Glutathione S-Transferase P (GSTP) known as a Phase II detoxification enzyme has more recently been identified as a modulator of MAP kinase-related cell-signaling pathways. It is known to be upregulated in many cancers including KRAS-driven tumors such as NSCLC. Here, Cina and colleagues demonstrate how an siRNA-based therapeutic formulated in a lipid nanoparticle (NBF-006) that enhances delivery to tumors led to tumor regression in a dose dependent manner in multiple in vivo models. Preclinical studies supported the advancement of NBF-006 into clinical studies. This advancement may enable future development of RNA therapeutics for the treatment of cancers.

The first-in-class N-myristoyltransferase inhibitor zelenirstat is currently undergoing phase IIa clinical trial evaluation. In AML, zelenirstat inhibits myristoylation, promoting the degradation of Src-family kinases and preventing signalling downstream of FLT3 and c-Kit receptors. Additionally, zelenirstat reduces mitochondrial complex I activity and AMPKß levels, leading to diminished oxidative phosphorylation, glycolysis and cellular ATP. Zelenirstat...

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