Innovatively, a small molecule capable of remodeling cyclophilin A (CYPA), a cellular chaperone, was designed to form a high-affinity, selective CYPA: drug: KRAS tricomplex [63] showing promising anti-tumor efficacy in cell and PDX models, and leading to ongoing phase 1 clinical trials (NCT05462717 and NCT05379985). The gene discussed is PPIA; the disease is neoplasm.