Identification of phenothiazine derivatives as UHM-binding inhibitors of early spliceosome assembly

Identification of phenothiazine derivatives as UHM-binding inhibitors of early spliceosome assembly

So far only a few compounds have been reported as splicing modulators. Here, the authors combine high-throughput screening, chemical synthesis, NMR, X-ray crystallography with functional studies and develop phenothiazines as inhibitors for the U2AF Homology Motif (UHM) domains of proteins that regul...

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Autores principales: Pravin Kumar Ankush Jagtap, Tomáš Kubelka, Komal Soni, Cindy L. Will, Divita Garg, Claudia Sippel, Tobias G. Kapp, Harish Kumar Potukuchi, Kenji Schorpp, Kamyar Hadian, Horst Kessler, Reinhard Lührmann, Felix Hausch, Thorsten Bach, Michael Sattler
Formato: article
Lenguaje:EN
Publicado: Nature Portfolio 2020
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Acceso en línea:https://doaj.org/article/816cddccf4d4425e993bdca998fb63bd
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Sumario:So far only a few compounds have been reported as splicing modulators. Here, the authors combine high-throughput screening, chemical synthesis, NMR, X-ray crystallography with functional studies and develop phenothiazines as inhibitors for the U2AF Homology Motif (UHM) domains of proteins that regulate splicing and show that they inhibit early spliceosome assembly on pre-mRNA substrates in vitro.

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