Structure of the human Cereblon–DDB1–lenalidomide complex reveals basis for responsiveness to thalidomide analogs von Chamberlain, Philip P, Lopez-Girona, Antonia, Miller, Karen, Carmel, Gilles, Pagarigan, Barbra, Chie-Leon, Barbara, Rychak, Emily, Corral, Laura G, Ren, Yan J, Wang, Maria, Riley, Mariko, Delker, Silvia L, Ito, Takumi, Ando, Hideki, Mori, Tomoyuki, Hirano, Yoshinori, Handa, Hiroshi, Hakoshima, Toshio, Daniel, Thomas O, Cathers, Brian E

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A Cereblon Modulator (CC-220) with Improved Degradation of Ikaros and Aiolos von Matyskiela, Mary E, Zhang, Weihong, Man, Hon-Wah, Muller, George, Khambatta, Godrej, Baculi, Frans, Hickman, Matthew, LeBrun, Laurie, Pagarigan, Barbra, Carmel, Gilles, Lu, Chin-Chun, Lu, Gang, Riley, Mariko, Satoh, Yoshitaka, Schafer, Peter, Daniel, Thomas O, Carmichael, James, Cathers, Brian E, Chamberlain, Philip P

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A novel cereblon modulator recruits GSPT1 to the CRL4(CRBN) ubiquitin ligase von Matyskiela, Mary E, Lu, Gang, Ito, Takumi, Pagarigan, Barbra, Lu, Chin-Chun, Miller, Karen, Fang, Wei, Wang, Nai-Yu, Nguyen, Derek, Houston, Jack, Carmel, Gilles, Tran, Tam, Riley, Mariko, Nosaka, Lyn'Al, Lander, Gabriel C, Gaidarova, Svetlana, Xu, Shuichan, Ruchelman, Alexander L, Handa, Hiroshi, Carmichael, James, Daniel, Thomas O, Cathers, Brian E, Lopez-Girona, Antonia, Chamberlain, Philip P

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Lenalidomide induces ubiquitination and degradation of CK1α in del(5q) MDS von Krönke, Jan, Fink, Emma C., Hollenbach, Paul W., MacBeth, Kyle J., Hurst, Slater N., Udeshi, Namrata D., Chamberlain, Philip P., Mani, D. R., Man, Hon Wah, Gandhi, Anita K., Svinkina, Tanya, Schneider, Rebekka K., McConkey, Marie, Järås, Marcus, Griffiths, Elizabeth, Wetzler, Meir, Bullinger, Lars, Cathers, Brian E., Carr, Steven A., Chopra, Rajesh, Ebert, Benjamin L.

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CC-90009: A Cereblon E3 Ligase Modulating Drug That Promotes Selective Degradation of GSPT1 for the Treatment of Acute Myeloid Leukemia von Hansen, Joshua D, Correa, Matthew, Alexander, Matt, Nagy, Mark, Huang, Dehua, Sapienza, John, Lu, Gang, LeBrun, Laurie A, Cathers, Brian E, Zhang, Weihong, Tang, Yang, Ammirante, Massimo, Narla, Rama K, Piccotti, Joseph R, Pourdehnad, Michael, Lopez-Girona, Antonia

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p97/VCP promotes degradation of CRBN substrate glutamine synthetase and neosubstrates von Van Nguyen, Thang, Li, Jing, Lu, Chin-Chun (Jean), Mamrosh, Jennifer L., Lu, Gang, Cathers, Brian E., Deshaies, Raymond J.

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Discovery of CRBN E3 Ligase Modulator CC-92480 for the Treatment of Relapsed and Refractory Multiple Myeloma von Hansen, Joshua D, Correa, Matthew, Nagy, Mark A, Alexander, Matt, Plantevin, Veronique, Grant, Virginia, Whitefield, Brandon, Huang, Dehua, Kercher, Timothy, Harris, Roy, Narla, Rama Krishna, Leisten, Jim, Tang, Yang, Moghaddam, Mehran, Ebinger, Katalin, Piccotti, Joseph, Havens, Courtney G, Cathers, Brian, Carmichael, James, Daniel, Thomas, Vessey, Rupert, Hamann, Lawrence G, Leftheris, Katerina, Mendy, Derek, Baculi, Frans, LeBrun, Laurie A, Khambatta, Gody, Lopez-Girona, Antonia

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CC-90009, a novel cereblon E3 ligase modulator, targets acute myeloid leukemia blasts and leukemia stem cells von Surka, Christine, Jin, Liqing, Mbong, Nathan, Lu, Chin-Chun, Jang, In Sock, Rychak, Emily, Mendy, Derek, Clayton, Thomas, Tindall, Elizabeth, Hsu, Christy, Fontanillo, Celia, Tran, Eileen, Contreras, Adrian, Ng, Stanley W.K., Matyskiela, Mary, Wang, Kai, Chamberlain, Philip, Cathers, Brian, Carmichael, James, Hansen, Joshua, Wang, Jean C.Y., Minden, Mark D., Fan, Jinhong, Pierce, Daniel W., Pourdehnad, Michael, Rolfe, Mark, Lopez-Girona, Antonia, Dick, John E., Lu, Gang

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Cereblon modulators: Low molecular weight inducers of protein degradation von Chamberlain, Philip P., Cathers, Brian E.

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Measuring cereblon as a biomarker of response or resistance to lenalidomide and pomalidomide requires use of standardized reagents and understanding of gene complexity von Gandhi, Anita K., Mendy, Derek, Waldman, Michelle, Chen, Gengxin, Rychak, Emily, Miller, Karen, Gaidarova, Svetlana, Ren, Yan, Wang, Maria, Breider, Michael, Carmel, Gilles, Mahmoudi, Afshin, Jackson, Pilgrim, Abbasian, Mahan, Cathers, Brian E., Schafer, Peter H., Daniel, Tom O., Lopez‐Girona, Antonia, Thakurta, Anjan, Chopra, Rajesh

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Increased hemoglobin affinity for oxygen with GBT1118 improves hypoxia tolerance in sickle cell mice von Dufu, Kobina, Williams, Alexander T., Muller, Cynthia R., Walser, Cynthia M., Lucas, Alfredo, Eaker, Allyn M., Alt, Carsten, Cathers, Brian E., Oksenberg, Donna, Cabrales, Pedro

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GBT021601 improves red blood cell health and the pathophysiology of sickle cell disease in a murine model von Dufu, Kobina, Alt, Carsten, Strutt, Steven, Partridge, James, Tang, Tzechiang, Siu, Vincent, Liao‐Zou, Hilary, Rademacher, Peter, Williams, Alexander T., Muller, Cynthia R., Geng, Xin, Pochron, Mira Patel, Dang, Annie Nguyen, Cabrales, Pedro, Li, Zhe, Oksenberg, Donna, Cathers, Brian E.

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Pomalidomide in combination with dexamethasone results in synergistic anti‐tumour responses in pre‐clinical models of lenalidomide‐resistant multiple myeloma von Rychak, Emily, Mendy, Derek, Shi, Tao, Ning, Yuhong, Leisten, Jim, Lu, Ling, Miller, Karen, Narla, Rama K., Orlowski, Robert Z., Raymon, Heather K., Bjorklund, Chad C., Thakurta, Anjan, Gandhi, Anita K., Cathers, Brian E., Chopra, Rajesh, Daniel, Thomas O., Lopez‐Girona, Antonia

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UBE2G1 governs the destruction of cereblon neomorphic substrates von Lu, Gang, Weng, Stephanie, Matyskiela, Mary, Zheng, Xinde, Fang, Wei, Wood, Scott, Surka, Christine, Mizukoshi, Reina, Lu, Chin-Chun, Mendy, Derek, Jang, In Sock, Wang, Kai, Marella, Mathieu, Couto, Suzana, Cathers, Brian, Carmichael, James, Chamberlain, Philip, Rolfe, Mark

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Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005 von Papa, Patrick, Whitefield, Brandon, Mortensen, Deborah S, Cashion, Dan, Huang, Dehua, Torres, Eduardo, Parnes, Jason, Sapienza, John, Hansen, Joshua, Correa, Matthew, Delgado, Mercedes, Harris, Roy, Hegde, Sayee, Norris, Stephen, Bahmanyar, Sogole, Plantevin-Krenitsky, Veronique, Liu, Zheng, Leftheris, Katerina, Kulkarni, Ashutosh, Bennett, Brydon, Hur, Eun Mi, Ringheim, Garth, Khambatta, Godrej, Chan, Henry, Muir, Jeffrey, Blease, Kate, Burnett, Kelven, LeBrun, Laurie, Morrison, Lisa, Celeridad, Maria, Khattri, Roli, Cathers, Brian E

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CC-223, a Potent and Selective Inhibitor of mTOR Kinase: In Vitro and In Vivo Characterization von Mortensen, Deborah S, Fultz, Kimberly E, Xu, Shuichan, Xu, Weiming, Packard, Garrick, Khambatta, Godrej, Gamez, James C, Leisten, Jim, Zhao, Jingjing, Apuy, Julius, Ghoreishi, Kamran, Hickman, Matt, Narla, Rama Krishna, Bissonette, Rene, Richardson, Samantha, Peng, Sophie X, Perrin-Ninkovic, Sophie, Tran, Tam, Shi, Tao, Yang, Wen Qing, Tong, Zeen, Cathers, Brian E, Moghaddam, Mehran F, Canan, Stacie S, Worland, Peter, Sankar, Sabita, Raymon, Heather K

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Inhibition of Human Telomerase by a G-Quadruplex-Interactive Compound von Sun, Daekyu, Thompson, Brian, Cathers, Brian E, Salazar, Miguel, Kerwin, Sean M, Trent, John O, Jenkins, Terence C, Neidle, Stephen, Hurley, Laurence H

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Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor von Plantevin Krenitsky, Véronique, Nadolny, Lisa, Delgado, Mercedes, Ayala, Leticia, Clareen, Steven S., Hilgraf, Robert, Albers, Ronald, Hegde, Sayee, D’Sidocky, Neil, Sapienza, John, Wright, Jonathan, McCarrick, Meg, Bahmanyar, Sogole, Chamberlain, Philip, Delker, Silvia L., Muir, Jeff, Giegel, David, Xu, Li, Celeridad, Maria, Lachowitzer, Jeff, Bennett, Brydon, Moghaddam, Mehran, Khatsenko, Oleg, Katz, Jason, Fan, Rachel, Bai, April, Tang, Yang, Shirley, Michael A., Benish, Brent, Bodine, Tracey, Blease, Kate, Raymon, Heather, Cathers, Brian E., Satoh, Yoshitaka

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Discovery of Mammalian Target of Rapamycin (mTOR) Kinase Inhibitor CC-223 von Mortensen, Deborah S, Perrin-Ninkovic, Sophie M, Shevlin, Graziella, Zhao, Jingjing, Packard, Garrick, Bahmanyar, Sogole, Correa, Matthew, Elsner, Jan, Harris, Roy, Lee, Branden G. S, Papa, Patrick, Parnes, Jason S, Riggs, Jennifer R, Sapienza, John, Tehrani, Lida, Whitefield, Brandon, Apuy, Julius, Bisonette, René R, Gamez, James C, Hickman, Matt, Khambatta, Godrej, Leisten, Jim, Peng, Sophie X, Richardson, Samantha J, Cathers, Brian E, Canan, Stacie S, Moghaddam, Mehran F, Raymon, Heather K, Worland, Peter, Narla, Rama Krishna, Fultz, Kimberly E, Sankar, Sabita

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Crystal structures of PRK1 in complex with the clinical compounds lestaurtinib and tofacitinib reveal ligand induced conformational changes von Chamberlain, Philip, Delker, Silvia, Pagarigan, Barbra, Mahmoudi, Afshin, Jackson, Pilgrim, Abbasian, Mahan, Muir, Jeff, Raheja, Neil, Cathers, Brian

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