Litcius/Paper detail

Small-Molecule Kinase Inhibitors for the Treatment of Nononcologic Diseases

Zhouling Xie, Xiaoxiao Yang, Yajun Duan, Jihong Han, Chenzhong Liao

2021Journal of Medicinal Chemistry94 citationsDOIOpen Access PDF

Abstract

Great successes have been achieved in developing small-molecule kinase inhibitors as anticancer therapeutic agents. However, kinase deregulation plays essential roles not only in cancer but also in almost all major disease areas. Accumulating evidence has revealed that kinases are promising drug targets for different diseases, including cancer, autoimmune diseases, inflammatory diseases, cardiovascular diseases, central nervous system disorders, viral infections, and malaria. Indeed, the first small-molecule kinase inhibitor for treatment of a nononcologic disease was approved in 2011 by the U.S. FDA. To date, 10 such inhibitors have been approved, and more are in clinical trials for applications other than cancer. This Perspective discusses a number of kinases and their small-molecule inhibitors for the treatment of diseases in nononcologic therapeutic fields. The opportunities and challenges in developing such inhibitors are also highlighted.

Topics & Concepts

KinaseSmall moleculeCancerDrug discoveryClinical trialDiseasePharmacologyDrugMedicineChemistryBioinformaticsBiologyInternal medicineBiochemistrySynthesis and biological activityCancer Mechanisms and TherapyClick Chemistry and Applications