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The LET7(K59D) or LET7(Q440K) single mutant relieved LET7 autoinhibition, resulting in increased phosphatase activities
Fukuchi, M
Estrogen receptor antagonist ICI182,780 exacerbates ischemic injury in female mouse
The oral small-molecule inhibitor INCB001158 (CB-1158), targeting this axis, has entered first-inhuman phase I studies and has been explored in combination with PD-1 inhibitors, suggesting that relieving substrate depletion-driven immunosuppression is clinically feasible from a safety and pharmacodynamic perspective, although its therapeutic efficacy remains to be fully established (116)
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