Title |
Rapamycin and mTOR kinase inhibitors
|
---|---|
Published in |
BMC Chemistry, May 2008
|
DOI | 10.1007/s12154-008-0003-5 |
Pubmed ID | |
Authors |
Lisa M. Ballou, Richard Z. Lin |
Abstract |
Mammalian target of rapamycin (mTOR) is a protein kinase that controls cell growth, proliferation, and survival. mTOR signaling is often upregulated in cancer and there is great interest in developing drugs that target this enzyme. Rapamycin and its analogs bind to a domain separate from the catalytic site to block a subset of mTOR functions. These drugs are extremely selective for mTOR and are already in clinical use for treating cancers, but they could potentially activate an mTOR-dependent survival pathway that could lead to treatment failure. By contrast, small molecules that compete with ATP in the catalytic site would inhibit all of the kinase-dependent functions of mTOR without activating the survival pathway. Several non-selective mTOR kinase inhibitors have been described and here we review their chemical and cellular properties. Further development of selective mTOR kinase inhibitors holds the promise of yielding potent anticancer drugs with a novel mechanism of action. |
X Demographics
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 2 | 17% |
Unknown | 10 | 83% |
Demographic breakdown
Type | Count | As % |
---|---|---|
Members of the public | 11 | 92% |
Practitioners (doctors, other healthcare professionals) | 1 | 8% |
Mendeley readers
Geographical breakdown
Country | Count | As % |
---|---|---|
United States | 8 | 1% |
United Kingdom | 5 | <1% |
Brazil | 3 | <1% |
India | 1 | <1% |
Germany | 1 | <1% |
France | 1 | <1% |
Poland | 1 | <1% |
Unknown | 647 | 97% |
Demographic breakdown
Readers by professional status | Count | As % |
---|---|---|
Student > Ph. D. Student | 131 | 20% |
Student > Bachelor | 118 | 18% |
Student > Master | 86 | 13% |
Researcher | 78 | 12% |
Student > Doctoral Student | 39 | 6% |
Other | 93 | 14% |
Unknown | 122 | 18% |
Readers by discipline | Count | As % |
---|---|---|
Agricultural and Biological Sciences | 186 | 28% |
Biochemistry, Genetics and Molecular Biology | 156 | 23% |
Medicine and Dentistry | 68 | 10% |
Immunology and Microbiology | 28 | 4% |
Pharmacology, Toxicology and Pharmaceutical Science | 26 | 4% |
Other | 75 | 11% |
Unknown | 128 | 19% |