thiones

Summary

Top Publications

  1. ncbi Synthesis and anti-inflammatory activity of 1-acylthiosemicarbazides, 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazole-3-thiones
    Erhan Palaska
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
    Farmaco 57:101-7. 2002
  2. ncbi Fyn inhibition by cycloalkane-fused 1,2-dithiole-3-thiones enhances antioxidant capacity and protects mitochondria from oxidative injury
    Ja Hyun Koo
    Innovative Drug Research Center for Metabolic and Inflammatory Disease, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea
    Mol Pharmacol 82:27-36. 2012
  3. ncbi Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen
    T U Mayer
    Department of Cell Biology, and Institute of Chemistry and Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 286:971-4. 1999
  4. pmc Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5
    T M Kapoor
    Department of Cell Biology, Harvard Medical School, Boston, Massachusetts 02115, USA
    J Cell Biol 150:975-88. 2000
  5. ncbi Myosin IIA regulates cell motility and actomyosin-microtubule crosstalk
    Sharona Even-Ram
    Craniofacial Developmental Biology and Regeneration Branch, National Institute of Dental and Craniofacial Research NIDCR, National Institutes of Health, Bethesda, MD 20892, USA
    Nat Cell Biol 9:299-309. 2007
  6. ncbi New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site
    Usman Ghani
    Department of Medical Biochemistry, King Saud University, Riyadh 11461, Saudi Arabia
    Bioorg Med Chem 18:4042-8. 2010
  7. ncbi Correcting improper chromosome-spindle attachments during cell division
    Michael A Lampson
    Laboratory of Chemistry and Cell Biology, Rockefeller University, New York, NY 10021, USA
    Nat Cell Biol 6:232-7. 2004
  8. ncbi Phosphatidylcholine-specific phospholipase C activation in epithelial ovarian cancer cells
    Francesca Spadaro
    Section of Molecular and Cellular Imaging, Department of Cell Biology and Neurosciences, Istituto Superiore di Sanita, Rome, Italy
    Cancer Res 68:6541-9. 2008
  9. pmc Enhanced expression of the transcription factor Nrf2 by cancer chemopreventive agents: role of antioxidant response element-like sequences in the nrf2 promoter
    Mi Kyoung Kwak
    Department of Environmental Health Sciences, Johns Hopkins Bloomberg School of Public Health, Baltimore, Maryland 21205, USA
    Mol Cell Biol 22:2883-92. 2002
  10. pmc Potent induction of total cellular GSH and NQO1 as well as mitochondrial GSH by 3H-1,2-dithiole-3-thione in SH-SY5Y neuroblastoma cells and primary human neurons: protection against neurocytotoxicity elicited by dopamine, 6-hydroxydopamine, 4-hydroxy-2-no
    Zhenquan Jia
    Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, 2265 Kraft Drive, Blacksburg, VA 24060, USA
    Brain Res 1197:159-69. 2008

Research Grants

  1. Dithiole thiones and ones--Chemistry to Biochemistry
    JAMES FISHBEIN; Fiscal Year: 2005
  2. TLR Signal Inhibition: a Novel Therapeutic Paradigm
    Leonard D Kohn; Fiscal Year: 2010
  3. TLR Signal Inhibition: a Novel Therapeutic Paradigm
    Leonard Kohn; Fiscal Year: 2005
  4. Steroids and Stem Cell in Carcinogenesis
    Doris Benbrook; Fiscal Year: 2004
  5. Mechanism of SHeA2 Action in Ovarian Cancer
    Doris Benbrook; Fiscal Year: 2009
  6. CDP-choline: Mechanisms in Cerebral Ischemia
    RAO ADIBHATLA; Fiscal Year: 2006
  7. Chemical genetic analysis of intracellular Transport
    Tarun Kapoor; Fiscal Year: 2007
  8. Choline Tracers for Imaging of Cancer
    Timothy DeGrado; Fiscal Year: 2007
  9. Role of EGFR in Viral Infected Lung Epithelial Cells
    Martha M Monick; Fiscal Year: 2010
  10. Mechanisms of Microtubule Dynamic Turnover
    Patricia Wadsworth; Fiscal Year: 2009

Detail Information

Publications214 found, 100 shown here

  1. ncbi Synthesis and anti-inflammatory activity of 1-acylthiosemicarbazides, 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazole-3-thiones
    Erhan Palaska
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Hacettepe University, Ankara, Turkey
    Farmaco 57:101-7. 2002
    ..Side effects of the compounds were examined on gastric mucosa, liver and stomach and none of the compounds showed significant side effects compared with reference nonsteroidal anti-inflammatory drugs (NSAIDs)...
  2. ncbi Fyn inhibition by cycloalkane-fused 1,2-dithiole-3-thiones enhances antioxidant capacity and protects mitochondria from oxidative injury
    Ja Hyun Koo
    Innovative Drug Research Center for Metabolic and Inflammatory Disease, College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, Seoul, Korea
    Mol Pharmacol 82:27-36. 2012
    ....
  3. ncbi Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen
    T U Mayer
    Department of Cell Biology, and Institute of Chemistry and Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 286:971-4. 1999
    ..All previously known small molecules that specifically affect the mitotic machinery target tubulin. Monastrol will therefore be a particularly useful tool for studying mitotic mechanisms...
  4. pmc Probing spindle assembly mechanisms with monastrol, a small molecule inhibitor of the mitotic kinesin, Eg5
    T M Kapoor
    Department of Cell Biology, Harvard Medical School, Boston, Massachusetts 02115, USA
    J Cell Biol 150:975-88. 2000
    ..Monastrol is thus a useful tool to study mitotic processes, detection and correction of chromosome malorientation, and contributions of Eg5 to spindle assembly and maintenance...
  5. ncbi Myosin IIA regulates cell motility and actomyosin-microtubule crosstalk
    Sharona Even-Ram
    Craniofacial Developmental Biology and Regeneration Branch, National Institute of Dental and Craniofacial Research NIDCR, National Institutes of Health, Bethesda, MD 20892, USA
    Nat Cell Biol 9:299-309. 2007
    ..We conclude that myosin IIA negatively regulates cell migration and suggest that it maintains a balance between the actomyosin and microtubule systems by regulating microtubule dynamics...
  6. ncbi New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site
    Usman Ghani
    Department of Medical Biochemistry, King Saud University, Riyadh 11461, Saudi Arabia
    Bioorg Med Chem 18:4042-8. 2010
    A series of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides were tailored and synthesized as new potent inhibitors of tyrosinase...
  7. ncbi Correcting improper chromosome-spindle attachments during cell division
    Michael A Lampson
    Laboratory of Chemistry and Cell Biology, Rockefeller University, New York, NY 10021, USA
    Nat Cell Biol 6:232-7. 2004
    ..Our results provide direct evidence for a mechanism required for the maintenance of genome integrity during cell division...
  8. ncbi Phosphatidylcholine-specific phospholipase C activation in epithelial ovarian cancer cells
    Francesca Spadaro
    Section of Molecular and Cellular Imaging, Department of Cell Biology and Neurosciences, Istituto Superiore di Sanita, Rome, Italy
    Cancer Res 68:6541-9. 2008
    ..These findings warrant further investigations on the role of PC-PLC and on the effects of its inhibition on the pathways responsible for constitutive EOC cell stimulation and cell proliferation...
  9. pmc Enhanced expression of the transcription factor Nrf2 by cancer chemopreventive agents: role of antioxidant response element-like sequences in the nrf2 promoter
    Mi Kyoung Kwak
    Department of Environmental Health Sciences, Johns Hopkins Bloomberg School of Public Health, Baltimore, Maryland 21205, USA
    Mol Cell Biol 22:2883-92. 2002
    ....
  10. pmc Potent induction of total cellular GSH and NQO1 as well as mitochondrial GSH by 3H-1,2-dithiole-3-thione in SH-SY5Y neuroblastoma cells and primary human neurons: protection against neurocytotoxicity elicited by dopamine, 6-hydroxydopamine, 4-hydroxy-2-no
    Zhenquan Jia
    Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, 2265 Kraft Drive, Blacksburg, VA 24060, USA
    Brain Res 1197:159-69. 2008
    ....
  11. ncbi Validating the mitotic kinesin Eg5 as a therapeutic target in pancreatic cancer cells and tumor xenografts using a specific inhibitor
    Min Liu
    Department of Genetics and Cell Biology, College of Life Sciences, Nankai University, 94 Weijin Road, Tianjin 300071, China
    Biochem Pharmacol 76:169-78. 2008
    ..Furthermore, treatment of nude mice bearing tumor xenografts of human pancreatic cancer results in pronounced tumor regression by triggering apoptosis. These data thus indicate Eg5 as a potential target for pancreatic cancer treatment...
  12. pmc The small molecule Hesperadin reveals a role for Aurora B in correcting kinetochore-microtubule attachment and in maintaining the spindle assembly checkpoint
    Silke Hauf
    Research Institute of Molecular Pathology, Dr Bohr Gasse 7, 1030 Vienna, Austria
    J Cell Biol 161:281-94. 2003
    ..Together, our data suggest that Aurora B is required to generate unattached kinetochores on monooriented chromosomes, which in turn could promote bipolar attachment as well as maintain checkpoint signaling...
  13. ncbi Synthesis and antimicrobial activity of novel 5-(1-adamantyl)-2-aminomethyl-4-substituted-1,2,4-triazoline-3-thiones
    Ali A El-Emam
    Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, P O Box 2457, Riyadh 11451, Saudi Arabia Electronic address
    Eur J Med Chem 68:96-102. 2013
    ..None of the newly synthesized compounds were proved to possess marked activity against C. albicans. ..
  14. ncbi Synthesis and preliminary anticancer activity of new 1,4-dihydro-3-(3-hydroxy-2-naphthyl)-4-substituted-5H-1,2,4-triazoline-5-thiones
    A Duran
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Marmara University, Istanbul, Turkey
    Farmaco 57:559-64. 2002
    1,4-Dihydro-3-(3-hydroxy-2-naphthyl)-4-substituted-5H-L2,4-triazolinc-5-thiones were synthesized. The structures of original eight compounds were confirmed by elemental analysis, 1H NMR and mass spectral methods...
  15. pmc The centromere geometry essential for keeping mitosis error free is controlled by spindle forces
    Jadranka Loncarek
    Division of Molecular Medicine, Wadsworth Center, Albany, New York State Department of Health, Albany, New York 12201 0509, USA
    Nature 450:745-9. 2007
    ..Thus, proper architecture of the centromere makes an important contribution to achieving high fidelity of chromosome segregation...
  16. ncbi Design, synthesis and trypanocidal evaluation of novel 1,2,4-triazoles-3-thiones derived from natural piperine
    Tatiany Nunes Franklim
    Departamento de Quimica, Instituto de Ciencias Exatas, Universidade Federal Rural do Rio de Janeiro, BR 465, Km 07, CEP 23 890 000, Seropedica, RJ, Brazil
    Molecules 18:6366-82. 2013
    ..herein describes the synthesis and the assessment of the trypanocidal activity of thirteen new 1,2,4-triazole-3-thiones obtained from natural piperine, the main constituent of the dry fruits of Piper nigrum...
  17. ncbi Novel synthesis of 1-aroyl-3-aryl-4-substituted imidazole-2-thiones
    Run Sheng Zeng
    Department of Chemistry, Suzhou University, Suzhou 215006, Jiangsu Province, China
    Org Lett 5:1657-9. 2003
    reaction: see text] An efficient route to 1-aroyl-3-aryl-4-substituted imidazole-2-thiones (2, 4-6) has been developed...
  18. ncbi Improvement in solubility and dissolution rate of 1, 2-dithiole-3-thiones upon complexation with beta-cyclodextrin and its hydroxypropyl and sulfobutyl ether-7 derivatives
    G Dollo
    Laboratoire de Pharmacie Galénique et Biopharmacie and Laboratoire de Chimie Analytique, Faculte des Sciences Pharmaceutiques et Biologiques, Universite de Rennes I, 35043 Rennes Cedex, France
    J Pharm Sci 88:889-95. 1999
    Inclusion complexes between beta-cyclodextrin derivatives and 1, 2-dithione-3-thiones were studied in aqueous solution and in the solid state...
  19. ncbi Chromosomes can congress to the metaphase plate before biorientation
    Tarun M Kapoor
    Laboratory of Chemistry and Cell Biology, Rockefeller University, New York, NY 10021, USA
    Science 311:388-91. 2006
    ..This congression mechanism depended on the kinetochore-associated, plus end-directed microtubule motor CENP-E (kinesin-7)...
  20. ncbi Synthesis and biological activities of some novel aminomethyl derivatives of 4-substituted-5-(2-thienyl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones
    Metin Koparir
    Firat University, Faculty of Science, Department of Chemistry, 23169 Elazig, Turkiye
    Eur J Med Chem 63:340-6. 2013
    ..Some of the compounds were found to exhibit significant antimicrobial and antioxidant activity...
  21. ncbi Generation of superoxide from reaction of 3H-1,2-dithiole-3-thione with thiols: implications for dithiolethione chemoprotection
    Zhenquan Jia
    Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, Blacksburg, VA 24060, USA
    Mol Cell Biochem 307:185-91. 2008
    ..These findings demonstrate that D3T reacts with thiols, particularly a dithiol, generating superoxide, which may provide a mechanistic explanation for induction of Nrf2-dependent phase 2 enzymes by D3T...
  22. pmc 5,6-Dihydrocyclopenta[c][1,2]-dithiole-3(4H)-thione is a promising cancer chemopreventive agent in the urinary bladder
    Joseph D Paonessa
    Department of Cancer Prevention and Control, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    Chem Biol Interact 180:119-26. 2009
    ..In conclusion, CPDT potently and preferentially induces Phase 2 enzymes in the bladder epithelium and Nrf2 is its key mediator...
  23. ncbi Phosphatidylcholine-specific phospholipase C inhibitor, tricyclodecan-9-yl xanthogenate (D609), increases phospholipase D-mediated phosphatidylcholine hydrolysis in UMR-106 osteoblastic osteosarcoma cells
    A T Singh
    Department of Molecular Pharmacology and Biological Chemistry, Northwestern University Medical School, Chicago, IL 60611 3008, USA
    Biochim Biophys Acta 1487:201-8. 2000
    ..The studies reveal a novel action of this inhibitor on signaling in osteoblastic cells which might influence downstream responses...
  24. pmc Effects of disulfiram and dopamine beta-hydroxylase knockout on cocaine-induced seizures
    Meriem Gaval-Cruz
    Department of Human Genetics, Emory University, 301 Whitehead Biomedical Research Building, 615 Michael Street, Atlanta, GA 30322, USA
    Pharmacol Biochem Behav 89:556-62. 2008
    ..These results suggest that disulfiram enhances CIS via two distinct mechanisms: it both increases CIS frequency by inhibiting DBH and increases CIS frequency in a DBH-independent manner...
  25. ncbi Cooperation of phosphatidylcholine-specific phospholipase C and basic fibroblast growth factor in the neural differentiation of mesenchymal stem cells in vitro
    Nan Wang
    Institute of Developmental Biology, School of Life Science, Shandong University, Jinan 250100, China
    Int J Biochem Cell Biol 40:294-306. 2008
    ..Moreover, basic fibroblast growth factor could contribute to rescuing the differentiated cells from death through decreasing overly high mitochondrial membrane potentials and reactive oxygen species levels...
  26. ncbi Design, synthesis and anti-Parkinsonian evaluation of 3-alkyl/aryl-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidine-2(3H)-thiones against neuroleptic-induced catalepsy and oxidative stress in mice
    Faizul Azam
    Laboratory of Medicinal Chemistry, Faculty of Pharmacy, University of Seventh October, Misurata, Libya
    J Enzyme Inhib Med Chem 25:818-26. 2010
    A series of 3-alkyl/aryl-8-(furan-2-yl)thiazolo[5,4-e][1,2,4]triazolo[1,5-c]pyrimidine-2(3H)-thiones (3a-3f) were synthesised in good yield and evaluated for their anti-Parkinsonian and neuroprotective potential...
  27. pmc Hydrogen peroxide is a second messenger in phase 2 enzyme induction by cancer chemopreventive dithiolethiones
    Ryan Holland
    Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, 1000 Hilltop Circle, Baltimore, Maryland 21250, USA CA91032
    Chem Res Toxicol 22:1427-34. 2009
    ....
  28. pmc Role of transcription factor Nrf2 in the induction of hepatic phase 2 and antioxidative enzymes in vivo by the cancer chemoprotective agent, 3H-1, 2-dimethiole-3-thione
    M K Kwak
    Department of Environmental Health Sciences, Johns Hopkins School of Hygiene and Public Health, Baltimore, Maryland 21205, USA
    Mol Med 7:135-45. 2001
    ..Knowledge of the factors controlling the specificity of actions of enzyme inducers will be exceedingly helpful in the design and isolation of more efficient and selective chemoprotective agents...
  29. ncbi Anti-inflammatory and gastrointestinal effects of a novel diclofenac derivative
    Ling Li
    Cardiovascular Biology Research Group, Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, 18 Medical Drive, Singapore 117597
    Free Radic Biol Med 42:706-19. 2007
    ..Administration of S-diclofenac (47.2 micromol/kg, i.p.) to conscious rats significantly increased plasma H2S concentration (at 45 min and 6 h). We propose that H2S release from S-diclofenac in vivo contributes to the observed effects...
  30. pmc Kinesin-5 is essential for growth-cone turning
    Vidya C Nadar
    Department of Neurobiology and Anatomy, Drexel University College of Medicine, Philadelphia, PA 19129, USA
    Curr Biol 18:1972-7. 2008
    ..We propose that kinesin-5 permits MTs to selectively invade one side of the growth cone by opposing their entry into the other side...
  31. pmc Interplay of microtubule dynamics and sliding during bipolar spindle formation in mammalian cells
    Swapna Kollu
    Department of Biochemistry, Dartmouth Medical School, Hanover, NH 03755, USA
    Curr Biol 19:2108-13. 2009
    ..Thus, the temporal requirement for microtubule sliding generated by Eg5 activity during bipolar spindle assembly in mammalian cells is regulated by changes in the dynamic behavior of microtubules during mitosis...
  32. pmc Reorganization of the microtubule array in prophase/prometaphase requires cytoplasmic dynein-dependent microtubule transport
    Nasser M Rusan
    Department of Biology, Program in Molecular and Cellular Biology, Morrill Science Center, University of Massachusetts, N Pleasant Street, Amherst, MA 01003, USA
    J Cell Biol 158:997-1003. 2002
    ..The data demonstrate that dynamic astral Mts search the cytoplasm for other Mts, as well as chromosomes, in mitotic cells...
  33. ncbi Role of phase 2 enzyme induction in chemoprotection by dithiolethiones
    M K Kwak
    Department of Environmental Health Sciences, Johns Hopkins University Bloomberg School of Public Health, 615 North Wolfe Street, Baltimore, MD 21205, USA
    Mutat Res 480:305-15. 2001
    ..induction has led to the recognition or isolation of novel, potent chemopreventive agents such as 1,2-dithiole-3-thiones, terpenoids and the isothiocyanate sulforaphane...
  34. ncbi Progress on kinesin spindle protein inhibitors as anti-cancer agents
    Yingjie Zhang
    Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, 250012 Ji nan, Shandong, China
    Anticancer Agents Med Chem 8:698-704. 2008
    ..Accordingly, more and more interest has been focused on the development of high effective and selective KSPi. This review will focus on some kinds of KSPi on the basis of introducing structure and function of KSP...
  35. ncbi Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5
    Michael Gartner
    University of Leipzig, Institute for Organic Chemistry, Johannisallee 29, 04103 Leipzig, Germany
    Chembiochem 6:1173-7. 2005
  36. ncbi Monastrol, a selective inhibitor of the mitotic kinesin Eg5, induces a distinctive growth profile of dendrites and axons in primary cortical neuron cultures
    Seung Yong Yoon
    Department of Anatomy and Cell Biology, University of Ulsan College of Medicine, Seoul, Korea
    Cell Motil Cytoskeleton 60:181-90. 2005
    ..Taken together, we conclude that Eg5 acts distinctively on dendrites and axons in neurons and suggest a putative model of how Eg5 works distinctively on dendrites and axons...
  37. pmc Disulfiram attenuates drug-primed reinstatement of cocaine seeking via inhibition of dopamine β-hydroxylase
    Jason P Schroeder
    Department of Human Genetics, Emory University School of Medicine, Atlanta, GA 30322, USA
    Neuropsychopharmacology 35:2440-9. 2010
    ..Our results suggest that disulfiram's efficacy in the treatment of cocaine addiction is associated with the inhibition of DBH and interference with the ability of environmental stimuli to trigger relapse...
  38. ncbi Phosphatidylcholine-specific phospholipase C in mitogen-stimulated fibroblasts
    Carlo Ramoni
    Department of Cell Biology and Neurosciences, Istituto Superiore di Sanita, Rome, Italy
    Exp Cell Res 299:370-82. 2004
    ..These effects were associated with a D609-induced long-lasting cell cycle block in Go...
  39. pmc ATPase mechanism of Eg5 in the absence of microtubules: insight into microtubule activation and allosteric inhibition by monastrol
    Jared C Cochran
    Department of Biological Sciences, University of Pittsburgh, Pittsburgh, Pennsylvania 15260, USA
    Biochemistry 44:16633-48. 2005
    ....
  40. ncbi Potentiation of kinesin spindle protein inhibitor-induced cell death by modulation of mitochondrial and death receptor apoptotic pathways
    Ulka Vijapurkar
    Schering Plough Biopharma, Palo Alto, CA, USA
    Cancer Res 67:237-45. 2007
    ..This study has elucidated cellular responses induced by KSP inhibitors, and the results provide insights for a more effective cancer treatment with these agents...
  41. ncbi Monastrol, a prototype anti-cancer drug that inhibits a mitotic kinesin, induces rapid bursts of axonal outgrowth from cultured postmitotic neurons
    Saad A Haque
    Department of Neurobiology and Anatomy, Drexel University College of Medicine, Philadelphia, Pennsylvania 19129, USA
    Cell Motil Cytoskeleton 58:10-6. 2004
    ..The comparatively modest toxic effects on the neurons over time are a hopeful sign for clinicians interested in using anti-Eg5 drugs for cancer therapy...
  42. ncbi Synthesis and antimycobacterial activity of 3,5-disubstituted thiadiazine thiones
    D Katiyar
    Division of Medicinal Chemistry, Central Drug Research Institute, Lucknow 226001, India
    Bioorg Med Chem 11:4369-75. 2003
    A series of 3,5-disubstituted thiadiazine thiones (4-24) have been synthesized by reaction of primary amines with carbon disulphide followed by cyclocondensation of the resulting intermediate with formaldehyde and primary amines or amino ..
  43. ncbi Abrogation of hyperosmotic impairment of insulin signaling by a novel class of 1,2-dithiole-3-thiones through the inhibition of S6K1 activation
    Eun Ju Bae
    College of Pharmacy, Seoul National University, Sillim dong, Kwanak gu, Seoul 151 742, Korea
    Mol Pharmacol 73:1502-12. 2008
    ..This study investigated whether oltipraz and a novel class of 1,2-dithiole-3-thiones were capable of preventing insulin resistance induced by hyperosmotic stress, thereby enhancing insulin-dependent ..
  44. ncbi Identification of novel transcriptional networks in response to treatment with the anticarcinogen 3H-1,2-dithiole-3-thione
    Yong Huang
    W Harry Feinstone Center for Genomic Research, University of Memphis, Memphis, Tennessee 38152, USA
    Physiol Genomics 24:144-53. 2006
    ..000331) pathways. These findings showed a profound impact of D3T on lipid metabolism and anti-inflammatory/immune-suppressive response, indicating a broader cytoprotective effect of this compound than previously expected...
  45. ncbi Sphingomyelin synthase as a potential target for D609-induced apoptosis in U937 human monocytic leukemia cells
    Aimin Meng
    Department of Pathology and Laboratory Medicine, Medical University of South Carolina, Charleston, SC 29425, USA
    Exp Cell Res 292:385-92. 2004
    ..These results suggest that SMS is a potential target of D609 and inhibition of SMS may contribute to D609-induced tumor cell death via modulation of the cellular levels of ceramide and DAG...
  46. ncbi A computational approach to the synthesis of 1,3,5-thiadiazinane-2-thiones in aqueous medium: theoretical evidence for water-promoted heterocyclization
    Julieta Coro
    Laboratorio de Síntesis Orgánica, Facultad de Quimica, Universidad de La Habana, 10400, Ciudad Habana, Cuba
    J Mol Model 14:641-7. 2008
    Based on experimental evidence and DFT studies, a probable cyclization route to 1,3,5-thiadiazinanes-2-thiones in aqueous medium is proposed...
  47. pmc Novel dithiolethione-modified nonsteroidal anti-inflammatory drugs in human hepatoma HepG2 and colon LS180 cells
    Sara E Bass
    Basic Research Program, Science Applications International Corporation Frederick, Inc, and Laboratory of Metabolism, National Cancer Institute Frederick, Frederick, Maryland, USA
    Clin Cancer Res 15:1964-72. 2009
    ..In this study, we investigated the activities of a new class of NSAIDs containing dithiolethione moieties (S-NSAID) on both arms of carcinogenesis...
  48. ncbi Evaluation of the cancer chemopreventive potency of dithiolethione analogs of oltipraz
    B D Roebuck
    Department of Pharmacology and Toxicology, Dartmouth Medical School, Hanover, NH 03755, USA
    Carcinogenesis 24:1919-28. 2003
    ..While efficacy in humans has yet to be tested, D3T is clearly more potent than oltipraz and serves as a useful molecular probe for determining the key events associated with protection by this class of agents...
  49. ncbi Molecular docking, structure-activity relationship and biological evaluation of the anticancer drug monastrol as a pteridine reductase inhibitor in a clinical isolate of Leishmania donovani
    Jaspreet Kaur
    Drug Target Discovery and Development Division, Central Drug Research Institute, Chattar Manzil Palace, PO Box No 173, Lucknow 226001, CSIR, India
    J Antimicrob Chemother 65:1742-8. 2010
    ..Using the pteridine reductase (PTR1) enzyme of Leishmania as the target, the objective of our study was to find a drug candidate that can enter the clinical development process after being evaluated for safety and efficacy in animals...
  50. pmc The hydrogen sulphide-releasing derivative of diclofenac protects against ischaemia-reperfusion injury in the isolated rabbit heart
    G Rossoni
    Department of Pharmacology, Chemotherapy and Medical Toxicology, University of Milan, Milan, Italy
    Br J Pharmacol 153:100-9. 2008
    ..Hydrogen sulphide (H(2)S) is an endogenous gaseous mediator active in the multilevel regulation of pathophysiological functions in mammalian cardiovascular tissues...
  51. pmc Nrf2-mediated transcriptional induction of antioxidant response in mouse embryos exposed to ethanol in vivo: implications for the prevention of fetal alcohol spectrum disorders
    Jian Dong
    Bowles Center for Alcohol Studies and Department of Cell and Developmental Biology University of North Carolina at Chapel Hill, Chapel Hill, North Carolina 27599 7178, USA
    Antioxid Redox Signal 10:2023-33. 2008
    ..In addition, the potency of D3T in inducing antioxidants as well as in diminishing ethanol-induced apoptosis suggests that further exploration of the antiteratogenic effect of this compound will be fruitful...
  52. ncbi A study of the electrospray ionisation and ion-trap fragmentation of [M - H](-) ions of new 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazin-2-thiones
    R Martinez-Alvarez
    Departamento de Quimica Organica, Facultad de Ciencias Quimicas, Universidad Complutense, E 28040 Madrid, Spain
    Rapid Commun Mass Spectrom 15:758-62. 2001
    ..ESI) in negative mode of the pharmacologically significant 3,5-disubstituted tetrahydro-2H-1,3,5-thiadiazin-2-thiones, and their subsequent fragmentations using an ion-trap mass spectrometer, have been investigated...
  53. ncbi Effect of S-diclofenac, a novel hydrogen sulfide releasing derivative, on carrageenan-induced hindpaw oedema formation in the rat
    Jenab Sidhapuriwala
    Department of Pharmacology, Cardiovascular Biology Research Group, Yong Loo Lin School of Medicine, National University of Singapore, 18 Medical Drive, Singapore, 117597, Singapore
    Eur J Pharmacol 569:149-54. 2007
    ..It is proposed that the enhanced anti-inflammatory effect of S-diclofenac relates to its ability to release H(2)S at the inflamed site. These data provide evidence for an anti-inflammatory effect of H(2)S...
  54. pmc Dithiolethiones for cancer chemoprevention: where do we stand?
    Yuesheng Zhang
    Department of Cancer Prevention and Control, Roswell Park Cancer Institute, Elm and Carlton Streets, Buffalo, NY 14263, USA
    Mol Cancer Ther 7:3470-9. 2008
    ..Further investigation of these compounds may lead to development of effective and safe agents for cancer prevention in humans...
  55. ncbi Induction of apoptosis by monastrol, an inhibitor of the mitotic kinesin Eg5, is independent of the spindle checkpoint
    Gregory M Chin
    DNAX Research Institute of Molecular and Cellular Biology Research Institute, Palo Alto, California, USA
    Mol Cancer Ther 5:2580-91. 2006
    ..Furthermore, these results show that inactivation of the kinesin Eg5 can induce apoptosis in tumor cells in the absence of critical spindle checkpoint components...
  56. ncbi Cellular localization and functional role of phosphatidylcholine-specific phospholipase C in NK cells
    C Ramoni
    Laboratories of Immunology and Cell Biology, Istituto Superiore di Sanita, Rome, Italy
    J Immunol 167:2642-50. 2001
    ..These newly detected mechanisms of PC-PLC translocation and function support an essential role of this enzyme in regulated granule exocytosis and NK-mediated cytotoxicity...
  57. ncbi Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5
    Zoltan Maliga
    Program in Biophysics, Harvard University, Boston, MA 02115, USA
    Chem Biol 9:989-96. 2002
    ..Future structural studies should help in designing more potent Eg5 inhibitors for possible use as anticancer drugs and cell biological reagents...
  58. pmc Induction of DT-diaphorase by 1,2-dithiole-3-thiones in human tumour and normal cells and effect on anti-tumour activity of bioreductive agents
    G P Doherty
    Manitoba Institute of Cell Biology, Manitoba Cancer Treatment and Research Foundation, Department of Pharmacology, University of Manitoba, Winnipeg, Canada
    Br J Cancer 77:1241-52. 1998
    ..agents, such as mitomycin C (MMC) and EO9, and is inducible by many compounds, including 1,2-dithiole-3-thiones (D3Ts)...
  59. ncbi Monastrol stabilises an attached low-friction mode of Eg5
    I M T C Crevel
    Curr Biol 14:R411-2. 2004
  60. ncbi Raphanusanin-induced genes and the characterization of RsCSN3, a raphanusanin-induced gene in etiolated radish hypocotyls
    - Moehninsi
    Graduate School of Life and Environmental Sciences, University of Tsukuba, Ibaraki 305 8572, Japan
    Phytochemistry 69:2781-92. 2008
    ....
  61. ncbi Synthesis, antimicrobial, and anti-HIV-1 activity of certain 5-(1-adamantyl)-2-substituted thio-1,3,4-oxadiazoles and 5-(1-adamantyl)-3-substituted aminomethyl-1,3,4-oxadiazoline-2-thiones
    Ali A El-Emam
    Department of Pharmaceutical Chemistry, College of Pharmacy, King Saud University, Riyadh 11451, Saudi Arabia
    Bioorg Med Chem 12:5107-13. 2004
    ..in ethanol at room temperature yielded the corresponding 5-(1-adamantyl)-3-arylaminomethyl-1,3,4-oxadiazoline-2-thiones 4a-m or 5-(1-adamantyl)-3-(4-substituted-1-piperazinylmethyl)-1,3,4-oxadiazoline-2-thiones 5a-h, respectively...
  62. pmc The kinesin Eg5 drives poleward microtubule flux in Xenopus laevis egg extract spindles
    David T Miyamoto
    Department of Systems Biology, Harvard Medical School, Boston, MA 02115, USA
    J Cell Biol 167:813-8. 2004
    ..Our results suggest that ensembles of nonprocessive Eg5 motors drive flux in metaphase Xenopus extract spindles...
  63. ncbi Flexible heteroarotinoids (Flex-Hets) exhibit improved therapeutic ratios as anti-cancer agents over retinoic acid receptor agonists
    Doris M Benbrook
    Departments of Obstetrics and Gynecology, University of Oklahoma Health Sciences Center, Oklahoma City, OK 73190, USA
    Invest New Drugs 23:417-28. 2005
    ..In conclusion, Flex-Hets exhibit improved therapeutic ratios for multiple cancer types over RAR and/or RXR agonists...
  64. ncbi Determining the position of the cell division plane
    Julie C Canman
    University of North Carolina, Department of Biology, 607 Fordham Hall, CB 3280, Chapel Hill, North Carolina 27699 3280, USA
    Nature 424:1074-8. 2003
    ..Our data are consistent with a model in which chromosomes supply microtubules with factors that promote microtubule stability and furrowing...
  65. ncbi High performance liquid chromatographic analysis and preclinical pharmacokinetics of the heteroarotinoid antitumor agent, SHetA2
    Yilong Zhang
    College of Pharmacy, The Ohio State University, Columbus, OH 43210, USA
    Cancer Chemother Pharmacol 58:561-9. 2006
    ..The objective was to develop and validate a HPLC/UV method for the determination of SHetA2, and study the pharmacokinetics of SHetA2 in the mouse...
  66. pmc Eg5 is static in bipolar spindles relative to tubulin: evidence for a static spindle matrix
    T M Kapoor
    Laboratory of Chemistry and Cell Biology, Rockefeller University, New York, NY 10021, USA
    J Cell Biol 154:1125-33. 2001
    ..We discuss alternative interpretations of the Eg5 dynamics we observe, ideas for the biochemical nature of a spindle matrix, and implications for Eg5 function...
  67. ncbi Synthesis, evaluation and structure-activity relationships of 5-alkyl-2,3-dihydroimidazo[1,2-c] quinazoline, 2,3-dihydroimidazo[1,2-c]quinazolin-5(6H)-thiones and their oxo-analogues as new potential bronchodilators
    R H Bahekar
    Medicinal Chemistry Division, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, A P, India
    Arzneimittelforschung 51:284-92. 2001
    ..two series of 5-alkyl-2,3-dihydroimidazo[1,2-c]quinazolines (Va-1), 2,3-dihydroimidazo[1,2-c]quinazolin-5-(6H)-thiones (VIIIa-d) and their oxo-analogues (IXa-d) have been designed...
  68. ncbi Phototropic stimulation induces the conversion of glucosinolate to phototropism-regulating substances of radish hypocotyls
    T Hasegawa
    Institute of Applied Biochemistry, University of Tsukuba, Ibaraki, Japan
    Phytochemistry 54:275-9. 2000
    ..These results suggest that phototropic stimulation promotes myrosinase activity in the illuminated side of radish hypocotyls, releasing bioactive MTBI from inactive MTBG and simultaneously producing bioactive raphanusanins...
  69. pmc Identification of an unintended consequence of Nrf2-directed cytoprotection against a key tobacco carcinogen plus a counteracting chemopreventive intervention
    Joseph D Paonessa
    Department of Cancer Prevention and Control, Roswell Park Cancer Institute, Buffalo, New York 14263, USA
    Cancer Res 71:3904-11. 2011
    ..Thus, CPDT exemplifies a counteracting solution to the dilemma posed by Nrf2...
  70. ncbi Upregulation of cellular glutathione by 3H-1,2-dithiole-3-thione as a possible treatment strategy for protecting against acrolein-induced neurocytotoxicity
    Zhenquan Jia
    Division of Biomedical Sciences, Edward Via Virginia College of Osteopathic Medicine, Virginia Tech Corporate Research Center, 2265 Kraft Drive, Blacksburg, VA 24060, USA
    Neurotoxicology 30:1-9. 2009
    ..Taken together, this study demonstrates that upregulation of GSH is a predominant mechanism underlying D3T-mediated protection against acrolein-induced neurocytotoxicity...
  71. ncbi Copper(II) sulfamate: an efficient catalyst for the one-pot synthesis of 3,4-dihydropyrimidine-2(1H)-ones and thiones
    Chen Jiang Liu
    School of Science, Xi an Jiaotong University, Xi an, PR China
    Molecules 14:763-70. 2009
    ..Compared to the classical Biginelli reaction conditions, the present method has the advantages of good yields, short reaction times and experimental simplicity...
  72. ncbi Treatment with H2S-releasing diclofenac protects mice against acute pancreatitis-associated lung injury
    Madhav Bhatia
    Department of Pharmacology and Cardiovascular Biology Research Group, National University of Singapore
    Shock 29:84-8. 2008
    ..These results suggest the usefulness of H(2)S-releasing nonsteroidal anti-inflammatory drugs as potential treatments for pancreatitis-associated lung injury...
  73. ncbi Induction of phase II enzymes by 3H-1,2-dithiole-3-thione: dose-response study in rats
    Rex Munday
    AgResearch, Ruakura Agricultural Research Centre, Private Bag 3123, Hamilton, New Zealand
    Carcinogenesis 25:1721-5. 2004
    ..The inductive potency of D3T makes it a most promising candidate for use as a chemoprotective agent...
  74. ncbi Preferential killing of tetraploid tumor cells by targeting the mitotic kinesin Eg5
    Santiago Rello-Varona
    INSERM U848, Institut Gustave Roussy, and Université de Paris 11, Villejuif, France
    Cell Cycle 8:1030-5. 2009
    ..In conclusion, tetraploid cells are particular vulnerable to undergo mitotic catastrophe after genetic or pharmacological inhibition of Eg5...
  75. ncbi The synthetic heteroarotinoid SHetA2 induces apoptosis in squamous carcinoma cells through a receptor-independent and mitochondria-dependent pathway
    Kyung Hee Chun
    Department of Thoracic Head and Neck Medical Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Res 63:3826-32. 2003
    ..Further investigation of the potential of SHetA2 in prevention and therapy of HNSCC is warranted also because of much lower toxicities compared with receptor active retinoids...
  76. pmc Minus-end capture of preformed kinetochore fibers contributes to spindle morphogenesis
    Alexey Khodjakov
    Division of Molecular Medicine, Wadsworth Center, New York State Department of Health, Albany, NY 12201, USA
    J Cell Biol 160:671-83. 2003
    ..We propose that the capture and incorporation of preformed K-fibers complements the microtubule plus-end capture mechanism and contributes to spindle formation in vertebrates...
  77. ncbi Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5
    Sébastien Brier
    Laboratoire de Spectrométrie de Masse des Protéines, Institut de Biologie Structurale CEA CNRS UJF, 41, rue Jules Horowitz, 38027 Grenoble Cedex 01, France
    Biochemistry 43:13072-82. 2004
    ..It is likely that S-trityl-l-cysteine and monastrol inhibit HsEg5 by a similar mechanism. The common inhibitor binding region appears to represent a "hot spot" for HsEg5 that could be exploited for further inhibitor screening...
  78. ncbi Contrasting effects of phosphatidylinositol- and phosphatidylcholine-specific phospholipase C on apoptosis in cultured endothelial cells
    Xia Liu
    Institute of Developmental Biology, School of Life Science, Shandong University, Jinan, China
    Endothelium 13:205-11. 2006
    ..Contrarily, suppression of PC-PLC promoted the phosphorylation of Akt. The data suggested that PI-PLC and PC-PLC might control the apoptosis by jointly regulating Akt phosphorylation, P53 expression, and affecting cell cycle in VECs...
  79. ncbi Induction of Nrf2-regulated genes by 3H-1, 2-dithiole-3-thione through the ERK signaling pathway in murine keratinocytes
    Sarala Manandhar
    College of Pharmacy, Yeungnam University, 214 1 Dae Dong, Gyeongsan si, Gyeongsangbuk do 712 749, South Korea
    Eur J Pharmacol 577:17-27. 2007
    ....
  80. ncbi Mechanism of cytosol phospholipase C and sphingomyelinase-induced lysosome destabilization
    Xiang Wang
    Institute of Biophysics, Chinese Academy of Sciences, Beijing 100101, China
    Biochimie 88:913-22. 2006
    ..The results suggest that cytosolic phospholipase C and sphingomyelinase may be responsible for the alterations in lysosomal stability by increasing the ion permeability...
  81. pmc Kinesin 5-independent poleward flux of kinetochore microtubules in PtK1 cells
    Lisa A Cameron
    Department of Biology, University of North Carolina at Chapel Hill, 27599, USA
    J Cell Biol 173:173-9. 2006
    ..One candidate, Kif2a (kinesin 13), was detected at minus ends of fluxing kinetochore fibers. Kif2a remains associated with the ends of K fibers upon disruption of the spindle by dynein/dynactin inhibition, and these K fibers flux...
  82. pmc Prophase microtubule arrays undergo flux-like behavior in mammalian cells
    Nick P Ferenz
    Department of Biology and Program in Molecular and Cellular Biology, University of Massachusetts, Amherst, MA 01003, USA
    Mol Biol Cell 18:3993-4002. 2007
    ..We propose that the marked reduction in rate and directionality of microtubule motion from prophase to metaphase results from changes in microtubule organization during spindle formation...
  83. ncbi In vivo protection by the xanthate tricyclodecan-9-yl-xanthogenate against amyloid beta-peptide (1-42)-induced oxidative stress
    M Perluigi
    Department of Biochemical Sciences, University of Rome La Sapienza, Rome 00185, Italy
    Neuroscience 138:1161-70. 2006
    ..Based on the above data, we suggest that tricyclodecan-9-yl-xanthogenate is a potent antioxidant and could be of importance for the treatment of Alzheimer's disease and other oxidative stress-related disorders...
  84. pmc A structural model for monastrol inhibition of dimeric kinesin Eg5
    Troy C Krzysiak
    Department of Biological Sciences, University of Pittsburgh, Pittsburgh, PA 15260, USA
    EMBO J 25:2263-73. 2006
    ....
  85. ncbi Inhibitors of kinesin Eg5: antiproliferative activity of monastrol analogues against human glioblastoma cells
    Christine Muller
    Institute of Pharmacy, University of Regensburg, Universitatsstrasse 31, 93040, Regensburg, Germany
    Cancer Chemother Pharmacol 59:157-64. 2007
    ....
  86. ncbi [Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen]
    Makoto Kinoshita
    Tanpakushitsu Kakusan Koso 52:1796-9. 2007
  87. ncbi New chemical tools for investigating human mitotic kinesin Eg5
    Emmanuel Klein
    Institut Gilbert Laustriat, CNRS Université Louis Pasteur, Faculte de Pharmacie, 74 route du Rhin, 67401 Illkirch, France
    Bioorg Med Chem 15:6474-88. 2007
    ..The results obtained led to the identification of structure-activity relationships further used to design an affinity matrix that can be used for fast and efficient purification of Eg5 from crude lysate of eukaryotic cells...
  88. pmc Cellular mechanisms of burst firing-mediated long-term depression in rat neocortical pyramidal cells
    Antonny Czarnecki
    Department of Physiology, University of Bern, Buhlplatz 5, 3012 Bern, Switzerland
    J Physiol 578:471-9. 2007
    ..Thus burst-firing constitutes a signal by which coincident synaptic inputs are proportionally downsized. Overall, our data thus suggest a mechanism by which synaptic weights can be reconfigured during non-rapid eye movement sleep...
  89. ncbi Rapid preparation of the mitotic kinesin Eg5 inhibitor monastrol using controlled microwave-assisted synthesis
    Doris Dallinger
    Christian Doppler Laboratory for Microwave Chemistry and Institute of Chemistry, Karl Franzens University Graz, Heinrichstrasse 28, A 8010 Graz, Austria
    Nat Protoc 2:317-21. 2007
    ..Monastrol synthesis can be conducted in approximately 2 h by employing the precipitation/filtration purification method...
  90. ncbi Inhibition of PC-PLC blocked the survival of mouse neural cells by up-regulating the expression of integrin beta4 and Rb
    Xin Lv
    Institute of Developmental Biology, School of Life Science, Shandong University, Jinan, China
    Dev Neurosci 28:499-504. 2006
    ..The changes of intracellular ROS level induced by D609 indicated that a modest level of ROS might be indispensable to neural cell survival...
  91. ncbi Priming by tumor necrosis factor-alpha of human neutrophil NADPH-oxidase activity induced by anti-proteinase-3 or anti-myeloperoxidase antibodies
    Dominique Reumaux
    Faculte des Sciences Pharmaceutiques et Biologiques, Universite de Lille 2, 3 rue du Professeur Laguesse, 59006 Lille Cedex, France
    J Leukoc Biol 80:1424-33. 2006
    ..Our results indicate direct effects of TNF-alpha in facilitating neutrophil activation by these antibodies and further support the importance of cytoskeletal rearrangements in this priming process...
  92. ncbi Calcium signaling in human airway goblet cells following purinergic activation
    Andrea H Rossi
    CF Pulmonary Research and Treatment Center, Department of Cell and Molecular Physiology, University of North Carolina, Chapel Hill, NC 27599 7248, USA
    Am J Physiol Lung Cell Mol Physiol 292:L92-8. 2007
    ..1 +/- 7% of the ATPgammaS control peak), brief rise in Ca(i)(2+). This diminutive signal likely denotes a local Ca(2+) gradient, which may be associated with the mucin granule exocytotic process...
  93. pmc Kinesin-5 motors are required for organization of spindle microtubules in Silvetia compressa zygotes
    Nick T Peters
    Department of Biology, University of Utah, Salt Lake City, UT 84112, USA
    BMC Plant Biol 6:19. 2006
    ..Monastrol, a chemical inhibitor specific to the Kinesin-5 family of motor proteins, was used to examine the functional roles of Kinesin-5 proteins during the first, asymmetric cell division cycle in the brown alga Silvetia compressa...
  94. ncbi Phosphatidylcholine-specific phospholipase C, p53 and ROS in the association of apoptosis and senescence in vascular endothelial cells
    Yizhe Cheng
    Institute of Developmental Biology, School of Life Science, Shandong University, Jinan 250100, China
    FEBS Lett 580:4911-5. 2006
    ..The data suggested that PC-PLC was involved in the association of apoptosis and senescence. Its function might be closely related to the level of p53 in VECs...
  95. ncbi Suppressing phosphatidylcholine-specific phospholipase C and elevating ROS level, NADPH oxidase activity and Rb level induced neuronal differentiation in mesenchymal stem cells
    Nan Wang
    Institute of Developmental Biology, School of Life Science, Shandong University, Jinan, China
    J Cell Biochem 100:1548-57. 2007
    ..Furthermore, the level of Rb protein was evidently elevated. Our data suggested that PC-PLC mediated neuronal differentiation of rat MSCs by elevating NADPH oxidase activity, ROS level, and up-regulating the expression of Rb protein...
  96. ncbi Crystal structure of HsEg5 in complex with clinical candidate CK0238273 provides insight into inhibitory mechanism, potency, and specificity
    Bin Zhang
    ArQule Biomedical Institute, ArQule Incorporated, 333 Providence Highway, Norwood, MA 02062, USA
    Biochem Biophys Res Commun 372:565-70. 2008
    ..We believe that the combination of these interactions defines the superior potency and specificity of CK0238273...
  97. ncbi Allosteric inhibition of kinesin-5 modulates its processive directional motility
    Benjamin H Kwok
    Laboratory of Chemistry and Cell Biology, The Rockefeller University, 1230 York Avenue, New York, New York 10021, USA
    Nat Chem Biol 2:480-5. 2006
    ..Monastrol suppresses the directional processive motility of microtubule-bound Eg5. These data on Eg5's allosteric inhibition will impact these inhibitors' use as probes and development as chemotherapeutic agents...
  98. ncbi Methylmercury-induced toxicity is mediated by enhanced intracellular calcium through activation of phosphatidylcholine-specific phospholipase C
    Mi Sun Kang
    Department of Environmental and Health Chemistry, College of Pharmacy, Chung Ang University, Seoul, 221 Huksuk Dong, Dongjak Ku, Seoul 156 756, South Korea
    Toxicol Appl Pharmacol 216:206-15. 2006
    ..Our results demonstrated that MeHg-induced toxicity was linked to elevation of [Ca(2+)](i) through activation of PC-PLC, but not attributable to the signaling pathways such as cPLA(2), A-SMase, and PKC, or to the generation of ROS...
  99. pmc In vivo administration of D609 leads to protection of subsequently isolated gerbil brain mitochondria subjected to in vitro oxidative stress induced by amyloid beta-peptide and other oxidative stressors: relevance to Alzheimer's disease and other oxidativ
    Mubeen Ahmad Ansari
    Department of Chemistry, University of Kentucky, Lexington, KY 40506, USA
    Free Radic Biol Med 41:1694-703. 2006
    ..These antiapoptotic findings are discussed with reference to the potential use of this brain-accessible glutathione mimetic in the treatment of oxidative stress-related neurodegenerative disorders, including AD...
  100. ncbi Role of mitotic motors, dynein and kinesin, in the induction of abnormal centrosome integrity and multipolar spindles in cultured V79 cells exposed to dimethylarsinic acid
    Takafumi Ochi
    Department of Toxicology and Environmental Health, Faculty of Pharmaceutical Sciences, Teikyo University, Sagamiko, Kanagawa 199 0195, Japan
    Mutat Res 499:73-84. 2002
    ..In addition, the results suggest that kinesin plays a role not only in the induction of mitotic centrosome abnormality, but also in maintenance...
  101. pmc Phospholipases C and A2 control lysosome-mediated IL-1 beta secretion: Implications for inflammatory processes
    Cristina Andrei
    Cell Transport Unit, Department of Oncogenesis, National Cancer Research Institute, 16132 Genoa, Italy
    Proc Natl Acad Sci U S A 101:9745-50. 2004
    ..This activation is ultimately responsible for lysosome exocytosis and IL-1 beta secretion...

Research Grants28

  1. Dithiole thiones and ones--Chemistry to Biochemistry
    JAMES FISHBEIN; Fiscal Year: 2005
    ..proposal is to understand the detailed molecular basis for the cancer chemopreventitive effects of 1,2-dithiole-3-thiones and 1,2-dithiole-3-ones...
  2. TLR Signal Inhibition: a Novel Therapeutic Paradigm
    Leonard D Kohn; Fiscal Year: 2010
    ..pursuing studies based on its Phase I award, IC has shown that a lead compound from a family of tautomeric cyclic thiones (TCTs), phenylmethimazole (C10), is effective in multiple in vitro and/or in vivo models of autoimmune-..
  3. TLR Signal Inhibition: a Novel Therapeutic Paradigm
    Leonard Kohn; Fiscal Year: 2005
    ..Our company has identified a class of compounds, tautomeric cyclic thiones (TCT), that we believe can inhibit pathologic TLR expression and/or signaling and fit this need...
  4. Steroids and Stem Cell in Carcinogenesis
    Doris Benbrook; Fiscal Year: 2004
    ..This research will enhance our understanding of the process of carcinogenesis and chemoprevention, which could ultimately translate into strategies and pharmaceuticals for prevention of cancer. ..
  5. Mechanism of SHeA2 Action in Ovarian Cancer
    Doris Benbrook; Fiscal Year: 2009
    ..The elucidation of the proteins involved in the SHetA2 pathwayswill provide potential biomarkers for ovarian cancer diagnosis, prevention and treatment strategies. ..
  6. CDP-choline: Mechanisms in Cerebral Ischemia
    RAO ADIBHATLA; Fiscal Year: 2006
    ..Arachidonic acid activates neutral sphingomyelinase, resulting in membrane disintegration. PCCT activity was stimulated by exogenous CDP-choline. Aim 2 will be tested in gerbil transient forebrain ischemia. ..
  7. Chemical genetic analysis of intracellular Transport
    Tarun Kapoor; Fiscal Year: 2007
    ..It is likely that these small molecules will lead to the identification of new targets for therapeutic agents and improved treatments of human diseases. ..
  8. Choline Tracers for Imaging of Cancer
    Timothy DeGrado; Fiscal Year: 2007
    ..abstract_text> ..
  9. Role of EGFR in Viral Infected Lung Epithelial Cells
    Martha M Monick; Fiscal Year: 2010
    ..Completion of these studies will add to our understanding of mechanisms of RSV infection of airway epithelium and the role of targeted signaling pathways in the subsequent inflammation and life span of infected cells. ..
  10. Mechanisms of Microtubule Dynamic Turnover
    Patricia Wadsworth; Fiscal Year: 2009
    ..Learning how normal cells construct a mitotic spindle is an important first step towards understanding defective cell division in cancer. ..
  11. ASYMMETRIC SYNTHESIS OF ANTITUMOR AGENTS
    MICHAEL CRIMMINS; Fiscal Year: 2005
    ..Laulimalide stimulates tubulin polymerization more effectively than paclitaxel. Laulimalide is a representative of a new class of microtubule stabilizing agents with promise for therapeutic potential. ..
  12. ASYMMETRIC SYNTHESIS OF NOVEL NATURAL PRODUCTS
    MICHAEL CRIMMINS; Fiscal Year: 2006
    ..Synthesis of the biologically active agents guanacastepene, and SCH 351448 will also be pursued. ..
  13. NOVEL RADIOTRACERS FOR ANDROGEN RECEPTOR IMAGING
    MARCIAN VAN DORT; Fiscal Year: 2001
    ..abstract_text> ..
  14. ASYMMETRIC SYNTHESIS OF IONOPHORE/MACROLIDE ANTIBIOTICS
    David Evans; Fiscal Year: 2005
    ..Our goal has been to set in place all of the reactions necessary for the rapid assemblage of any polyketide target structure. ..
  15. Origins of Spontaneous Mutagenesis
    Joseph Guttenplan; Fiscal Year: 2005
    ..abstract_text> ..
  16. Chemopreventive Efficacy of Broccoli Sprouts in Humans
    Thomas Kensler; Fiscal Year: 2004
    ..abstract_text> ..
  17. Purchase of Leica TCS SP2 Confocal Microscope
    Patricia Wadsworth; Fiscal Year: 2002
    ....
  18. Protection by Induction of Ubiquitin-Proteasome Systems
    Thomas Kensler; Fiscal Year: 2005
    ....
  19. Automated Synthesis of F-18 Fluorocholine
    Timothy DeGrado; Fiscal Year: 2002
    ..abstract_text> ..
  20. Synthesis of Polyketides and Terpenes
    David A Evans; Fiscal Year: 2010
    ..As a consequence, organic synthesis is a critical discipline that continues to have an important impact on the fields of both medicine and biology. ..
  21. Cellular Signaling Mechanisms in Macrophage Activation.
    Joseph Cuschieri; Fiscal Year: 2007
    ..Through an enhanced understanding of these mechanisms it is our goal that potential therapeutic targets may be discovered to regulate the inflammatory response following trauma/hemorrhage and ischemia/reperfusion. ..
  22. Mutagenicity of tobacco smoke in human cell co-cultures
    Joseph Guttenplan; Fiscal Year: 2007
    ..Clearly, it is preferable to determine their potential risk prospectively, rather than retrospectively. [unreadable] [unreadable] [unreadable]..
  23. Isothiocyanates in the Chemoprevention of Bladder Cancer
    Yuesheng Zhang; Fiscal Year: 2007
    ..Aim 5 will determine the efficacy of an orally administered ITC in inhibiting N-butyl-N- (4-hydroxybutyl)-nitrosamine-induced bladder tumorigenesis in F344 rats. ..
  24. PET TRACERS FOR MYOCARDIAL FATTY ACID OXIDATION
    Timothy DeGrado; Fiscal Year: 2003
    ....
  25. ASYMMETRIC SYNTHESIS OF VANCOMYCIN ANTIBIOTICS
    David Evans; Fiscal Year: 2001
    ..During the course of this project we intend to confirm (correct) the absolute stereochemical assignments of the principal members of this family by total synthesis. ..
  26. Zinc transport and homeostasis in cortical neurons
    Robert Colvin; Fiscal Year: 2002
    ..What is the identity of Zn2+ containing compartments in the cell body and processes of cortical neurons?..
  27. Micromass LCT Mass Spectrometer
    MICHAEL CRIMMINS; Fiscal Year: 2004
    ..The major users group is highly dependent on rapid turn around mass spectral data. Since there is currently no Departmental mass spectrometry facility, the research programs of the major users have been seriously hampered for some time. ..