…a fluorescent signal that indicates enzyme activity. Peptide Inhibitors Peptide inhibitors generally come in a few broad classes: substrate mimics, allosteric inhibitors, and protein-protein interaction (PPI) inhibitors. Substrate mimics are…
…and cMEPP Synthase (IspF). Additionally, EBI has expanded the tools of identifying potential inhibitors by creating “easy to use” enzyme assay kits to search for potential inhibitors at specific steps…
…al. 2020; PDB entry 7K2V). Model shows cryo-EM densities for predicted PIKfyve’s CCT (yellow) and kinase (blue) domains. Disease Association & PIKfyve Inhibitors PIKfyve has been associated with several diseases…
…and Inhibitors.” The Journal of Organic Chemistry 66(20): 6705. 2. Hast, M. A., C. B. Nichols, et al. (2011). “Structures of Cryptococcus neoformans Protein Farnesyltransferase Reveal Strategies for Developing Inhibitors…
The PI3-Kinase Activity Fluorescence Polarization Assay determines PI3-K activity through quantification of its product, PI(3,4,5)P3 (PIP3). Sample Type: in vitro determination of PI3-K activity in cancer tissues and cell lines…
…et al. “Synthesis, Structure-Activity Relationships, and Biological Evaluation of Fatty Alcohol Phosphates as Lysophosphatidic Acid Receptor Ligands, Activators of PPAR?, and Inhibitors of Autotaxin” J. Med. Chem. 2005, 48, 4919-4930…
…inhibitors for anti-cancer therapy. B13 (or D-NMAPPD) is a potent ceramidase inhibitor which causes aopotosis in a number of cell lines including colorectal, HL60, melanoma, and keratinocyes. References 1) A….
…Publications 1. Phan, R. M. and C. D. Poulter (2001). “Synthesis of (S)-Isoprenoid Thiodiphosphates as Substrates and Inhibitors.” The Journal of Organic Chemistry 66(20): 6705. 2. Lee, L. V., B….
…Selective Benzoxazepin Inhibitors of the ï¡-Isoform of Phosphoinositide 3-Kinase Culminating in the Identification of (S)-2-((2-(1-isopropyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)oxy)propanamide (GDC-0326).” J Med Chem 59(3): 985-1002. 3. Yin, Y., et al. (2019). “Design, synthesis and…
…small-molecule inhibitors for anti-cancer therapy. Ceranib-2 inhibits cellular CDase activity with an IC50 = 28 uM in SKOV3 cells and does not show significant cytotoxity up to 100uM. Incubations of…