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Page 1
LIG1 is a synthetic lethal target in BRCA1 mutant cancers.
Martires LCM, Ahronian LG, Pratt CB, Das NM, Zhang X, Whittington DA, Zhang H, Shen B, Come J, McCarren P, Liu MS, Min C, Feng T, Jahic H, Ali JA, Aird DR, Li F, Andersen JN, Huang A, Mallender WD, Nicholson HE. Martires LCM, et al. Among authors: whittington da. Mol Cancer Ther. 2025 Jan 27. doi: 10.1158/1535-7163.MCT-24-0598. Online ahead of print. Mol Cancer Ther. 2025. PMID: 39868490
Discovery of TNG908: A Selective, Brain Penetrant, MTA-Cooperative PRMT5 Inhibitor That Is Synthetically Lethal with MTAP-Deleted Cancers.
Cottrell KM, Briggs KJ, Whittington DA, Jahic H, Ali JA, Davis CB, Gong S, Gotur D, Gu L, McCarren P, Tonini MR, Tsai A, Wilker EW, Yuan H, Zhang M, Zhang W, Huang A, Maxwell JP. Cottrell KM, et al. Among authors: whittington da. J Med Chem. 2024 Apr 25;67(8):6064-6080. doi: 10.1021/acs.jmedchem.4c00133. Epub 2024 Apr 10. J Med Chem. 2024. PMID: 38595098 Free PMC article.
Ubiquitinated PCNA Drives USP1 Synthetic Lethality in Cancer.
Simoneau A, Engel JL, Bandi M, Lazarides K, Liu S, Meier SR, Choi AH, Zhang H, Shen B, Martires L, Gotur D, Pham TV, Li F, Gu L, Gong S, Zhang M, Wilker E, Pan X, Whittington DA, Throner S, Maxwell JP, Chen Y, Yu Y, Huang A, Andersen JN, Feng T. Simoneau A, et al. Among authors: whittington da. Mol Cancer Ther. 2023 Feb 1;22(2):215-226. doi: 10.1158/1535-7163.MCT-22-0409. Mol Cancer Ther. 2023. PMID: 36228090 Free PMC article.
Next generation Fc scaffold for multispecific antibodies.
Estes B, Sudom A, Gong D, Whittington DA, Li V, Mohr C, Li D, Riley TP, Shi SD, Zhang J, Garces F, Wang Z. Estes B, et al. Among authors: whittington da. iScience. 2021 Nov 15;24(12):103447. doi: 10.1016/j.isci.2021.103447. eCollection 2021 Dec 17. iScience. 2021. PMID: 34877503 Free PMC article.
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Frohn M, Liu L, Siegmund AC, Qian W, Amegadzie A, Chen N, Tan H, Hickman D, Wood S, Wen PH, Bartberger MD, Whittington DA, Allen JR, Bourbeau MP. Frohn M, et al. Among authors: whittington da. Bioorg Med Chem Lett. 2020 Jul 15;30(14):127240. doi: 10.1016/j.bmcl.2020.127240. Epub 2020 May 4. Bioorg Med Chem Lett. 2020. PMID: 32527542
Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors.
Lanman BA, Allen JR, Allen JG, Amegadzie AK, Ashton KS, Booker SK, Chen JJ, Chen N, Frohn MJ, Goodman G, Kopecky DJ, Liu L, Lopez P, Low JD, Ma V, Minatti AE, Nguyen TT, Nishimura N, Pickrell AJ, Reed AB, Shin Y, Siegmund AC, Tamayo NA, Tegley CM, Walton MC, Wang HL, Wurz RP, Xue M, Yang KC, Achanta P, Bartberger MD, Canon J, Hollis LS, McCarter JD, Mohr C, Rex K, Saiki AY, San Miguel T, Volak LP, Wang KH, Whittington DA, Zech SG, Lipford JR, Cee VJ. Lanman BA, et al. Among authors: whittington da. J Med Chem. 2020 Jan 9;63(1):52-65. doi: 10.1021/acs.jmedchem.9b01180. Epub 2019 Dec 24. J Med Chem. 2020. PMID: 31820981
Discovery of AM-6494: A Potent and Orally Efficacious β-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A, Siegmund AC, Wen PH, Whittington DA, Allen JR, Wood S. Pettus LH, et al. Among authors: whittington da. J Med Chem. 2020 Mar 12;63(5):2263-2281. doi: 10.1021/acs.jmedchem.9b01034. Epub 2019 Oct 18. J Med Chem. 2020. PMID: 31589043
AMG 176, a Selective MCL1 Inhibitor, Is Effective in Hematologic Cancer Models Alone and in Combination with Established Therapies.
Caenepeel S, Brown SP, Belmontes B, Moody G, Keegan KS, Chui D, Whittington DA, Huang X, Poppe L, Cheng AC, Cardozo M, Houze J, Li Y, Lucas B, Paras NA, Wang X, Taygerly JP, Vimolratana M, Zancanella M, Zhu L, Cajulis E, Osgood T, Sun J, Damon L, Egan RK, Greninger P, McClanaghan JD, Gong J, Moujalled D, Pomilio G, Beltran P, Benes CH, Roberts AW, Huang DC, Wei A, Canon J, Coxon A, Hughes PE. Caenepeel S, et al. Among authors: whittington da. Cancer Discov. 2018 Dec;8(12):1582-1597. doi: 10.1158/2159-8290.CD-18-0387. Epub 2018 Sep 25. Cancer Discov. 2018. PMID: 30254093
73 results