This webpage was produced as an assignment for Genetics 564, an undergraduate capstone course at the University of Wisconsin-Madison.
What is chemical genetics?
Chemical genetics is the study of proteins and signal transduction pathways by screening of libraries of small molecules. This may elucidate small molecules that can permeate the cell membrane and bind to specific parts of proteins in a reversible manner. This is useful because these molecules can often be translated into drugs or offer information about protein structure.
- A chemical library is a set of chemicals that will be used in a specific assay.
- A focused library is more targeted, and may involve changing a molecule in small ways.
- A diversity-oriented library is more diverse, and may include molecules with many different properties.
Everolimus
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Everolimus is currently being studied for use in targeted therapy of several manifestations of TSC, including renal cell carcinomas, renal angiomyolipomas, subendymal giant cell astrocytomas [4]. Loss of TSC1/TSC2 (tumor suppressor genes) results in hyper-activation of mTORC1, resulting in aberrant growth and proliferation, and thus formation of these growths [4]. mTOR stands for mammalian target of rapamycin. Thus, evorolimus, a derivative of rapamycin is expected to abrogate growth by inhibiting mTORC1.
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References
[1] National Center for Biotechnology Information. PubChem Compound Database; CID=6442177. https://pubchem.ncbi.nlm.nih.gov/compound/6442177
[2] Drugs.com (2016). Afinitor Information from Drugs.com. Cerner Multum, Inc. https://www.drugs.com/afinitor.html
[3] Drugs.com (2015). Zortress Information from Drugs.com. Cerner Multum, Inc. https://www.drugs.com/zortress.html
[4] Kwiatkowski, David J et al. (2016) Response to Everolimus Is Seen in TSC-Associated SEGAs and Angiomyolipomas Independent of Mutation Type and Site in TSC1 and TSC2. European Journal of Human Genetics 23(12), 1665–1672.
Image References
Header: http://media.vocativ.com/photos/2016/02/drugs-pills-0323153180635513.jpg
Everolimus: https://pubchem.ncbi.nlm.nih.gov/compound/6442177
[1] National Center for Biotechnology Information. PubChem Compound Database; CID=6442177. https://pubchem.ncbi.nlm.nih.gov/compound/6442177
[2] Drugs.com (2016). Afinitor Information from Drugs.com. Cerner Multum, Inc. https://www.drugs.com/afinitor.html
[3] Drugs.com (2015). Zortress Information from Drugs.com. Cerner Multum, Inc. https://www.drugs.com/zortress.html
[4] Kwiatkowski, David J et al. (2016) Response to Everolimus Is Seen in TSC-Associated SEGAs and Angiomyolipomas Independent of Mutation Type and Site in TSC1 and TSC2. European Journal of Human Genetics 23(12), 1665–1672.
Image References
Header: http://media.vocativ.com/photos/2016/02/drugs-pills-0323153180635513.jpg
Everolimus: https://pubchem.ncbi.nlm.nih.gov/compound/6442177