PPAR-based DMLs for metabolic disease

DMLs that Inhibit Multiple Kinases for Treating Cancer 

The first kinase inhibitor to be developed for clinical use was imatinib 42, first marketed in 2001 for chronic myelogenous leukemia (CML). The clinical effectiveness of imatinib for the treatment of CML is now thought to be due to its multi-kinase activity, inhibiting PDGFR and c-KIT, in addition to its well known activity as a Bcr-Abl kinase inhibitor. Resistance to imatinib can become a problem due to mutations in the Abl gene. Dual Src/Abl inhibitors are currently of interest for the treatment of CML 

FIGURE 27.10 Dual PPARo/y agonist for treating metabolic disease. 

To enhance efficacy, various other kinase targets with a potential role in angiogenesis and tumor growth have been 

FIGURE 27.11 DMLs that inhibit multiple kinases for treating cancer. 

---