PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer von Raina, Kanak, Lu, Jing, Qian, Yimin, Altieri, Martha, Gordon, Deborah, Rossi, Ann Marie K., Wang, Jing, Chen, Xin, Dong, Hanqing, Siu, Kam, Winkler, James D., Crew, Andrew P., Crews, Craig M., Coleman, Kevin G.

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Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1 von Crew, Andrew P, Raina, Kanak, Dong, Hanqing, Qian, Yimin, Wang, Jing, Vigil, Dominico, Serebrenik, Yevgeniy V, Hamman, Brian D, Morgan, Alicia, Ferraro, Caterina, Siu, Kam, Neklesa, Taavi K, Winkler, James D, Coleman, Kevin G, Crews, Craig M

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Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance von Salami, Jemilat, Alabi, Shanique, Willard, Ryan R., Vitale, Nick J., Wang, Jing, Dong, Hanqing, Jin, Meizhong, McDonnell, Donald P., Crew, Andrew P., Neklesa, Taavi K., Crews, Craig M.

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Preclinical characterization of OSI-027, a potent and selective inhibitor of mTORC1 and mTORC2: distinct from rapamycin von Bhagwat, Shripad V, Gokhale, Prafulla C, Crew, Andrew P, Cooke, Andy, Yao, Yan, Mantis, Christine, Kahler, Jennifer, Workman, Jennifer, Bittner, Mark, Dudkin, Lorina, Epstein, David M, Gibson, Neil W, Wild, Robert, Arnold, Lee D, Houghton, Peter J, Pachter, Jonathan A

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Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4 von Lu, Jing, Qian, Yimin, Altieri, Martha, Dong, Hanqing, Wang, Jing, Raina, Kanak, Hines, John, Winkler, James D., Crew, Andrew P., Coleman, Kevin, Crews, Craig M.

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A highly effective one-pot synthesis of quinolines from o-nitroarylcarbaldehydes von Li, An-Hu, Ahmed, Eilaf, Chen, Xin, Cox, Matthew, Crew, Andrew P, Dong, Han-Qing, Jin, Meizhong, Ma, Lifu, Panicker, Bijoy, Siu, Kam W, Steinig, Arno G, Stolz, Kathryn M, Tavares, Paula A R, Volk, Brian, Weng, Qinghua, Werner, Doug, Mulvihill, Mark J

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OSI-930 : A novel selective inhibitor of kit and kinase insert domain receptor tyrosine kinases with antitumor activity in mouse xenograft models von GARTON, Andrew J, CREW, Andrew P. A, BITTNER, Mark A, KEILY, John F, BRINER, Paul, HIDDEN, Chris, SREBERNAK, Mary C, PIRRIT, Carrie, O'CONNOR, Matthew, ANNA CHAN, VULEVIC, Bojana, HENNINGER, Dwight, FRANKLIN, Maryland, HART, Karen, SENNELLO, Regina, LI, An-Hu, TAO ZHANG, RICHARDSON, Frank, EMERSON, David L, CASTELHANO, Arlindo L, ARNOLD, Lee D, GIBSON, Neil W, COOKE, Andrew R, WYNNE, Graham M, CASTALDO, Linda, KAHLER, Jennifer, WINSKI, Shannon L, FRANKS, April, BROWN, Eric N

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The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study von Burslem, George M., Smith, Blake E., Lai, Ashton C., Jaime-Figueroa, Saul, McQuaid, Daniel C., Bondeson, Daniel P., Toure, Momar, Dong, Hanqing, Qian, Yimin, Wang, Jing, Crew, Andrew P., Hines, John, Crews, Craig M.

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Discovery of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1: Optimization of kinase selectivity and pharmacokinetics von Hornberger, Keith R., Chen, Xin, Crew, Andrew P., Kleinberg, Andrew, Ma, Lifu, Mulvihill, Mark J., Wang, Jing, Wilde, Victoria L., Albertella, Mark, Bittner, Mark, Cooke, Andrew, Kadhim, Salam, Kahler, Jennifer, Maresca, Paul, May, Earl, Meyn, Peter, Romashko, Darlene, Tokar, Brianna, Turton, Roy

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Palladium-Catalyzed Direct Heck Arylation of Dual π-Deficient/π-Excessive Heteroaromatics. Synthesis of C-5 Arylated Imidazo[1,5-a]pyrazines von Wang, Jian-Xin, McCubbin, J. Adam, Jin, Meizhong, Laufer, Radoslaw S, Mao, Yunyu, Crew, Andrew P, Mulvihill, Mark J, Snieckus, Victor

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Discovery of potent, selective and orally bioavailable imidazo[1,5-a]pyrazine derived ACK1 inhibitors von Jin, Meizhong, Wang, Jing, Kleinberg, Andrew, Kadalbajoo, Mridula, Siu, Kam W., Cooke, Andrew, Bittner, Mark A., Yao, Yan, Thelemann, April, Ji, Qunsheng, Bhagwat, Shripad, Mulvihill, Kristen M., Rechka, Josef A., Pachter, Jonathan A., Crew, Andrew P., Epstein, David, Mulvihill, Mark J.

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The Crystal Structure of a Constitutively Active Mutant RON Kinase Suggests an Intramolecular Autophosphorylation Hypothesis von Wang, Jing, Steinbacher, Stefan, Augustin, Martin, Schreiner, Patrick, Epstein, David, Mulvihill, Mark J, Crew, Andrew P

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Discovery and optimization of 7-aminofuro[2,3-c]pyridine inhibitors of TAK1 von Hornberger, Keith R., Berger, Dan M., Crew, Andrew P., Dong, Hanqing, Kleinberg, Andrew, Li, An-Hu, Medeiros, Matthew R., Mulvihill, Mark J., Siu, Kam, Tarrant, James, Wang, Jing, Weng, Felix, Wilde, Victoria L., Albertella, Mark, Bittner, Mark, Cooke, Andrew, Gray, Michael J., Maresca, Paul, May, Earl, Meyn, Peter, Peick, William, Romashko, Darlene, Tanowitz, Michael, Tokar, Brianna

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Imidazo[1,5- a]pyrazines: Orally efficacious inhibitors of mTORC1 and mTORC2 von Crew, Andrew P., Bhagwat, Shripad V., Dong, Hanqing, Bittner, Mark A., Chan, Anna, Chen, Xin, Coate, Heather, Cooke, Andrew, Gokhale, Prafulla C., Honda, Ayako, Jin, Meizhong, Kahler, Jennifer, Mantis, Christine, Mulvihill, Mark J., Tavares-Greco, Paula A., Volk, Brian, Wang, Jing, Werner, Douglas S., Arnold, Lee D., Pachter, Jonathan A., Wild, Robert, Gibson, Neil W.

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Synthesis of Substituted Imidazo[1,5-a]pyrazines via Mono-, Di-, and Directed Remote Metalation Strategies von Board, Johnathan, Wang, Jian-Xin, Crew, Andrew P, Jin, Meizhong, Foreman, Kenneth, Mulvihill, Mark J, Snieckus, Victor

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Novel BET protein proteolysis-targeting chimera exerts superior lethal activity than bromodomain inhibitor (BETi) against post-myeloproliferative neoplasm secondary (s) AML cells von Saenz, D T, Fiskus, W, Qian, Y, Manshouri, T, Rajapakshe, K, Raina, K, Coleman, K G, Crew, A P, Shen, A, Mill, C P, Sun, B, Qiu, P, Kadia, T M, Pemmaraju, N, DiNardo, C, Kim, M-S, Nowak, A J, Coarfa, C, Crews, C M, Verstovsek, S, Bhalla, K N

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Abstract 43: Discovery of ARV-110, a first in class androgen receptor degrading PROTAC for the treatment of men with metastatic castration resistant prostate cancer von Snyder, Lawrence B., Neklesa, Taavi K., Chen, Xin, Dong, Hanqing, Ferraro, Caterina, Gordon, Deborah A., Macaluso, Jennifer, Pizzano, Jennifer, Wang, Jing, Willard, Ryan R., Vitale, Nicholas, Peck, Ron, Moore, Marcia Dougan, Crews, Craig M., Houston, John, Crew, Andrew P., Taylor, Ian

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Abstract 44: The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer von Snyder, Lawrence B., Flanagan, John J., Qian, Yimin, Gough, Sheryl M., Andreoli, Monica, Bookbinder, Mark, Cadelina, Gregory, Bradley, John, Rousseau, Emma, Chandler, Julian, Willard, Ryan, Pizzano, Jennifer, Crews, Craig M., Crew, Andrew P., Houston, John, Moore, Marcia Dougan, Peck, Ron, Taylor, Ian

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ARV-110: An oral androgen receptor PROTAC degrader for prostate cancer von Neklesa, Taavi, Snyder, Lawrence B, Willard, Ryan R, Vitale, Nicholas, Pizzano, Jennifer, Gordon, Deborah A, Bookbinder, Mark, Macaluso, Jennifer, Dong, Hanqing, Ferraro, Caterina, Wang, Gan, Wang, Jing, Crews, Craig M, Houston, John, Crew, Andrew P, Taylor, Ian

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Abstract 5236: ARV-110: An androgen receptor PROTAC degrader for prostate cancer von Neklesa, Taavi, Snyder, Lawrence B., Willard, Ryan R., Vitale, Nicholas, Raina, Kanak, Pizzano, Jennifer, Gordon, Deborah, Bookbinder, Mark, Macaluso, Jennifer, Dong, Hanqing, Liu, Zheng, Ferraro, Caterina, Wang, Gan, Wang, Jing, Crews, Craig M., Houston, John, Crew, Andrew P., Taylor, Ian

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