Research advances in kinase enzymes and inhibitors for cardiovascular disease treatment
| Autor: | Sana Saffour, Faris El-Dahiyat, Rand Shahin, Maha Habash, O. H. Shaheen |
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| Rok vydání: | 2017 |
| Předmět: |
0301 basic medicine
Drug Heart disease kinase inhibitor media_common.quotation_subject Context (language use) Review Pharmacology Biology 03 medical and health sciences medicine PKC Disease treatment Protein kinase C media_common ROCK II protein kinases Kinase cardiovascular GSK-3β medicine.disease MAPK inhibitor CaMK-II 030104 developmental biology Biotechnology |
| Zdroj: | Future Science OA |
| ISSN: | 2056-5623 |
| DOI: | 10.4155/fsoa-2017-0010 |
| Popis: | The targeting of protein kinases has great future potential for the design of new drugs against cardiovascular diseases (CVDs). Enormous efforts have been made toward achieving this aim. Unfortunately, kinase inhibitors designed to treat CVDs have suffered from numerous limitations such as poor selectivity, bad permeability and toxicity. So, where are we now in terms of discovering effective kinase targeting drugs to treat CVDs? Various drug design techniques have been approached for this purpose since the discovery of the inhibitory activity of Staurosporine against protein kinase C in 1986. This review aims to provide context for the status of several emerging classes of direct kinase modulators to treat CVDs and discuss challenges that are preventing scientists from finding new kinase drugs to treat heart disease. Lay abstract Various protein kinase enzymes are distinctly involved in diverse signal pathways involved in regulating cardiac function in health and disease states. In 1986, the inhibitory activity of Staurosporine against protein kinase C was revealed, and since then, the interest in finding active kinase inhibitors for use in medicine has grown. Numerous kinase inhibitors have been synthesized in the last two decades, yet none has found its way to the market as a cardiovascular disease treatment; thus, more scientific efforts are needed in this regard. |
| Databáze: | OpenAIRE |
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