Validating cancer drug targets through chemical genetics Journal Article
| Authors: | Burkard, M. E.; Jallepalli, P. V. |
| Article Title: | Validating cancer drug targets through chemical genetics |
| Abstract: | Targeted therapies for cancer promise to revolutionize treatment by specifically inactivating pathways needed for the growth of tumor cells. The most prominent example of such therapy is imatinib (Gleevec), which targets the BCR-ABL kinase and provides an effective low-toxicity treatment for chronic myelogenous leukemia. This success has spawned myriad efforts to develop similarly targeted drugs for other cancers. Unfortunately, the high expectations of these efforts have not yet been realized, likely due to the genetic diversity among and within tumors, as well as the complex and largely unpredictable interactions of drug-like compounds with innumerable targets that affect cellular and organismal metabolism. While improvements in sequencing technologies are beginning to address the first problem, solving the second problem requires methods for linking specific features of the cancer genome to their optimally targeted therapies. One approach, referred to as chemical genetics, accomplishes this by genetic control of chemical susceptibility. Chemical genetics is a crucial tool for the rational development of cancer drugs. © 2010 Elsevier B.V. |
| Keywords: | signal transduction; protein kinase b; gene mutation; gene translocation; mutation; clinical trial; review; sorafenib; bevacizumab; erlotinib; raf protein; sunitinib; drug efficacy; nonhuman; antineoplastic agents; drug targeting; neoplasm; animals; imatinib; stem cell factor receptor; unindexed drug; vasculotropin receptor; melanoma; breast cancer; epidermal growth factor receptor 2; lung cancer; antineoplastic activity; drug effect; drug resistance, neoplasm; drug discovery; inhibitor; dasatinib; protein tyrosine kinase; chronic myeloid leukemia; drug selectivity; drug specificity; phosphatidylinositol 3 kinase; cancer resistance; temsirolimus; protein kinase inhibitors; polo like kinase 1; colon cancer; gefitinib; pazopanib; chemical genetics; liver cancer; ras protein; flavopiridol; bcr abl protein; genes, ras; kidney cancer; nilotinib; k ras protein; drug sensitivity; antiangiogenic activity; lapatinib; mutagenesis; fibroblast growth factor receptor 2; resistance; cyclin dependent kinase 1; platelet derived growth factor beta receptor; kinase; b raf kinase inhibitor; molecularly targeted therapy; cyclin dependent kinase 2; cd135 antigen |
| Journal Title: | Biochimica et Biophysica Acta (BBA) - Reviews on Cancer |
| Volume: | 1806 |
| Issue: | 2 |
| ISSN: | 0304-419X |
| Publisher: | Elsevier B.V. |
| Date Published: | 2010-12-01 |
| Start Page: | 251 |
| End Page: | 257 |
| Language: | English |
| DOI: | 10.1016/j.bbcan.2010.08.002 |
| PUBMED: | 20708654 |
| PROVIDER: | scopus |
| PMCID: | PMC3028588 |
| DOI/URL: | |
| Notes: | --- - "Export Date: 20 April 2011" - "CODEN: BBACE" - "Source: Scopus" |
