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Network pharmacology of JAK inhibitors
Moodley, Devapregasan, Yoshida, Hideyuki, Mostafavi, Sara, Asinovski, Natasha, Ortiz-Lopez, Adriana, Symanowicz, Peter, Telliez, Jean-Baptiste, Hegen, Martin, Clark, James D., Mathis, Diane, Benoist, Christophe
Published in Proceedings of the National Academy of Sciences - PNAS (30.08.2016)
Published in Proceedings of the National Academy of Sciences - PNAS (30.08.2016)
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Discovery of a JAK3-Selective Inhibitor: Functional Differentiation of JAK3-Selective Inhibition over pan-JAK or JAK1-Selective Inhibition
Telliez, Jean-Baptiste, Dowty, Martin E, Wang, Lu, Jussif, Jason, Lin, Tsung, Li, Li, Moy, Erick, Balbo, Paul, Li, Wei, Zhao, Yajuan, Crouse, Kimberly, Dickinson, Caitlyn, Symanowicz, Peter, Hegen, Martin, Banker, Mary Ellen, Vincent, Fabien, Unwalla, Ray, Liang, Sidney, Gilbert, Adam M, Brown, Matthew F, Hayward, Matthew, Montgomery, Justin, Yang, Xin, Bauman, Jonathan, Trujillo, John I, Casimiro-Garcia, Agustin, Vajdos, Felix F, Leung, Louis, Geoghegan, Kieran F, Quazi, Amira, Xuan, Dejun, Jones, Lyn, Hett, Erik, Wright, Katherine, Clark, James D, Thorarensen, Atli
Published in ACS chemical biology (16.12.2016)
Published in ACS chemical biology (16.12.2016)
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Utility of animal models for identification of potential therapeutics for rheumatoid arthritis
Hegen, M, Keith, J C, Collins, M, Nickerson-Nutter, C L
Published in Annals of the rheumatic diseases (01.11.2008)
Published in Annals of the rheumatic diseases (01.11.2008)
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