Research

The ECBDC capabilities enable rapid exploration of biological systems through high throughput biology and small molecule screening in a large scale across biological disciplines and across disease types. Example collaborative research projects from the center are given below.

Johns MA, Meyerkord-Belton CL, Du Y, Fu H. (2014) The Emory Chemical Biology Discovery Center: leveraging academic innovation to advance novel targets through HTS and beyond.  Comb Chem High Throughput Screen. 2014 Mar;17(3):290-6. PMID: 24409950

Cancer

Gu L, Zhang H, Liu T, Zhou S, Du Y, Xiong J, Yi S, Qu CK, Fu H, Zhou M. (2016) Discovery of Dual Inhibitors of MDM2 and XIAP for Cancer Treatment. Cancer Cell. 2016 Oct 10;30(4):623-636. doi: 10.1016/j.ccell.2016.08.015. PMID: 27666947

Li Z, Ivanov AA, Su R, Gonzalez-Pecchi V, Qi Q, Liu S, Webber P, McMillan E, Rusnak L, Pham C, Chen X, Mo X, Revennaugh B, Zhou W, Marcus A, Harati S, Chen X, Johns MA, White MA, Moreno C, Cooper LA, Du Y, Khuri FR, Fu H. (2017) The OncoPPi network of cancer-focused protein-protein interactions to inform biological insights and therapeutic strategies. Nat Commun. 2017 Feb 16;8:14356. doi: 10.1038/ncomms14356. PMID: 28205554

Cencic R, Hall DR, Robert F, Du Y, Min J, Li L, Qui M, Lewis I, Kurtkaya S, Dingledine R, Fu H, Kozakov D, Vajda S, Pelletier J. (2011) Reversing chemoresistance by small molecule inhibition of the translation initiation complex eIF4F.  Proc Natl Acad Sci U S A. 2011 Jan 18;108(3):1046-51. doi: 10.1073/pnas.1011477108. Erratum in: Proc Natl Acad Sci U S A. 2011 Apr 19;108(16):6689. PMID:21191102

Tran TC, Sneed B, Haider J, Blavo D, White A, Aiyejorun T, Baranowski TC, Rubinstein AL, Doan TN, Dingledine R, Sandberg EM. (2007) Automated, quantitative screening assay for antiangiogenic compounds using transgenic zebrafish.  Cancer Res. 2007 Dec 1;67(23):11386-92. PMID: 18056466

Sun A, Moore TW, Gunther JR, Kim MS, Rhoden E, Du Y, Fu H, Snyder JP, Katzenellenbogen JA. (2011) Discovering small-molecule estrogen receptor α/coactivator binding inhibitors: high-throughput screening, ligand development, and models for enhanced potency. ChemMedChem. 2011 Apr 4;6(4):654-66. doi: 10.1002/cmdc.201000507. PMID: 21365764

Neurological diseases

Zhang Z, Obianyo O, Dall E, Du Y, Fu H, Liu X, Kang SS, Song M, Yu SP, Cabrele C, Schubert M, Li X, Wang JZ, Brandstetter H, Ye K. (2017) Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740. doi: 10.1038/ncomms14740. PMID:28345579

Jiang J, Ganesh T, Du Y, Quan Y, Serrano G, Qui M, Speigel I, Rojas A, Lelutiu N, Dingledine R. (2012) Small molecule antagonist reveals seizure-induced mediation of neuronal injury by prostaglandin E2 receptor subtype EP2.  Proc Natl Acad Sci U S A. 2012 Feb 21;109(8):3149-54. doi: 10.1073/pnas.1120195109. PMID: 22323596

Jiang J, Ganesh T, Du Y, Thepchatri P, Rojas A, Lewis I, Kurtkaya S, Li L, Qui M, Serrano G, Shaw R, Sun A, Dingledine R. (2010) Neuroprotection by selective allosteric potentiators of the EP2 prostaglandin receptor. Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2307-12. doi: 10.1073/pnas.0909310107. PMID:20080612

Hansen KB, Mullasseril P, Dawit S, Kurtkaya NL, Yuan H, Vance KM, Orr AG, Kvist T, Ogden KK, Le P, Vellano KM, Lewis I, Kurtkaya S, Du Y, Qui M, Murphy TJ, Snyder JP, Bräuner-Osborne H, Traynelis SF. (2010) Implementation of a fluorescence-based screening assay identifies histamine H3 receptor antagonists clobenpropit and iodophenpropit as subunit-selective N-methyl-D-aspartate receptor antagonists. J Pharmacol Exp Ther. 2010 Jun;333(3):650-62. doi: 10.1124/jpet.110.166256. PMID: 20197375

Infectious diseases

Giroud C, Du Y, Marin M, Min Q, Jui NT, Fu H, Melikyan GB. (2017) Screening and Functional Profiling of Small-Molecule HIV-1 Entry and Fusion Inhibitors. Assay Drug Dev Technol. 2017 Feb/Mar;15(2):53-63. doi: 10.1089/adt.2017.777. PMID: 28322598

Marin M, Du Y, Giroud C, Kim JH, Qui M, Fu H, Melikyan GB. (2015) High-Throughput HIV-Cell Fusion Assay for Discovery of Virus Entry Inhibitors.  Assay Drug Dev Technol. 2015 Apr;13(3):155-66. doi: 10.1089/adt.2015.639. PMID: 25871547

Yoon JJ, Chawla D, Paal T, Ndungu M, Du Y, Kurtkaya S, Sun A, Snyder JP, Plemper RK. (2008) High-throughput screening-based identification of paramyxovirus inhibitors. J Biomol Screen. 2008 Aug;13(7):591-608. doi: 10.1177/1087057108321089. PMID: 18626114

Cardiovascular diseases

Smith SM, Min J, Ganesh T, Diebold B, Kawahara T, Zhu Y, McCoy J, Sun A, Snyder JP, Fu H, Du Y, Lewis I, Lambeth JD. Ebselen and congeners inhibit NADPH oxidase 2-dependent superoxide generation by interrupting the binding of regulatory subunits.  Chem Biol. 2012 Jun 22;19(6):752-63. doi: 10.1016/j.chembiol.2012.04.015. PMID:22726689

Cross-cutting areas

Horton JR, Liu X, Gale M, Wu L, Shanks JR, Zhang X, Webber PJ, Bell JS, Kales SC, Mott BT, Rai G, Jansen DJ, Henderson MJ, Urban DJ, Hall MD, Simeonov A, Maloney DJ, Johns MA, Fu H, Jadhav A, Vertino PM, Yan Q, Cheng X. (2011) Structural Basis for KDM5A Histone Lysine Demethylase Inhibition by Diverse Compounds. Cell Chem Biol. 2016 Jul 21;23(7):769-81. doi: 10.1016/j.chembiol.2016.06.006. PMID:27427228

Zhao J, Du Y, Horton JR, Upadhyay AK, Lou B, Bai Y, Zhang X, Du L, Li M, Wang B, Zhang L, Barbieri JT, Khuri FR, Cheng X, Fu H. Discovery and structural characterization of a small molecule 14-3-3 protein-protein interaction inhibitor. Proc Natl Acad Sci U S A. 2011 Sep 27;108(39):16212-6. doi: 10.1073/pnas.1100012108. PMID: 21908710 

Du Y, Nikolovska-Coleska Z, Qui M, Li L, Lewis I, Dingledine R, Stuckey JA, Krajewski K, Roller PP, Wang S, Fu H. (2011) A dual readout F2 assay that combines fluorescence resonance energy transfer (FRET) and fluorescence polarization (FP) for monitoring bimolecular interactionsAssay Drug Devel Technol 9(4):382-93. doi: 10.1089/adt.2010.0292. Epub 2011 Mar 11. PMID:21395401

Thepchatri P, Min J, Ganesh T, Du Y, Lewis I, Kurtkaya S, Prussia A, Li L, Sneed B, Plemper RK, Fu H, Liotta DC, Snyder JP, Dingledine R, Sun A. (2009) Cancer and virus leads by HTS, chemical design and SEA data mining. Curr Top Med Chem. 2009;9(13):1159-71. Review. PMID: 19807668