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. 2023 Feb 22;13(3):417. doi: 10.3390/biom13030417

Table 3.

Summary of representative p300 inhibitors and their main functions.

Name Structure Main Function Clinical Trial Landscape References
C646 graphic file with name biomolecules-13-00417-i001.jpg C646 regulates tumour cell drug resistance in cancers such as prostate cancer. C646 can enhance the antitumour activity in colorectal cancer by blocking the acetylation of TRIB3 and promoting the degradation of TRIB3. C646 can block the tumour cell cycle, induce tumour cell apoptosis, and inhibit tumour cell proliferation and growth in lung cancer and melanoma N/A [108,122,130]
A485 graphic file with name biomolecules-13-00417-i002.jpg A485 regulates antitumour activity in a variety of solid tumours such as melanoma and prostate cancer and in haematological tumours (such as multiple myeloma, acute myeloid leukaemia, and non-Hodgkin lymphoma). Combination of an anti-PD-L1 antibody with A485 can further enhance its antitumour efficacy N/A [70,124,133,139]
CCS1477 graphic file with name biomolecules-13-00417-i003.jpg CCS1477 can exert anticancer effects in prostate cancer by decreasing AR expression and regulating C-MYC gene expression Phase I/IIa clinical trial for patients with advanced solid tumours [78]
B029-2 graphic file with name biomolecules-13-00417-i004.jpg B029-2 can inhibit glycolysis, induce tumour cell cycle arrest, and inhibit tumour cell proliferation, thus delaying the malignant progression of liver cancer N/A [71]
B026 graphic file with name biomolecules-13-00417-i005.jpg B026 can significantly inhibit the expression of MYC in leukaemia cell lines and lymphoma cell lines and significantly decrease the level of H3K27Ac, and it has better effects and stability than A485. In addition, B026 can inhibit the proliferation of prostate cancer Cells N/A [140]
CCT077791 graphic file with name biomolecules-13-00417-i006.jpg CCT077791 treatment for 24 h inhibited colon cancer cell proliferation by reducing the H3 and H4 acetylation levels in HCT116 and HT29 cells N/A [105]
CBP30 graphic file with name biomolecules-13-00417-i007.jpg CBP30 can impair Treg differentiation and inhibit their function, which in turn enhances antitumor immune function and exerts antitumour effects. CBP30 also inhibits human Th17 responses N/A [137,141]