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Page 1
Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.
Schönherr H, Ayaz P, Taylor AM, Casaletto JB, Touré BB, Moustakas DT, Hudson BM, Valverde R, Zhao S, O'Hearn PJ, Foster L, Sharon DA, Garfinkle S, Giordanetto F, Lescarbeau A, Kurukulasuriya R, Gerami-Moayed N, Maglic D, Bruderek K, Naik G, Gunaydin H, Mader MM, Boezio AA, McLean TH, Chen R, Wang Y, Shaw DE, Watters J, Bergstrom DA. Schönherr H, et al. Among authors: o hearn pj. Proc Natl Acad Sci U S A. 2024 Feb 6;121(6):e2317756121. doi: 10.1073/pnas.2317756121. Epub 2024 Feb 1. Proc Natl Acad Sci U S A. 2024. PMID: 38300868 Free PMC article.
RLY-4008, the First Highly Selective FGFR2 Inhibitor with Activity across FGFR2 Alterations and Resistance Mutations.
Subbiah V, Sahai V, Maglic D, Bruderek K, Touré BB, Zhao S, Valverde R, O'Hearn PJ, Moustakas DT, Schönherr H, Gerami-Moayed N, Taylor AM, Hudson BM, Houde DJ, Pal D, Foster L, Gunaydin H, Ayaz P, Sharon DA, Goyal L, Schram AM, Kamath S, Sherwin CA, Schmidt-Kittler O, Jen KY, Ricard F, Wolf BB, Shaw DE, Bergstrom DA, Watters J, Casaletto JB. Subbiah V, et al. Among authors: o hearn pj. Cancer Discov. 2023 Sep 6;13(9):2012-2031. doi: 10.1158/2159-8290.CD-23-0475. Cancer Discov. 2023. PMID: 37270847 Free PMC article.
Discovery of a Selective Phosphoinositide-3-Kinase (PI3K)-γ Inhibitor (IPI-549) as an Immuno-Oncology Clinical Candidate.
Evans CA, Liu T, Lescarbeau A, Nair SJ, Grenier L, Pradeilles JA, Glenadel Q, Tibbitts T, Rowley AM, DiNitto JP, Brophy EE, O'Hearn EL, Ali JA, Winkler DG, Goldstein SI, O'Hearn P, Martin CM, Hoyt JG, Soglia JR, Cheung C, Pink MM, Proctor JL, Palombella VJ, Tremblay MR, Castro AC. Evans CA, et al. ACS Med Chem Lett. 2016 Jul 22;7(9):862-7. doi: 10.1021/acsmedchemlett.6b00238. eCollection 2016 Sep 8. ACS Med Chem Lett. 2016. PMID: 27660692 Free PMC article.
Synthetic silvestrol analogues as potent and selective protein synthesis inhibitors.
Liu T, Nair SJ, Lescarbeau A, Belani J, Peluso S, Conley J, Tillotson B, O'Hearn P, Smith S, Slocum K, West K, Helble J, Douglas M, Bahadoor A, Ali J, McGovern K, Fritz C, Palombella VJ, Wylie A, Castro AC, Tremblay MR. Liu T, et al. J Med Chem. 2012 Oct 25;55(20):8859-78. doi: 10.1021/jm3011542. Epub 2012 Oct 12. J Med Chem. 2012. PMID: 23025805
Discovering the anti-cancer potential of non-oncology drugs by systematic viability profiling.
Corsello SM, Nagari RT, Spangler RD, Rossen J, Kocak M, Bryan JG, Humeidi R, Peck D, Wu X, Tang AA, Wang VM, Bender SA, Lemire E, Narayan R, Montgomery P, Ben-David U, Garvie CW, Chen Y, Rees MG, Lyons NJ, McFarland JM, Wong BT, Wang L, Dumont N, O'Hearn PJ, Stefan E, Doench JG, Harrington CN, Greulich H, Meyerson M, Vazquez F, Subramanian A, Roth JA, Bittker JA, Boehm JS, Mader CC, Tsherniak A, Golub TR. Corsello SM, et al. Among authors: o hearn pj. Nat Cancer. 2020 Feb;1(2):235-248. doi: 10.1038/s43018-019-0018-6. Epub 2020 Jan 20. Nat Cancer. 2020. PMID: 32613204 Free PMC article.