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Discovery of PF-07265028, A Selective Small Molecule Inhibitor of Hematopoietic Progenitor Kinase 1 (HPK1) for the Treatment of Cancer.
Gallego RA, Cho-Schultz S, Del Bel M, Dechert-Schmitt AM, Donaldson JS, He M, Jalaie M, Kania R, Matthews J, McTigue M, Tuttle JB, Risley H, Zhou D, Zhou R, Ahmad OK, Bernier L, Berritt S, Braganza J, Chen Z, Cianfrogna JA, Collins M, Costa Jones C, Cronin CN, Davis C, Dress K, Edwards M, Farrell W, France SP, Grable N, Johnson E, Johnson TW, Jones R, Knauber T, Lafontaine J, Loach RP, Maestre M, Miller N, Moen M, Monfette S, Morse P, Nager AR, Niosi M, Richardson P, Rohner AK, Sach NW, Timofeevski S, Tucker JW, Vetelino B, Zhang L, Nair SK. Gallego RA, et al. Among authors: rohner ak. J Med Chem. 2024 Dec 26;67(24):22002-22038. doi: 10.1021/acs.jmedchem.4c01930. Epub 2024 Dec 9. J Med Chem. 2024. PMID: 39651809 Clinical Trial.
Design and Synthesis of Functionally Active 5-Amino-6-Aryl Pyrrolopyrimidine Inhibitors of Hematopoietic Progenitor Kinase 1.
Gallego RA, Bernier L, Chen H, Cho-Schultz S, Chung L, Collins M, Del Bel M, Elleraas J, Costa Jones C, Cronin CN, Edwards M, Fang X, Fisher T, He M, Hoffman J, Huo R, Jalaie M, Johnson E, Johnson TW, Kania RS, Kraus M, Lafontaine J, Le P, Liu T, Maestre M, Matthews J, McTigue M, Miller N, Mu Q, Qin X, Ren S, Richardson P, Rohner A, Sach N, Shao L, Smith G, Su R, Sun B, Timofeevski S, Tran P, Wang S, Wang W, Zhou R, Zhu J, Nair SK. Gallego RA, et al. J Med Chem. 2023 Apr 13;66(7):4888-4909. doi: 10.1021/acs.jmedchem.2c02038. Epub 2023 Mar 20. J Med Chem. 2023. PMID: 36940470
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: rohner ak. 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.