Cheminfomatic-based Drug Discovery of Human Tyrosine Kinase Inhibitors
| Autor: | Anthony Wutoh, Terry-Elinor Reid, Xiang Simon Wang, Joseph M. Fortunak |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Drug
Models Molecular media_common.quotation_subject Quantitative Structure-Activity Relationship 02 engineering and technology Bioinformatics 01 natural sciences Receptor tyrosine kinase Article Food and drug administration Drug Discovery Medicine Humans Protein Kinase Inhibitors media_common biology Molecular Structure Drug discovery business.industry General Medicine Protein-Tyrosine Kinases 021001 nanoscience & nanotechnology 0104 chemical sciences 010404 medicinal & biomolecular chemistry Receptor tyrosine kinase inhibitor biology.protein Pharmacophore Signal transduction 0210 nano-technology business Tyrosine kinase |
| Zdroj: | Current topics in medicinal chemistry. 16(13) |
| ISSN: | 1873-4294 |
| Popis: | Receptor Tyrosine Kinases (RTKs) are essential components for regulating cell-cell signaling and communication events in cell growth, proliferation, differentiation, survival and metabolism. Deregulation of RTKs and their associated signaling pathways can lead to a wide variety of human diseases such as immunodeficiency, diabetes, arterosclerosis, psoriasis and cancer. Thus RTKs have become one of the most important drug targets families in recent decade. Pharmaceutical companies have dedicated their research efforts towards the discovery of small-molecule inhibitors of RTKs, many of which had been approved by the U.S. Food and Drug Administration (US FDA) or are currently in clinical trials. The great successes in the development of small-molecule inhibitors of RTKs are largely attributed to the use of modern cheminformatic approaches to identifying lead scaffolds. Those include the quantitative structure-activity relationship (QSAR) modeling, as well as the structure-, and ligand-based pharmacophore modeling techniques in this case. Herein we inspected the literature thoroughly in an effort to conduct a comparative analysis of major findings regarding the essential structure-activity relationships (SARs)/pharmacophore features of known active RTK inhibitors, most of which were collected from cheminformatic modeling approaches. |
| Databáze: | OpenAIRE |
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