Highly Selective Inhibition of Tyrosine Kinase 2 (TYK2) for the Treatment of Autoimmune Diseases: Discovery of the Allosteric Inhibitor BMS-986165
Wrobleski, Stephen T, Moslin, Ryan, Lin, Shuqun, Zhang, Yanlei, Spergel, Steven, Kempson, James, Tokarski, John S, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Shuster, David, Gillooly, Kathleen, Yang, Xiaoxia, Heimrich, Elizabeth, McIntyre, Kim W, Chaudhry, Charu, Khan, Javed, Ruzanov, Max, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Sun, Huadong, Huang, Christine, D’Arienzo, Celia, Aranibar, Nelly, Chiney, Manoj, Chimalakonda, Anjaneya, Pitts, William J, Lombardo, Louis, Carter, Percy H, Burke, James R, Weinstein, David S
Published in Journal of medicinal chemistry (24.10.2019)
Published in Journal of medicinal chemistry (24.10.2019)
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Journal Article
DCAF11 Supports Targeted Protein Degradation by Electrophilic Proteolysis-Targeting Chimeras
Zhang, Xiaoyu, Luukkonen, Lena M, Eissler, Christie L, Crowley, Vincent M, Yamashita, Yu, Schafroth, Michael A, Kikuchi, Shota, Weinstein, David S, Symons, Kent T, Nordin, Brian E, Rodriguez, Joe L, Wucherpfennig, Thomas G, Bauer, Ludwig G, Dix, Melissa M, Stamos, Dean, Kinsella, Todd M, Simon, Gabriel M, Baltgalvis, Kristen A, Cravatt, Benjamin F
Published in Journal of the American Chemical Society (07.04.2021)
Published in Journal of the American Chemical Society (07.04.2021)
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Autoimmune pathways in mice and humans are blocked by pharmacological stabilization of the TYK2 pseudokinase domain
Burke, James R, Cheng, Lihong, Gillooly, Kathleen M, Strnad, Joann, Zupa-Fernandez, Adriana, Catlett, Ian M, Zhang, Yifan, Heimrich, Elizabeth M, McIntyre, Kim W, Cunningham, Mark D, Carman, Julie A, Zhou, Xiadi, Banas, Dana, Chaudhry, Charu, Li, Sha, D'Arienzo, Celia, Chimalakonda, Anjaneya, Yang, XiaoXia, Xie, Jenny H, Pang, Jian, Zhao, Qihong, Rose, Shawn M, Huang, Jinwen, Moslin, Ryan M, Wrobleski, Stephen T, Weinstein, David S, Salter-Cid, Luisa M
Published in Science translational medicine (24.07.2019)
Published in Science translational medicine (24.07.2019)
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Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
Gong, Hua, Weinstein, David S., Lu, Zhonghui, Duan, James J.-W., Stachura, Sylwia, Haque, Lauren, Karmakar, Ananta, Hemagiri, Hemalatha, Raut, Dhanya Kumar, Gupta, Arun Kumar, Khan, Javed, Camac, Dan, Sack, John S., Pudzianowski, Andrew, Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Borowski, Virna, Xie, Jenny H., Sun, Huadong, D'Arienzo, Celia, Dabros, Marta, Galella, Michael A., Wang, Faye, Weigelt, Carolyn A., Zhao, Qihong, Foster, William, Somerville, John E., Salter-Cid, Luisa M., Barrish, Joel C., Carter, Percy H., Dhar, T.G. Murali
Published in Bioorganic & medicinal chemistry letters (15.01.2018)
Published in Bioorganic & medicinal chemistry letters (15.01.2018)
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Journal Article
Azaxanthene Based Selective Glucocorticoid Receptor Modulators: Design, Synthesis, and Pharmacological Evaluation of (S)-4-(5-(1-((1,3,4-Thiadiazol-2-yl)amino)-2-methyl-1-oxopropan-2-yl)-5H-chromeno[2,3-b]pyridin-2-yl)-2-fluoro-N,N-dimethylbenzamide (BMS-776532) and Its Methylene Homologue (BMS-791826)
Weinstein, David S, Gong, Hua, Doweyko, Arthur M, Cunningham, Mark, Habte, Sium, Wang, Jin Hong, Holloway, Deborah A, Burke, Christine, Gao, Ling, Guarino, Victor, Carman, Julie, Somerville, John E, Shuster, David, Salter-Cid, Luisa, Dodd, John H, Nadler, Steven G, Barrish, Joel C
Published in Journal of medicinal chemistry (27.10.2011)
Published in Journal of medicinal chemistry (27.10.2011)
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Journal Article
Development of a Practical Synthesis of Functionalized Azaxanthene-Derived Nonsteroidal Glucocorticoid Receptor Modulators
Conlon, David A, Natalie, Kenneth J, Cuniere, Nicolas, Razler, Thomas M, Zhu, Jason, de Mas, Nuria, Tymonko, Steven, Fraunhoffer, Kenneth J, Sortore, Eric, Rosso, Victor W, Xu, Zhongmin, Adams, Monica L, Patel, Anisha, Huang, Jun, Gong, Hua, Weinstein, David S, Quiroz, Fernando, Chen, Doris C
Published in Organic process research & development (20.05.2016)
Published in Organic process research & development (20.05.2016)
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Journal Article
Discovery of BMS-986202: A Clinical Tyk2 Inhibitor that Binds to Tyk2 JH2
Liu, Chunjian, Lin, James, Langevine, Charles, Smith, Daniel, Li, Jianqing, Tokarski, John S., Khan, Javed, Ruzanov, Max, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Gillooly, Kathleen M., Shuster, David, Zhang, Yifan, Thankappan, Anil, McIntyre, Kim W., Chaudhry, Charu, Elzinga, Paul A., Chiney, Manoj, Chimalakonda, Anjaneya, Lombardo, Louis J., Macor, John E., Carter, Percy H., Burke, James R., Weinstein, David S.
Published in Journal of medicinal chemistry (14.01.2021)
Published in Journal of medicinal chemistry (14.01.2021)
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Journal Article
Identification of N‑Methyl Nicotinamide and N‑Methyl Pyridazine-3-Carboxamide Pseudokinase Domain Ligands as Highly Selective Allosteric Inhibitors of Tyrosine Kinase 2 (TYK2)
Moslin, Ryan, Zhang, Yanlei, Wrobleski, Stephen T, Lin, Shuqun, Mertzman, Michael, Spergel, Steven, Tokarski, John S, Strnad, Joann, Gillooly, Kathleen, McIntyre, Kim W, Zupa-Fernandez, Adriana, Cheng, Lihong, Sun, Huadong, Chaudhry, Charu, Huang, Christine, D’Arienzo, Celia, Heimrich, Elizabeth, Yang, Xiaoxia, Muckelbauer, Jodi K, Chang, ChiehYing, Tredup, Jeffrey, Mulligan, Dawn, Xie, Dianlin, Aranibar, Nelly, Chiney, Manoj, Burke, James R, Lombardo, Louis, Carter, Percy H, Weinstein, David S
Published in Journal of medicinal chemistry (24.10.2019)
Published in Journal of medicinal chemistry (24.10.2019)
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Journal Article
Tyrosine Kinase 2-mediated Signal Transduction in T Lymphocytes Is Blocked by Pharmacological Stabilization of Its Pseudokinase Domain
Tokarski, John S., Zupa-Fernandez, Adriana, Tredup, Jeffrey A., Pike, Kristen, Chang, ChiehYing, Xie, Dianlin, Cheng, Lihong, Pedicord, Donna, Muckelbauer, Jodi, Johnson, Stephen R., Wu, Sophie, Edavettal, Suzanne C., Hong, Yang, Witmer, Mark R., Elkin, Lisa L., Blat, Yuval, Pitts, William J., Weinstein, David S., Burke, James R.
Published in The Journal of biological chemistry (24.04.2015)
Published in The Journal of biological chemistry (24.04.2015)
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Journal Article
Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase
Baltgalvis, Kristen A., Lamb, Kelsey N., Symons, Kent T., Wu, Chu-Chiao, Hoffman, Melissa A., Snead, Aaron N., Song, Xiaodan, Glaza, Thomas, Kikuchi, Shota, Green, Jason C., Rogness, Donald C., Lam, Betty, Rodriguez-Aguirre, Maria E., Woody, David R., Eissler, Christie L., Rodiles, Socorro, Negron, Seth M., Bernard, Steffen M., Tran, Eileen, Pollock, Jonathan, Tabatabaei, Ali, Contreras, Victor, Williams, Heather N., Pastuszka, Martha K., Sigler, John J., Pettazzoni, Piergiorgio, Rudolph, Markus G., Classen, Moritz, Brugger, Doris, Claiborne, Christopher, Plancher, Jean-Marc, Cuartas, Isabel, Seoane, Joan, Burgess, Laurence E., Abraham, Robert T., Weinstein, David S., Simon, Gabriel M., Patricelli, Matthew P., Kinsella, Todd M.
Published in Nature (London) (09.05.2024)
Published in Nature (London) (09.05.2024)
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Journal Article
Author Correction: Chemoproteomic discovery of a covalent allosteric inhibitor of WRN helicase
Baltgalvis, Kristen A., Lamb, Kelsey N., Symons, Kent T., Wu, Chu-Chiao, Hoffman, Melissa A., Snead, Aaron N., Song, Xiaodan, Glaza, Thomas, Kikuchi, Shota, Green, Jason C., Rogness, Donald C., Lam, Betty, Rodriguez-Aguirre, Maria E., Woody, David R., Eissler, Christie L., Rodiles, Socorro, Negron, Seth M., Bernard, Steffen M., Tran, Eileen, Pollock, Jonathan, Tabatabaei, Ali, Contreras, Victor, Williams, Heather N., Pastuszka, Martha K., Sigler, John J., Pettazzoni, Piergiorgio, Rudolph, Markus G., Classen, Moritz, Brugger, Doris, Claiborne, Christopher, Plancher, Jean-Marc, Cuartas, Isabel, Seoane, Joan, Burgess, Laurence E., Abraham, Robert T., Weinstein, David S., Simon, Gabriel M., Patricelli, Matthew P., Kinsella, Todd M.
Published in Nature (London) (18.07.2024)
Published in Nature (London) (18.07.2024)
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Journal Article
Structure–activity relationship study of central pyridine-derived TYK2 JH2 inhibitors: Optimization of the PK profile through C4′ and C6 variations
Xiao, Zili, Yang, Michael G., Liu, Chunjian, Sherwood, Trevor, Gilmore, John L., Lin, James, Li, Peng, Wu, Dauh-Rurng, Tokarski, John, Li, Sha, Cheng, Lihong, Xie, Chunshan, Fan, Jingsong, Dierks, Elizabeth, Strnad, Joann, Cvijic, Mary Ellen, Khan, Javed, Ruzanov, Max, Galella, Michael, Khandelwal, Purnima, Dyckman, Alaric J., Mathur, Arvind, Lombardo, Louis J., Macor, John E, Carter, Percy H., Aranibar, Nelly, Burke, James R., Weinstein, David S.
Published in Bioorganic & medicinal chemistry letters (15.07.2023)
Published in Bioorganic & medicinal chemistry letters (15.07.2023)
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Journal Article
Identification of Imidazo[1,2‑b]pyridazine Derivatives as Potent, Selective, and Orally Active Tyk2 JH2 Inhibitors
Liu, Chunjian, Lin, James, Moslin, Ryan, Tokarski, John S, Muckelbauer, Jodi, Chang, ChiehYing, Tredup, Jeffrey, Xie, Dianlin, Park, Hyunsoo, Li, Peng, Wu, Dauh-Rurng, Strnad, Joann, Zupa-Fernandez, Adriana, Cheng, Lihong, Chaudhry, Charu, Chen, Jing, Chen, Cliff, Sun, Huadong, Elzinga, Paul, D’arienzo, Celia, Gillooly, Kathleen, Taylor, Tracy L, McIntyre, Kim W, Salter-Cid, Luisa, Lombardo, Louis J, Carter, Percy H, Aranibar, Nelly, Burke, James R, Weinstein, David S
Published in ACS medicinal chemistry letters (14.03.2019)
Published in ACS medicinal chemistry letters (14.03.2019)
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Journal Article
Discovery of acylurea isosteres of 2-acylaminothiadiazole in the azaxanthene series of glucocorticoid receptor agonists
Gong, Hua, Yang, Michael, Xiao, Zili, Doweyko, Arthur M., Cunningham, Mark, Wang, Jinhong, Habte, Sium, Holloway, Deborah, Burke, Christine, Shuster, David, Gao, Ling, Carman, Julie, Somerville, John E., Nadler, Steven G., Salter-Cid, Luisa, Barrish, Joel C., Weinstein, David S.
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
Published in Bioorganic & medicinal chemistry letters (01.08.2014)
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Journal Article
Improving the Pharmacokinetic and CYP Inhibition Profiles of Azaxanthene-Based Glucocorticoid Receptor ModulatorsIdentification of (S)‑5-(2-(9-Fluoro-2-(4-(2-hydroxypropan-2-yl)phenyl)‑5H‑chromeno[2,3‑b]pyridin-5-yl)-2-methylpropanamido)‑N‑(tetrahydro‑2H‑pyran-4-yl)-1,3,4-thiadiazole-2-carboxamide (BMS-341)
Yang, Michael G, Dhar, T. G. Murali, Xiao, Zili, Xiao, Hai-Yun, Duan, James J.-W, Jiang, Bin, Galella, Michael A, Cunningham, Mark, Wang, Jinhong, Habte, Sium, Shuster, David, McIntyre, Kim W, Carman, Julie, Holloway, Deborah A, Somerville, John E, Nadler, Steven G, Salter-Cid, Luisa, Barrish, Joel C, Weinstein, David S
Published in Journal of medicinal chemistry (28.05.2015)
Published in Journal of medicinal chemistry (28.05.2015)
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Journal Article
Dimethyl-diphenyl-propanamide Derivatives As Nonsteroidal Dissociated Glucocorticoid Receptor Agonists
Yang, Bingwei V, Weinstein, David S, Doweyko, Lidia M, Gong, Hua, Vaccaro, Wayne, Huynh, Tram, Xiao, Hai-yun, Doweyko, Arthur M, Mckay, Lorraine, Holloway, Deborah A, Somerville, John E, Habte, Sium, Cunningham, Mark, McMahon, Michele, Townsend, Robert, Shuster, David, Dodd, John H, Nadler, Steven G, Barrish, Joel C
Published in Journal of medicinal chemistry (09.12.2010)
Published in Journal of medicinal chemistry (09.12.2010)
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Journal Article
Pyrazole-based sulfonamide and sulfamides as potent inhibitors of mammalian 15-lipoxygenase
Ngu, Khehyong, Weinstein, David S., Liu, Wen, Langevine, Charles, Combs, Donald W., Zhuang, Shaobin, Chen, Xing, Madsen, Cort S., Harper, Timothy W., Ahmad, Saleem, Robl, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.07.2011)
Published in Bioorganic & medicinal chemistry letters (15.07.2011)
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Journal Article
Novel two-step, one-pot synthesis of primary acylureas
Xiao, Zili, Yang, Michael G., Tebben, Andrew J., Galella, Michael A., Weinstein, David S.
Published in Tetrahedron letters (03.11.2010)
Published in Tetrahedron letters (03.11.2010)
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Journal Article
Discovery of selective imidazole-based inhibitors of mammalian 15-lipoxygenase: Highly potent against human enzyme within a cellular environment
Weinstein, David S., Liu, Wen, Ngu, Khehyong, Langevine, Charles, Combs, Donald W., Zhuang, Shaobin, Chen, Cindy, Madsen, Cort S., Harper, Timothy W., Robl, Jeffrey A.
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
Published in Bioorganic & medicinal chemistry letters (15.09.2007)
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