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Yeast as a model system for anticancer drug discovery.
Simon JA, Bedalov A. Simon JA, et al. Among authors: bedalov a. Nat Rev Cancer. 2004 Jun;4(6):481-92. doi: 10.1038/nrc1372. Nat Rev Cancer. 2004. PMID: 15170450 Review. No abstract available.
Identification of inhibitors of chromatin modifying enzymes using the yeast phenotypic screens.
Newcomb B, Bedalov A. Newcomb B, et al. Among authors: bedalov a. Methods Mol Biol. 2009;548:145-60. doi: 10.1007/978-1-59745-540-4_8. Methods Mol Biol. 2009. PMID: 19521823 Free PMC article.
A multitude of enzymes that modify histones and remodel nucleosomes are required for the formation, maintenance, and propagation of the transcriptionally repressed chromatin state in eukaryotes. ...
A multitude of enzymes that modify histones and remodel nucleosomes are required for the formation, maintenance, and propagation of t
The androgen-regulated protease TMPRSS2 activates a proteolytic cascade involving components of the tumor microenvironment and promotes prostate cancer metastasis.
Lucas JM, Heinlein C, Kim T, Hernandez SA, Malik MS, True LD, Morrissey C, Corey E, Montgomery B, Mostaghel E, Clegg N, Coleman I, Brown CM, Schneider EL, Craik C, Simon JA, Bedalov A, Nelson PS. Lucas JM, et al. Among authors: bedalov a. Cancer Discov. 2014 Nov;4(11):1310-25. doi: 10.1158/2159-8290.CD-13-1010. Epub 2014 Aug 13. Cancer Discov. 2014. PMID: 25122198 Free PMC article.
By screening combinatorial peptide libraries, we identified a spectrum of TMPRSS2 substrates that include pro-hepatocyte growth factor (HGF). ...Chemical library screens identified a potent bioavailable TMPRSS2 inhibitor that suppressed prostate cancer metastasis in …
By screening combinatorial peptide libraries, we identified a spectrum of TMPRSS2 substrates that include pro-hepatocyte growth facto …
Identification and characterization of small-molecule inhibitors of hepsin.
Chevillet JR, Park GJ, Bedalov A, Simon JA, Vasioukhin VI. Chevillet JR, et al. Among authors: bedalov a. Mol Cancer Ther. 2008 Oct;7(10):3343-51. doi: 10.1158/1535-7163.MCT-08-0446. Mol Cancer Ther. 2008. PMID: 18852137 Free PMC article.
Hepsin is a type II transmembrane serine protease overexpressed in the majority of human prostate cancers. We recently demonstrated that hepsin promotes prostate cancer progression and metastasis and thus represents a potential therapeutic target. ...Four compounds …
Hepsin is a type II transmembrane serine protease overexpressed in the majority of human prostate cancers. We recently demonstrated t …
Pharmacogenetics: yeast lead the way.
Foss E, Bedalov A. Foss E, et al. Among authors: bedalov a. Chem Biol. 2006 Mar;13(3):236-8. doi: 10.1016/j.chembiol.2006.03.001. Chem Biol. 2006. PMID: 16638528
Their results suggest that drug responses are regulated by a limited number of loci, and that this system can identify clusters of functionally similar molecules....
Their results suggest that drug responses are regulated by a limited number of loci, and that this system can identify clusters of fu …
Antitumor activity of a small-molecule inhibitor of human silent information regulator 2 enzymes.
Heltweg B, Gatbonton T, Schuler AD, Posakony J, Li H, Goehle S, Kollipara R, Depinho RA, Gu Y, Simon JA, Bedalov A. Heltweg B, et al. Among authors: bedalov a. Cancer Res. 2006 Apr 15;66(8):4368-77. doi: 10.1158/0008-5472.CAN-05-3617. Cancer Res. 2006. PMID: 16618762
Hereby, we describe the identification of a compound we named cambinol that inhibits NAD-dependent deacetylase activity of human SIRT1 and SIRT2. ...Treatment of BCL6-expressing Burkitt lymphoma cells with cambinol as a single agent induced apoptosis, which was acco …
Hereby, we describe the identification of a compound we named cambinol that inhibits NAD-dependent deacetylase activity of human SIRT …
Identification of selective inhibitors of NAD+-dependent deacetylases using phenotypic screens in yeast.
Hirao M, Posakony J, Nelson M, Hruby H, Jung M, Simon JA, Bedalov A. Hirao M, et al. Among authors: bedalov a. J Biol Chem. 2003 Dec 26;278(52):52773-82. doi: 10.1074/jbc.M308966200. Epub 2003 Oct 8. J Biol Chem. 2003. PMID: 14534292
The two enzymes are highly homologous yet have different sensitivity to the small-molecule inhibitor splitomicin (compound 1) (Bedalov, A., Gatbonton, T., Irvine, W. ...A. (2001) Proc. Natl. Acad. Sci. U. S. A. 98, 15113-15118). We have now defined …
The two enzymes are highly homologous yet have different sensitivity to the small-molecule inhibitor splitomicin (compound 1) (Bedalov
Genetic basis of proteome variation in yeast.
Foss EJ, Radulovic D, Shaffer SA, Ruderfer DM, Bedalov A, Goodlett DR, Kruglyak L. Foss EJ, et al. Among authors: bedalov a. Nat Genet. 2007 Nov;39(11):1369-75. doi: 10.1038/ng.2007.22. Epub 2007 Oct 21. Nat Genet. 2007. PMID: 17952072
A number of studies have recently shown that messenger RNA levels vary among individuals of a species and that genetic linkage analysis can be used to identify quantitative trait loci that influence these levels. ...Here we describe a label-free, mass spectro
A number of studies have recently shown that messenger RNA levels vary among individuals of a species and that genetic linkage
Telomere length as a quantitative trait: genome-wide survey and genetic mapping of telomere length-control genes in yeast.
Gatbonton T, Imbesi M, Nelson M, Akey JM, Ruderfer DM, Kruglyak L, Simon JA, Bedalov A. Gatbonton T, et al. Among authors: bedalov a. PLoS Genet. 2006 Mar;2(3):e35. doi: 10.1371/journal.pgen.0020035. Epub 2006 Mar 17. PLoS Genet. 2006. PMID: 16552446 Free PMC article.
Furthermore, we crossed a wild isolate to a laboratory strain and analyzed telomere length in 122 progeny. Genome-wide linkage analysis among these segregants revealed two loci that account for 30%-35% of telomere length-variation between the strains. These findings …
Furthermore, we crossed a wild isolate to a laboratory strain and analyzed telomere length in 122 progeny. Genome-wide linkage …
Identification and characterization of Sir2 inhibitors through phenotypic assays in yeast.
Posakony J, Hirao M, Bedalov A. Posakony J, et al. Among authors: bedalov a. Comb Chem High Throughput Screen. 2004 Nov;7(7):661-8. doi: 10.2174/1386207043328346. Comb Chem High Throughput Screen. 2004. PMID: 15578928 Review.
Yeast Sir2 is a defining member of a large family of protein deacetylases found in organisms ranging from bacteria to humans. ...However, years of extensive research did generate a large body of knowledge about the cellular roles of Sir2 in yeast long before …
Yeast Sir2 is a defining member of a large family of protein deacetylases found in organisms ranging from bacteria to humans. …
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