Protein kinases are considered as attractive drug targets because of their direct involvement in several life-threatening diseases. The overexpression of kinases is reported in varying types of cancers, thus kinases are being targeted when designing and developing small-molecule inhibitors. This targeted, structure-based drug design is rapidly gaining momentum; several anticancer drugs that target specific kinases are under different stages of clinical trials. The new opportunities, developments and results in this field are almost unbelievable compared with the situation less than a decade ago. Hence, we propose to integrate the knowledge of kinase inhibitors and therapeutic potential with their implications in the clinical management of cancer and associated diseases.

The success in developing superior drugs targeting specific signalling molecules has had a significant impact on the pipelines of pharmaceutical companies, leading to the development of multiple marketed kinase inhibitors. Designing selective small molecules against kinases has the potential to offer better potency and selectivity than was previously achievable. In this issue, authors will discuss how the different classes of kinases are exploited as potential drug targets with a special focus on anticancer therapy. We also aim to focus on the mechanism of action of these potential kinase targeting drugs. Overall, the content will encompass the challenges and opportunities for future kinase inhibitor development for anticancer therapy.

Original papers, Review, Mini Review, Perspective, and General Commentaries are all welcome. The scope includes, but is not limited to the following topics:

• Structural features of kinases and their implication in drug discovery
• Anticancer compounds targeting kinases under clinical trials
• Approaches to develop kinase inhibitors in the realm of cancer therapeutics
• Clinical efficacy of kinase signalling in disease progression
• FDA approved anticancer kinase inhibitors: Future and challenges

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