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Page 1
Discovery of JNJ-64264681: A Potent and Selective Covalent Inhibitor of Bruton's Tyrosine Kinase.
Tichenor MS, Wiener JJM, Rao NL, Bacani GM, Wei J, Pooley Deckhut C, Barbay JK, Kreutter KD, Chang L, Clancy KW, Murrey HE, Wang W, Ahn K, Huber M, Rex E, Coe KJ, Wu J, Rui H, Sepassi K, Gaudiano M, Bekkers M, Cornelissen I, Packman K, Seierstad M, Xiouras C, Bembenek SD, Alexander R, Milligan C, Balasubramanian S, Lebsack AD, Venable JD, Philippar U, Edwards JP, Hirst G. Tichenor MS, et al. Among authors: philippar u. J Med Chem. 2022 Nov 10;65(21):14326-14336. doi: 10.1021/acs.jmedchem.2c01026. Epub 2022 Oct 31. J Med Chem. 2022. PMID: 36314537
Discovery of an Oral, Beyond-Rule-of-Five Mcl-1 Protein-Protein Interaction Modulator with the Potential of Treating Hematological Malignancies.
Romanov-Michailidis F, Hsiao CC, Urner LM, Jerhaoui S, Surkyn M, Miller B, Vos A, Dominguez Blanco M, Bueters R, Vinken P, Bekkers M, Walker D, Pietrak B, Eyckmans W, Dores-Sousa JL, Joo Koo S, Lento W, Bauser M, Philippar U, Rombouts FJR. Romanov-Michailidis F, et al. Among authors: philippar u. J Med Chem. 2023 May 11;66(9):6122-6148. doi: 10.1021/acs.jmedchem.2c01953. Epub 2023 Apr 28. J Med Chem. 2023. PMID: 37114951
Macrocyclic Carbon-Linked Pyrazoles As Novel Inhibitors of MCL-1.
Demin S, Peschiulli A, Velter AI, Vos A, De Boeck B, Miller B, Rombouts FJR, Reuillon T, Lento W, Blanco MD, Jouffroy M, Steyvers H, Bekkers M, Altrocchi C, Pietrak B, Koo SJ, Szewczuk L, Attar R, Philippar U. Demin S, et al. Among authors: philippar u. ACS Med Chem Lett. 2023 Jul 3;14(7):955-961. doi: 10.1021/acsmedchemlett.3c00141. eCollection 2023 Jul 13. ACS Med Chem Lett. 2023. PMID: 37465311 Free PMC article.
Discovery of JNJ-74856665: A Novel Isoquinolinone DHODH Inhibitor for the Treatment of AML.
DeRatt LG, Zhang Z, Pietsch C, Cisar JS, Zhang X, Wang W, Tanner A, Matico R, Shaffer P, Jacoby E, Kazmi F, Shukla N, Bush TL, Patrick A, Philippar U, Attar R, Edwards JP, Kuduk SD. DeRatt LG, et al. Among authors: philippar u. J Med Chem. 2024 Jul 11;67(13):11254-11272. doi: 10.1021/acs.jmedchem.4c00809. Epub 2024 Jun 18. J Med Chem. 2024. PMID: 38889244
Preclinical efficacy of the potent, selective menin-KMT2A inhibitor JNJ-75276617 (bleximenib) in KMT2A- and NPM1-altered leukemias.
Kwon MC, Thuring JW, Querolle O, Dai X, Verhulst T, Pande V, Marien A, Goffin D, Wenge DV, Yue H, Cutler JA, Jin C, Perner F, Hogeling SM, Shaffer PL, Jacobs F, Vinken P, Cai W, Keersmaekers V, Eyassu F, Bhogal B, Verstraeten K, El Ashkar S, Perry JA, Jayaguru P, Barreyro L, Kuchnio A, Darville N, Krosky D, Urbanietz G, Verbist B, Edwards JP, Cowley GS, Kirkpatrick R, Steele R, Ferrante L, Guttke C, Daskalakis N, Pietsch EC, Wilson DM, Attar R, Elsayed Y, Fischer ES, Schuringa JJ, Armstrong SA, Packman K, Philippar U. Kwon MC, et al. Among authors: philippar u. Blood. 2024 Sep 12;144(11):1206-1220. doi: 10.1182/blood.2023022480. Blood. 2024. PMID: 38905635 Free PMC article.
Identification of isoquinolinone DHODH inhibitor isosteres.
DeRatt LG, Zhang Z, Pietsch EC, Cisar J, Wang A, Wang CY, Tanner A, Shaffer P, Jacoby E, Kazmi F, Shukla N, Philippar U, Attar RM, Edwards JP, Kuduk SD. DeRatt LG, et al. Among authors: philippar u. Bioorg Med Chem Lett. 2024 Nov 15;113:129965. doi: 10.1016/j.bmcl.2024.129965. Epub 2024 Sep 14. Bioorg Med Chem Lett. 2024. PMID: 39284456
SETDB1 suppresses NK cell-mediated immunosurveillance in acute myeloid leukemia with granulo-monocytic differentiation.
Chang YH, Yamamoto K, Fujino T, Wang TW, Sugimoto E, Zhang W, Yabushita T, Suzaki K, Pietsch EC, Weir BA, Crescenzo R, Cowley GS, Attar R, Philippar U, Wunderlich M, Mizukawa B, Zheng Y, Enomoto Y, Imai Y, Kitamura T, Goyama S. Chang YH, et al. Among authors: philippar u. Cell Rep. 2024 Aug 27;43(8):114536. doi: 10.1016/j.celrep.2024.114536. Epub 2024 Aug 2. Cell Rep. 2024. PMID: 39096901 Free article.
BCL10 Mutations Define Distinct Dependencies Guiding Precision Therapy for DLBCL.
Xia M, David L, Teater M, Gutierrez J, Wang X, Meydan C, Lytle A, Slack GW, Scott DW, Morin RD, Onder O, Elenitoba-Johnson KSJ, Zamponi N, Cerchietti L, Lu T, Philippar U, Fontan L, Wu H, Melnick AM. Xia M, et al. Among authors: philippar u. Cancer Discov. 2022 Aug 5;12(8):1922-1941. doi: 10.1158/2159-8290.CD-21-1566. Cancer Discov. 2022. PMID: 35658124 Free PMC article.
33 results