New Insights into Kinase Inhibitors II
A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Bioorganic Chemistry".
Deadline for manuscript submissions: 31 March 2025 | Viewed by 3104
Special Issue Editor
2. Dipartimento Salute della Donna e del Bambino, Università degli Studi di Padova, Padua, Italy
Interests: anticancer compounds; chemotherapy resistance; kinase inhibitors; antimitotic compounds; cancer pharmacology
Special Issues, Collections and Topics in MDPI journals
Special Issue Information
Dear Colleagues,
This issue is a continuation of the previous successful Special Issue “New Insights into Kinase Inhibitors”.
In the last 30 years, kinases have been widely studied as drug targets to inhibit proliferation and angiogenesis in cancer therapy. Kinase inhibitors now represent one of the major classes of chemotherapeutics, with 52 kinase inhibitors having been approved as anticancer agents.
To date, 538 kinases are found to be active in the human body, where they are responsible for the phosphorylation of up to one-third of the proteome in controlling migration, survival, proliferation, and other processes via phosphorylation cascades. Moreover, aberrant kinase activity has been described to have an important role not only in cancer but also in inflammatory, degenerative, immunological, metabolic, and cardiovascular diseases.
Although their druggability and clinical safety profile make kinases attractive targets, the majority of kinases are still unexplored, and the field of kinase inhibitors is still growing.
This Special Issue will highlight new insights into the discovery of new kinase inhibitors, from the investigation of new targets to the identification of novel small molecules. Contributions to this issue, both in the form of original articles or reviews, may focus on powerful strategies and technological advances in the synthesis of more efficient and selective compounds, new strategies to overcome kinase inhibitors resistance, and improvements regarding the use of kinase inhibitors in oncology and other pathologies, in which therapeutic combinations with less toxic and off-target effects are considered.
Dr. Roberta Bortolozzi
Guest Editor
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Keywords
- kinase inhibitors
- kinase inhibitors chemistry
- therapy resistance
- combination therapy
- antitumoral activity
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Related Special Issues
- New Insights into Kinase Inhibitors II in Molecules (1 article)
- New Insights into Kinase Inhibitors II in Molecules (1 article)
Planned Papers
The below list represents only planned manuscripts. Some of these manuscripts have not been received by the Editorial Office yet. Papers submitted to MDPI journals are subject to peer-review.
Title: Clinical Impact of Kinase Inhibitors in various Central Nervous System Disorders
Authors: Rishi M. Nadar1, Suhrud Pathak1, Sindhu Ramesh1, Timothy Moore1, Jun Ren2,3, *, Muralikrishnan Dhanasekaran1*,
Affiliation: 1Department of Drug Discovery and Development, Auburn University Harrison School of Pharmacy, Auburn, AL, USA.
2Department of Cardiology, Zhongshan Hospital Fudan University, Shanghai, China.
3Department of Laboratory Medicine and Pathology, University of Washington, Seattle, WA, USA.
Abstract: Neurodegenerative diseases are currently incurable, irreversible, and debilitating neurological conditions caused by increased specific neuronal cell death in a well-defined region of the brain. Common neurodegenerative diseases include Alzheimer's (AD), Parkinson's disease (PD), and Huntington's disease (HD). Most neurodegenerative disorders affect the adult/elderly population of those in advanced ages of 65 years or older and are projected to escalate drastically in the future. AD is responsible for the majority of cases of disability and morbidity in the elderly and is the most prevalent cause of dementia worldwide. PD is the second most typical neurodegenerative disorder characterized by progressive loss of both motor and non-motor functions due to nigral dopaminergic neurodegeneration. Motor symptoms include bradykinesia, postural instability, rigidity, and tremors. At the same time, non-motor symptoms can present as mood disorders, anxiety, depression, and cognitive impairment, which occur before motor symptoms. While some cases of neurologic diseases are reversible and are related to depression, drug intoxication, and hormone imbalances, 80% of cases of neurodegenerative disorders are irreversible. A number of hypotheses have been advanced to describe the pathogenesis of neurodegenerative diseases, with one of the main current theories being the role of kinases. It is suggested that kinases have a substantial role in the etiopathology of major neurodegenerative diseases. Thus, kinases are a current novel drug target as supported by the significant kinase inhibitors being validated by in-silico, in vitro, in vivo, and clinical trials. The protein kinase gene family comprises more than five hundred gene families and represents nearly 2% of all human genes. Functionally, protein kinases assist the transfer of the terminal phosphate group of adenosine triphosphate (ATP) to an amino acid residue (serine, threonine, tyrosine) within a polypeptide chain. A large number of proteins (20%) may be altered by the activity of kinase activity which consequently results in a functional change of the target protein by altering cellular activity, location, or association with other proteins. Accordingly, protein kinases control a wide variety of cellular functions through the coordinated transmission and intensification of cellular stimuli into distinct biological responses through coordinated signal transduction cascades. Anomalous regulation of protein kinase activity results in abnormal protein deposition, oxidative stress, apoptosis, inflammation, excitotoxicity, and mitochondrial dysfunction associated with assorted predictable disease states such as cancer, inflammatory diseases, metabolic syndromes, autoimmune pathologies, and neurological/ neurodegenerative disorders. Thus, identifying appropriate kinase inhibitors that can cross the blood-brain barriers can significantly reduce neurodegeneration and improve healthcare. The current review article will establish the valuable clinical Impact of kinase Inhibitors on various neurodegenerative disorders.
