New Frontiers in Kinases: Second Generation Inhibitors-Going beyond Cancer.

Abstract

It is a great pleasure to introduce the Special Issue “New Frontiers in Kinases: Second Generation Inhibitors”, which includes contributions from ACS Medicinal Chemistry Letters, Journal of Medicinal Chemistry, ACS Chemical Biology, and Biochemistry. The kinase area has been heavily studied with more than 500,000 published articles, the vast majority of which focus on cancer. We are now just beginning to unlock the potential of noncancer kinase targets. ACS Medicinal Chemistry Letters received an impressive number of high-quality submissions. Although it would go much beyond the scope of this editorial to comment in detail on all studies contained here, I would like to highlight a few representative studies that are very much in line with the theme and aims of this Issue: (a) Harrison et al. report on the “Discovery and Development of a Dual LIM-kinase and ROCK Inhibitor for the Treatment of Glaucoma”; (b) Rosse et al. present a Patent Highlight on “Novel Azaindazole Sulfonamides Inhibitors of Serum and Glucocorticoid Regulated Kinase”; (c) Thompson et al. in a Viewpoint speculate on the prospects for the development of Class II PI3K inhibitors; and (d) Goodwin et al. present an inhibitor mechanism study on the “Discovery of a Type III Inhibitor of LIM Kinase 2 that Binds in a DFG-out Conformation”. These representative studies provide a flavor of the diverse and exciting science in emerging areas assembled in this Special Issue. I would like to thank our authors for their many outstanding contributions. We also thank the numerous reviewers who, sometimes on rather short notice, diligently evaluated these manuscripts. Special thanks go to the Editors of ACS Medicinal Chemistry Letters and the editorial office staff for their continuous support of this project. Last but not least, we very much hope that the readers of ACS Medicinal Chemistry Letters will enjoy this Special Issue on New Frontiers on Kinases.