What is chemical genomics?Chemical genomics is the study of chemical modifications, especially small molecules, that affects the genome. It has two approaches: forward and reverse. Forward chemical genetics are used to understand small molecules and its activity in the cell. In reverse chemical genetics, compound collections probe the protein of interest. The small molecules usually inhibit or (rarely) stimulate protein function [1].
The compounds can be searched through the website PubChem. |
Compounds for PFKFB3
Figure 1. PFKFB3 kinase inhibitor 69
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PubChem contains 4 compounds relative to PFKFB3. One of them is a novel inhibitor, PFKFB3 kinase inhibitor 69. Inhibitors of PFKFB3 are usually sought as a treatment for cancer, as PFKFB3’s function in the cell cycle is upregulated in cancer cells [2]. In the case of diabetes and pancreatic cells, the upregulation of PFKFB3 has been correlated with slower beta-cell death in response to the HIF1 alpha pathway. Thus, I suspect that inhibition of the gene is not desirable in diabetic models [3]. |
Reference
[1] Thorpe DS. Forward & reverse chemical genetics using SPOS-based combinatorial chemistry. Comb Chem High Throughput Screen. 2003;6(7):623-647. doi:10.2174/138620703771981205
[2]Lu L, Chen Y, Zhu Y. The molecular basis of targeting PFKFB3 as a therapeutic strategy against cancer. Oncotarget. 2017;8(37):62793-62802. Published 2017 Jul 24. doi:10.18632/oncotarget.19513
[3]Nomoto H, Pei L, Montemurro C, et al. Activation of the HIF1α/PFKFB3 stress response pathway in beta cells in type 1 diabetes. Diabetologia. 2020;63(1):149-161. doi:10.1007/s00125-019-05030-5
Image references
Header: https://www.nature.com/jhg/
Figure 1: https://pubchem.ncbi.nlm.nih.gov/compound/122690758
[1] Thorpe DS. Forward & reverse chemical genetics using SPOS-based combinatorial chemistry. Comb Chem High Throughput Screen. 2003;6(7):623-647. doi:10.2174/138620703771981205
[2]Lu L, Chen Y, Zhu Y. The molecular basis of targeting PFKFB3 as a therapeutic strategy against cancer. Oncotarget. 2017;8(37):62793-62802. Published 2017 Jul 24. doi:10.18632/oncotarget.19513
[3]Nomoto H, Pei L, Montemurro C, et al. Activation of the HIF1α/PFKFB3 stress response pathway in beta cells in type 1 diabetes. Diabetologia. 2020;63(1):149-161. doi:10.1007/s00125-019-05030-5
Image references
Header: https://www.nature.com/jhg/
Figure 1: https://pubchem.ncbi.nlm.nih.gov/compound/122690758
This web page was produced as an assignment for Genetics 564, an undergraduate capstone course at UW-Madison
Haeun Lee
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Haeun Lee
[email protected]
[email protected]