molecules of the month


WASp activator

in vivo antitumor activity

fortuitous scaffold hopping from ibrutinib

bioRxiv, 25 November 2022

Institute of Oncology Research, Bellinzona, CH

EG-011 chemical structure WASp activator- Institute of Oncology Research, Bellinzona, CH
3 mins read

WASp as a new target for hematological cancers. Wiskott-Aldrich syndrome protein (WASp) is a protein almost exclusively expressed in hematopoetic cells that promotes actin polymerization. The WAS gene plays an important but not fully understood role in human immune cell biology, illustrated by WASp deletion in B-cells inducing autoimmunity in WAS patients or 15% of patients with WAS mutations developing lymphoma in another study. Small molecules have been reported to modulate WASp function, as demonstrated by the elucidation of wiskostatin’s WASp inhibition MOA or the antiproliferative activity of the WASp degradation promoter, SMC #13, in lymphoma and leukemia models. However, tools for understanding WASp biology are still limited. WASp is phosphorylated by a variety of kinases resulting in different effects,…

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