Y. Barenholz

The beginning and advancement of most diseases are closely linked to the abnormal expression or aggregation of proteins.[1], [2] The conventional approach in drug discovery has been to develop small molecule inhibitors that can occupy the active pocket or binding site of the target protein, thereby impeding or blocking the function of pathogenic proteins.

Malignant tumor poses a serious threat to human health, with increasing morbidity and mortality in recent years [1], [2], [3], [4]. Currently, clinical antitumor treatments primarily consist of surgery, radiotherapy, chemotherapy, targeted therapy, and immunotherapy, all of which are focused on inhibiting tumor growth and only prolonging the survival of tumor patients slightly [5], [6].

Pyroptosis is a gasdermin-triggered programmed cell death paradigm with the release of inflammatory substances, inspiring new insights into alleviating immunosuppression and promote a systemic immune response [1], [2], [3], [4]. The general mechanism is considered as the cleavage of gasdermins by activated caspases, and the released gasdermin-N punch holes in the cell membrane [5], [6], [7].