Protein-Protein Interactions
HDM2 with Small Molecule Inhibitor
Thermofluor screening allows the direct assessment of ligand binding to protein domains involved in protein-protein interactions without necessitating development of a custom ligand-displacement assay.
Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activat p53 in cells. Grasberger BL, et.al. J Med Chem. 2005 Feb 24;48(4):909-12. [Thermofluor discovery of compounds inhibiting protein:protein interactions] PMID: 15715460
1,4-Benzodiazepine-2,5-diones as small molecule antagonists of the HDM2-p53 interaction: discovery and SAR. Parks DJ, et.al. Bioorg Med Chem Lett. 2005 Feb 1;15(3):765-70. [Thermofluor discovery of compounds inhibiting protein:protein interactions] PMID: 15664854
Benzodiazepinedione inhibitors of the Hdm2:p53 complex suppress human tumor cell proliferation in vitro and sensitize tumors to doxorubicin in vivo. Koblish HK, et.al. Mol Cancer Ther. 2006 Jan;5(1):160-9. [Development of compounds inhibiting protein:protein interactions] PMID: 16432175
New inhibitors of prion replication that target the amyloid precursor. Charvériat M, et.al. J Gen Virol (2009) 90:1294-1301 [Fluorescence thermal shift assay for assessment of prion protein aggregation inhibitors] PMID: 19264641