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Table 2 LSD1 inhibitors’ effects on immune functions

From: LSD1: an emerging face in altering the tumor microenvironment and enhancing immune checkpoint therapy

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]