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pro vyhledávání: '"Blagg, J."'
Akademický článek
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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
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
http://europepmc.org/articles/PMC6580095
Autor:
Meyers, J., Chessum, N.E.A., Ali, S., Mok, N.Y., Wilding, B., Pasqua, A.E., Rowlands, M., Tucker, M.J., Evans, L.E., Rye, C.S., O'Fee, L., Le Bihan, Y.V., Burke, R., Carter, M., Workman, P., Blagg, J., Brown, N., van Montfort, R.L.M., Jones, K., Cheeseman, M.D.
Publikováno v:
'ACS Medicinal Chemistry Letters ', vol: 9, pages: 1199-1204 (2018)
Polypharmacology is often a key contributor to the efficacy of a drug, but is also a potential risk. We investigated two hits discovered via a cell-based phenotypic screen, the CDK9 inhibitor CCT250006 (1) and the pirin ligand CCT245232 (2), to estab
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=illesrfpubli::8483914b8d324d4b9c754866455e6a23
https://epn-library.esrf.fr/flora/jsp/index_view_direct_anonymous.jsp?record=doc:PUB_ESRF:51196
https://epn-library.esrf.fr/flora/jsp/index_view_direct_anonymous.jsp?record=doc:PUB_ESRF:51196
Akademický článek
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The conformation of the activation loop (T-loop) of protein kinases underlies enzymatic activity and influences the binding of small-molecule inhibitors. By using single-molecule fluorescence spectroscopy, we have determined that phosphorylated Auror
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=od______1032::0d3d9356b023a239855ef7dbe6f9da60
http://hdl.handle.net/10044/1/49334
http://hdl.handle.net/10044/1/49334
Akademický článek
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Autor:
Moore, A. S.1,2,3 Andrew.Moore@icr.ac.uk, Blagg, J.2, Linardopoulos, S.2,4, Pearson, A. D. J.1,3
Publikováno v:
Leukemia (08876924). Apr2010, Vol. 24 Issue 4, p671-678. 8p. 1 Color Photograph, 3 Charts.
Treatment of (S)-(η6-N,N-dimethylamphetamine)Cr(CO)3, with n-butyllithium below -40°C gives a stable benzylic carbanion via loss of the pro-R-benzylic proton. Warming of this anion above -40°C gives (η6-E-β-methylstyrene)Cr(CO)3 via an ElcB type
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::54ef6f35dd9b56a2dc1cdc37a224c1e0
https://doi.org/10.1016/s0040-4020(01)90323-0
https://doi.org/10.1016/s0040-4020(01)90323-0