C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays

Autor: Le Bihan, Y-V, Lanigan, RM, Atrash, B, McLaughlin, MG, Velupillai, S, Malcolm, AG, England, KS, Ruda, GF, Mok, NY, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, JM, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, FI, Fedorov, O, Brennan, PE, Burke, R, Van Montfort, RLM, Rossanese, OW, Blagg, J, Bavetsias, V

Publikováno v: European Journal of Medicinal Chemistry
Le Bihan, Y-V, Lanigan, R M, Atrash, B, McLaughlin, M G, Velupillai, S, Malcolm, A G, England, K S, Ruda, G F, Mok, N Y, Tumber, A, Tomlin, K, Saville, H, Shehu, E, McAndrew, C, Carmichael, L, Bennett, J M, Jeganathan, F, Eve, P, Donovan, A, Hayes, A, Wood, F, Raynaud, F I, Fedorov, O, Brennan, P, Burke, R, van Montfort, R L M, Rossanese, O W, Blagg, J & Bavetsias, V 2019, ' C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-ones: Studies towards the identification of potent, cell penetrant Jumonji C domain containing histone lysine demethylase 4 subfamily (KDM4) inhibitors, compound profiling in cell-based target engagement assays ', European Journal of Medicinal Chemistry, vol. 177, pp. 316-337 . https://doi.org/10.1016/j.ejmech.2019.05.041

Residues in the histone substrate binding sites that differ between the KDM4 and KDM5 subfamilies were identified. Subsequently, a C8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one series was designed to rationally exploit these residue differences bet

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=pmid_dedup__::b23e38e79895cd396b4e21c1fb1c9678
http://europepmc.org/articles/PMC6580095

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Selective FLT3 inhibition of FLT3-ITD⁺ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patterns.

Autor: Moore, A S, Faisal, A, de Castro, D Gonzalez, Bavetsias, V, Sun, C, Atrash, B, Valenti, M, de Haven Brandon, A, Avery, S, Mair, D, Mirabella, F, Swansbury, J, Pearson, A D J, Workman, P, Blagg, J, Raynaud, F I, Eccles, S A, Linardopoulos, S

Publikováno v: Leukemia (08876924); Jul2012, Vol. 26 Issue 7, p1462-1470, 9p, 5 Graphs

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