BIIB021, an orally available, fully synthetic small-molecule inhibitor of the heat shock protein Hsp90
Lundgren, Karen, Zhang, Hong, Brekken, John, Huser, Nanni, Powell, Rachel E, Timple, Noel, Busch, David J, Neely, Laura, Sensintaffar, John L, Yang, Yong-ching, McKenzie, Andres, Friedman, Jessica, Scannevin, Robert, Kamal, Adeela, Hong, Kevin, Kasibhatla, Srinivas R, Boehm, Marcus F, Burrows, Francis J
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Published in Molecular cancer therapeutics (01.04.2009)
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7‘-Substituted Benzothiazolothio- and Pyridinothiazolothio-Purines as Potent Heat Shock Protein 90 Inhibitors
Zhang, Lin, Fan, Junhua, Vu, Khang, Hong, Kevin, Le Brazidec, Jean-Yves, Shi, Jiandong, Biamonte, Marco, Busch, David J, Lough, Rachel E, Grecko, Roy, Ran, Yingqing, Sensintaffar, John L, Kamal, Adeela, Lundgren, Karen, Burrows, Francis J, Mansfield, Robert, Timony, Gregg A, Ulm, Edgar H, Kasibhatla, Srinivas R, Boehm, Marcus F
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Discovery of 2‑Indole-acylsulfonamide Myeloid Cell Leukemia 1 (Mcl-1) Inhibitors Using Fragment-Based Methods
Pelz, Nicholas F, Bian, Zhiguo, Zhao, Bin, Shaw, Subrata, Tarr, James C, Belmar, Johannes, Gregg, Claire, Camper, DeMarco V, Goodwin, Craig M, Arnold, Allison L, Sensintaffar, John L, Friberg, Anders, Rossanese, Olivia W, Lee, Taekyu, Olejniczak, Edward T, Fesik, Stephen W
Published in Journal of medicinal chemistry (10.03.2016)
Published in Journal of medicinal chemistry (10.03.2016)
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Optimization of Potent and Selective Tricyclic Indole Diazepinone Myeloid Cell Leukemia‑1 Inhibitors Using Structure-Based Design
Shaw, Subrata, Bian, Zhiguo, Zhao, Bin, Tarr, James C, Veerasamy, Nagarathanam, Jeon, Kyu Ok, Belmar, Johannes, Arnold, Allison L, Fogarty, Stuart A, Perry, Evan, Sensintaffar, John L, Camper, DeMarco V, Rossanese, Olivia W, Lee, Taekyu, Olejniczak, Edward T, Fesik, Stephen W
Published in Journal of medicinal chemistry (22.03.2018)
Published in Journal of medicinal chemistry (22.03.2018)
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Discovery of Potent Myeloid Cell Leukemia‑1 (Mcl-1) Inhibitors That Demonstrate in Vivo Activity in Mouse Xenograft Models of Human Cancer
Lee, Taekyu, Christov, Plamen P, Shaw, Subrata, Tarr, James C, Zhao, Bin, Veerasamy, Nagarathanam, Jeon, Kyu Ok, Mills, Jonathan J, Bian, Zhiguo, Sensintaffar, John L, Arnold, Allison L, Fogarty, Stuart A, Perry, Evan, Ramsey, Haley E, Cook, Rebecca S, Hollingshead, Melinda, Davis Millin, Myrtle, Lee, Kyung-min, Koss, Brian, Budhraja, Amit, Opferman, Joseph T, Kim, Kwangho, Arteaga, Carlos L, Moore, William J, Olejniczak, Edward T, Savona, Michael R, Fesik, Stephen W
Published in Journal of medicinal chemistry (25.04.2019)
Published in Journal of medicinal chemistry (25.04.2019)
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Structure-Based Discovery of Potent, Orally Bioavailable Benzoxazepinone-Based WD Repeat Domain 5 Inhibitors
Teuscher, Kevin B., Mills, Jonathan J., Tian, Jianhua, Han, Changho, Meyers, Kenneth M., Sai, Jiqing, South, Taylor M., Crow, Mackenzie M., Van Meveren, Mayme, Sensintaffar, John L., Zhao, Bin, Amporndanai, Kangsa, Moore, William J., Stott, Gordon M., Tansey, William P., Lee, Taekyu, Fesik, Stephen W.
Published in Journal of medicinal chemistry (28.12.2023)
Published in Journal of medicinal chemistry (28.12.2023)
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Discovery of a Myeloid Cell Leukemia 1 (Mcl-1) Inhibitor That Demonstrates Potent In Vivo Activities in Mouse Models of Hematological and Solid Tumors
Tarr, James C., Salovich, James M., Aichinger, Martin, Jeon, KyuOk, Veerasamy, Nagarathanam, Sensintaffar, John L., Arnhof, Heribert, Samwer, Matthias, Christov, Plamen P., Kim, Kwangho, Wunberg, Tobias, Schweifer, Norbert, Trapani, Francesca, Arnold, Allison, Martin, Florian, Zhao, Bin, Miriyala, Nagaraju, Sgubin, Danielle, Fogarty, Stuart, Moore, William J., Stott, Gordon M., Olejniczak, Edward T., Engelhardt, Harald, Rudolph, Dorothea, Lee, Taekyu, McConnell, Darryl B., Fesik, Stephen W.
Published in Journal of medicinal chemistry (22.08.2024)
Published in Journal of medicinal chemistry (22.08.2024)
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Structure-based discovery of potent WD repeat domain 5 inhibitors that demonstrate efficacy and safety in preclinical animal models
Teuscher, Kevin B, Chowdhury, Somenath, Meyers, Kenneth M, Tian, Jianhua, Sai, Jiqing, Van Meveren, Mayme, South, Taylor M, Sensintaffar, John L, Rietz, Tyson A, Goswami, Soumita, Wang, Jing, Grieb, Brian C, Lorey, Shelly L, Howard, Gregory C, Liu, Qi, Moore, William J, Stott, Gordon M, Tansey, William P, Lee, Taekyu, Fesik, Stephen W
Published in Proceedings of the National Academy of Sciences - PNAS (03.01.2023)
Published in Proceedings of the National Academy of Sciences - PNAS (03.01.2023)
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Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core
Tian, Jianhua, Teuscher, Kevin B, Aho, Erin R, Alvarado, Joseph R, Mills, Jonathan J, Meyers, Kenneth M, Gogliotti, Rocco D, Han, Changho, Macdonald, Jonathan D, Sai, Jiqing, Shaw, J. Grace, Sensintaffar, John L, Zhao, Bin, Rietz, Tyson A, Thomas, Lance R, Payne, William G, Moore, William J, Stott, Gordon M, Kondo, Jumpei, Inoue, Masahiro, Coffey, Robert J, Tansey, William P, Stauffer, Shaun R, Lee, Taekyu, Fesik, Stephen W
Published in Journal of medicinal chemistry (23.01.2020)
Published in Journal of medicinal chemistry (23.01.2020)
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Discovery and biological characterization of potent myeloid cell leukemia‐1 inhibitors
Lee, Taekyu, Bian, Zhiguo, Zhao, Bin, Hogdal, Leah J., Sensintaffar, John L., Goodwin, Craig M., Belmar, Johannes, Shaw, Subrata, Tarr, James C., Veerasamy, Nagarathanam, Matulis, Shannon M., Koss, Brian, Fischer, Melissa A., Arnold, Allison L., Camper, DeMarco V., Browning, Carrie F., Rossanese, Olivia W., Budhraja, Amit, Opferman, Joseph, Boise, Lawrence H., Savona, Michael R., Letai, Anthony, Olejniczak, Edward T., Fesik, Stephen W.
Published in FEBS letters (01.01.2017)
Published in FEBS letters (01.01.2017)
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Fragment-Based Screen of SARS-CoV‑2 Papain-like Protease (PLpro)
Taylor, Ashley J., Amporndanai, Kangsa, Rietz, Tyson A., Zhao, Bin, Thiruvaipati, Anusha, Wei, Qiangqiang, South, Taylor M., Crow, Mackenzie M., Apakama, Chideraa, Sensintaffar, John L., Phan, Jason, Lee, Taekyu, Fesik, Stephen W.
Published in ACS medicinal chemistry letters (08.08.2024)
Published in ACS medicinal chemistry letters (08.08.2024)
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Rationally Designed High-Affinity 2-Amino-6-halopurine Heat Shock Protein 90 Inhibitors That Exhibit Potent Antitumor Activity
Kasibhatla, Srinivas R, Hong, Kevin, Biamonte, Marco A, Busch, David J, Karjian, Patricia L, Sensintaffar, John L, Kamal, Adeela, Lough, Rachel E, Brekken, John, Lundgren, Karen, Grecko, Roy, Timony, Gregg A, Ran, Yingqing, Mansfield, Robert, Fritz, Lawrence C, Ulm, Edgar, Burrows, Francis J, Boehm, Marcus F
Published in Journal of medicinal chemistry (14.06.2007)
Published in Journal of medicinal chemistry (14.06.2007)
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Abstract 3551: Discovery of orally bioavailable novel Mcl-1 inhibitors that exhibit selective anti-proliferative activity in Mcl-1 sensitive cancer cell lines
Lee, Taekyu, Bian, Zhiguo, Belmar, Johannes, Shaw, Subrata, Tarr, James C., Zhao, Bin, Pelz, Nick, Camper, DeMarco, Goodwin, Craig M., Arnold, Allison L., Sensintaffar, John L., Browning, Carrie F., Rossanese, Olivia W., Olejniczak, Edward T., Fesik, Stephen W.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Orally Active Purine-Based Inhibitors of the Heat Shock Protein 90
Biamonte, Marco A, Shi, Jiandong, Hong, Kevin, Hurst, David C, Zhang, Lin, Fan, Junhua, Busch, David J, Karjian, Patricia L, Maldonado, Angelica A, Sensintaffar, John L, Yang, Yong-Ching, Kamal, Adeela, Lough, Rachel E, Lundgren, Karen, Burrows, Francis J, Timony, Gregg A, Boehm, Marcus F, Kasibhatla, Srinivas R
Published in Journal of medicinal chemistry (26.01.2006)
Published in Journal of medicinal chemistry (26.01.2006)
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Abstract 3987: Predicting MCL1 inhibitor sensitivity in large cell line panels using a gene expression signature
Wernitznig, Andreas, Rudolph, Dorothea, Samwer, Matthias, Schweifer, Norbert, Trapani, Francesca, Wunberg, Tobias, Arnhof, Heribert, Lee, Teakyu, Sensintaffar, John L., Olejniczak, Edward T., Benes, Cyril H., Fesik, Stephen W., Kraut, Norbert
Published in Cancer research (Chicago, Ill.) (01.07.2019)
Published in Cancer research (Chicago, Ill.) (01.07.2019)
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Discovery and Structure-Based Optimization of Potent and Selective WDR5 Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core
Tian, Jianhua, Teuscher, Kevin B., Aho, Erin R., Alvarado, Joseph R., Mills, Jonathan J., Meyers, Kenneth M., Gogliotti, Rocco D., Han, Changho, Macdonald, Jonathan D., Sai, Jiqing, Shaw, J. Grace, Sensintaffar, John L., Zhao, Bin, Rietz, Tyson A., Thomas, Lance R., Payne, William G., Moore, William J., Stott, Gordon M., Kondo, Jumpei, Inoue, Masahiro, Coffey, Robert J., Tansey, William P., Stauffer, Shaun R., Lee, Taekyu, Fesik, Stephen W.
Published in Journal of medicinal chemistry (07.01.2020)
Published in Journal of medicinal chemistry (07.01.2020)
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Discovery and Structure-Based Optimization of Potent and Selective WD Repeat Domain 5 (WDR5) Inhibitors Containing a Dihydroisoquinolinone Bicyclic Core
Tian, Jianhua, Teuscher, Kevin B., Aho, Erin R., Alvarado, Joseph R., Mills, Jonathan J., Meyers, Kenneth M., Gogliotti, Rocco D., Han, Changho, Macdonald, Jonathan D., Sai, Jiqing, Shaw, J. Grace, Sensintaffar, John L., Zhao, Bin, Rietz, Tyson A., Thomas, Lance R., Payne, William G., Moore, William J., Stott, Gordon M., Kondo, Jumpei, Inoue, Masahiro, Coffey, Robert J., Tansey, William P., Stauffer, Shaun R., Lee, Taekyu, Fesik, Stephen W.
Published in Journal of medicinal chemistry (20.12.2019)
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Published in Journal of medicinal chemistry (20.12.2019)
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Abstract 3727: Small molecule Mcl-1 inhibitors induce apoptosis and death in multiple cancer subtypes in vitro
Sensintaffar, John L., Arnold, Allison, Goodwin, Craig, Hogdal, Leah, Shaw, Subrata, Tarr, James C., Lee, Taekyu, Olejniczak, Edward, Fesik, Stephen W.
Published in Cancer research (Chicago, Ill.) (15.07.2016)
Published in Cancer research (Chicago, Ill.) (15.07.2016)
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Discovery and biological characterization of potent myeloid cell leukemia-1 inhibitors
Lee, Taekyu, Bian, Zhiguo, Zhao, Bin, Hogdal, Leah J., Sensintaffar, John L., Goodwin, Craig M., Belmar, Johannes, Shaw, Subrata, Tarr, James C., Veerasamy, Nagarathanam, Matulis, Shannon M., Koss, Brian, Fischer, Melissa A., Arnold, Allison L., Camper, DeMarco V., Browning, Carrie F., Rossanese, Olivia W., Budhraja, Amit, Opferman, Joseph, Boise, Lawrence H., Savona, Michael R., Letai, Anthony, Olejniczak, Edward T., Fesik, Stephen W.
Published in FEBS letters (19.12.2016)
Published in FEBS letters (19.12.2016)
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