Shaping current and future kinase drug discovery

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This special issue on "Shaping current and future kinase drug discovery" has been edited with the purpose of providing current achievements and future perspectives in the exciting field of kinase drug discovery. Kinase inhibitors are one of the most important targets for drug development. In recent years, the field of kinase drug discovery has resulted in unprecedented expansion of a new generation of drugs, with over 25 small molecules currently available in the market. As their rate of emergence in the market continues to grow, researchers in academia and industry have found new technologies to accelerate the discovery of novel kinase inhibitors. Protein kinases are enzymes that mediate phosphorylation of proteins which is one of the main post translational modifications of proteins. There is a transfer of a phosphate group in to certain parts of proteins that enable protein functionality. While phosphorylation is essential for maintaining a number of physiological activities inside cells, abnormal phosphorylation becomes a cause or a consequence of a disease. There are over 400 diseases including various cancers, Alzheimer’s disease and dementia that are reported to be linked with kinase mediated phosphorylation of proteins. Discovery of kinase inhibitors is an integral part of medicinal chemistry involving the design, chemical synthesis and development of new bio-active molecules such as drugs. The scope of this special issue addresses the urgent need to discover new inhibitors of kinases, trends in high throughput screening technologies for kinase assays, challenges in designing kinase inhibitors and their role in future needs of clinicians in the evolution of drugs.
The first review paper titled ‘Biosensors for screening kinase inhibitors’ is a survey of techniques used by the researchers to study phosphorylation of proteins for the development of kinase inhibitor screening. Highly sophisticated assays and devices have been reported in the literature to study kinase activity. The main emphasis of the review is to highlight the need to develop simple biosensors to study phosphorylation of proteins. The second paper titled ‘Heterocyclic analogues as kinase inhibitors” discusses new paradigms in kinase inhibition, primarily based on heterocyclic moieties which are important chemical constituents of kinase inhibitors. ‘Expert Opinion on Therapeutics implications of Superoxide Dismutase: Trends and Future Prospects’ studies the potential research of Superoxide Dismutase (SOD) in therapeutics including the trend of SOD research, potential patents filed, clinical trials performed, structural biology and cellular signaling associated with SOD. The last paper entitled ‘Structural basis for drug resistance mechanisms against EGFR’ highlights an important fundamental problem of drug resistance, which is developed very fast by the infected cell, while indirectly emphasizing the need to development new small molecule inhibitors. I hope that this special issue will increase the interest in the area of protein phosphorylation and kinases and will give the reader a consistent picture of the importance to speed up the discovery of kinase inhibitors. I am thankful to all the authors and the reviewers and express my sincere appreciation for their valuable contributions to this Issue. I also appreciate the Associate Editor Ambreen Irshad Sheikh for giving me the opportunity to organize and edit such an interesting issue and for her continuous assistance throughout the production process. I would like to dedicate this special issue to the hard work and continuous dedication of all academics and researchers around the world in their respective area of research.
Original languageEnglish
Place of PublicationUAE
Number of pages2469
ISBN (Electronic)1873-4294 (eISSN)
Publication statusPublished (in print/issue) - 22 Nov 2017


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