Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, T. Matt, Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, J. William, Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Kluge, Arthur F., Patane, Michael A., Van Drie, John H., Wang, Ce, McElligott, David, Kesicki, Ed, Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, Bromberg, Kenneth D.
Published in Nature (London) (05.10.2017)
Published in Nature (London) (05.10.2017)
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Journal Article
Novel Modes of Inhibition of Wild-Type Isocitrate Dehydrogenase 1 (IDH1): Direct Covalent Modification of His315
Jakob, Clarissa G, Upadhyay, Anup K, Donner, Pamela L, Nicholl, Emily, Addo, Sadiya N, Qiu, Wei, Ling, Christopher, Gopalakrishnan, Sujatha M, Torrent, Maricel, Cepa, Steven P, Shanley, Jason, Shoemaker, Alexander R, Sun, Chaohong C, Vasudevan, Anil, Woller, Kevin R, Shotwell, J. Brad, Shaw, Bailin, Bian, Zhiguo, Hutti, Jessica E
Published in Journal of medicinal chemistry (09.08.2018)
Published in Journal of medicinal chemistry (09.08.2018)
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Journal Article
Discovery of Potent Azetidine-Benzoxazole MerTK Inhibitors with In Vivo Target Engagement
Frey, Robin R., Jana, Navendu, Gorman, Jacob V., Wang, Jin, Smith, Heath A., Bromberg, Kenneth D., Thakur, Ashish, Doktor, Stella Z., Indulkar, Anura S., Jakob, Clarissa G., Upadhyay, Anup K., Qiu, Wei, Manaves, Vlasios, Gambino, Frank, Valentino, Stephen A., Montgomery, Debra, Zhou, Yebin, Li, Tao, Buchanan, Fritz G., Ferguson, Debra C., Kurnick, Matthew D., Kapecki, Nicolas, Lai, Albert, Michaelides, Michael R., Penning, Thomas D.
Published in Journal of medicinal chemistry (10.10.2024)
Published in Journal of medicinal chemistry (10.10.2024)
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Journal Article
Discovery of A‑910, a Highly Potent and Orally Bioavailable Dual MerTK/Axl-Selective Tyrosine Kinase Inhibitor
Yu, Yiyun, Jang, Miyeon, Miyashiro, Julie, Clark, Richard F., Zhu, Gui-Dong, Gong, Jane, Dai, Yujia, Frey, Robin R., Penning, Thomas D., Kim, Hadong, Lee, Hyung Ki, Kim, Jin Kwan, Ryu, Ki Moon, Park, Seong Jin, Yoon, Taeyoung, Li, Tao, Kurnick, Matthew D., Kapecki, Nicolas J., Li, Leiming, Gorman, Jacob V., Montgomery, Debra A., Manaves, Vlasios, Bromberg, Kenneth D., Doktor, Stella Z., Thakur, Ashish, Wang, Jin, Smith, Heath A., Buchanan, Fritz G., Ferguson, Debra C., Torrent, Maricel, Jakob, Clarissa G., Qiu, Wei, Upadhyay, Anup K., Martin, Ruth L., Lai, Albert, Michaelides, Michael R.
Published in Journal of medicinal chemistry (10.10.2024)
Published in Journal of medicinal chemistry (10.10.2024)
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Journal Article
Discovery of spirohydantoins as selective, orally bioavailable inhibitors of p300/CBP histone acetyltransferases
Ji, Zhiqin, Clark, Richard F., Bhat, Vikram, Matthew Hansen, T., Lasko, Loren M., Bromberg, Kenneth D., Manaves, Vlasios, Algire, Mikkel, Martin, Ruth, Qiu, Wei, Torrent, Maricel, Jakob, Clarissa G., Liu, Hong, Cole, Philip A., Marmorstein, Ronen, Kesicki, Edward A., Lai, Albert, Michaelides, Michael R.
Published in Bioorganic & medicinal chemistry letters (01.05.2021)
Published in Bioorganic & medicinal chemistry letters (01.05.2021)
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Journal Article
Structure reveals function of the dual variable domain immunoglobulin (DVD-Ig™) molecule
Jakob, Clarissa G, Edalji, Rohinton, Judge, Russell A, DiGiammarino, Enrico, Li, Yingchun, Gu, Jijie, Ghayur, Tariq
Published in mAbs (01.05.2013)
Published in mAbs (01.05.2013)
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Journal Article
Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer
Petros, Andrew M, Korepanova, Alla, Jakob, Clarissa G, Qiu, Wei, Panchal, Sanjay C, Wang, Jie, Dietrich, Justin D, Brewer, Jason T, Pohlki, Frauke, Kling, Andreas, Wilcox, Kyle, Lakics, Viktor, Bahnassawy, Lamiaa, Reinhardt, Peter, Partha, Sarathy Karunan, Bodelle, Pierre M, Lake, Marc, Charych, Erik I, Stoll, Vincent S, Sun, Chaohong, Mohler, Eric G
Published in Journal of medicinal chemistry (25.04.2019)
Published in Journal of medicinal chemistry (25.04.2019)
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Journal Article
SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding
Curtin, Michael L., Pliushchev, Marina A., Li, Huan-Qiu, Torrent, Maricel, Dietrich, Justin D., Jakob, Clarissa G., Zhu, Haizhong, Zhao, Hongyu, Wang, Ying, Ji, Zhiqin, Clark, Richard F., Sarris, Kathy A., Selvaraju, Sujatha, Shaw, Bailin, Algire, Mikkel A., He, Yupeng, Richardson, Paul L., Sweis, Ramzi F., Sun, Chaohong, Chiang, Gary G., Michaelides, Michael R.
Published in Bioorganic & medicinal chemistry letters (01.04.2017)
Published in Bioorganic & medicinal chemistry letters (01.04.2017)
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Journal Article
Discovery of A‑893, A New Cell-Active Benzoxazinone Inhibitor of Lysine Methyltransferase SMYD2
Sweis, Ramzi F., Wang, Zhi, Algire, Mikkel, Arrowsmith, Cheryl H., Brown, Peter J., Chiang, Gary G., Guo, Jun, Jakob, Clarissa G., Kennedy, Steven, Li, Fengling, Maag, David, Shaw, Bailin, Soni, Nirupama B., Vedadi, Masoud, Pappano, William N.
Published in ACS medicinal chemistry letters (11.06.2015)
Published in ACS medicinal chemistry letters (11.06.2015)
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Journal Article
The structure of dual-variable-domain immunoglobulin molecules alone and bound to antigen
Correia, Ivan, Sung, Joyce, Burton, Randall, Jakob, Clarissa G., Carragher, Bridget, Ghayur, Tariq, Radziejewski, Czeslaw
Published in mAbs (01.05.2013)
Published in mAbs (01.05.2013)
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Journal Article
The EED protein–protein interaction inhibitor A-395 inactivates the PRC2 complex
He, Yupeng, Selvaraju, Sujatha, Curtin, Michael L, Jakob, Clarissa G, Zhu, Haizhong, Comess, Kenneth M, Shaw, Bailin, The, Juliana, Lima-Fernandes, Evelyne, Szewczyk, Magdalena M, Cheng, Dong, Klinge, Kelly L, Li, Huan-Qiu, Pliushchev, Marina, Algire, Mikkel A, Maag, David, Guo, Jun, Dietrich, Justin, Panchal, Sanjay C, Petros, Andrew M, Sweis, Ramzi F, Torrent, Maricel, Bigelow, Lance J, Senisterra, Guillermo, Li, Fengling, Kennedy, Steven, Wu, Qin, Osterling, Donald J, Lindley, David J, Gao, Wenqing, Galasinski, Scott, Barsyte-Lovejoy, Dalia, Vedadi, Masoud, Buchanan, Fritz G, Arrowsmith, Cheryl H, Chiang, Gary G, Sun, Chaohong, Pappano, William N
Published in Nature chemical biology (01.04.2017)
Published in Nature chemical biology (01.04.2017)
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Journal Article
Author Correction: Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours
Lasko, Loren M., Jakob, Clarissa G., Edalji, Rohinton P., Qiu, Wei, Montgomery, Debra, Digiammarino, Enrico L., Hansen, T. Matt, Risi, Roberto M., Frey, Robin, Manaves, Vlasios, Shaw, Bailin, Algire, Mikkel, Hessler, Paul, Lam, Lloyd T., Uziel, Tamar, Faivre, Emily, Ferguson, Debra, Buchanan, Fritz G., Martin, Ruth L., Torrent, Maricel, Chiang, Gary G., Karukurichi, Kannan, Langston, J. William, Weinert, Brian T., Choudhary, Chunaram, de Vries, Peter, Kluge, Arthur F., Patane, Michael A., Van Drie, John H., Wang, Ce, McElligott, David, Kesicki, Edward A., Marmorstein, Ronen, Sun, Chaohong, Cole, Philip A., Rosenberg, Saul H., Michaelides, Michael R., Lai, Albert, Bromberg, Kenneth D.
Published in Nature (London) (01.06.2018)
Published in Nature (London) (01.06.2018)
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Journal Article
The SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity
Bromberg, Kenneth D, Mitchell, Taylor R H, Upadhyay, Anup K, Jakob, Clarissa G, Jhala, Manisha A, Comess, Kenneth M, Lasko, Loren M, Li, Conglei, Tuzon, Creighton T, Dai, Yujia, Li, Fengling, Eram, Mohammad S, Nuber, Alexander, Soni, Niru B, Manaves, Vlasios, Algire, Mikkel A, Sweis, Ramzi F, Torrent, Maricel, Schotta, Gunnar, Sun, Chaohong, Michaelides, Michael R, Shoemaker, Alex R, Arrowsmith, Cheryl H, Brown, Peter J, Santhakumar, Vijayaratnam, Martin, Alberto, Rice, Judd C, Chiang, Gary G, Vedadi, Masoud, Barsyte-Lovejoy, Dalia, Pappano, William N
Published in Nature chemical biology (01.03.2017)
Published in Nature chemical biology (01.03.2017)
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Journal Article
Ligand association rates to the inner-variable-domain of a dual-variable-domain immunoglobulin are significantly impacted by linker design
DiGiammarino, Enrico L., Harlan, John E., Walter, Karl A., Ladror, Uri S., Edalji, Rohinton P., Hutchins, Charles W., Lake, Marc R., Greischar, Amy J., Liu, Junjian, Ghayur, Tariq, Jakob, Clarissa G.
Published in mAbs (01.09.2011)
Published in mAbs (01.09.2011)
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Journal Article
A potent erythropoietin-mimicking human antibody interacts through a novel binding site
Liu, Zhihong, Stoll, Vincent S., DeVries, Peter J., Jakob, Clarissa G., Xie, Nancy, Simmer, Robert L., Lacy, Susan E., Egan, David A., Harlan, John E., Lesniewski, Richard R., Reilly, Edward B.
Published in Blood (01.10.2007)
Published in Blood (01.10.2007)
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Journal Article
Crystal Structures of DPP-IV (CD26) from Rat Kidney Exhibit Flexible Accommodation of Peptidase-Selective Inhibitors
Longenecker, Kenton L, Stewart, Kent D, Madar, David J, Jakob, Clarissa G, Fry, Elizabeth H, Wilk, Sherwin, Lin, Chun W, Ballaron, Stephen J, Stashko, Michael A, Lubben, Thomas H, Yong, Hong, Pireh, Daisy, Pei, Zhonghua, Basha, Fatima, Wiedeman, Paul E, von Geldern, Thomas W, Trevillyan, James M, Stoll, Vincent S
Published in Biochemistry (Easton) (20.06.2006)
Published in Biochemistry (Easton) (20.06.2006)
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Journal Article
Structure of MurF from Streptococcus pneumoniae co‐crystallized with a small molecule inhibitor exhibits interdomain closure
Longenecker, Kenton L., Stamper, Geoffrey F., Hajduk, Philip J., Fry, Elizabeth H., Jakob, Clarissa G., Harlan, John E., Edalji, Rohinton, Bartley, Diane M., Walter, Karl A., Solomon, Larry R., Holzman, Thomas F., Gu, Yu Gui, Lerner, Claude G., Beutel, Bruce A., Stoll, Vincent S.
Published in Protein science (01.12.2005)
Published in Protein science (01.12.2005)
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Journal Article
Liver-Selective Glucocorticoid Antagonists: A Novel Treatment for Type 2 Diabetes
von Geldern, Thomas W, Tu, Noah, Kym, Philip R, Link, James T, Jae, Hwan-Soo, Lai, Chunqiu, Apelqvist, Theresa, Rhonnstad, Patrik, Hagberg, Lars, Koehler, Konrad, Grynfarb, Marlena, Goos-Nilsson, Annika, Sandberg, Johnny, Österlund, Marie, Barkhem, Tomas, Höglund, Marie, Wang, Jiahong, Fung, Steven, Wilcox, Denise, Nguyen, Phong, Jakob, Clarissa, Hutchins, Charles, Färnegårdh, Mathias, Kauppi, Björn, Öhman, Lars, Jacobson, Peer B
Published in Journal of medicinal chemistry (12.08.2004)
Published in Journal of medicinal chemistry (12.08.2004)
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Journal Article
Synthesis and structure–activity relationship of 3,4′-bispyridinylethylenes: Discovery of a potent 3-isoquinolinylpyridine inhibitor of protein kinase B (PKB/Akt) for the treatment of cancer
Li, Qun, Woods, Keith W., Thomas, Sheela, Zhu, Gui-Dong, Packard, Garrick, Fisher, John, Li, Tongmei, Gong, Jianchun, Dinges, Jurgen, Song, Xiaohong, Abrams, Jason, Luo, Yan, Johnson, Eric F., Shi, Yan, Liu, Xuesong, Klinghofer, Vered, Des Jong, Ron, Oltersdorf, Tilman, Stoll, Vincent S., Jakob, Clarissa G., Rosenberg, Saul H., Giranda, Vincent L.
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
Published in Bioorganic & medicinal chemistry letters (01.04.2006)
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Journal Article
Discovery of Potent Inhibitors of Dihydroneopterin Aldolase Using CrystaLEAD High-Throughput X-ray Crystallographic Screening and Structure-Directed Lead Optimization
Sanders, William J, Nienaber, Vicki L, Lerner, Claude G, McCall, J. Owen, Merrick, Sean M, Swanson, Susan J, Harlan, John E, Stoll, Vincent S, Stamper, Geoffrey F, Betz, Stephen F, Condroski, Kevin R, Meadows, Robert P, Severin, Jean M, Walter, Karl A, Magdalinos, Peter, Jakob, Clarissa G, Wagner, Rolf, Beutel, Bruce A
Published in Journal of medicinal chemistry (25.03.2004)
Published in Journal of medicinal chemistry (25.03.2004)
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Journal Article