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From Pyrazolones to Azaindoles: Evolution of Active-Site SHP2 Inhibitors Based on Scaffold Hopping and Bioisosteric Replacement.
Mostinski Y, Heynen GJJE, López-Alberca MP, Paul J, Miksche S, Radetzki S, Schaller D, Shanina E, Seyffarth C, Kolomeets Y, Ziebart N, de Schryver J, Oestreich S, Neuenschwander M, Roske Y, Heinemann U, Rademacher C, Volkamer A, von Kries JP, Birchmeier W, Nazaré M. Mostinski Y, et al. Among authors: heynen gjje. J Med Chem. 2020 Dec 10;63(23):14780-14804. doi: 10.1021/acs.jmedchem.0c01265. Epub 2020 Nov 19. J Med Chem. 2020. PMID: 33210922
Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma.
Sun C, Wang L, Huang S, Heynen GJ, Prahallad A, Robert C, Haanen J, Blank C, Wesseling J, Willems SM, Zecchin D, Hobor S, Bajpe PK, Lieftink C, Mateus C, Vagner S, Grernrum W, Hofland I, Schlicker A, Wessels LF, Beijersbergen RL, Bardelli A, Di Nicolantonio F, Eggermont AM, Bernards R. Sun C, et al. Nature. 2014 Apr 3;508(7494):118-22. doi: 10.1038/nature13121. Epub 2014 Mar 26. Nature. 2014. PMID: 24670642 Free article.
SUMOylation inhibition overcomes proteasome inhibitor resistance in multiple myeloma.
Heynen GJJE, Baumgartner F, Heider M, Patra U, Holz M, Braune J, Kaiser M, Schäffer I, Bamopoulos SA, Ramberger E, Murgai A, Ng YLD, Demel UM, Laue D, Liebig S, Krüger J, Janz M, Nogai A, Schick M, Mertins P, Müller S, Bassermann F, Krönke J, Keller U, Wirth M. Heynen GJJE, et al. Blood Adv. 2023 Feb 28;7(4):469-481. doi: 10.1182/bloodadvances.2022007875. Blood Adv. 2023. PMID: 35917568 Free PMC article.