Research Topics
Genomes and GenesSpecies | Aiming SunSummaryAffiliation: Emory University Country: USA Publications
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Publications
Monoketone analogs of curcumin, a new class of Fanconi anemia pathway inhibitorsIgor Landais
Department of Biochemistry and Molecular Biology, Oregon Health and Science University, Portland, USA
Mol Cancer 8:133. 2009..Curcumin was previously identified as a weak inhibitor of FANCD2-Ub. The aim of this study is to identify derivatives of curcumin with better activity and specificity...- Curcumin analog cytotoxicity against breast cancer cells: exploitation of a redox-dependent mechanismAiming Sun
Department of Chemistry, Emory University, Atlanta, GA 30322, United States
Bioorg Med Chem Lett 19:6627-31. 2009..Compared with the yellow, somewhat light sensitive and nearly water insoluble compounds 1 and 2, the glutathione conjugates represent a promising new series of stable and soluble anti-tumor pro-drugs... - Potent non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complexAiming Sun
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, USA
J Med Chem 51:3731-41. 2008..Elaborating on the preliminary structure-activity (SAR) study, the present work presents the synthesis and SAR of a much broader range of low nanomolar nonpeptidic MV inhibitors and speculates on the role of the CF 3 functionality... - Non-nucleoside inhibitors of the measles virus RNA-dependent RNA polymerase complex activity: Synthesis and in vitro evaluationAiming Sun
Department of Chemistry, 1515 Dickey Drive, Emory University, Atlanta, GA 30322, USA
Bioorg Med Chem Lett 17:5199-203. 2007..The synthesis of 16677 and several analogs together with effects on MV replication is described. The most potent analog displays nanomolar inhibition against the MV and a selectivity ratio (CC(50)/IC(50)) of ca. 16,500... - Discovering small-molecule estrogen receptor ?/coactivator binding inhibitors: high-throughput screening, ligand development, and models for enhanced potencyAiming Sun
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, GA 30322, USA
ChemMedChem 6:654-66. 2011.... - Nonnucleoside inhibitor of measles virus RNA-dependent RNA polymerase complex activityLaura K White
Division of Infectious Diseases, Emory University School of Medicine, Atlanta, GA 30322, USA
Antimicrob Agents Chemother 51:2293-303. 2007..Singly or in combination with the fusion inhibitors, this novel compound class has high developmental potential as a potent therapeutic against MV and will likely further the mechanistic characterization of the viral polymerase complex... - High-throughput screening-based identification of paramyxovirus inhibitorsJeong Joong Yoon
Division of Pediatric Infectious Diseases, Department of Pediatrics, Emory Children s Center, Emory University School of Medicine, Atlanta, Georgia 30322, USA
J Biomol Screen 13:591-608. 2008..Representatives of the last class may open avenues for the development of broad-range paramyxovirus inhibitors through hit-to-lead chemistry... - Nonpeptide inhibitors of measles virus entryAiming Sun
Department of Chemistry, Emory University, 1515 Dickey Drive, Atlanta, Georgia 30322, USA
J Med Chem 49:5080-92. 2006.... - Design of a small-molecule entry inhibitor with activity against primary measles virus strainsRichard K Plemper
Department of Microbiology and Immunology, 3086 Rollins Research Center, 1510 Clifton Road, Emory University School of Medicine, Atlanta, GA 30322, USA
Antimicrob Agents Chemother 49:3755-61. 2005..6 to 3.0 microM, depending on the MV genotype) against a panel of wild-type MV strains representative of viruses that are currently endemic in the field... - Synthesis of EF24-tripeptide chloromethyl ketone: a novel curcumin-related anticancer drug delivery systemAiming Sun
Department of Chemistry, Emory University, Atlanta, Georgia 30322, USA
J Med Chem 49:3153-8. 2006..When breast cancer cells (MDA-MB-231) and human melanoma cells (RPMI-7951) are treated with the complex, the cells are arrested to a greater extent than EF24 alone by comparison with controls... - Two domains that control prefusion stability and transport competence of the measles virus fusion proteinJoshua Doyle
Department of Microbiology and Immunology, 3086 Rollins Research Center, 1510 Clifton Road, Emory University School of Medicine, Atlanta, GA 30322, USA
J Virol 80:1524-36. 2006..The data support the conclusion that residues located in the head domain of the F trimer and the HR-B region contribute jointly to controlling F conformational stability... - Cancer and virus leads by HTS, chemical design and SEA data miningPahk Thepchatri
Chemical Biology Discovery Center, 1510 Clifton Road, Emory University, Atlanta, GA 30322, USA
Curr Top Med Chem 9:1159-71. 2009..In parallel with HTS, a unique component of the Emory virtual screening (VS) effort, namely, substructure enrichment analysis (SEA) program has been utilized in several cases... - Synthesis and SAR study of N-(4-hydroxy-3-(2-hydroxynaphthalene-1-yl)phenyl)-arylsulfonamides: heat shock protein 90 (Hsp90) inhibitors with submicromolar activity in an in vitro assayThota Ganesh
Chemical Biology Discovery Center, Emory University, 1510 Clifton Road, Atlanta, GA 30322, USA
Bioorg Med Chem Lett 18:4982-7. 2008..In this report, we present a new and general method for the synthesis of a variety of analogs around this scaffold, and discuss their structure-activity relationships... - Targeted delivery of paclitaxel to tumor cells: synthesis and in vitro evaluationJohn M Ndungu
Department of Chemistry, 1515 Dickey Drive, Emory University, Atlanta, Georgia 30322, USA
J Med Chem 53:3127-32. 2010..The activity order against PTX-sensitive KB 3-1 cells is C2'-PTX-FFRmk-fVIIa > PTX > C2'-PTX-FFRck. The C2' complex shows an IC(50) of 12 nM against the PTX-sensitive cell line and 130 nM against PTX-resistant cells... - EF24, a novel synthetic curcumin analog, induces apoptosis in cancer cells via a redox-dependent mechanismBrian K Adams
Program in Molecular and Systems Pharmacology, Emory University, Atlanta, GA 30322, USA
Anticancer Drugs 16:263-75. 2005..We therefore propose that the anticancer effect of a novel curcumin analog, EF24, is mediated in part by redox-mediated induction of apoptosis... - Target analysis of the experimental measles therapeutic AS-136AJeong Joong Yoon
Department of Pediatrics, Emory University School of Medicine and Children s Healthcare of Atlanta, Atlanta, GA 30322, USA
Antimicrob Agents Chemother 53:3860-70. 2009..Taken together, these data support the hypothesis that acquiring mutations in these L domains may reduce virus fitness... - Inhibition of IkappaB kinase-nuclear factor-kappaB signaling pathway by 3,5-bis(2-flurobenzylidene)piperidin-4-one (EF24), a novel monoketone analog of curcuminAndrea L Kasinski
Emory University School of Medicine, Atlanta, GA 30322, USA
Mol Pharmacol 74:654-61. 2008..The effective inhibition of TNF-alpha-induced NF-kappaB signaling by EF24 extends the therapeutic application of EF24 to other NF-kappaB-dependent diseases, including inflammatory diseases such as rheumatoid arthritis... - A target site for template-based design of measles virus entry inhibitorsRichard K Plemper
Department of Microbiology and Immunology, School of Medicine, Emory University, Atlanta, GA 30322, USA
Proc Natl Acad Sci U S A 101:5628-33. 2004..This template-based design approach for MV may be applicable to other clinically relevant members of the paramyxovirus family... - Neuroprotection by selective allosteric potentiators of the EP2 prostaglandin receptorJianxiong Jiang
Department of Pharmacology, Emory Chemical Biology Discovery Center, Emory University, Atlanta, GA 30322, USA
Proc Natl Acad Sci U S A 107:2307-12. 2010..Our results strongly reinforce the notion that activation of EP2 receptors by endogenous PGE(2) released in a cell-injury setting is neuroprotective... - Targeting tissue factor-expressing tumor angiogenesis and tumors with EF24 conjugated to factor VIIaMamoru Shoji
Winship Cancer Institute, Emory University, Atlanta, GA 30322, USA
J Drug Target 16:185-97. 2008..It may also prove to be useful for treating drug-resistant tumors and micro-metastases in addition to primary tumors... - Discovery of aminoquinolines as a new class of potent inhibitors of heat shock protein 90 (Hsp90): Synthesis, biology, and molecular modelingThota Ganesh
Chemical Biology Discovery Center, 1510 Clifton Road, Emory University, Atlanta, GA 30322, USA
Bioorg Med Chem 16:6903-10. 2008..These compounds represent a new class of Hsp90 inhibitors with simple chemical structures... - Inhibition of the NF-?B signaling pathway by the curcumin analog, 3,5-Bis(2-pyridinylmethylidene)-4-piperidone (EF31): Anti-inflammatory and anti-cancer propertiesANLYS OLIVERA
Department of Psychiatry and Behavioral Sciences, Emory University, 1365 B Clifton Road, Atlanta, GA 30322, USA
Int Immunopharmacol 12:368-77. 2012..Thus, EF31 represents a promising curcumin analog for further therapeutic development... - Adding a lysine mimic in the design of potent inhibitors of histone lysine methyltransferasesYanqi Chang
Department of Biochemistry, Emory University, Atlanta, GA 30322, USA
J Mol Biol 400:1-7. 2010..We suggest that adding a lysine or methyl-lysine mimic should be considered in the design of small-molecule inhibitors for other methyl-lysine writers, erasers, and readers... - 3-Fluoropiperidines and N-methyl-3-fluoropiperidinium salts: the persistence of axial fluorineAiming Sun
Department of Chemistry, Emory University, Atlanta, GA 30322, USA
Chemistry 11:1579-91. 2005..H-N hydrogen bonds are reported to be weak and few in number, the CF...HN charge-dipole orienting effect is a powerful directing force that matches the hydrogen-bond in both its energetic contribution and conformational consequences... - Sphingoid bases and de novo ceramide synthesis: enzymes involved, pharmacology and mechanisms of actionDavid S Menaldino
Department of Chemistry, Emory University, Atlanta, GA 30322-0230, USA
Pharmacol Res 47:373-81. 2003..Through studying such compounds, there is now a greater understanding of the metabolism and mechanism(s) of action of naturally occurring sphingoid bases as well as of these analogs...