Definition

A small molecule inhibitor of the Sec61 translocon, with potential antineoplastic activity. Upon administration, Sec61 inhibitor KZR-261 targets Sec61 and inhibits the translocation of multiple secreted and transmembrane proteins into the endoplasmic reticulum (ER) through the Sec61 channel. This inhibits the secretion pathway and prevents the expression of these secreted and transmembrane proteins, which may include cytokines, oncogenic receptors, angiogenic factors and immune checkpoint molecules that are involved in tumor growth, metastasis and immune evasion. This may result in anti-tumor activities. Sec61 translocon plays a key role in regulating the translocation of secreted and transmembrane proteins into the ER.