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

Optimization of permeability in a series of pyrrolotriazine inhibitors of IRAK4

Authors: Degorce, Sébastien L., Anjum, Rana, Dillman, Keith S., Drew, Lisa, Groombridge, Sam D., Halsall, Christopher T., Lenz, Eva M., Lindsay, Nicola A., Mayo, Michele F., Pink, Jennifer H., Robb, Graeme R., Scott, James S., Stokes, Stephen, Xue, Yafeng

Source: In Bioorganic & Medicinal Chemistry 15 February 2018 26(4):913-924

Sensitivity to PI3K and AKT inhibitors is mediated by divergent molecular mechanisms in subtypes of DLBCL

Authors: Erdmann, Tabea, Klener, Pavel, Lynch, James T., Grau, Michael, Vočková, Petra, Molinsky, Jan, Tuskova, Diana, Hudson, Kevin, Polanska, Urszula M., Grondine, Michael, Mayo, Michele, Dai, Beiying, Pfeifer, Matthias, Erdmann, Kristian, Schwammbach, Daniela, Zapukhlyak, Myroslav, Staiger, Annette M., Ott, German, Berdel, Wolfgang E., Davies, Barry R., Cruzalegui, Francisco, Trneny, Marek, Lenz, Peter, Barry, Simon T., Lenz, Georg

Source: In Blood 20 July 2017 130(3):310-322

Prediction of pharmacokinetics and pharmacodynamics in human for IRAK4 targeted protein degrader

Authors: Chen, Dapeng, Rong, Haojing, Mayo, Michele, McDonald, Alice, Campbell, Veronica, Zheng, Xiaozhang, Agarwal, Sagar, Weiss, Matt, Slavin, Anthony

Source: In Drug Metabolism and Pharmacokinetics April 2024 55 Supplement

A novel anti-CD37 antibody-drug conjugate with multiple anti-tumor mechanisms for the treatment of B-cell malignancies

Authors: Deckert, Jutta, Park, Peter U., Chicklas, Sharon, Yi, Yong, Li, Min, Lai, Katharine C., Mayo, Michele F., Carrigan, Christina N., Erickson, Hans K., Pinkas, Jan, Lutz, Robert J., Chittenden, Thomas, Lambert, John M.

Source: In Blood 14 November 2013 122(20):3500-3510

Antitumors combinations containing antibodies recognizing specifically CD38 and bortezomib

Lorvotuzumab mertansine, a CD56-targeting antibody-drug conjugate with potent antitumor activity against small cell lung cancer in human xenograft models

Authors: Whiteman, Kathleen R, Johnson, Holly A, Mayo, Michele F, Audette, Charlene A, Carrigan, Christina N, LaBelle, Alyssa, Zukerberg, Lawrence, Lambert, John M, Lutz, Robert J

Source: MAbs. 6(2):556-566

Availability: http://explore.bl.uk/primo_library/libweb/action/display.do?tabs=detailsTab&gathStatTab=true&ct=display&fn=search&doc=ETOCvdc_100050682226.0x000001&indx=1&recIds=ETOCvdc_100050682226.0x000001

Development of KT-253, a Highly Potent and Selective Heterobifunctional MDM2 Degrader for the Treatment of Acute Myeloid Leukemia

Authors: Mayo, Michele ^*, Chutake, Yogesh ^*, Karnik, Rahul ^*, McDonald, Alice ^*, Cho, Patricia S. ^*, Filiatrault, Jessica ^*, Chen, Dapeng ^*, Dixit, Vaishali ^*, Proctor, William ^*, Breitkopf, Susanne ^*, Qi, Frank ^*, Hu, Kan-Nian ^*, Sharma, Kirti ^*, Ewesuedo, Reggie ^*, Weiss, Matt ^*, Growney, Joseph D. ^*, Williams, Juliet ^*, Schalm, Stefanie S ^*

Source: In Blood 15 November 2022 140 Supplement 1:6239-6240

A First-in-Class STAT3 Degrader KT-333 in Development for Treatment of Hematologic Cancers

Authors: Liu, Phillip CC, Dixit, Vaishali, Mayo, Michele, Dey, Joyoti, Yuan, Karen, Karnik, Rahul, Walther, Dirk, Shi, Yatao, Sharma, Kirti, Rong, Haojing, Yang, Bin, Gollerkeri, Ashwin, Gollob, Jared, DeSavi, Chris

Source: In Blood 23 November 2021 138 Supplement 1:1865-1865

This result is not displayed to guests.
Login for full access.

This result is not displayed to guests.
Login for full access.

Mechanisms of the Anti-Tumor Activity of STAT3 Degraders in Lymphoma

Authors: Rong, Haojing ^*, Sharma, Kirti ^*, Csibi, Fred ^*, Yang, Bin ^*, Rusin, Scott ^*, Shi, Yatao ^*, Dey, Joyoti ^*, Karnik, Rahul ^*, Mayo, Michele ^*, Yuan, Karen ^*, Chutake, Yogesh ^*, McDonald, Alice ^*, Zhu, Sean ^*, Ji, Nan ^*, Liu, Phillip ^*, Li, Henry ^*, Walker, Duncan, Gollob, Jared ^*, Mainolfi, Nello ^*, Desavi, Chris ^*

Source: In Blood 5 November 2020 136 Supplement 1:42-42

Ktx-120, a Novel Irakimid Degrader of IRAK4 and IMiD Substrates Shows Preferential Activity and Induces Regressions in MYD88-Mutant DLBCL CDX and PDX Models

Authors: Walker, Duncan, Mayo, Michele ^*, Klaus, Christine ^*, Chen, Dapeng ^*, Bhaduri, Samyabrata ^*, Sharma, Kirti ^*, Rusin, Scott ^*, McDonald, Alice ^*, Gollob, Jared ^*, Mainolfi, Nello ^*, Weiss, Matt ^*

Source: In Blood 5 November 2020 136 Supplement 1:41-41

P464: PULSE DOSING OF POTENT AND SELECTIVE HETEROBIFUNCTIONAL MDM2 DEGRADER KT‐253 DRIVES TUMOR REGRESSION AND DEMONSTRATES DIFFERENTIATED PHARMACOLOGY COMPARED TO P53/MDM2 SMALL MOLECULE INHIBITORS.

Authors: Schalm, Stefanie, Chutake, Yogesh, Breitkopf, Susanne, Mayo, Michele, Dumont, Nancy, Chen, Dapeng, Dixit, Vaishali, Karnik, Rahul, Mcdonald, Alice, Filiatrault, Jessica, Proctor, William, Qi, Frank, Hu, Kan‐Nian, Weiss, Matt, Gollerkeri, Ashwin, Sharma, Kirti, D Growney, Joseph, Williams, Juliet

Source: HemaSphere; 2023 Supplement 3, Vol. 7, p1-2, 2p

This result is not displayed to guests.
Login for full access.

Small Molecule-Induced, Selective STAT3 Degradation Leads to Anti-Tumor Activity in STAT3-Dependent Heme Malignancies

Authors: Csibi, Fred ^*, Ji, Nan ^*, Yang, Bin ^*, Yuan, Karen ^*, Mayo, Michele ^*, Rong, Haojing ^*, Rusin, Scott ^*, Sharma, Kirti ^*, Loh, Christine ^*, Li, Henry ^*, Townson, Sharon ^*, Chen, Jesse ^*, Kamadurai, Hari ^*, Walker, Duncan, Gollob, Jared ^*, Mainolfi, Nello ^*

Source: In Blood 13 November 2019 134 Supplement 1:3803-3803

This result is not displayed to guests.
Login for full access.

This result is not displayed to guests.
Login for full access.

Discovery of a Series of 5-Azaquinazolines as Orally Efficacious IRAK4 Inhibitors Targeting MyD88L265PMutant Diffuse Large B Cell Lymphoma

Authors: Degorce, Sébastien L., Anjum, Rana, Bloecher, Andrew, Carbajo, Rodrigo J., Dillman, Keith S., Drew, Lisa, Halsall, Christopher T., Lenz, Eva M., Lindsay, Nicola A., Mayo, Michele F., Pink, Jennifer H., Robb, Graeme R., Rosen, Alan, Scott, James S., Xue, Yafeng

Source: Journal of Medicinal Chemistry; November 2019, Vol. 62 Issue: 21 p9918-9930, 13p