PLX-4545 is an orally active, selective molecular glue degrader targeting IKZF2 . Through a molecular glue mechanism, PLX-4545 binds to CRBN , recruits IKZF2 to form a ternary complex, and promotes its ubiquitination and proteasomal degradation. This further converts inhibitory regulatory T cells (T reg ) into effector-like T cells, enhances CD8 + T cell responses, and modulates the T eff :T reg balance. PLX-4545 also increases the production of the inflammatory cytokine IL-2 and reduces the suppressive activity of T reg . PLX-4545 can be used in cancer immunotherapy research, and exhibits a synergistic effect when combined with immune checkpoint inhibitors such as anti- PD1 .
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