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Cambinol is an investigational histone deacetylase inhibitor that may have future use in cancer treatment.
Cambinol is an investigational histone deacetylase inhibitor that may have future use in cancer treatment.
Cambinol inhibits the NAD-dependant deacetylases SIRT1 and SIRT2, members of a protein family known as sirtuins. Inhibiting SIRT1 and SIRT2 while cells are under stress increases acetylation of p53, Ku70, and Foxo3a. This inhibition sensitizes cells to the action of drugs like etoposide and paclitaxel, not just other drugs that damage DNA. Although the mechanism of this sensitizing is not defined, it is not dependent on p53, Ku70, or Foxo3a. The independent mechanism suggests the existence of more molecular targets. Cambinol is noncompetitive against NAD and competitive against H-4 peptide, substrates of SIRT2. Inhibiting SIRT2 increases the acetylation of tubulin. Cambinol also increases the acetylation of BCL6, a protein necessary for oncogenesis. Cambinol is also a weak inhibitor of SIRT5.
每项发明一条，涵盖美国、欧洲、PCT 与中国的同族专利。
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