molecules of the month

Compound 39

oral GCN2 kinase inhibitor

TGI in LL2 syngeneic mouse model

SAR opt. from literature starting point

J. Med. Chem.

RAPT Therapeutics, South San Francisco, CA

Compound 39 chemical structure oral GCN2 kinase inhibitor - RAPT Therapeutics, South San Francisco, CA
5 mins read

Context. “Compound 39” (RAPT Therapeutics) is a general control nonderepressible 2 (GCN2) protein kinase inhibitor. As the master regulator of the integrated stress response triggered by cellular stress in the tumor microenvironment, GCN2 has been implicated in tumor progression and immune escape, making the kinase an attractive oncotarget. Notably, GCN2 expression triggers the activation of myeloid-derived suppressive cells (MDSCs), which have been associated with T cell suppression and poor prognosis in cancer patients. Targeting GCN2 presents a novel approach to inhibiting MDSCs-mediated immune suppression. However, skeptics of this approach, backed by findings from an in vivo mechanistic study, speculate that systemic targeting of GCN2 may harm the expression of specific immune cells, such as CD8+ T-cells. In an in vitro…

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