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Page 1
Design of potent and selective inhibitors to overcome clinical anaplastic lymphoma kinase mutations resistant to crizotinib.
Huang Q, Johnson TW, Bailey S, Brooun A, Bunker KD, Burke BJ, Collins MR, Cook AS, Cui JJ, Dack KN, Deal JG, Deng YL, Dinh D, Engstrom LD, He M, Hoffman J, Hoffman RL, Johnson PS, Kania RS, Lam H, Lam JL, Le PT, Li Q, Lingardo L, Liu W, Lu MW, McTigue M, Palmer CL, Richardson PF, Sach NW, Shen H, Smeal T, Smith GL, Stewart AE, Timofeevski S, Tsaparikos K, Wang H, Zhu H, Zhu J, Zou HY, Edwards MP. Huang Q, et al. Among authors: tsaparikos k. J Med Chem. 2014 Feb 27;57(4):1170-87. doi: 10.1021/jm401805h. Epub 2014 Feb 6. J Med Chem. 2014. PMID: 24432909 Free article.
PF-06463922, an ALK/ROS1 Inhibitor, Overcomes Resistance to First and Second Generation ALK Inhibitors in Preclinical Models.
Zou HY, Friboulet L, Kodack DP, Engstrom LD, Li Q, West M, Tang RW, Wang H, Tsaparikos K, Wang J, Timofeevski S, Katayama R, Dinh DM, Lam H, Lam JL, Yamazaki S, Hu W, Patel B, Bezwada D, Frias RL, Lifshits E, Mahmood S, Gainor JF, Affolter T, Lappin PB, Gukasyan H, Lee N, Deng S, Jain RK, Johnson TW, Shaw AT, Fantin VR, Smeal T. Zou HY, et al. Among authors: tsaparikos k. Cancer Cell. 2015 Jul 13;28(1):70-81. doi: 10.1016/j.ccell.2015.05.010. Epub 2015 Jul 2. Cancer Cell. 2015. PMID: 26144315 Free PMC article.
Discovery of a highly potent, selective, orally bioavailable inhibitor of KAT6A/B histone acetyltransferases with efficacy against KAT6A-high ER+ breast cancer.
Sharma S, Chung CY, Uryu S, Petrovic J, Cao J, Rickard A, Nady N, Greasley S, Johnson E, Brodsky O, Khan S, Wang H, Wang Z, Zhang Y, Tsaparikos K, Chen L, Mazurek A, Lapek J, Kung PP, Sutton S, Richardson PF, Greenwald EC, Yamazaki S, Jones R, Maegley KA, Bingham P, Lam H, Stupple AE, Kamal A, Chueh A, Cuzzupe A, Morrow BJ, Ren B, Carrasco-Pozo C, Tan CW, Bhuva DD, Allan E, Surgenor E, Vaillant F, Pehlivanoglu H, Falk H, Whittle JR, Newman J, Cursons J, Doherty JP, White KL, MacPherson L, Devlin M, Dennis ML, Hattarki MK, De Silva M, Camerino MA, Butler MS, Dolezal O, Pilling P, Foitzik R, Stupple PA, Lagiakos HR, Walker SR, Hediyeh-Zadeh S, Nuttall S, Spall SK, Charman SA, Connor T, Peat TS, Avery VM, Bozikis YE, Yang Y, Zhang M, Monahan BJ, Voss AK, Thomas T, Street IP, Dawson SJ, Dawson MA, Lindeman GJ, Davis MJ, Visvader JE, Paul TA. Sharma S, et al. Among authors: tsaparikos k. Cell Chem Biol. 2023 Oct 19;30(10):1191-1210.e20. doi: 10.1016/j.chembiol.2023.07.005. Epub 2023 Aug 8. Cell Chem Biol. 2023. PMID: 37557181 Free article.
Antitumor Efficacy of the Dual PI3K/mTOR Inhibitor PF-04691502 in a Human Xenograft Tumor Model Derived from Colorectal Cancer Stem Cells Harboring a PIK3CA Mutation.
Fang DD, Zhang CC, Gu Y, Jani JP, Cao J, Tsaparikos K, Yuan J, Thiel M, Jackson-Fisher A, Zong Q, Lappin PB, Hayashi T, Schwab RB, Wong A, John-Baptiste A, Bagrodia S, Los G, Bender S, Christensen J, Vanarsdale T. Fang DD, et al. Among authors: tsaparikos k. PLoS One. 2013 Jun 27;8(6):e67258. doi: 10.1371/journal.pone.0067258. Print 2013. PLoS One. 2013. PMID: 23826249 Free PMC article.
Combined gemcitabine and CHK1 inhibitor treatment induces apoptosis resistance in cancer stem cell-like cells enriched with tumor spheroids from a non-small cell lung cancer cell line.
Fang DD, Cao J, Jani JP, Tsaparikos K, Blasina A, Kornmann J, Lira ME, Wang J, Jirout Z, Bingham J, Zhu Z, Gu Y, Los G, Hostomsky Z, Vanarsdale T. Fang DD, et al. Among authors: tsaparikos k. Front Med. 2013 Dec;7(4):462-76. doi: 10.1007/s11684-013-0270-6. Epub 2013 Jul 2. Front Med. 2013. PMID: 23820871
A CD3-bispecific molecule targeting P-cadherin demonstrates T cell-mediated regression of established solid tumors in mice.
Fisher TS, Hooper AT, Lucas J, Clark TH, Rohner AK, Peano B, Elliott MW, Tsaparikos K, Wang H, Golas J, Gavriil M, Haddish-Berhane N, Tchistiakova L, Gerber HP, Root AR, May C. Fisher TS, et al. Among authors: tsaparikos k. Cancer Immunol Immunother. 2018 Feb;67(2):247-259. doi: 10.1007/s00262-017-2081-0. Epub 2017 Oct 24. Cancer Immunol Immunother. 2018. PMID: 29067496 Free PMC article.
Combination of 4-1BB agonist and PD-1 antagonist promotes antitumor effector/memory CD8 T cells in a poorly immunogenic tumor model.
Chen S, Lee LF, Fisher TS, Jessen B, Elliott M, Evering W, Logronio K, Tu GH, Tsaparikos K, Li X, Wang H, Ying C, Xiong M, VanArsdale T, Lin JC. Chen S, et al. Among authors: tsaparikos k. Cancer Immunol Res. 2015 Feb;3(2):149-60. doi: 10.1158/2326-6066.CIR-14-0118. Epub 2014 Nov 11. Cancer Immunol Res. 2015. PMID: 25387892
PF-03814735, an orally bioavailable small molecule aurora kinase inhibitor for cancer therapy.
Jani JP, Arcari J, Bernardo V, Bhattacharya SK, Briere D, Cohen BD, Coleman K, Christensen JG, Emerson EO, Jakowski A, Hook K, Los G, Moyer JD, Pruimboom-Brees I, Pustilnik L, Rossi AM, Steyn SJ, Su C, Tsaparikos K, Wishka D, Yoon K, Jakubczak JL. Jani JP, et al. Among authors: tsaparikos k. Mol Cancer Ther. 2010 Apr;9(4):883-94. doi: 10.1158/1535-7163.MCT-09-0915. Epub 2010 Mar 30. Mol Cancer Ther. 2010. PMID: 20354118
Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.
Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M. Gomes B, et al. Among authors: tsaparikos k. Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19. Mol Cancer Ther. 2018. PMID: 30232146
Biochemical and pharmacological characterization of human c-Met neutralizing monoclonal antibody CE-355621.
Michaud NR, Jani JP, Hillerman S, Tsaparikos KE, Barbacci-Tobin EG, Knauth E, Putz H Jr, Campbell M, Karam GA, Chrunyk B, Gebhard DF, Green LL, Xu JJ, Dunn MC, Coskran TM, Lapointe JM, Cohen BD, Coleman KG, Bedian V, Vincent P, Kajiji S, Steyn SJ, Borzillo GV, Los G. Michaud NR, et al. Among authors: tsaparikos ke. MAbs. 2012 Nov-Dec;4(6):710-23. doi: 10.4161/mabs.22160. Epub 2012 Sep 24. MAbs. 2012. PMID: 23007574 Free PMC article.
13 results