Discovery of KT-474a Potent, Selective, and Orally Bioavailable IRAK4 Degrader for the Treatment of Autoimmune Diseases.

Authors: Zheng, Xiaozhang, Ji, Nan, Campbell, Veronica, Slavin, Anthony, Zhu, Xiao, Chen, Dapeng, Rong, Haojing, Enerson, Brad, Mayo, Michele, Sharma, Kirti, Browne, Chris M., Klaus, Christine R., Li, Haoran, Massa, Ginny, McDonald, Alice A., Shi, Yatao, Sintchak, Mike, Skouras, Stephanie, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 10/24/2024, Vol. 67 Issue 20, p18022-18037, 16p

Discovery of KT-413, a Targeted Protein Degrader of IRAK4 and IMiD Substrates Targeting MYD88 Mutant Diffuse Large B‑Cell Lymphoma.

Authors: Weiss, Matthew M., Zheng, Xiaozhang, Ji, Nan, Browne, Chris M., Campbell, Veronica, Chen, Dapeng, Enerson, Brad, Fei, Xue, Huang, Xin, Klaus, Christine R., Li, Haoran, Mayo, Michele, McDonald, Alice A., Paul, Atanu, Rong, Haojing, Sharma, Kirti, Shi, Yatao, Slavin, Anthony, Walther, Dirk M., Yuan, Karen

Source: Journal of Medicinal Chemistry; 7/11/2024, Vol. 67 Issue 13, p10548-10566, 19p

DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs and Hypomethylating Agents in MLL-Rearranged Leukemia Cells

Authors: Klaus, Christine R., Iwanowicz, Dorothy, Johnston, Danielle, Campbell, Carly A., Smith, Jesse J., Moyer, Mikel P., Copeland, Robert A., Olhava, Edward J., Scott, Margaret Porter, Pollock, Roy M., Daigle, Scott R., Raimondi, Alejandra ^*

Source: In The Journal of Pharmacology and Experimental Therapeutics September 2014 350(3):646-656

Potent inhibition of DOT1L as treatment of MLL-fusion leukemia

Authors: Daigle, Scott R., Olhava, Edward J., Therkelsen, Carly A., Basavapathruni, Aravind, Jin, Lei, Boriack-Sjodin, P. Ann, Allain, Christina J., Klaus, Christine R., Raimondi, Alejandra, Scott, Margaret Porter, Waters, Nigel J., Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M. ^*

Source: In Blood 8 August 2013 122(6):1017-1025

Durable tumor regression in genetically altered malignant rhabdoid tumors by inhibition of methyltransferase EZH2

Authors: Knutson, Sarah K., Warholic, Natalie M., Wigle, Tim J., Klaus, Christine R., Allain, Christina J., Raimondi, Alejandra, Scott, Margaret Porter, Chesworth, Richard, Moyer, Mikel P., Copeland, Robert A., Richon, Victoria M., Pollock, Roy M., Kuntz, Kevin W., Keilhack, Heike

Source: Proceedings of the National Academy of Sciences of the United States of America, 2013 May 01. 110(19), 7922-7927.

Access URL: https://www.jstor.org/stable/42656406

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EZH2 Inhibitor EPZ-6438 Synergizes With Anti-Lymphoma Therapies In Preclinical Models

Authors: Johnston, L. Danielle, Knutson, Sarah, Warholic, Natalie, Klaus, Christine R, Wigle, Tim J., Iwanowicz, Dorothy, Littlefield, Bruce A., Scott, Margaret Porter, Smith, Jesse J, Moyer, Mikel P, Copeland, Robert A., Pollock, Roy M., Kuntz, Kevin W, Keilhack, Heike, Raimondi, Alejandra

Source: In Blood 15 November 2013 122(21):4416-4416

DOT1L Inhibitor EPZ-5676 Displays Synergistic Antiproliferative Activity in Combination with Standard of Care Drugs or DNA Hypomethylating Agents in MLL-Rearranged Leukemia Cells

Authors: Klaus, Christine R ^*, Daigle, Scott R. ^*, Iwanowics, Dorothy ^*, Johnston, L. Danielle ^*, Therkelsen, Carly A ^*, Smith, Jesse J ^*, Moyer, Mikel P ^*, Copeland, Robert A., Olhava, Edward J ^*, Scott, Margaret Porter ^*, Pollock, Roy M. ^*, Raimondi, Alejandra ^*

Source: In Blood 15 November 2013 122(21):3930-3930

Preclinical Characterization of E7438, a Potent, Selective Inhibitor of Protein Methyltransferase EZH2 with Robust Antitumor Activity Against EZH2 Mutated Non-Hodgkin Lymphoma Xenografts in Mice

Authors: Keilhack, Heike ^*, Yokoi, Akira ^*, Knutson, Sarah K ^*, Wigle, Tim ^*, Warholic, Natalie ^*, Kawano, Satoshi ^*, Minoshima, Yukinori ^*, Huang, Kuan-Chun ^*, Kuznetsov, Galina ^*, Kumar, Namita ^*, Klaus, Christine R ^*, Allain, Christina J ^*, Raimondi, Alejandra ^*, Scott, Margaret Porter ^*, Chesworth, Richard ^*, Moyer, Mikel P ^*, Uenaka, Toshimitsu ^*, Copeland, Robert A ^*, Richon, Victoria M, Pollock, Roy M ^*, Kuntz, Kevin W ^*

Source: In Blood 16 November 2012 120(21):3712-3712

Preclinical Characterization of a Potent, Selective Inhibitor of the Protein Methyltransferase DOT1L for Use in the Treatment of MLL-Rearranged Leukemia.

Authors: Pollock, Roy M ^*, Daigle, Scott R ^*, Therkelsen, Carly A ^*, Basavapathruni, Aravind ^*, Jin, Lei ^*, Allain, Christina J ^*, Klaus, Christine R ^*, Raimondi, Alejandra ^*, Scott, Margaret Porter ^*, Chesworth, Richard ^*, Moyer, Mikel P ^*, Copeland, Robert A ^*, Richon, Victoria M, Olhava, Edward J ^*

Source: In Blood 16 November 2012 120(21):2379-2379

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