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Novel Piperidinyl-Azetidines as Potent and Selective CCR4 Antagonists Elicit Antitumor Response as a Single Agent and in Combination with Checkpoint Inhibitors.
Robles O, Jackson JJ, Marshall L, Talay O, Chian D, Cutler G, Diokno R, Hu DX, Jacobson S, Karbarz E, Kassner PD, Ketcham JM, McKinnell J, Meleza C, Reilly MK, Riegler E, Shunatona HP, Wadsworth A, Younai A, Brockstedt DG, Wustrow DJ, Zibinsky M. Robles O, et al. Among authors: kassner pd. J Med Chem. 2020 Aug 13;63(15):8584-8607. doi: 10.1021/acs.jmedchem.0c00988. Epub 2020 Jul 28. J Med Chem. 2020. PMID: 32667798
Discovery of a Potent and Selective CCR4 Antagonist That Inhibits Treg Trafficking into the Tumor Microenvironment.
Jackson JJ, Ketcham JM, Younai A, Abraham B, Biannic B, Beck HP, Bui MHT, Chian D, Cutler G, Diokno R, Hu DX, Jacobson S, Karbarz E, Kassner PD, Marshall L, McKinnell J, Meleza C, Okal A, Pookot D, Reilly MK, Robles O, Shunatona HP, Talay O, Walker JR, Wadsworth A, Wustrow DJ, Zibinsky M. Jackson JJ, et al. Among authors: kassner pd. J Med Chem. 2019 Jul 11;62(13):6190-6213. doi: 10.1021/acs.jmedchem.9b00506. Epub 2019 Jul 1. J Med Chem. 2019. PMID: 31259550
Discovery of Potent, Selective, and Orally Bioavailable Inhibitors of USP7 with In Vivo Antitumor Activity.
Leger PR, Hu DX, Biannic B, Bui M, Han X, Karbarz E, Maung J, Okano A, Osipov M, Shibuya GM, Young K, Higgs C, Abraham B, Bradford D, Cho C, Colas C, Jacobson S, Ohol YM, Pookot D, Rana P, Sanchez J, Shah N, Sun M, Wong S, Brockstedt DG, Kassner PD, Schwarz JB, Wustrow DJ. Leger PR, et al. Among authors: kassner pd. J Med Chem. 2020 May 28;63(10):5398-5420. doi: 10.1021/acs.jmedchem.0c00245. Epub 2020 May 6. J Med Chem. 2020. PMID: 32302140
Novel, Selective Inhibitors of USP7 Uncover Multiple Mechanisms of Antitumor Activity In Vitro and In Vivo.
Ohol YM, Sun MT, Cutler G, Leger PR, Hu DX, Biannic B, Rana P, Cho C, Jacobson S, Wong ST, Sanchez J, Shah N, Pookot D, Abraham B, Young K, Suthram S, Marshall LA, Bradford D, Kozon N, Han X, Okano A, Maung J, Colas C, Schwarz J, Wustrow D, Brockstedt DG, Kassner PD. Ohol YM, et al. Among authors: kassner pd. Mol Cancer Ther. 2020 Oct;19(10):1970-1980. doi: 10.1158/1535-7163.MCT-20-0184. Epub 2020 Aug 11. Mol Cancer Ther. 2020. PMID: 32788207
Tumors establish resistance to immunotherapy by regulating Treg recruitment via CCR4.
Marshall LA, Marubayashi S, Jorapur A, Jacobson S, Zibinsky M, Robles O, Hu DX, Jackson JJ, Pookot D, Sanchez J, Brovarney M, Wadsworth A, Chian D, Wustrow D, Kassner PD, Cutler G, Wong B, Brockstedt DG, Talay O. Marshall LA, et al. Among authors: kassner pd. J Immunother Cancer. 2020 Nov;8(2):e000764. doi: 10.1136/jitc-2020-000764. J Immunother Cancer. 2020. PMID: 33243932 Free PMC article.
EBV+ tumors exploit tumor cell-intrinsic and -extrinsic mechanisms to produce regulatory T cell-recruiting chemokines CCL17 and CCL22.
Jorapur A, Marshall LA, Jacobson S, Xu M, Marubayashi S, Zibinsky M, Hu DX, Robles O, Jackson JJ, Baloche V, Busson P, Wustrow D, Brockstedt DG, Talay O, Kassner PD, Cutler G. Jorapur A, et al. Among authors: kassner pd. PLoS Pathog. 2022 Jan 13;18(1):e1010200. doi: 10.1371/journal.ppat.1010200. eCollection 2022 Jan. PLoS Pathog. 2022. PMID: 35025968 Free PMC article.
Potent GCN2 Inhibitor Capable of Reversing MDSC-Driven T Cell Suppression Demonstrates In Vivo Efficacy as a Single Agent and in Combination with Anti-Angiogenesis Therapy.
Jackson JJ, Shibuya GM, Ravishankar B, Adusumilli L, Bradford D, Brockstedt DG, Bucher C, Bui M, Cho C, Colas C, Cutler G, Dukes A, Han X, Hu DX, Jacobson S, Kassner PD, Katibah GE, Ko MYM, Kolhatkar U, Leger PR, Ma A, Marshall L, Maung J, Ng AA, Okano A, Pookot D, Poon D, Ramana C, Reilly MK, Robles O, Schwarz JB, Shakhmin AA, Shunatona HP, Sreenivasan R, Tivitmahaisoon P, Xu M, Zaw T, Wustrow DJ, Zibinsky M. Jackson JJ, et al. Among authors: kassner pd. J Med Chem. 2022 Oct 13;65(19):12895-12924. doi: 10.1021/acs.jmedchem.2c00736. Epub 2022 Sep 20. J Med Chem. 2022. PMID: 36127295
Clinical and molecular effects of oral CCR4 antagonist RPT193 in atopic dermatitis: A Phase 1 study.
Bissonnette R, DuBois J, Facheris P, Del Duca E, Kim M, Correa Da Rosa J, Trujillo DL, Bose S, Pagan AD, Wustrow D, Brockstedt DG, Wong B, Kassner PD, Jankicevic J, Ho W, Cheng LE, Guttman-Yassky E. Bissonnette R, et al. Among authors: kassner pd. Allergy. 2024 Apr;79(4):924-936. doi: 10.1111/all.15949. Epub 2023 Nov 20. Allergy. 2024. PMID: 37984453 Clinical Trial.
41 results