Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

Fragment-based discovery of a chemical probe for the PWWP1 domain of NSD3

Here, we report the fragment-based discovery of BI-9321, a potent, selective and cellular active antagonist of the NSD3-PWWP1 domain. The human NSD3 protein is encoded by the WHSC1L1 gene located in the 8p11-p12 amplicon, frequently amplified in breast and squamous lung cancer. Recently, it was demo...

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Príomhchruthaitheoirí: Böttcher, J, Dilworth, D, Reiser, U, Neumüller, R, Schleicher, M, Petronczki, M, Zeeb, M, Mischerikow, N, Allali-Hassani, A, Szewczyk, M, Li, F, Kennedy, S, Vedadi, M, Barsyte-Lovejoy, D, Brown, P, Huber, K, Rogers, C, Wells, C, Fedorov, O, Rumpel, K, Zoephel, A, Mayer, M, Wunberg, T, Böse, D, Zahn, S, Arnhof, H, Berger, H, Reiser, C, Hörmann, A, Krammer, T, Corcokovic, M, Sharps, B, Winkler, S, Häring, D, Cockcroft, X, Fuchs, J, Müllauer, B, Weiss-Puxbaum, A, Gerstberger, T, Boehmelt, G, Vakoc, C, Arrowsmith, C, Pearson, M, McConnell, D
Formáid: Journal article
Teanga:English
Foilsithe / Cruthaithe: Nature Research 2019

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