Abstract
Exploring Novel Opportunities for Aureolic Acids as Anticancer Drugs
Highlights
The aureolic acids are a family of polyglycosylated aromatic polyketides bearing a tricyclic core that includes mithramycin A, chromomycin A3, olivomycin A, UCH9 and durhamycin A (Figure 1) [1]
Mithramycin A (MTM) and chromomycin A3 (CRM) are the most representative members of the family, MTM being approved as an anticancer drug in 1970, and used originally for the treatment of several types of cancer, Paget’s bone disease and hypercalcemia [5,6,7]
MTM has just been identified as the top candidate from a high-throughput screening of over 50,000 compounds to inhibit the aberrant EWS-FLI1 fusion transcription factor, associated to the malignant transformation and progression of Ewing sarcoma family of tumors (ESFTs) [15]
Summary
The aureolic acids are a family of polyglycosylated aromatic polyketides bearing a tricyclic core that includes mithramycin A, chromomycin A3, olivomycin A, UCH9 and durhamycin A (Figure 1) [1]. Exploring Novel Opportunities for Aureolic Acids as Anticancer Drugs Regarding CRM, despite being 10 times more active than MTM against several tumor cell lines, it has been limited clinically due to severe toxicity [8].
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