Research Topics
Genomes and GenesSpecies | Yung Chi ChengSummaryAffiliation: Yale University Country: USA Publications
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Publications
Interaction of a traditional Chinese Medicine (PHY906) and CPT-11 on the inflammatory process in the tumor microenvironmentEna Wang
Infectious Disease and Immunogenetics Section IDIS, Department of Transfusion Medicine, Clinical Center and trans NIH Center for Human Immunology CHI, National Institutes of Health, Bethesda, Maryland 20892, USA
BMC Med Genomics 4:38. 2011..Animal studies documented a decrease in global toxicity and an increase in therapeutic effectiveness of chemotherapy when combined with PHY906...- A comprehensive platform for quality control of botanical drugs (PhytomicsQC): a case study of Huangqin Tang (HQT) and PHY906Robert Tilton
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06510, USA
Chin Med 5:30. 2010..Based on comprehensive chemical and biological fingerprints correlated with pharmacology, we propose a general approach called PhytomicsQC to botanical quality control... - New targets and inhibitors of HBV replication to combat drug resistanceYung Chi Cheng
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, SHM B254, New Haven, CT 06510, USA
J Clin Virol 34:S147-50. 2005..Drugs targeting on other viral unique targets are needed. A new class of chemicals with novel action against HBV replication was discovered. A brief description of their mode of action is given... - Comparative study of the persistence of anti-HIV activity of deoxynucleoside HIV reverse transcriptase inhibitors after removal from cultureElijah Paintsil
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
AIDS Res Ther 6:5. 2009..Therefore, a better indicator of the pharmacodynamic property of an inhibitor. The persistence of anti-HIV activity assay may complement in vitro potency assays to better predict in vivo performance of nucleoside analogs... - Phosphorylation of pyrimidine L-deoxynucleoside analog diphosphates. Kinetics of phosphorylation and dephosphorylation of nucleoside analog diphosphates and triphosphates by 3-phosphoglycerate kinasePreethi Krishnan
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
J Biol Chem 277:31593-600. 2002..This study also suggests the potential impact of nucleoside analog diphosphates and triphosphates on the multiple cellular functions of PGK, which may contribute to the action of the analogs... - Novel role of 3-phosphoglycerate kinase, a glycolytic enzyme, in the activation of L-nucleoside analogs, a new class of anticancer and antiviral agentsPreethi Krishnan
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
J Biol Chem 278:36726-32. 2003.... - Characterization of human UMP/CMP kinase and its phosphorylation of D- and L-form deoxycytidine analogue monophosphatesJieh Yuan Liou
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
Cancer Res 62:1624-31. 2002..UMP/CMPK localized predominantly to the cytoplasm. In addition, 196-amino acid UMP/CMPK was the actual form of UMP/CMPK, rather than the 228-amino acid form as suggested before... - Impact of novel human immunodeficiency virus type 1 reverse transcriptase mutations P119S and T165A on 4'-ethynylthymidine analog resistance profileGuangwei Yang
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA
Antimicrob Agents Chemother 53:4640-6. 2009..g., more than 50-fold resistance) will be difficult to develop. The previously observed 130-fold resistance of the virus with P119S/T165A/M184V to 4'-Ed4T may be partly due to mutations both in the RT sequence and outside the RT sequence... - Highly selective action of triphosphate metabolite of 4'-ethynyl D4T: a novel anti-HIV compound against HIV-1 RTGuangwei Yang
Department of Pharmacology, School of Medicine, Yale University, 333 Cedar Street, New Haven, CT 06520, USA
Antiviral Res 73:185-91. 2007..4'-Ed4TTP showed much less inhibitory effects toward major host DNA polymerases. Overall, our results suggest that 4'-Ed4TTP is the active form for anti-HIV-1 activity via its inhibitory effect against RT... - Comparison of the phosphorylation of 4'-ethynyl 2',3'-dihydro-3'-deoxythymidine with that of other anti-human immunodeficiency virus thymidine analogsChih Hung Hsu
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
Antimicrob Agents Chemother 51:1687-93. 2007..Qualitatively, the metabolism of 4'-ethynyl D4T is more similar to that of AZT than to that of its progenitor, D4T... - Intracellular metabolism and persistence of the anti-human immunodeficiency virus activity of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel thymidine analogElijah Paintsil
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, SHM B226, New Haven, CT 06520, USA
Antimicrob Agents Chemother 51:3870-9. 2007..4'-Ed4T is a promising antiviral candidate for HIV type 1 chemotherapy... - Unique antiviral mechanism discovered in anti-hepatitis B virus research with a natural product analogueChunxiao Ying
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520 8066, USA
Proc Natl Acad Sci U S A 104:8526-31. 2007..This mechanism is unique and different from other anti-HBV compounds previously described... - Determinants of individual variation in intracellular accumulation of anti-HIV nucleoside analog metabolitesElijah Paintsil
Department of Pediatrics, Yale University School of Medicine, New Haven, CT 06520, USA
Antimicrob Agents Chemother 55:895-903. 2011.... - TREX1 acts in degrading damaged DNA from drug-treated tumor cellsChuan Jen Wang
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
DNA Repair (Amst) 8:1179-89. 2009..Ubiquitously expressed in normal tissues, TREX1 may act in degrading DNA in all cell types undergoing a dying process before phagocytosis occurs... - Assessment of the effect of phosphorylated metabolites of anti-human immunodeficiency virus and anti-hepatitis B virus pyrimidine analogs on the behavior of human deoxycytidylate deaminaseJieh Yuan Liou
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
Mol Pharmacol 63:105-10. 2003.... - Apurinic/apyrimidinic endonuclease-1 protein level is associated with the cytotoxicity of L-configuration deoxycytidine analogs (troxacitabine and beta-L-2',3'-dideoxy-2',3'-didehydro-5-fluorocytidine) but not D-configuration deoxycytidine analogs (gemcitWing Lam
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
Mol Pharmacol 69:1607-14. 2006..In conclusion, this study supports the hypothesis that APE-1 plays a critical role in the actions of L-configuration but not D-configuration nucleoside analogs... - UMP/CMPK is not the critical enzyme in the metabolism of pyrimidine ribonucleotide and activation of deoxycytidine analogs in human RKO cellsRong Hu
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, USA
PLoS ONE 6:e19490. 2011..However, no detailed study has yet addressed the role of this protein in nucleotide metabolism in cells... - Discovery of a synthetic dual inhibitor of HIV and HCV infection based on a tetrabutoxy-calix[4]arene scaffoldLun K Tsou
Department of Chemistry, Yale University, New Haven, CT 06520, United States
Bioorg Med Chem Lett 20:2137-9. 2010..Structural activity relationship studies demonstrate the effects of lower-rim alkylation in maintaining cone conformation and upper-rim interacting head groups on the calix[4]arene play key roles for its potent dual antiviral activities... - Identification of chemicals and their metabolites from PHY906, a Chinese medicine formulation, in the plasma of a patient treated with irinotecan and PHY906 using liquid chromatography/tandem mass spectrometry (LC/MS/MS)Wei Zhang
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA
J Chromatogr A 1217:5785-93. 2010..These findings demonstrated that LC/MS/MS was and effective and reliable method for studying the parent chemicals of the Chinese herbal medicine PHY906 and their metabolites in a patient with metastatic colorectal cancer... - Effect of hypoxia on the expression of phosphoglycerate kinase and antitumor activity of troxacitabine and gemcitabine in non-small cell lung carcinomaWing Lam
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06510, USA
Mol Cancer Ther 8:415-23. 2009..p.). In conclusion, the hypoxia, which commonly exists in non-small cell lung carcinoma or other solid tumors resistant to radiotherapy or chemotherapy, is a favorable determinant to enhance the antitumor activity of L-OddC in vivo... - Analysis of deoxyribonucleotide pools in human cancer cell lines using a liquid chromatography coupled with tandem mass spectrometry techniqueWei Zhang
Department of Pharmacology, Section of Medical Oncology, Yale School of Medicine, New Haven, CT 06520, USA
Biochem Pharmacol 82:411-7. 2011..This LC/MS/MS assay is simple, fast, and sensitive, and it represents a significant advance over previously published methodologies... - Phosphorylation of Cytidine, Deoxycytidine, and Their Analog Monophosphates by Human UMP/CMP Kinase Is Differentially Regulated by ATP and MagnesiumChih Hung Hsu
Department of Pharmacology, Yale University School of Medicine, 333 Cedar St, SHM B226, New Haven, CT 06520, USA
Mol Pharmacol 67:806-14. 2005..We thus propose novel models for the phosphorylation action of human UMP/CMP kinase... - X-ray repair cross-complementing gene I protein plays an important role in camptothecin resistanceShin Young Park
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
Cancer Res 62:459-65. 2002..These results indicate that CPT resistance in our cells could be partly attributable to the overexpression of XRCC1... - A novel class of meso-tetrakis-porphyrin derivatives exhibits potent activities against hepatitis C virus genotype 1b replicons in vitroYao Cheng
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA
Antimicrob Agents Chemother 54:197-206. 2010..Our results demonstrate the potential use of tetracarboxyphenylporphyrins as potent anti-HCV agents... - DCB-3503, a tylophorine analog, inhibits protein synthesis through a novel mechanismYing Wang
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, United States of America
PLoS ONE 5:e11607. 2010..The inhibition of growth leads to cancer cell differentiation instead of cell death. However, the mechanisms of action of tylophorine analogs is unknown... - Structure-activity studies of phenanthroindolizidine alkaloids as potential antitumor agentsWenli Gao
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA
Bioorg Med Chem Lett 17:4338-42. 2007..05 for DCB-3503 and P<0.01 for PA-7). Their potent antitumor activities correlated with their potent NF-kappaB-inhibitory effects and their cyclin D1 down-regulatory effects... - Reversal of TNP-470-induced endothelial cell growth arrest by guanine and guanine nucleosidesJohn Hines
Department of Molecular, Cellular, and Developmental Biology, Yale University, New Haven, Connecticut 06520 8103, USA
J Pharmacol Exp Ther 334:729-38. 2010..Determining the mechanism whereby this causes restoration of endothelial cell proliferation is an ongoing investigation... - The four-herb Chinese medicine PHY906 reduces chemotherapy-induced gastrointestinal toxicityWing Lam
Yale University School of Medicine, New Haven, CT 06520, USA
Sci Transl Med 2:45ra59. 2010..Our results show that the herbal medicine PHY906 can counteract the toxicity of CPT-11 via several mechanisms that act simultaneously... - Helioxanthin analogue 8-1 inhibits duck hepatitis B virus replication in cell cultureChunxiao Ying
Department of Pharmacology, Yale University School of Medicine, New Haven, CT, USA
Antivir Chem Chemother 21:97-103. 2010..Helioxanthin analogue 8-1 displayed potent anti-HBV activity in human HBV in vitro and in animal models, with a unique antiviral mechanism. Its antiviral activity in other HBV system needs further study... - Expression of deoxynucleotide carrier is not associated with the mitochondrial DNA depletion caused by anti-HIV dideoxynucleoside analogs and mitochondrial dNTP uptakeWing Lam
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
Mol Pharmacol 67:408-16. 2005..We conclude that DNC does not play an important role in the delayed cytotoxicity (mtDNA depletion) of anti-HIV dideoxynucleoside analogs and dNTPs uptake into mitochondria... - Liquid chromatography/mass spectrometry analysis of PHY906, a Chinese medicine formulation for cancer therapyMin Ye
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06520, USA
Rapid Commun Mass Spectrom 21:3593-607. 2007..All the compounds identified from PHY906 were further assigned in the four individual herbs, and some of them are reported for the first time... - The exonuclease activity of human apurinic/apyrimidinic endonuclease (APE1). Biochemical properties and inhibition by the natural dinucleotide Gp4GKai Ming Chou
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
J Biol Chem 278:18289-96. 2003..APE1 may exist in two different conformations, and each conformation has a preference for a substrate. The different conformations can be affected by MgCl(2) or salt concentrations... - A phase I study of the chinese herbal medicine PHY906 as a modulator of irinotecan-based chemotherapy in patients with advanced colorectal cancerShivaani Kummar
Department of Medicine and Pharmacology, Developmental Therapeutics Program, Yale Cancer Center, Yale University School of Medicine, New Haven, CT, USA
Clin Colorectal Cancer 10:85-96. 2011..Treatment with PHY906 did not alter the pharmacokinetics of 5-FU, irinotecan, or the irinotecan metabolite SN-38... - Inhibition of hepatitis B virus gene expression and replication by helioxanthin and its derivativeYing Li
Department of Pharmacology, Yale University School of Medicine, New Haven, CT, USA
Antivir Chem Chemother 16:193-201. 2005..Both compounds inhibited HBV RNA and protein expression in addition to inhibiting HBV DNA... - Impacts of baicalein analogs with modification of the 6th position of A ring on the activity toward NF-kappaB-, AP-1-, or CREB-mediated transcriptionSheng Teng Huang
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street SHM B 226A, New Haven, CT 06510, USA
Bioorg Med Chem Lett 18:5046-9. 2008..Modification of baicalein at the 6th position could alter the specificity of action toward different cellular targets. Flavonoids could be chemophores in the development of drugs targeted at different signal transcriptional pathway... - Blocking HIV-1 entry by a gp120 surface binding inhibitorLun K Tsou
Department of Chemistry, Yale University, New Haven, CT 06520, United States
Bioorg Med Chem Lett 22:3358-61. 2012..Together, these data provide evidence that the proteomimetic compound represents a novel class of HIV-1 viral entry inhibitor that functions through protein surface recognition in analogy to an antibody... - Mechanism of inhibition of human immunodeficiency virus type 1 reverse transcriptase by a stavudine analogue, 4'-ethynyl stavudine triphosphateGuangwei Yang
Department of Pharmacology, School of Medicine, Yale University, 333 Cedar Street, New Haven, CT 06520, USA
Antimicrob Agents Chemother 52:2035-42. 2008..The structural basis for the higher binding affinity of 4'-Ed4TTP than of d4TTP could be the additional binding of the 4'-ethynyl group in a preformed hydrophobic pocket by A114, Y115, M184, F160, and part of D185... - ATP modulates poly(ADP-ribose) polymerase-1-facilitated topoisomerase I-linked DNA religation in the presence of camptothecinShin Young Park
Department of Pharmacology, Yale University School of Medicine, P O Box 208066, New Haven, CT 06520 8066, USA
Mol Pharmacol 73:1829-37. 2008..5 mM or higher) promoted DNA religation by a PARP-1-independent mechanism. Our study implies the possible role of ATP and other nucleotides in the regulation of topoisomerase I activity in the presence of camptothecin analogs... - Simple and convenient g-quadruplex-based turn-on fluorescence assay for 3' ? 5' exonuclease activityChung Hang Leung
School of Chinese Medicine and Department of Chemistry, Hong Kong Baptist University, Kowloon Tong, Hong Kong, China, and Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, United States
Anal Chem 83:463-6. 2011..A proof-of-concept of this assay has been demonstrated for prokaryotic Exonuclease III (ExoIII) and human TREX1... - Quantitation of paclitaxel and its two major metabolites using a liquid chromatography-electrospray ionization tandem mass spectrometryWei Zhang
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
J Chromatogr B Analyt Technol Biomed Life Sci 879:2018-22. 2011..8% in terms of relative error. The total run time was 7.0 min. This assay offers advantages in terms of expediency, and suitability for the analysis of paclitaxel and its metabolites in various biological fluids... - IPdR: a novel oral radiosensitizerMuhammad Wasif Saif
Yale University School of Medicine, Division of Medical Oncology, New Haven, CT 06520, USA
Expert Opin Investig Drugs 16:1415-24. 2007..In this paper, the authors review the development, mechanism of action, preclinical data and rationale for clinical studies... - Systemic Bcl-2 antisense oligodeoxynucleotide in combination with cisplatin cures EBV+ nasopharyngeal carcinoma xenografts in SCID miceJill Lacy
Department of Internal Medicine, Yale University School of Medicine, New Haven, CT 06520 8028, USA
Int J Cancer 119:309-16. 2006..The sequence-dependency of these effects is consistent with an antisense mechanism. These studies suggest that Bcl-2 may represent a biologically relevant target for the development of novel combinatorial therapies for NPC... - Nucleoplasmic calcium is required for cell proliferationMichele A Rodrigues
Department of Medicine, Yale University School of Medicine, New Haven, Connecticut 06520 8019, USA
J Biol Chem 282:17061-8. 2007.... - Synthesis and antiviral activity of helioxanthin analoguesHosup Yeo
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
J Med Chem 48:534-46. 2005..7 and 2.5 microM, respectively). Collectively, these molecules represent a novel set of antiviral compounds with unique structural features... - Decreased levels of UMP kinase as a mechanism of fluoropyrimidine resistanceRita Humeniuk
The Graduate School of Biomedical Sciences, Department of Pharmacology, Robert Wood Johnson Medical School, University of Medicine and Dentistry of New Jersey, Piscataway, New Jersey 08903, USA
Mol Cancer Ther 8:1037-44. 2009..Our findings provide new insights into the mechanisms of acquired resistance to 5-FU in colorectal cancer and implicate UMPK as an important mechanism of clinical resistance to pulse 5-FU treatment in some patients... - The impact of hypoxic treatment on the expression of phosphoglycerate kinase and the cytotoxicity of troxacitabine and gemcitabineWing Lam
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06520, USA
Mol Pharmacol 72:536-44. 2007..The knockdown of HIF-1alpha in inducible shRNA in RKO cells reduced the cytotoxicity of L-OddC but not dFdC under hypoxic conditions. In conclusion, hypoxia is an important factor that may potentiate the activity of L-OddC... - Structural analogs of tylophora alkaloids may not be functional analogsWenli Gao
Department of Pharmacology, Yale University School of Medicine, New Haven, CT 06510, USA
Bioorg Med Chem Lett 18:704-9. 2008..Because they do not have an identical spectrum of targets, the studied compounds are structural, but may not be functional analogs... - Reverse transcriptase activity of hepatitis B virus (HBV) DNA polymerase within core capsid: interaction with deoxynucleoside triphosphates and anti-HBV L-deoxynucleoside analog triphosphatesWing Lam
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
Mol Pharmacol 65:400-6. 2004..The L526M, M550V, and L526M/M550V mutations caused varying degrees of resistance to the different M-nucleoside triphosphates... - Regulation of inflammation by the NF-?B pathway in ovarian cancer stem cellsAliza L Leizer
Department of Obstetrics Gynecology and Reproductive Sciences, Yale University, New Haven, CT 06520, USA
Am J Reprod Immunol 65:438-47. 2011..The aim of this study is to determine whether the inhibition of NF?B by Eriocalyxin B (EriB) in the OCSCs may induce cell death in otherwise chemoresistant cells... - Novel mode of action of tylophorine analogs as antitumor compoundsWenli Gao
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut, USA
Cancer Res 64:678-88. 2004..In summary, these tylophorine analogs are a unique class of antitumor compounds that have a mode of action different from known antitumor drugs... - Retention of metabolites of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine, a novel anti-human immunodeficiency virus type 1 thymidine analog, in cellsXin Wang
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, SHM B226, New Haven, CT 06520, USA
Antimicrob Agents Chemother 53:3317-24. 2009..The results demonstrated that no detectable 4'-Ed4TMP efflux and the less efficient efflux of 4'-Ed4T nucleoside from cells might be one of the biochemical determinants of its persistent antiviral activity in cell culture... - Phosphorylation of pyrimidine deoxynucleoside analog diphosphates: selective phosphorylation of L-nucleoside analog diphosphates by 3-phosphoglycerate kinasePreethi Krishnan
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520, USA
J Biol Chem 277:5453-9. 2002..The enzymatic process of phosphorylation of L- and D-nucleoside analog diphosphates is different in cells... - Synthesis and biological evaluation of 2',3'-didehydro-2',3'-dideoxy-9-deazaguanosine, a monophosphate prodrug and two analogues, 2',3'-dideoxy-9-deazaguanosine and 2',3'-didehydro-2',3'-dideoxy-9-deazainosineMao-Chin Liu
Department of Pharmacology and Developmental Therapeutics Program, Cancer Center, Yale University School of Medicine, New Haven, Connecticut, USA
Nucleosides Nucleotides Nucleic Acids 24:135-45. 2005..Compounds 1-4 were found to be inactive against the human immunodeficiency virus and exhibited minimal to no cytotoxic activity against the L1210 leukemia, CCRF-CEM lymphoblastic leukemia, and B16F10 melanoma in vitro... - Behavior of thymidylate kinase toward monophosphate metabolites and its role in the metabolism of 1-(2'-deoxy-2'-fluoro-beta-L-arabinofuranosyl)-5-methyluracil (Clevudine) and 2',3'-didehydro-2',3'-dideoxythymidine in cellsRong Hu
Department of Pharmacology, Yale University School of Medicine, 333 Cedar St, New Haven, CT 06520, USA
Antimicrob Agents Chemother 49:2044-9. 2005..In conclusion, this is the first demonstration of the behavior of TMPK toward L-FMAUMP. This study indicates that human TMPK can phosphorylate L-FMAUMP and play a critical role in L-FMAU metabolism in cells... - Novel mechanism of inhibition of nuclear factor-kappa B DNA-binding activity by diterpenoids isolated from Isodon rubescensChung-Hang Leung
Department of Pharmacology, School of Medicine, Yale University, 333 Cedar Street, New Haven, CT 06520-8066, USA
Mol Pharmacol 68:286-97. 2005..The diterpenoid structure could therefore serve as a scaffold for the development of more potent and selective NF-kappaB inhibitors that target regulated gene transcription... - Eriocalyxin B inhibits nuclear factor-kappaB activation by interfering with the binding of both p65 and p50 to the response element in a noncompetitive mannerChung-Hang Leung
Department of Pharmacology, School of Medicine, Yale University, 333 Cedar Street, New Haven, CT 06520-8066, USA
Mol Pharmacol 70:1946-55. 2006..Modification of the structure of this class of compounds becomes the key to the control of the behavior of the compound against different cellular signaling pathways... - Inhibition of cell growth and nuclear factor-kappaB activity in pancreatic cancer cell lines by a tylophorine analogue, DCB-3503Her-Shyong Shiah
Department of Pharmacology, Yale University School of Medicine, 333 Cedar Street, New Haven, CT 06510, USA
Mol Cancer Ther 5:2484-93. 2006..It is a potentially useful compound in the management of cancers in which cyclin D1 overexpression and high NF-kappaB activity play a pivotal role... - (Z)- and (E)-[2-Fluoro-2-(hydroxymethyl)cyclopropylidene]methylpurines and -pyrimidines, a new class of methylenecyclopropane analogues of nucleosides: synthesis and antiviral activityShaoman Zhou
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, MI 48201-1379, USA
J Med Chem 47:6964-72. 2004..3-7.6 microM, respectively, whereas only 12a was effective against hepatitis B virus (HBV) with EC(50) 15 microM. Analogues 11a and 12a were weak substrates for adenosine deaminase... - Synthesis and antiviral activity of (Z)- and (E)-2,2-[bis(hydroxymethyl)cyclopropylidene]methylpurines and -pyrimidines: second-generation methylenecyclopropane analogues of nucleosidesShaoman Zhou
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA
J Med Chem 47:566-75. 2004..3 microM) and 2,6-diaminopurine 5h against hepatitis B virus (HBV, EC(50) = 4 microM). Adenine analogues 5a and 6a were moderately active as substrates for adenosine deaminase... - 3'-Carbon-substituted pyrimidine nucleosides having a 2',3'-dideoxy and 2',3'-didehydro-2',3'-dideoxy structure: synthesis and antiviral evaluationHiroki Kumamoto
School of Pharmaceutical Sciences, Showa University, 1 5 8 Hatanodai, Shinagawa ku, Tokyo, Japan
Antivir Chem Chemother 17:225-34. 2006..Some 2',3'-dideoxycytidine (ddC) analogues were also synthesized. Antiviral evaluation revealed that none of these analogues showed activity against HIV, hepatitis B virus, herpes simplex virus-1 (HSV-1) and HSV-2... - Nucleotides and pronucleotides of 2,2-bis(hydroxymethyl)methylenecyclopropane analogues of purine nucleosides: synthesis and antiviral activityZhaohua Yan
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA
J Med Chem 48:91-9. 2005..3 and 7.3 microM, respectively, and hepatitis B virus (HBV, EC(50) 4.1 microM). Cyclic phosphate 10a was the most effective analogue against HBV (EC(50) 0.8 microM)... - 9-{[3-fluoro-2-(hydroxymethyl)cyclopropylidene]methyl}adenines and -guanines. Synthesis and antiviral activity of all stereoisomers1Shaoman Zhou
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA
J Med Chem 49:6120-8. 2006..2 microM). Analogues 9a, 10a, and 11a are moderate substrates for adenosine deaminase. The structure-activity relationships will be discussed in context with other methylenecyclopropane analogues... - Synthesis of a highly active new anti-HIV agent 2',3'-didehydro-3'-deoxy-4'-ethynylthymidineKazuhiro Haraguchi
School of Pharmaceutical Sciences, Showa University, 1-5-8 Hatanodai, Shinagawa-ku, Tokyo 142-8555, Japan
Bioorg Med Chem Lett 13:3775-7. 2003..The compounds were assayed for their ability to inhibit the replication of HIV in cell culture. The 4'-ethynyl analogue (15) was found to be more potent and less toxic than the parent compound stavudine... - Structure-activity relationships of (S,Z)-2-aminopurine methylenecyclopropane analogues of nucleosides. Variation of purine-6 substituents and activity against herpesviruses and hepatitis B virusXinchao Chen
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA
J Med Chem 46:1531-7. 2003..Analogues 3a and 4i were the most active anti-VZV agents whereas compounds 3h, 3i, and 4h inhibited the replication of HBV in a micromolar concentration range... - Activity against human immunodeficiency virus type 1, intracellular metabolism, and effects on human DNA polymerases of 4'-ethynyl-2-fluoro-2'-deoxyadenosineHirotomo Nakata
Department of Infectious, Kumamoto University School of Medicine, 1 1 1 Honjo, Kumamoto, Japan
Antimicrob Agents Chemother 51:2701-8. 2007..2 microM, and 0.2 microM, respectively. These data warrant further development of EFdA as a potential therapeutic agent for those patients who harbor wild-type HIV-1 and/or multidrug-resistant variants... - Synthesis and anti-HIV activity of 4'-substituted 4'-thiothymidines: a new entry based on nucleophilic substitution of the 4'-acetoxy groupKazuhiro Haraguchi
School of Pharmaceutical Sciences, Showa University, 1 5 8 Hatanodai, Shinagawa ku, Tokyo, Japan
J Med Chem 51:1885-93. 2008..It is noteworthy that 36 and 37 were also inhibitory against replication of HIV variant resistant to 3TC (HIV-1 M184V), being as potent as against HIV-1 IIIB... - Anabolism of amdoxovir: phosphorylation of dioxolane guanosine and its 5'-phosphates by mammalian phosphotransferasesJoy Y Feng
Gilead Sciences, 4 University Place, 4611 University Drive, Durham, NC 27707, USA
Biochem Pharmacol 68:1879-88. 2004..5 nM) of DXG-TP was detected as the primary metabolite. Our study demonstrated that 5'-nucleotidase, GMP kinase, creatine kinase, and NDP kinase could be responsible for the activation of DXG in vivo... - Anti-human immunodeficiency virus type 1 activity and resistance profile of 2',3'-didehydro-3'-deoxy-4'-ethynylthymidine in vitroTakao Nitanda
Division of Antiviral Chemotherapy, Center for Chronic Viral Diseases, Graduate School of Medical and Dental Sciences, Kagoshima University, 8-35-1, Sakuragaoka, Kagoshima 890-8544, Japan
Antimicrob Agents Chemother 49:3355-60. 2005..Since 4'-Ed4T has increased anti-HIV-1 activity, decreased cytotoxicity, and a different resistance profile, it should be considered for further development as a new member of NRTIs... - Phosphoralaninate pronucleotides of pyrimidine methylenecyclopropane analogues of nucleosides: synthesis and antiviral activityAmalraj Ambrose
Department of Chemistry, Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, Michigan 48201-1379, USA
Nucleosides Nucleotides Nucleic Acids 24:1763-74. 2005..Deprotection with hydrazine in pyridine-acetic acid gave pronucleotides 3e and 4e. The Z-cytosine analogue 3e was active against HCMV and EBV The cytosine E-isomer 4e was moderately effective against EBV... - Synthesis, antiviral, and antitumor activity of 2-substituted purine methylenecyclopropane analogues of nucleosidesXinrong Qin
Developmental Therapeutics Program, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, MI 48201-1379, USA
Bioorg Med Chem 14:1247-54. 2006..From the group of 9a,b and 10a,b, the fluoro analogues 9a and 10a exhibited antitumor activity but only the Z-isomer 9a had a selective effect... - Tryptophanyl phosphoramidates as prodrugs of synadenol and its E-isomer: synthesis and biological activityRuifang Wang
Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Detroit, MI 48201-1379, USA
Bioorg Med Chem Lett 12:2467-70. 2002..The E-isomer 3c was effective only against EBV with parameters suggesting intracellular delivery of the respective phosphate. Compound 2c has a moderate but selective activity against solid tumors...
Research Grants
- BIOCHEMICAL PHARMACOLOGY OF ANTI-HIV-COMPOUNDSYung Chi Cheng; Fiscal Year: 2005..The information obtained will be useful for our understanding the differences in the effectiveness of anti-HIV-1 nucleoside analogs among different individuals and in a given patient through a period of treatment. ..
- NUCLEOSIDE ANALOGS AS ANTICANCER COMPOUNDSYung Chi Cheng; Fiscal Year: 2005..abstract_text> ..
- Biochemical Pharmacology of Anti-HIV CompoundsYung Chi Cheng; Fiscal Year: 2007..4'-Ed4T could have the potential to replace AZT or D4T in anti-HIV HARRT and in overcoming drug resistant virus to other anti-HIV drugs at the relevant dosage without causing toxicity. ..
- Mechanism and in vivo anti-HBV study of a novel class of non-nucleoside compoundsYung Chi Cheng; Fiscal Year: 2007..The studies proposed will provide information about not only the potential of the novel compound 8-1, as an anti-HBV drug, but also the roles of liver enriched transcription factors in regulation of HBV transcription. ..
- NUCLEOSIDE ANALOGS AS ANTICANCER COMPOUNDSYung Chi Cheng; Fiscal Year: 2007..It should yield novel information for understanding the biochemical determinants of the action of L-OddC, the biochemistry of the enzymes studied and possible novel use of L-OddC for the treatment of solid tumor. ..
- BIOCHEMICAL ASPECTS OF CHEMOTHERAPYYung Chi Cheng; Fiscal Year: 2007....
- NUCLEOSIDE ANALOGS AS ANTICANCER COMPOUNDSYung Chi Cheng; Fiscal Year: 2007..It should yield novel information for understanding the biochemical determinants of the action of L-OddC, the biochemistry of the enzymes studied and possible novel use of L-OddC for the treatment of solid tumor. ..
- Biochemical Pharmacology of Anti-HIV CompoundsYung Chi Cheng; Fiscal Year: 2009..4'-Ed4T could have the potential to replace AZT or D4T in anti-HIV HARRT and in overcoming drug resistant virus to other anti-HIV drugs at the relevant dosage without causing toxicity. ..
- Mechanism and in vivo anti-HBV study of a novel class of non-nucleoside compoundsYung Chi Cheng; Fiscal Year: 2010..The studies proposed will provide information about not only the potential of the novel compound 8-1, as an anti-HBV drug, but also the roles of liver enriched transcription factors in regulation of HBV transcription. ..
- BIOCHEMICAL PHARMACOLOGY OF ANTIHIV-1 COMPOUNDSYung Chi Cheng; Fiscal Year: 2000....
- NUCLEOSIDE ANALOGS AS ANTICANCER COMPOUNDSYung Chi Cheng; Fiscal Year: 2000..This proposed study should provide information not only in terms of new drug discovery, but also some basic knowledge regarding the biochemical pharmacology of deoxynucleosides. ..
- Biochemical Pharmacology of Anti-HIV CompoundsYung Chi Cheng; Fiscal Year: 2010..PUBLIC HEALTH RELEVANCE: Host Factors affecting antiviral activity of HIV nucleoside analogs, HIV replication and novel mechanism of resistant to a new anti-HIV compound, 4'-Ed4T. ..