SI | Name | Category | Immunologic activity | Ref |
---|---|---|---|---|
1 | Phenelzine | Irreversible MAO inhibitor | • Inhibit FAD and CoREST binding to LSD1 • Increase transcription and activation of M1 macrophage signature genes • Decrease CAF-mediated resistance to chemotherapy | [56] |
2 | Bomedemstat | Irreversible LSD1 inhibitor | • Increase MHC-I expression • Increase CD8 T cell infiltration in tumor | [104] |
3 | ORY-1001 | Irreversible FAD binding LSD1 inhibitor | • Combined with PD-L1 antibody therapy it increases tumor cell killing | [37] |
4 | SP-2577 | Reversible LSD1 inhibitor | • Stimulate IFN-dependent antitumor immunity | [99] |
5 | GSK2879552 | Irreversible LSD1 inhibitor | • Prolong responses to PD-1 blockade | [43] |
6 | Tranylcypromine | Irreversible LSD1 inhibitor | • Increase MHC-I stabilization • Stimulate CD8 T cell activation | [69] |
7 | Amsacrine derivative compound 6x | LSD1 inhibitor | • Suppress expression of PD-L1 • Promote T-cell killing response | [112] |
8 | Chlorpromazine derivative compound 3 s | LSD1 inhibitor | • Suppress expression of PD-L1 • Promote T-cell killing response | [113] |