Blockade of Oncogenic NOTCH1 with the SERCA Inhibitor CAD204520 in T Cell Acute Lymphoblastic Leukemia.

doi:10.1016/j.chembiol.2020.04.002

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Article

Blockade of Oncogenic NOTCH1 with the SERCA Inhibitor CAD204520 in T Cell Acute Lymphoblastic Leukemia.

Cell chemical biology - 18 Jun 2020

Marchesini Matteo, Gherli Andrea, Montanaro Anna, Patrizi Laura, Sorrentino Claudia, Pagliaro Luca, Rompietti Chiara, Kitara Samuel, Heit Sabine, Olesen Claus E, Møller Jesper V, Savi Monia, Bocchi Leonardo, Vilella Rocchina, Rizzi Federica, Baglione Marilena, Rastelli Giorgia, Loiacono Caterina, La Starza Roberta, Mecucci Cristina, Stegmaier Kimberly, Aversa Franco, Stilli Donatella, Lund Winther Anne-Marie, Sportoletti Paolo, Bublitz Maike, Dalby-Brown William, Roti Giovanni

Abstract excerpt

The identification of SERCA (sarco/endoplasmic reticulum calcium ATPase) as a target for modulating gain-of-function NOTCH1 mutations in Notch-dependent cancers has spurred the development of this compound class for cancer therapeutics. Despite the innate toxicity challenge associated with SERCA inhibition, we identified CAD204520, a small molecule with better drug-like properties and reduced off-target Ca2+...

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PMID: 32386594
DOI: 10.1016/j.chembiol.2020.04.002
PMCID: PMC7305996

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