| 生化机理 |
NVP-LCQ195 (AT9311; LCQ195) is a small molecule heterocyclic compound which inhibits CDK1, CDK2 and CDK5, as well as CDK3 and CDK9. Cell cycle regulators, such as cyclin-dependent kinases (CDKs), are appealing targets for multiple myeloma (MM) therapy given the increased proliferative rates of tumour cells in advanced versus early stages of MM. NVP-LCQ195 induced cell cycle arrest and eventual apoptotic cell death of MM cells, even at sub-μmol/l concentrations, spared non-malignant cells, and overcame the protection conferred to MM cells by stroma or cytokines of the bone marrow milieu. |
