Targeting the AAA ATPase p97 as an Approach to Treat Cancer through Disruption of Protein Homeostasis
Anderson, Daniel J., Le Moigne, Ronan, Djakovic, Stevan, Kumar, Brajesh, Rice, Julie, Wong, Steve, Wang, Jinhai, Yao, Bing, Valle, Eduardo, Kiss von Soly, Szerenke, Madriaga, Antonett, Soriano, Ferdie, Menon, Mary-Kamala, Wu, Zhi Yong, Kampmann, Martin, Chen, Yuwen, Weissman, Jonathan S., Aftab, Blake T., Yakes, F. Michael, Shawver, Laura, Zhou, Han-Jie, Wustrow, David, Rolfe, Mark
Published in Cancer cell (09.11.2015)
Published in Cancer cell (09.11.2015)
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Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083)
Zhou, Han-Jie, Wang, Jinhai, Yao, Bing, Wong, Steve, Djakovic, Stevan, Kumar, Brajesh, Rice, Julie, Valle, Eduardo, Soriano, Ferdie, Menon, Mary-Kamala, Madriaga, Antonett, Kiss von Soly, Szerenke, Kumar, Abhinav, Parlati, Francesco, Yakes, F. Michael, Shawver, Laura, Le Moigne, Ronan, Anderson, Daniel J, Rolfe, Mark, Wustrow, David
Published in Journal of medicinal chemistry (24.12.2015)
Published in Journal of medicinal chemistry (24.12.2015)
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Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity
Leger, Paul R, Hu, Dennis X, Biannic, Berenger, Bui, Minna, Han, Xinping, Karbarz, Emily, Maung, Jack, Okano, Akinori, Osipov, Maksim, Shibuya, Grant M, Young, Kyle, Higgs, Christopher, Abraham, Betty, Bradford, Delia, Cho, Cynthia, Colas, Christophe, Jacobson, Scott, Ohol, Yamini M, Pookot, Deepa, Rana, Payal, Sanchez, Jerick, Shah, Niket, Sun, Michael, Wong, Steve, Brockstedt, Dirk G, Kassner, Paul D, Schwarz, Jacob B, Wustrow, David J
Published in Journal of medicinal chemistry (28.05.2020)
Published in Journal of medicinal chemistry (28.05.2020)
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Journal Article
The p97 Inhibitor CB-5083 Is a Unique Disrupter of Protein Homeostasis in Models of Multiple Myeloma
Le Moigne, Ronan, Aftab, Blake T, Djakovic, Stevan, Dhimolea, Eugen, Valle, Eduardo, Murnane, Megan, King, Emily M, Soriano, Ferdie, Menon, Mary-Kamala, Wu, Zhi Yong, Wong, Stephen T, Lee, Grace J, Yao, Bing, Wiita, Arun P, Lam, Christine, Rice, Julie, Wang, Jinhai, Chesi, Marta, Bergsagel, P Leif, Kraus, Marianne, Driessen, Christoph, Kiss von Soly, Szerenke, Yakes, F Michael, Wustrow, David, Shawver, Laura, Zhou, Han-Jie, Martin, 3rd, Thomas G, Wolf, Jeffrey L, Mitsiades, Constantine S, Anderson, Daniel J, Rolfe, Mark
Published in Molecular cancer therapeutics (01.11.2017)
Published in Molecular cancer therapeutics (01.11.2017)
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Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors
Robles, Omar, Jackson, Jeffrey J, Marshall, Lisa, Talay, Oezcan, Chian, David, Cutler, Gene, Diokno, Raymond, Hu, Dennis X, Jacobson, Scott, Karbarz, Emily, Kassner, Paul D, Ketcham, John M, McKinnell, Jenny, Meleza, Cesar, Reilly, Maureen K, Riegler, Erin, Shunatona, Hunter P, Wadsworth, Angela, Younai, Ashkaan, Brockstedt, Dirk G, Wustrow, David J, Zibinsky, Mikhail
Published in Journal of medicinal chemistry (13.08.2020)
Published in Journal of medicinal chemistry (13.08.2020)
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EBV+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22
Jorapur, Aparna, Marshall, Lisa A, Jacobson, Scott, Xu, Mengshu, Marubayashi, Sachie, Zibinsky, Mikhail, Hu, Dennis X, Robles, Omar, Jackson, Jeffrey J, Baloche, Valentin, Busson, Pierre, Wustrow, David, Brockstedt, Dirk G, Talay, Oezcan, Kassner, Paul D, Cutler, Gene
Published in PLoS pathogens (01.01.2022)
Published in PLoS pathogens (01.01.2022)
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Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy
Jackson, Jeffrey J., Shibuya, Grant M., Ravishankar, Buvana, Adusumilli, Lavanya, Bradford, Delia, Brockstedt, Dirk G., Bucher, Cyril, Bui, Minna, Cho, Cynthia, Colas, Christoph, Cutler, Gene, Dukes, Adrian, Han, Xinping, Hu, Dennis X., Jacobson, Scott, Kassner, Paul D., Katibah, George E., Ko, Michelle Yoo Min, Kolhatkar, Urvi, Leger, Paul R., Ma, Anqi, Marshall, Lisa, Maung, Jack, Ng, Andrew A., Okano, Akinori, Pookot, Deepa, Poon, Daniel, Ramana, Chandru, Reilly, Maureen K., Robles, Omar, Schwarz, Jacob B., Shakhmin, Anton A., Shunatona, Hunter P., Sreenivasan, Raashi, Tivitmahaisoon, Parcharee, Xu, Mengshu, Zaw, Thant, Wustrow, David J., Zibinsky, Mikhail
Published in Journal of medicinal chemistry (13.10.2022)
Published in Journal of medicinal chemistry (13.10.2022)
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Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment
Jackson, Jeffrey J, Ketcham, John M, Younai, Ashkaan, Abraham, Betty, Biannic, Berenger, Beck, Hilary P, Bui, Minna H. T, Chian, David, Cutler, Gene, Diokno, Raymond, Hu, Dennis X, Jacobson, Scott, Karbarz, Emily, Kassner, Paul D, Marshall, Lisa, McKinnell, Jenny, Meleza, Cesar, Okal, Abood, Pookot, Deepa, Reilly, Maureen K, Robles, Omar, Shunatona, Hunter P, Talay, Oezcan, Walker, James R, Wadsworth, Angela, Wustrow, David J, Zibinsky, Mikhail
Published in Journal of medicinal chemistry (11.07.2019)
Published in Journal of medicinal chemistry (11.07.2019)
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Journal Article
Discovery of a Potent and Selective CCR4 Antagonist That Inhibits T-reg Trafficking into the Tumor Microenvironment
Jackson, Jeffrey J., Ketcham, John M., Younai, Ashkaan, Abraham, Betty, Biannic, Berenger, Beck, Hilary P., Bui, Minna H. T., Chian, David, Cutler, Gene, Diokno, Raymond, Hu, Dennis X., Jacobson, Scott, Karbarz, Emily, Kassner, Paul D., Marshall, Lisa, McKinnell, Jenny, Meleza, Cesar, Okal, Abood, Pookot, Deepa, Reilly, Maureen K., Robles, Omar, Shunatona, Hunter P., Talay, Oezcan, Walker, James R., Wadsworth, Angela, Wustrow, David J., Zibinsky, Mikhail
Published in Journal of medicinal chemistry (11.07.2019)
Published in Journal of medicinal chemistry (11.07.2019)
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Characterization of N-(Adamantan-1-ylmethyl)-5-[(3R-aminopyrrolidin-1-yl)methyl]-2-chloro-benzamide, a P2X7 Antagonist in Animal Models of Pain and Inflammation
Broom, Daniel C, Matson, David J, Bradshaw, Elizabeth, Buck, Marianne E, Meade, Robin, Coombs, Susan, Matchett, Michele, Ford, Kristen K, Yu, Weifeng, Yuan, Jun, Sun, Synthia H, Ochoa, Ricardo, Krause, James E, Wustrow, David J, Cortright, Daniel N
Published in The Journal of pharmacology and experimental therapeutics (01.12.2008)
Published in The Journal of pharmacology and experimental therapeutics (01.12.2008)
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Structure−Activity Relationships of Pregabalin and Analogues That Target the α2-δ Protein
Belliotti, Thomas R, Capiris, Thomas, Ekhato, I. Victor, Kinsora, Jack J, Field, Mark J, Heffner, Thomas G, Meltzer, Leonard T, Schwarz, Jacob B, Taylor, Charles P, Thorpe, Andrew J, Vartanian, Mark G, Wise, Lawrence D, Zhi-Su, Ti, Weber, Mark L, Wustrow, David J
Published in Journal of medicinal chemistry (07.04.2005)
Published in Journal of medicinal chemistry (07.04.2005)
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Discovery of a novel potent GABA(B) receptor agonist
Xu, Feng, Peng, Ge, Phan, Thu, Dilip, Usha, Chen, Jian Lu, Chernov-Rogan, Tania, Zhang, Xuexiang, Grindstaff, Kent, Annamalai, Thamil, Koller, Kerry, Gallop, Mark A, Wustrow, David J
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
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Journal Article
Discovery of a novel potent GABAB receptor agonist
Xu, Feng, Peng, Ge, Phan, Thu, Dilip, Usha, Chen, Jian Lu, Chernov-Rogan, Tania, Zhang, Xuexiang, Grindstaff, Kent, Annamalai, Thamil, Koller, Kerry, Gallop, Mark A, Wustrow, David J
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
Published in Bioorganic & medicinal chemistry letters (01.11.2011)
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Journal Article
Tumors establish resistance to immunotherapy by regulating Treg recruitment via CCR4
Marshall, Lisa A, Marubayashi, Sachie, Jorapur, Aparna, Jacobson, Scott, Zibinsky, Mikhail, Robles, Omar, Hu, Dennis Xiaozhou, Jackson, Jeffrey J, Pookot, Deepa, Sanchez, Jerick, Brovarney, Martin, Wadsworth, Angela, Chian, David, Wustrow, David, Kassner, Paul D, Cutler, Gene, Wong, Brian, Brockstedt, Dirk G, Talay, Oezcan
Published in Journal for immunotherapy of cancer (26.11.2020)
Published in Journal for immunotherapy of cancer (26.11.2020)
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Oxadiazolone bioisosteres of pregabalin and gabapentin
Wustrow, David J., Belliotti, Thomas R., Capiris, Thomas, Kneen, Clare O., Bryans, Justin S., Field, Mark J., Williams, Dic, El-Kattan, Ayman, Buchholz, Lisa, Kinsora, Jack J., Lotarski, Susan M., Vartanian, Mark G., Taylor, Charles P., Donevan, Sean D., Thorpe, Andrew J., Schwarz, Jacob B.
Published in Bioorganic & medicinal chemistry letters (2009)
Published in Bioorganic & medicinal chemistry letters (2009)
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Novel Cyclopropyl β-Amino Acid Analogues of Pregabalin and Gabapentin That Target the α2-δ Protein
Schwarz, Jacob B, Gibbons, Sian E, Graham, Shelley R, Colbry, Norman L, Guzzo, Peter R, Le, Van-Duc, Vartanian, Mark G, Kinsora, Jack J, Lotarski, Susan M, Li, Zheng, Dickerson, Melvin R, Su, Ti-Zhi, Weber, Mark L, El-Kattan, Ayman, Thorpe, Andrew J, Donevan, Sean D, Taylor, Charles P, Wustrow, David J
Published in Journal of medicinal chemistry (21.04.2005)
Published in Journal of medicinal chemistry (21.04.2005)
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Journal Article
1-Benzylbenzimidazoles : The discovery of a novel series of bradykinin B1 receptor antagonists
QIN GUO, CHANDRASEKHAR, Jayaraman, BROOM, Daniel, KERSHAW, Mark T, SIMMERMACHER-MAYER, Jean, YAO PENG, HODGETTS, Kevin J, IHLE, David, WUSTROW, David J, CHENARD, Bertrand L, KRAUSE, James E, HUTCHISON, Alan, ALDERMAN, Dawn, CHENG, Charles, CORTRIGHT, Daniel
Published in Bioorganic & medicinal chemistry letters (15.09.2008)
Published in Bioorganic & medicinal chemistry letters (15.09.2008)
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The design and synthesis of human branched-chain amino acid aminotransferase inhibitors for treatment of neurodegenerative diseases
Hu, Lain-Yen, Boxer, Peter A., Kesten, Suzanne R., Lei, Huangshu J., Wustrow, David J., Moreland, David W., Zhang, Liming, Ahn, Kay, Ryder, Todd R., Liu, Xiaohong, Rubin, John R., Fahnoe, Kelly, Carroll, Richard T., Dutta, Satavisha, Fahnoe, Douglass C., Probert, Albert W., Roof, Robin L., Rafferty, Michael F., Kostlan, Catherine R., Scholten, Jeffrey D., Hood, Molly, Ren, Xiao-Dan, Schielke, Gerald P., Su, Ti-Zhi, Taylor, Charles P., Mistry, Anil, McConnell, Patrick, Hasemann, Charles, Ohren, Jeffrey
Published in Bioorganic & medicinal chemistry letters (01.05.2006)
Published in Bioorganic & medicinal chemistry letters (01.05.2006)
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Journal Article
Aminopyrazine CB1 receptor inverse agonists
Wustrow, David J., Maynard, George D., Yuan, Jun, Zhao, He, Mao, Jianmin, Guo, Qin, Kershaw, Mark, Hammer, Jack, Brodbeck, Robbin M., Near, Kristen E., Zhou, Dan, Beers, David S., Chenard, Bertrand L., Krause, James E., Hutchison, Alan J.
Published in Bioorganic & medicinal chemistry (01.06.2008)
Published in Bioorganic & medicinal chemistry (01.06.2008)
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