Atra for modulating pin1 activity and stability

摘要: The present disclosure describes how all-retinoic acid (ATRA) binds and inhibits Pin1 activity induces degradation of the activated monomer selectively in cancer cells. Identification binding mechanism ATRA with confirm specificity to residues PPIase active site, thus demonstrating that drug-induced ablation has potent anticancer activity, such as acute promyelocytic leukemia (APL), by inducing PML-RARa degradation, well against other types diseases are associated overexpression, aggressive triple negative breast cancer, lupus, asthma, cocaine addiction, among others, due their unique ability simultaneously block numerous cancer-driving pathways, relatively lower toxicity. also provides a rationale for developing sustained released ATRA-containing formulations. formulations may be used combinations existing therapies including chemotherapy or molecularly targeted drugs standard care.