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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
Lipophilic Efficiency as an Important Metric in Drug Design.
Johnson TW, Gallego RA, Edwards MP. Johnson TW, et al. Among authors: gallego ra. J Med Chem. 2018 Aug 9;61(15):6401-6420. doi: 10.1021/acs.jmedchem.8b00077. Epub 2018 Apr 17. J Med Chem. 2018. PMID: 29589935 Review.
Multiple conformational states of the HPK1 kinase domain in complex with sunitinib reveal the structural changes accompanying HPK1 trans-regulation.
Johnson E, McTigue M, Gallego RA, Johnson TW, Timofeevski S, Maestre M, Fisher TS, Kania R, Sawasdikosol S, Burakoff S, Cronin CN. Johnson E, et al. Among authors: gallego ra. J Biol Chem. 2019 Jun 7;294(23):9029-9036. doi: 10.1074/jbc.AC119.007466. Epub 2019 Apr 24. J Biol Chem. 2019. PMID: 31018963 Free PMC article.
Randomized phase II trial of FOLFIRI-panitumumab compared with FOLFIRI alone in patients with RAS wild-type circulating tumor DNA metastatic colorectal cancer beyond progression to first-line FOLFOX-panitumumab: the BEYOND study (GEMCAD 17-01).
Aparicio J, Virgili Manrique AC, Capdevila J, Muñoz Boza F, Galván P, Richart P, Oliveres H, Páez D, Hernando J, Serrano S, Vera R, Hernandez-Yagüe X, Gallego RÁ, Riesco-Martinez MC, García de Albeniz X, Maurel J. Aparicio J, et al. Among authors: gallego ra. Clin Transl Oncol. 2022 Nov;24(11):2155-2165. doi: 10.1007/s12094-022-02868-x. Epub 2022 Jun 27. Clin Transl Oncol. 2022. PMID: 35761123 Free PMC article. Clinical Trial.