The dysregulation of protein kinase activity is associated with several diseases, including cancer. Thus, protein kinases represent one of the most promising drug targets in the fight against various types of malignancy. Approximately 538 kinases are encoded in the human genome and are involved in essential biological and cellular processes. The clinical efficacy of imatinib, the first drug to specifically target the Bcr-Abl tyrosine kinase and to be approved by the Food and Drug Administration (FDA) in 2001 for the treatment of chronic myeloid leukemia, paved the way for the development of small molecules as protein kinase inhibitors (KIs) in cancer treatment. There are currently 72 FDA-approved therapeutic agents targeting kinases and 62 of these drugs are used in targeted cancer therapy.
Despite the encouraging results obtained so far, the clinical use of KIs has many limitations such as drug resistance, toxicity and compromised efficacy. Therefore, the identification of novel, small molecule KIs still represents an unmet clinical need and a tricky challenge to be addressed. Much effort should be devoted to the search of new kinase targets for small-molecule inhibitors, also by using genomic analysis to find patient-specific therapeutic targets, as required by a precision medicine approach. On the other hand, it is important to refine new kinase inhibitors by high-throughput screening techniques as well as computational modelling studies. This Research Topic focuses on novel, small molecules targeting protein kinases in cancer treatment.
We welcome Original Research, Review, Mini Review and Perspective articles on themes including, but not limited to:
• Design and synthesis of kinase inhibitors including SAR and mechanism of action
• Lead optimization to increase the potency and selectivity against the drug target
• In vitro and in vivo biological evaluation
• Recent advances in multitarget drugs targeting protein kinases
• Molecular modelling studies on the interactions of new drug(s) with their target(s)
• Binding interaction studies using X-ray crystallography structures
The dysregulation of protein kinase activity is associated with several diseases, including cancer. Thus, protein kinases represent one of the most promising drug targets in the fight against various types of malignancy. Approximately 538 kinases are encoded in the human genome and are involved in essential biological and cellular processes. The clinical efficacy of imatinib, the first drug to specifically target the Bcr-Abl tyrosine kinase and to be approved by the Food and Drug Administration (FDA) in 2001 for the treatment of chronic myeloid leukemia, paved the way for the development of small molecules as protein kinase inhibitors (KIs) in cancer treatment. There are currently 72 FDA-approved therapeutic agents targeting kinases and 62 of these drugs are used in targeted cancer therapy.
Despite the encouraging results obtained so far, the clinical use of KIs has many limitations such as drug resistance, toxicity and compromised efficacy. Therefore, the identification of novel, small molecule KIs still represents an unmet clinical need and a tricky challenge to be addressed. Much effort should be devoted to the search of new kinase targets for small-molecule inhibitors, also by using genomic analysis to find patient-specific therapeutic targets, as required by a precision medicine approach. On the other hand, it is important to refine new kinase inhibitors by high-throughput screening techniques as well as computational modelling studies. This Research Topic focuses on novel, small molecules targeting protein kinases in cancer treatment.
We welcome Original Research, Review, Mini Review and Perspective articles on themes including, but not limited to:
• Design and synthesis of kinase inhibitors including SAR and mechanism of action
• Lead optimization to increase the potency and selectivity against the drug target
• In vitro and in vivo biological evaluation
• Recent advances in multitarget drugs targeting protein kinases
• Molecular modelling studies on the interactions of new drug(s) with their target(s)
• Binding interaction studies using X-ray crystallography structures
