An inhibitor of KDM5 demethylases reduces survival of drug-tolerant cancer cells
Vinogradova, Maia, Gehling, Victor S, Gustafson, Amy, Arora, Shilpi, Tindell, Charles A, Wilson, Catherine, Williamson, Kaylyn E, Guler, Gulfem D, Gangurde, Pranoti, Manieri, Wanda, Busby, Jennifer, Flynn, E Megan, Lan, Fei, Kim, Hyo-jin, Odate, Shobu, Cochran, Andrea G, Liu, Yichin, Wongchenko, Matthew, Yang, Yibin, Cheung, Tommy K, Maile, Tobias M, Lau, Ted, Costa, Michael, Hegde, Ganapati V, Jackson, Erica, Pitti, Robert, Arnott, David, Bailey, Christopher, Bellon, Steve, Cummings, Richard T, Albrecht, Brian K, Harmange, Jean-Christophe, Kiefer, James R, Trojer, Patrick, Classon, Marie
Published in Nature chemical biology (01.07.2016)
Published in Nature chemical biology (01.07.2016)
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Structural basis for dual-mode inhibition of the ABC transporter MsbA
Ho, Hoangdung, Miu, Anh, Alexander, Mary Kate, Garcia, Natalie K., Oh, Angela, Zilberleyb, Inna, Reichelt, Mike, Austin, Cary D., Tam, Christine, Shriver, Stephanie, Hu, Huiyong, Labadie, Sharada S., Liang, Jun, Wang, Lan, Wang, Jian, Lu, Yan, Purkey, Hans E., Quinn, John, Franke, Yvonne, Clark, Kevin, Beresini, Maureen H., Tan, Man-Wah, Sellers, Benjamin D., Maurer, Till, Koehler, Michael F. T., Wecksler, Aaron T., Kiefer, James R., Verma, Vishal, Xu, Yiming, Nishiyama, Mireille, Payandeh, Jian, Koth, Christopher M.
Published in Nature (London) (01.05.2018)
Published in Nature (London) (01.05.2018)
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Molecular Basis for Cyclooxygenase Inhibition by the Non-steroidal Anti-inflammatory Drug Naproxen
Duggan, Kelsey C., Walters, Matthew J., Musee, Joel, Harp, Joel M., Kiefer, James R., Oates, John A., Marnett, Lawrence J.
Published in The Journal of biological chemistry (05.11.2010)
Published in The Journal of biological chemistry (05.11.2010)
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The novel benzopyran class of selective cyclooxygenase-2 inhibitors. Part 2: The second clinical candidate having a shorter and favorable human half-life
Wang, Jane L., Limburg, David, Graneto, Matthew J., Springer, John, Hamper, Joseph Rogier Bruce, Liao, Subo, Pawlitz, Jennifer L., Kurumbail, Ravi G., Maziasz, Timothy, Talley, John J., Kiefer, James R., Carter, Jeffery
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300
Crawford, Terry D, Romero, F. Anthony, Lai, Kwong Wah, Tsui, Vickie, Taylor, Alexander M, de Leon Boenig, Gladys, Noland, Cameron L, Murray, Jeremy, Ly, Justin, Choo, Edna F, Hunsaker, Thomas L, Chan, Emily W, Merchant, Mark, Kharbanda, Samir, Gascoigne, Karen E, Kaufman, Susan, Beresini, Maureen H, Liao, Jiangpeng, Liu, Wenfeng, Chen, Kevin X, Chen, Zhongguo, Conery, Andrew R, Côté, Alexandre, Jayaram, Hariharan, Jiang, Ying, Kiefer, James R, Kleinheinz, Tracy, Li, Yingjie, Maher, Jonathan, Pardo, Eneida, Poy, Florence, Spillane, Kerry L, Wang, Fei, Wang, Jian, Wei, Xiaocang, Xu, Zhaowu, Xu, Zhongya, Yen, Ivana, Zawadzke, Laura, Zhu, Xiaoyu, Bellon, Steven, Cummings, Richard, Cochran, Andrea G, Albrecht, Brian K, Magnuson, Steven
Published in Journal of medicinal chemistry (08.12.2016)
Published in Journal of medicinal chemistry (08.12.2016)
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Structure of mammalian poly(ADP-ribose) glycohydrolase reveals a flexible tyrosine clasp as a substrate-binding element
Kim, In-Kwon, Kiefer, James R, Ho, Chris M W, Stegeman, Roderick A, Classen, Scott, Tainer, John A, Ellenberger, Tom
Published in Nature structural & molecular biology (01.06.2012)
Published in Nature structural & molecular biology (01.06.2012)
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Inhibition of bromodomain-containing protein 9 for the prevention of epigenetically-defined drug resistance
Crawford, Terry D., Vartanian, Steffan, Côté, Alexandre, Bellon, Steve, Duplessis, Martin, Flynn, E. Megan, Hewitt, Michael, Huang, Hon-Ren, Kiefer, James R., Murray, Jeremy, Nasveschuk, Christopher G., Pardo, Eneida, Romero, F. Anthony, Sandy, Peter, Tang, Yong, Taylor, Alexander M., Tsui, Vickie, Wang, Jian, Wang, Shumei, Zawadzke, Laura, Albrecht, Brian K., Magnuson, Steven R., Cochran, Andrea G., Stokoe, David
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
Published in Bioorganic & medicinal chemistry letters (01.08.2017)
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Journal Article
Fragment-Based Discovery of a Selective and Cell-Active Benzodiazepinone CBP/EP300 Bromodomain Inhibitor (CPI-637)
Taylor, Alexander M, Côté, Alexandre, Hewitt, Michael C, Pastor, Richard, Leblanc, Yves, Nasveschuk, Christopher G, Romero, F. Anthony, Crawford, Terry D, Cantone, Nico, Jayaram, Hariharan, Setser, Jeremy, Murray, Jeremy, Beresini, Maureen H, de Leon Boenig, Gladys, Chen, Zhongguo, Conery, Andrew R, Cummings, Richard T, Dakin, Leslie A, Flynn, E. Megan, Huang, Oscar W, Kaufman, Susan, Keller, Patricia J, Kiefer, James R, Lai, Tommy, Li, Yingjie, Liao, Jiangpeng, Liu, Wenfeng, Lu, Henry, Pardo, Eneida, Tsui, Vickie, Wang, Jian, Wang, Yongyun, Xu, Zhaowu, Yan, Fen, Yu, Dong, Zawadzke, Laura, Zhu, Xiaoqin, Zhu, Xiaoyu, Sims, Robert J, Cochran, Andrea G, Bellon, Steve, Audia, James E, Magnuson, Steven, Albrecht, Brian K
Published in ACS medicinal chemistry letters (12.05.2016)
Published in ACS medicinal chemistry letters (12.05.2016)
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Lead optimization of a pyrazolo[1,5-a]pyrimidin-7(4H)-one scaffold to identify potent, selective and orally bioavailable KDM5 inhibitors suitable for in vivo biological studies
Liang, Jun, Zhang, Birong, Labadie, Sharada, Ortwine, Daniel F., Vinogradova, Maia, Kiefer, James R., Gehling, Victor S., Harmange, Jean-Christophe, Cummings, Richard, Lai, Tommy, Liao, Jiangpeng, Zheng, Xiaoping, Liu, Yichin, Gustafson, Amy, Van der Porten, Erica, Mao, Weifeng, Liederer, Bianca M., Deshmukh, Gauri, Classon, Marie, Trojer, Patrick, Dragovich, Peter S., Murray, Lesley
Published in Bioorganic & medicinal chemistry letters (15.08.2016)
Published in Bioorganic & medicinal chemistry letters (15.08.2016)
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A Novel Mechanism of Cyclooxygenase-2 Inhibition Involving Interactions with Ser-530 and Tyr-385
Rowlinson, Scott W., Kiefer, James R., Prusakiewicz, Jeffery J., Pawlitz, Jennifer L., Kozak, Kevin R., Kalgutkar, Amit S., Stallings, William C., Kurumbail, Ravi G., Marnett, Lawrence J.
Published in The Journal of biological chemistry (14.11.2003)
Published in The Journal of biological chemistry (14.11.2003)
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Visualizing DNA replication in a catalytically active Bacillus DNA polymerase crystal
Beese, Lorena S, Kiefer, James R, Mao, Chen, Braman, Jeffrey C
Published in Nature (London) (15.01.1998)
Published in Nature (London) (15.01.1998)
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The novel benzopyran class of selective cyclooxygenase-2 inhibitors-part I: The first clinical candidate
Wang, Jane L., Carter, Jeffery, Kiefer, James R., Kurumbail, Ravi G., Pawlitz, Jennifer L., Brown, David, Hartmann, Susan J., Graneto, Matthew J., Seibert, Karen, Talley, John J.
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
Published in Bioorganic & medicinal chemistry letters (01.12.2010)
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High Resolution Crystal Structure of the Catalytic Domain of ADAMTS-5 (Aggrecanase-2)
Shieh, Huey-Sheng, Mathis, Karl J., Williams, Jennifer M., Hills, Robert L., Wiese, Joe F., Benson, Timothy E., Kiefer, James R., Marino, Margaret H., Carroll, Jeffery N., Leone, Joseph W., Malfait, Anne-Marie, Arner, Elizabeth C., Tortorella, Micky D., Tomasselli, Alfredo
Published in The Journal of biological chemistry (18.01.2008)
Published in The Journal of biological chemistry (18.01.2008)
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Investigation of the binding pocket of human hematopoietic prostaglandin (PG) D2 synthase (hH-PGDS): A tale of two waters
Trujillo, John I., Kiefer, James R., Huang, Wei, Day, Jacqueline E., Moon, Joseph, Jerome, Gina M., Bono, Christine P., Kornmeier, Christine M., Williams, Melanie L., Kuhn, Cyrille, Rennie, Glen R., Wynn, Thomas A., Carron, Christopher P., Thorarensen, Atli
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
Published in Bioorganic & medicinal chemistry letters (01.06.2012)
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Observing Translesion Synthesis of an Aromatic Amine DNA Adduct by a High-fidelity DNA Polymerase
Hsu, Gerald W., Kiefer, James R., Burnouf, Dominique, Becherel, Olivier J., Fuchs, Robert P.P., Beese, Lorena S.
Published in The Journal of biological chemistry (26.11.2004)
Published in The Journal of biological chemistry (26.11.2004)
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GDC-9545 (Giredestrant): A Potent and Orally Bioavailable Selective Estrogen Receptor Antagonist and Degrader with an Exceptional Preclinical Profile for ER+ Breast Cancer
Liang, Jun, Zbieg, Jason R., Blake, Robert A., Chang, Jae H., Daly, Stephen, DiPasquale, Antonio G., Friedman, Lori S., Gelzleichter, Thomas, Gill, Matthew, Giltnane, Jennifer M., Goodacre, Simon, Guan, Jane, Hartman, Steven J., Ingalla, Ellen Rei, Kategaya, Lorn, Kiefer, James R., Kleinheinz, Tracy, Labadie, Sharada S., Lai, Tommy, Li, Jun, Liao, Jiangpeng, Liu, Zhiguo, Mody, Vidhi, McLean, Neville, Metcalfe, Ciara, Nannini, Michelle A., Oeh, Jason, O’Rourke, Martin G., Ortwine, Daniel F., Ran, Yingqing, Ray, Nicholas C., Roussel, Fabien, Sambrone, Amy, Sampath, Deepak, Schutt, Leah K., Vinogradova, Maia, Wai, John, Wang, Tao, Wertz, Ingrid E., White, Jonathan R., Yeap, Siew Kuen, Young, Amy, Zhang, Birong, Zheng, Xiaoping, Zhou, Wei, Zhong, Yu, Wang, Xiaojing
Published in Journal of medicinal chemistry (26.08.2021)
Published in Journal of medicinal chemistry (26.08.2021)
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Discovery of GDC-0077 (Inavolisib), a Highly Selective Inhibitor and Degrader of Mutant PI3Kα
Hanan, Emily J., Braun, Marie-Gabrielle, Heald, Robert A., MacLeod, Calum, Chan, Connie, Clausen, Saundra, Edgar, Kyle A., Eigenbrot, Charles, Elliott, Richard, Endres, Nicholas, Friedman, Lori S., Gogol, Emily, Gu, Xiao-Hui, Thibodeau, Rebecca Hong, Jackson, Philip S., Kiefer, James R., Knight, Jamie D., Nannini, Michelle, Narukulla, Raman, Pace, Amanda, Pang, Jodie, Purkey, Hans E., Salphati, Laurent, Sampath, Deepak, Schmidt, Stephen, Sideris, Steve, Song, Kyung, Sujatha-Bhaskar, Swathi, Ultsch, Mark, Wallweber, Heidi, Xin, Jianfeng, Yeap, SiewKuen, Young, Amy, Zhong, Yu, Staben, Steven T.
Published in Journal of medicinal chemistry (22.12.2022)
Published in Journal of medicinal chemistry (22.12.2022)
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Trastuzumab does not bind rat or mouse ErbB2/neu: implications for selection of non-clinical safety models for trastuzumab-based therapeutics
Lewis Phillips, Gail, Guo, Jun, Kiefer, James R., Proctor, William, Bumbaca Yadav, Daniela, Dybdal, Noel, Shen, Ben-Quan
Published in Breast cancer research and treatment (01.01.2022)
Published in Breast cancer research and treatment (01.01.2022)
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