Publications by authors named "Baha'a Jabali"
Aberrant RET kinase signaling is activated in numerous cancers including lung, thyroid, breast, pancreatic, and prostate. Recent approvals of selective RET inhibitors, pralsetinib and selpercatinib, has shifted the focus of RET kinase drug discovery programs towards the development of selective inhibitors. However, selective inhibitors invariably lose efficacy as the selective nature of the inhibitor places Darwinian-like pressure on the tumor to bypass treatment through the selection of novel oncogenic drivers.
View Article and Find Full Text PDFArticle Synopsis
- The kinome's drug discovery methods have evolved significantly since imatinib, the first small molecule kinase inhibitor was approved.
- Macrocycles are gaining popularity for their ability to enhance drug properties, as shown by FDA-approved drugs like lorlatinib, pacritinib, and repotrectinib.
- This review emphasizes the clinical successes of macrocycles in targeting kinases, proving that macrocyclization is a validated strategy for drug discovery in this area.