thiourea

Summary

Summary: A photographic fixative used also in the manufacture of resins. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance may reasonably be anticipated to be a carcinogen (Merck Index, 9th ed). Many of its derivatives are ANTITHYROID AGENTS and/or FREE RADICAL SCAVENGERS.

Top Publications

  1. ncbi A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress
    Michael Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 307:935-9. 2005
  2. pmc The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter
    J Santo-Domingo
    Departamento de Bioquimica y Biologia Molecular y Fisiologia, Facultad de Medicina, Instituto de Biologia y Genetica Molecular, Universidad de Valladolid and Consejo Superior de Investigaciones Cientificas, Valladolid, Spain
    Br J Pharmacol 151:647-54. 2007
  3. doi Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivatives
    Carmen Limban
    Pharmaceutical Chemistry Department, University of Medicine and Pharmacy Carol Davila, Bucharest, Romania
    Molecules 16:7593-607. 2011
  4. doi Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moiety
    Mei Hang Chen
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, People s Republic of China
    J Agric Food Chem 57:1383-8. 2009
  5. pmc (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
    Shiv K Sharma
    Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Avenue, Detroit, Michigan 48202, USA
    J Med Chem 53:5197-212. 2010
  6. pmc Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalysts
    Robert R Knowles
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA
    Proc Natl Acad Sci U S A 107:20678-85. 2010
  7. pmc Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunction
    Guorui Dou
    Arnold and Beckman Macular Research Center, Doheny Eye Institute, 1355 San Pablo Street, Los Angeles, CA 90033, USA
    Free Radic Biol Med 53:1111-22. 2012
  8. doi Na+-Ca2+ exchanger contributes to Ca2+ extrusion in ATP-stimulated endothelium of intact rat aorta
    Roberto Berra-Romani
    School of Medicine, Department of Biomedicine, 13 Sur 2702, Colonia Volcanes, 72000 Puebla, Mexico
    Biochem Biophys Res Commun 395:126-30. 2010
  9. pmc Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors
    Hannes C A Drexler
    Department of Vascular Cell Biology, Max Planck Institute for Molecular Biomedicine, Muenster, Germany
    PLoS ONE 4:e4161. 2009
  10. pmc MreB drives de novo rod morphogenesis in Caulobacter crescentus via remodeling of the cell wall
    Constantin N Takacs
    Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut 06520, USA
    J Bacteriol 192:1671-84. 2010

Research Grants

Detail Information

Publications260 found, 100 shown here

  1. ncbi A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stress
    Michael Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA 02115, USA
    Science 307:935-9. 2005
    ..More broadly, salubrinal demonstrates the feasibility of selective pharmacological targeting of cellular dephosphorylation events...
  2. pmc The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporter
    J Santo-Domingo
    Departamento de Bioquimica y Biologia Molecular y Fisiologia, Facultad de Medicina, Instituto de Biologia y Genetica Molecular, Universidad de Valladolid and Consejo Superior de Investigaciones Cientificas, Valladolid, Spain
    Br J Pharmacol 151:647-54. 2007
    The thiourea derivative KB-R7943, originally developed as inhibitor of the plasma membrane Na(+)/Ca(2+) exchanger, has been shown to protect against myocardial ischemia-reperfusion injury...
  3. doi Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivatives
    Carmen Limban
    Pharmaceutical Chemistry Department, University of Medicine and Pharmacy Carol Davila, Bucharest, Romania
    Molecules 16:7593-607. 2011
    ..presence of one iodine, bromide or fluorine, and two or three chloride atoms on the N-phenyl substituent of the thiourea moiety, being significant especially on Pseudomonas aeruginosa and Staphylococcus aureus strains, known for their ..
  4. doi Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moiety
    Mei Hang Chen
    Center for Research and Development of Fine Chemicals, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, People s Republic of China
    J Agric Food Chem 57:1383-8. 2009
    ..5, 50.4, and 50.4%, respectively) as the commercial product Ningnanmycin (56.2%). This would appear to be the first report of the synthesis and antiviral activity of chiral thiourea derivatives containing an alpha-aminophosphonate moiety.
  5. pmc (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulators
    Shiv K Sharma
    Department of Pharmaceutical Sciences, Wayne State University, 259 Mack Avenue, Detroit, Michigan 48202, USA
    J Med Chem 53:5197-212. 2010
    ..These compounds represent an important new series of epigenetic modulators with the potential for use as antitumor agents...
  6. pmc Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalysts
    Robert R Knowles
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA
    Proc Natl Acad Sci U S A 107:20678-85. 2010
    ..This perspective will outline some recent efforts to elucidate the cooperative mechanisms responsible for stereoinduction in highly enantioselective reactions promoted by noncovalent catalysts...
  7. pmc Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunction
    Guorui Dou
    Arnold and Beckman Macular Research Center, Doheny Eye Institute, 1355 San Pablo Street, Los Angeles, CA 90033, USA
    Free Radic Biol Med 53:1111-22. 2012
    ..Thus, these data collectively demonstrate that αB crystallin provides critical protection of mitochondrial function during ER stress-induced RPE apoptosis...
  8. doi Na+-Ca2+ exchanger contributes to Ca2+ extrusion in ATP-stimulated endothelium of intact rat aorta
    Roberto Berra-Romani
    School of Medicine, Department of Biomedicine, 13 Sur 2702, Colonia Volcanes, 72000 Puebla, Mexico
    Biochem Biophys Res Commun 395:126-30. 2010
    ..These data show that, within the same preparation, NCX operates in both modes, depending on the chemical nature of the extracellular stimulus...
  9. pmc Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitors
    Hannes C A Drexler
    Department of Vascular Cell Biology, Max Planck Institute for Molecular Biomedicine, Muenster, Germany
    PLoS ONE 4:e4161. 2009
    ....
  10. pmc MreB drives de novo rod morphogenesis in Caulobacter crescentus via remodeling of the cell wall
    Constantin N Takacs
    Department of Molecular, Cellular and Developmental Biology, Yale University, New Haven, Connecticut 06520, USA
    J Bacteriol 192:1671-84. 2010
    ..Our results provide insight into MreB function in peptidoglycan remodeling and rod shape morphogenesis and suggest that MreB promotes the transglycosylase activity of penicillin-binding proteins...
  11. pmc Sex differences in the effects of inherited bitter thiourea sensitivity on body weight in 4-6-year-old children
    Kathleen L Keller
    Department of Research Medicine and the New York Obesity Research Center, St Luke s Roosevelt Hospital Center, Columbia University College of Physicians and Surgeons, New York, New York, USA
    Obesity (Silver Spring) 18:1194-200. 2010
    ..These results suggest that the TAS2R38 variation, PROP phenotype, and sex interact to impact obesity risk in children. Future studies should be done to determine how this trait influences energy balance...
  12. ncbi Antinociceptive pharmacology of N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea, a high-affinity competitive antagonist of the transient receptor potential vanilloid 1 receptor
    Lei Tang
    Department of Biopharmaceutical Sciences, and Cancer Center, University of Illinois, 833 South Woods St, Chicago, IL 60612, USA
    J Pharmacol Exp Ther 321:791-8. 2007
    ..Recently, N-(4-chlorobenzyl)-N'-(4-hydroxy-3-iodo-5-methoxybenzyl) thiourea (IBTU) was synthesized, and it was found in vitro to be a high-affinity competitive antagonist of cytoplasmic, ..
  13. pmc Isothioureas: potent inhibitors of nitric oxide synthases with variable isoform selectivity
    G J Southan
    William Harvey Research Institute, St Bartholomew s Hospital Medical College, London
    Br J Pharmacol 114:510-6. 1995
    ....
  14. ncbi Induction of autophagic cell death by a novel molecule is increased by hypoxia
    Marco Tafani
    Department of Cellular and Molecular Pathology, IRCCS San Raffaele Pisana, Rome, Italy
    Autophagy 4:1042-53. 2008
    ..These results indicate that activation of the autophagic pathway in hypoxic cells by the new molecule CR 3294, as well as by TFP or SW, can have potentially important implications for cancer treatment...
  15. ncbi Studies on the anti-proliferative effects of novel DNA-intercalating bipyridyl-thiourea-Pt(II) complexes against cisplatin-sensitive and -resistant human ovarian cancer cells
    Gaetano Marverti
    Dipartimento di Scienze Biomediche, Sezione di Chimica Biologica, Universita di Modena e Reggio Emilia, Via Campi 287, 41100 Modena, Italy
    J Inorg Biochem 102:699-712. 2008
    Six bipyridyl complexes of platinum(II) with thiourea, with different substituents on thiourea moiety [Pt(bipy)(R,R'NCSNR'',R''')(2)]Cl(2) (bipy=2,2'-bipyridine: R=R'=R''=R''' =H; R=Me, R'=R''=R'''=H; R=n-Bu, R'=R''=R'''=H; R=Et, R'=H, R''..
  16. pmc Enantioselective thiourea-catalyzed cationic polycyclizations
    Robert R Knowles
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 132:5030-2. 2010
    A new thiourea catalyst is reported for the enantioselective cationic polycyclization of hydroxylactams...
  17. ncbi Selective inhibition of eukaryotic translation initiation factor 2 alpha dephosphorylation potentiates fatty acid-induced endoplasmic reticulum stress and causes pancreatic beta-cell dysfunction and apoptosis
    Miriam Cnop
    Laboratory of Experimental Medicine, Universite Libre de Bruxelles, 1070 Brussels, Belgium
    J Biol Chem 282:3989-97. 2007
    ..This modifies the present paradigm regarding the beneficial role of eIF2alpha phosphorylation in beta-cells and must be taken into consideration when designing therapies to protect beta-cells in type 2 diabetes...
  18. pmc Mechanism of amido-thiourea catalyzed enantioselective imine hydrocyanation: transition state stabilization via multiple non-covalent interactions
    Stephan J Zuend
    Harvard University, Department of Chemistry and Chemical Biology, Cambridge, Massachusetts 02138, USA
    J Am Chem Soc 131:15358-74. 2009
    An experimental and computational investigation of amido-thiourea promoted imine hydrocyanation has revealed a new and unexpected mechanism of catalysis...
  19. ncbi Antifungal efficacy of chitosan and its thiourea derivatives upon the growth of some sugar-beet pathogens
    M Eweis
    Department of Botany, Faculty of Science, Cairo University, Cairo, Egypt
    Int J Biol Macromol 38:1-8. 2006
    Chitosan (CS) was modified by reaction with benzoyl thiocyanate to give a thiourea derivative (TUCS)...
  20. doi N-D-aldopentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives: potential anti-TB therapeutic agents
    Avraham Liav
    Department of Microbiology, Immunology and Pathology, Colorado State University, 1682 Campus Delivery, Fort Collins, CO 80523, USA
    Bioorg Med Chem Lett 18:2649-51. 2008
    Thiocarlide (THC; N,N'-bis[p-(isoamyloxy)phenyl]-thiourea; also known as isoxyl) has been used in the past as anti-tuberculosis agent...
  21. ncbi Acetylcholine-induced asynchronous calcium waves in intact human bronchial muscle bundle
    Jiazhen M Dai
    The James Hogg iCAPTURE Center for Cardiovascular and Pulmonary Research, University of British Columbia, and St Paul s Hospital, Room 166, 1081 Burrard Street, Vancouver, BC, V6Z 1Y6 Canada
    Am J Respir Cell Mol Biol 36:600-8. 2007
    ..These findings for the first time demonstrate the occurrence and the role of ACW in excitation-contraction coupling in adult human ASM...
  22. pmc Osteoporosis regulation by salubrinal through eIF2α mediated differentiation of osteoclast and osteoblast
    Long He
    Korea Research Institute of Bioscience and Biotechnology KRIBB, Korea
    Cell Signal 25:552-60. 2013
    ..In addition, modulation of ATF4 and NFATc1 expressions through eIF2α phosphorylation could be a valuable target for the treatment of osteoporosis...
  23. pmc Novel class of thiourea compounds that inhibit herpes simplex virus type 1 DNA cleavage and encapsidation: resistance maps to the UL6 gene
    M van Zeijl
    Department of Molecular Biology Virology, Wyeth Ayerst Research, Pearl River, New York 10965, USA
    J Virol 74:9054-61. 2000
    In our search for novel inhibitors of herpes simplex virus type 1 (HSV-1), a new class of thiourea inhibitors was discovered...
  24. doi Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activity
    Jan Balzarini
    Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
    Mol Pharmacol 75:1127-36. 2009
    Substituted 3'-thiourea derivatives of beta-thymidine (dThd) and 5'-thiourea derivatives of alpha-dThd have been evaluated for their inhibitory activity against recombinant human cytosolic dThd kinase-1 (TK-1), human mitochondrial TK-2, ..
  25. ncbi Differential branchial and renal handling of urea, acetamide and thiourea in the gulf toadfish Opsanus beta: evidence for two transporters
    M D McDonald
    McMaster University, Life Science Building, Hamilton, Ontario, Canada
    J Exp Biol 203:1027-37. 2000
    ..urinary ureteral catheters and injected with an iso-osmotic dose of (14)C-labelled urea analogue (acetamide or thiourea) calculated to bring plasma analogue concentrations close to plasma urea concentrations...
  26. doi Salubrinal promotes healing of surgical wounds in rat femurs
    Ping Zhang
    Department of Biomedical Engineering, Indiana University Purdue University Indianapolis, SL220, 723 West Michigan Street, Indianapolis, IN, 46202, USA
    J Bone Miner Metab 30:568-79. 2012
    ..In summary, the results herein demonstrate that subcutaneous administration of salubrinal accelerates healing of surgically generated bone holes through the modulation of eIF2α phosphorylation...
  27. pmc Salubrinal attenuates β-amyloid-induced neuronal death and microglial activation by inhibition of the NF-κB pathway
    Xiumei Huang
    Fujian Provincial Key Laboratory of Neurodegenerative Disease and Aging Research, College of Medicine, Xiamen University, Xiamen, Fujian, China
    Neurobiol Aging 33:1007.e9-17. 2012
    ..This study also suggests that modulation of Aβ-induced NF-κB activation could be a potential therapeutic strategy for Alzheimer's disease...
  28. doi Adsorption of platinum(IV) and palladium(II) from aqueous solution by thiourea-modified chitosan microspheres
    Limin Zhou
    Key Laboratory of Nuclear Resources and Environment Ministry of Education, East China Institute of Technology, Xuefu Road No 56, Fuzhou, Jiangxi 344000, PR China
    J Hazard Mater 172:439-46. 2009
    The chitosan microparticles were prepared using the inverse phase emulsion dispersion method and modified with thiourea (TCS)...
  29. doi Characteristics of equilibrium, kinetics studies for adsorption of Hg(II), Cu(II), and Ni(II) ions by thiourea-modified magnetic chitosan microspheres
    Limin Zhou
    Key Laboratory of Nuclear Resources and Environment East China Institute of Technology, Ministry of Education, Xuefu Road No 56, Fuzhou, Jiangxi 344000, PR China
    J Hazard Mater 161:995-1002. 2009
    Magnetic chitosan microspheres were prepared and chemically modified with thiourea (TMCS) for adsorption of metal ions...
  30. doi Rational design and 3D-pharmacophore mapping of 5'-thiourea-substituted alpha-thymidine analogues as mycobacterial TMPK inhibitors
    Carolina H Andrade
    Faculty of Pharmaceutical Sciences, Av Prof Lineu Prestes, 580, University of Sao Paulo, Sao Paulo, 05508 900, Brazil
    J Chem Inf Model 49:1070-8. 2009
    ..RI) 4D-QSAR formalism has been used to develop QSAR models and corresponding 3D-pharmacophores for a set of 5'-thiourea-substituted alpha-thymidine inhibitors...
  31. doi Synthesis of some urea and thiourea derivatives of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidine and their antagonistic effects on haloperidol-induced catalepsy and oxidative stress in mice
    Faizul Azam
    Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seventh October, Misurata, Libya
    Eur J Med Chem 44:3889-97. 2009
    A series of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7-yl urea and thiourea derivatives were designed and synthesized...
  32. doi Recovery of silver (I) using a thiourea-modified chitosan resin
    Lin Wang
    Institute of Oceanology, The Chinese Academy of Sciences, Qingdao, 266071, China
    J Hazard Mater 180:577-82. 2010
    ..The resin was synthesized by using O-carboxymethylated chitosan to cross-link a polymeric Schiff's base of thiourea/glutaraldehyde and characterized by IR. Batch method was applied for testing the resin's adsorption behavior...
  33. ncbi Evaluation of nitrification-inhibition measurements
    K Jonsson
    Department of Water and Environmental Engineering, Lund Institute of Technology, P O Box 118, SE 221 00 Lund, Sweden
    Water Sci Technol 43:201-8. 2001
    ..Allyl-thiourea (ATU), methanol, chromium and zinc were used as reference toxicants in combination with different kinds of full-..
  34. doi (Thio)urea organocatalysis--what can be learnt from anion recognition?
    Zhiguo Zhang
    Institut fur Organische Chemie, Justus Liebig Universitat Giessen, Heinrich Buff Ring 58, D 35392, Giessen, Germany
    Chem Soc Rev 38:1187-98. 2009
    ..In turn, the discovery and mechanistic elucidation of such reactions is likely to improve the understanding of enzyme active sites (108 references)...
  35. pmc KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex I
    Tatiana Brustovetsky
    Department of Pharmacology and Toxicology Stark Neuroscience Research Institute, Indiana University School of Medicine, Indianapolis, IN, USA
    Br J Pharmacol 162:255-70. 2011
    ..Here, the effects of KB-R7943 on N-methyl-D-aspartate (NMDA) receptors and mitochondrial complex I were tested...
  36. doi Comparative gene transfer between cationic and thiourea lipoplexes
    Marie Breton
    INSERM, U640, CNRS, UMR8151, Unite de Pharmacologie Chimique et Genetique, Universite Paris Descartes, Faculte de Pharmacie, Paris, France
    J Gene Med 12:45-54. 2010
    ..To further evaluate these lipids, we investigated the internalization process of the thiourea lipoplexes and their intracellular mechanism of transfection versus that of cationic lipoplexes.
  37. pmc Specific inhibition of human cytomegalovirus glycoprotein B-mediated fusion by a novel thiourea small molecule
    Thomas R Jones
    Infectious Disease Section, Wyeth Research, Pearl River, New York 10965, USA
    J Virol 78:1289-300. 2004
    ..Furthermore, CFI02 inhibits the cell-cell spread of HCMV. This is the first study of a potent and selective small molecule inhibitor of CMV fusion and cell-cell spread...
  38. doi Bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst: the asymmetric synthesis of dihydropyrimidines
    Yangyun Wang
    State Key Laboratory and Institute of Elemento Organic Chemistry, Nankai University, Tianjin, 300071, China
    Org Biomol Chem 9:3050-4. 2011
    An enantioselective Biginelli reaction has been developed by using a bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst and t-BuNH(2)·TFA as an additive in saturated brine at room temperature...
  39. doi The importance of the oxidative character of doubly charged metal cations in binding neutral bases. [Urea-M]2+ and [thiourea-M]2+ (M = Mg, Ca, Cu) complexes
    Cristina Trujillo
    Departamento de Quimica, C 9, Universidad Autonoma de Madrid, Cantoblanco, 28049 Madrid, Spain
    Phys Chem Chem Phys 10:3229-35. 2008
    ..of the electron density, namely AIM, ELF and NBO, yield coherent descriptions of the bonding in [urea-M](2+) and [thiourea-M](2+) (M = Mg, Ca, Cu) complexes, whose geometries have been optimized at the B3LYP/6-311+G(d,p) level of theory...
  40. ncbi Involvement of Na(+)/Ca(2+) exchanger in endothelial NO production and endothelium-dependent relaxation
    Jean Christophe Schneider
    Service de Physiologie Explorations Fonctionnelles, Centre Hospitalier Universitaire Cochon, Assistance Publique, Hopitaux de Paris, Universite Paris 5, 75014 Paris, France
    Am J Physiol Heart Circ Physiol 283:H837-44. 2002
    ..These findings confirm the key role of NCX in reverse mode on Ca(2+)-dependent NO production and endothelium-dependent relaxation...
  41. ncbi Functional differences of Na+/Ca2+ exchanger expression in Ca2+ transport system of smooth muscle of guinea pig stomach
    Yasushi Sakai
    Division of Physiolgy, Department of Occupational Therapy, School of Nursing and Rehabilitation Sciences, Yokohama, Japan
    Can J Physiol Pharmacol 83:791-7. 2005
    ..Results documented evidence that NCX2 isoform functionally contributes to Ca2+ extrusion and maintenance of contraction-relaxation cycle in gastric fundus smooth muscle...
  42. ncbi Structure-activity relationship study of the bacterial actin-like protein MreB inhibitors: effects of substitution of benzyl group in S-benzylisothiourea
    Noritaka Iwai
    Department of Bioengineering, Tokyo Institute of Technology, Japan
    Biosci Biotechnol Biochem 71:246-8. 2007
    ..A 2,4-Cl2-derivative was found to be the most effective compound, it was stronger than the original one in Gram-negative rod shaped-bacteria such as Escherichia coli and Salmonella typhimurium...
  43. doi The dimethylthiourea-induced attenuation of cisplatin nephrotoxicity is associated with the augmented induction of heat shock proteins
    Takayuki Tsuji
    First Department of Medicine, Hamamatsu University School of Medicine, 1 20 1 Handayama, Higashi ku, Hamamatsu, Shizuoka 431 3192, Japan
    Toxicol Appl Pharmacol 234:202-8. 2009
    ..The findings suggest that DMTU may afford protection against CDDP-induced ARF, partially through the early induction of cytoplasmic HSP60, thereby preventing the Bax-mediated apoptosis in renal tubular cells...
  44. ncbi Pharmacology of KB-R7943: a Na+-Ca2+ exchange inhibitor
    Md Shah Amran
    Department of Pharmacology, Interdisciplinary Graduate School of Medicine and Engineering, University of Yamanashi, Tamaho, Nakakoma, Yamanashi 409 3898, Japan
    Cardiovasc Drug Rev 21:255-76. 2003
    ....
  45. doi Highly enantio- and diastereoselective Mannich reactions of glycine Schiff bases with in situ generated N-Boc-imines catalyzed by a cinchona alkaloid thiourea
    Haile Zhang
    The Skaggs Institute for Chemical Biology and the Departments of Chemistry and Molecular Biology, The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037
    Org Lett 12:708-11. 2010
    ..Imines were generated in situ from bench-stable alpha-amido sulfones. Catalysis mediated by a cinchona alkaloid thiourea provided optically active alpha,beta-diamino acid derivatives with up to 99% ee and near-perfect ..
  46. pmc Direction-independent block of bi-directional Na+/Ca2+ exchange current by KB-R7943 in guinea-pig cardiac myocytes
    J Kimura
    Department of Pharmacology, Fukushima Medical University, School of Medicine, Fukushima 960 1295, Japan
    Br J Pharmacol 128:969-74. 1999
    ..The difference could be attributed to slow dissociation of the drug from the exchanger...
  47. ncbi Free radicals generated in yeast by the Salmonella test-negative carcinogens benzene, urethane, thiourea and auramine O
    R J Brennan
    Dept of Cancer Cell Biology, Harvard School of Public Health, Boston, MA 02115 6021, USA
    Mutat Res 403:65-73. 1998
    ..of intracellular free radical species by the diverse Salmonella-negative carcinogens benzene, urethane, thiourea and auramine O...
  48. pmc Effect of SEA0400, a novel inhibitor of sodium-calcium exchanger, on myocardial ionic currents
    Hikaru Tanaka
    Department of Pharmacology, Toho University School of Pharmaceutical Sciences, Funabashi, Chiba 274 8510, Japan
    Br J Pharmacol 135:1096-100. 2002
    ..These results indicate that SEA0400 is a potent and highly selective inhibitor of NCX, and would be a powerful tool for further studies on the role of NCX in the heart and the therapeutic potential of its inhibition...
  49. pmc Fundamental importance of Na+-Ca2+ exchange for the pacemaking mechanism in guinea-pig sino-atrial node
    Luke Sanders
    University Department of Pharmacology, Mansfield Road, Oxford OX1 3QT, UK
    J Physiol 571:639-49. 2006
    ....
  50. pmc The thioamides methimazole and thiourea inhibit growth of M. avium Subspecies paratuberculosis in culture
    Robert J Greenstein
    Department of Surgery, James J Peters VA Medical Center, Bronx, New York, United States of America
    PLoS ONE 5:e11099. 2010
    ..Because other thioamides treat tuberculosis, leprosy and M. avium complex, we hypothesized that a mode of action of some thioamide anti-thyrotoxicosis medications may include MAP growth inhibition...
  51. doi Docking and 3D QSAR study of thiourea analogs as potent inhibitors of influenza virus neuraminidase
    Jiaying Sun
    College of Bioengineering, Chongqing University, Chongqing 400044, China
    J Mol Model 16:1809-18. 2010
    Surflex-Dock was applied to study interactions between 30 thiourea analogs and neuraminidase (NA)...
  52. ncbi Development and application of Na+/Ca2+ exchange inhibitors
    Takahiro Iwamoto
    Department of Pharmacology, School of Medicine, Fukuoka University, Fukuoka, Japan
    Mol Cell Biochem 259:157-61. 2004
    ..Here, we summarize pharmacological profiles of KB-R7943 and SEA0400, the molecular mechanism of its action, and its future prospect as a novel pharmaceutical agent...
  53. ncbi Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growth
    Ineke Van Daele
    Laboratory for Medicinal Chemistry FFW, University of Gent, Harelbekestraat 72, 9000 Ghent, Belgium
    J Med Chem 50:5281-92. 2007
    ..Several hits identified within a series of 3'-C-branched thiourea-substituted beta-thymidine derivatives inspired us to construct a set of 5'-thiourea-substituted alpha-thymidine ..
  54. ncbi Calcium dynamics and vasomotion in rat mesenteric arteries
    Alexander Schuster
    Cellular Biophysics and Biomechanics Laboratory, Swiss Federal Institute of Technology, Lausanne, Switzerland
    J Cardiovasc Pharmacol 43:539-48. 2004
    ....
  55. ncbi Store-refilling involves both L-type calcium channels and reverse-mode sodium-calcium exchange in airway smooth muscle
    S Hirota
    Firestone Institute for Respiratory Health, St Joseph s Healthcare and Department of Medicine, McMaster University, Hamilton, ON, Canada L8N 4A6
    Eur Respir J 30:269-78. 2007
    ..3, respectively. Taken together, these data suggest that influx of calcium ions through both L-type calcium channels and the reverse-mode of the sodium-calcium exchanger is necessary for complete store-refilling in airway smooth muscle...
  56. pmc Asymmetric cooperative catalysis of strong Brønsted acid-promoted reactions using chiral ureas
    Hao Xu
    Department of Chemistry and Chemical Biology, Harvard University, Cambridge, MA 02138, USA
    Science 327:986-90. 2010
    ..A detailed experimental and computational analysis of this catalyst system has revealed the precise nature of the catalyst-substrate interactions and the likely basis for enantioinduction...
  57. ncbi MreB actin-mediated segregation of a specific region of a bacterial chromosome
    Zemer Gitai
    Department of Developmental Biology, Beckman Center, School of Medicine, Stanford University, California 94305, USA
    Cell 120:329-41. 2005
    ..MreB selectively interacts, directly or indirectly, with origin-proximal regions of the chromosome, arguing that the origin-proximal region segregates via an MreB-dependent mechanism not used by the rest of the chromosome...
  58. doi Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agents
    Peng Cheng Lv
    State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People s Republic of China
    Bioorg Med Chem 18:4606-14. 2010
    ..Compound C5 showed significant antiproliferative activity against MCF-7 with IC₅₀ of 0.08 μM. Therefore, compound C5 with potent inhibitory activity in tumor growth inhibition would be a potential anticancer agent...
  59. doi Effects of S-(3,4-dichlorobenzyl) isothiourea on different cellular events in the cyanobacterium Anabaena sp. strain PCC 7120
    Xuan Wu
    State Key Laboratory of Agricultural Microbiology, Huazhong Agricultural University, Wuhan 430070, People s Republic of China
    Res Microbiol 162:375-81. 2011
    ..An A22-resistant mutant named C23 was isolated by growing cells on A22-containing plates. It had normal appearance of cell shape, division and DNA content when treated by A22. However, this mutant retained a wild-type allele of mreB...
  60. doi A22 disrupts the bacterial actin cytoskeleton by directly binding and inducing a low-affinity state in MreB
    G J Bean
    Laboratory of Molecular Biology, University of Wisconsin, 1525 Linden Drive, Madison, Wisconsin 53706, USA
    Biochemistry 48:4852-7. 2009
    ..It also represents a novel mode of action for a cytoskeletal drug and the first biochemical characterization of the interaction between a small molecule inhibitor of the bacterial cytoskeleton and its target...
  61. doi A new entry to cascade organocatalysis: reactions of stable sulfur ylides and nitroolefins sequentially catalyzed by thiourea and DMAP
    Liang Qiu Lu
    Key Laboratory of Pesticide and Chemical Biology, Ministry of Education, College of Chemistry, Central China Normal University, 152 Luoyu Road, Wuhan, Hubei 430079, China
    J Am Chem Soc 130:6946-8. 2008
    ..A possible mechanism of this reaction has been proposed based on D- and 13C-labeling experiments...
  62. ncbi Cytotoxicity of a series of mono- and di-substituted thiourea in freshly isolated rat hepatocytes: a preliminary structure-toxicity relationship study
    R C Onderwater
    Leiden Amsterdam Center for Drug Research, Division of Molecular Toxicology, Vrije Universiteit, Amsterdam, The Netherlands
    Toxicology 125:117-29. 1998
    The cytotoxicity of a series of 12 mono- and 4 di-substituted thiourea containing compounds in freshly isolated rat hepatocytes was investigated...
  63. ncbi Thiourea toxicity in mouse C3H/10T1/2 cells expressing human flavin-dependent monooxygenase 3
    P Blaise Smith
    Department of Biochemistry, School of Medicine, Wake Forest University, Medical Center Boulevard, Winston Salem, NC 27157 1019, USA
    Biochem Pharmacol 63:1941-8. 2002
    ..Cytotoxicity in these clones after exposure to thiocarbamate compounds was assessed by clonogenic assay. Thiourea (TU), phenylthiourea (PTU), and alpha-naphthylthiourea (ANTU) were toxic to FMO 3 cells but not to parental and ..
  64. doi Label-free capacitive immunosensor for microcystin-LR using self-assembled thiourea monolayer incorporated with Ag nanoparticles on gold electrode
    Suchera Loyprasert
    Trace Analysis and Biosensor Research Center, Prince of Songkla University, Hat Yai, Songkhla, Thailand
    Biosens Bioelectron 24:78-86. 2008
    ..Anti-microcystin-LR (anti-MCLR) was immobilized on silver nanoparticles bound to a self-assembled thiourea monolayer. Interaction of anti-MCLR and MCLR were directly detected by capacitance measurement...
  65. ncbi Potentiometric detection of mercury(II) ions using a carbon paste electrode modified with substituted thiourea-functionalized highly ordered nanoporous silica
    Mehran Javanbakht
    Department of Chemistry, Amirkabir University of Technology, Tehran, Iran
    Anal Sci 25:789-94. 2009
    A potentiometric sensor is reported for the mercury(II) detection, which uses substituted thiourea-functionalized nanoporous silica (FTU-LUS-1) as the sensitive material...
  66. doi Mononuclear ferrocenophane structural motifs with two thiourea arms acting as a dual binding site for anions and cations
    Francisco Otón
    Departamento de Quimica Organica, Facultad de Quimica, Campus de Espinardo, Universidad de Murcia, E 30100 Murcia, Spain
    Inorg Chem 48:1566-76. 2009
    The synthesis of a new type of mononuclear ferrocenophane-based thiourea, in which the ferrocene moiety is simultaneously attached to two thiourea groups directly from 1,1'-bis(isothiocyanato)ferrocene, is reported...
  67. ncbi Functional coupling between the Na+/Ca2+ exchanger and nonselective cation channels during histamine stimulation in guinea pig tracheal smooth muscle
    Paola Algara-Suárez
    Departmento de Fisiologia, Facultad de Medicina, Universidad Autonoma de San Luis Potosi, San Luis Potosi, Mexico
    Am J Physiol Lung Cell Mol Physiol 293:L191-8. 2007
    ..We speculate that histamine induces Na(+) influx through NSCC that promotes the Ca(2+) entry mode of NCX and Ca(V)1.2 channel activation, thereby causing contraction...
  68. ncbi Ca(2+) signaling by TRPC3 involves Na(+) entry and local coupling to the Na(+)/Ca(2+) exchanger
    Christian Rosker
    Department of Pharmacology and Toxicology, Karl Franzens University Graz, A 8010 Graz, Austria
    J Biol Chem 279:13696-704. 2004
    ..We suggest functional and physical interaction of nonselective TRPC cation channels with NCX proteins as a novel principle of TRPC-mediated Ca(2+) signaling...
  69. ncbi Modulation of genotoxic effects in asbestos-exposed primary human mesothelial cells by radical scavengers, metal chelators and a glutathione precursor
    Ina Poser
    Institute of Pathology, University Hospital Regensburg, Germany
    Mutat Res 559:19-27. 2004
    ..Also, the iron content of the fiber plays an important role in radical formation, but nevertheless, chrysotile produces oxy radicals to a similar extent as crocidolite, probably by phagocytosis-mediated oxidative bursting...
  70. ncbi The reverse mode of the Na(+)/Ca(2+) exchanger provides a source of Ca(2+) for store refilling following agonist-induced Ca(2+) mobilization
    Simon Hirota
    Asthma Research Group, Firestone Institute for Respiratory Health, St Joseph s Healthcare, and Department of Medicine, McMaster University, Hamilton, Ontario, Canada
    Am J Physiol Lung Cell Mol Physiol 292:L438-47. 2007
    ..Furthermore, KB-R7943 abolished successive caffeine-induced Ca(2+) transients in single ASM cells. Together, these data suggest a role for the reverse mode of the NCX in refilling the SR in ASM following Ca(2+) mobilization...
  71. doi Neuronal nitric oxide synthase regulates basal microvascular tone in humans in vivo
    Michael D Seddon
    Department of Cardiology, King s College London School of Medicine, 125 Coldharbour Ln, London SE5 9NU, United Kingdom
    Circulation 117:1991-6. 2008
    ..These effects have been attributed to NO production by the endothelial NO synthase (eNOS); however, recent evidence suggests that a neuronal NO synthase (nNOS) may also be expressed in arterial vessels...
  72. doi Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapy
    Elvira Crescenzi
    Dipartimento di Biologia e Patologia Cellulare e Molecolare L Califano, Universita di Napoli Federico II, Naples, Italy
    Clin Cancer Res 14:1877-87. 2008
    ..We set out to find a means to specifically induce senescent tumor cells to undergo cell death and not to reenter the cell cycle that may have general application in cancer therapy...
  73. ncbi Synthesis of some novel thiourea derivatives obtained from 5-[(4-aminophenoxy)methyl]-4-alkyl/aryl-2,4-dihydro-3H-1,2,4-triazole-3-thiones and evaluation as antiviral/anti-HIV and anti-tuberculosis agents
    Ilkay Küçükgüzel
    Marmara University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Tibbiye cad No 49, Haydarpaşa 34668 Istanbul, Turkey
    Eur J Med Chem 43:381-92. 2008
    ..9 microg/ml. Compound 38 was the most active compound with 79% inhibition against M. tuberculosis H37Rv...
  74. ncbi Small molecule-based reversible reprogramming of cellular lifespan
    Jaejoon Won
    Department of Biological Sciences, Korea Advanced Institute of Science and Technology, Daejeon 305 701, Korea
    Nat Chem Biol 2:369-74. 2006
    ..These results might reflect the specific targeting of the kinase activities of ATM and ATR by CGK733 without affecting any other domains required for cell proliferation...
  75. ncbi Influence of erythrocytes on the hepatic distribution kinetics of urea and thiourea
    Selma Sahin
    Hacettepe University, Faculty of Pharmacy, Ankara, Turkey
    Eur J Pharm Sci 31:180-9. 2007
    The role of erythrocyte on the hepatic distribution kinetics of urea and thiourea was investigated in the in situ isolated perfused rat liver...
  76. doi A pharmacoproteomic approach implicates eukaryotic elongation factor 2 kinase in ER stress-induced cell death
    M Boyce
    Department of Cell Biology, Harvard Medical School, Boston, MA, USA
    Cell Death Differ 15:589-99. 2008
    ..Our work identifies eEF-2K as a new component of the ER stress response and underlines the utility of novel small molecules in discovering new cell biology...
  77. ncbi Metabolism of 1-(3-[3-(4-cyanobenzyl)-3H-imidazol-4-yl]-propyl)-3-(6-methoxypyridin-3-yl)-1-(2-trifluoromethylbenzyl)thiourea (YH3945), a novel anti-cancer drug, in rats using the 14C-labeled compound
    Jaeick Lee
    Bioanalysis and Biotransformation Research Center, Korea Institute of Science and Technology, P O BOX 131, Chungryang, Seoul 136 791, South Korea
    Rapid Commun Mass Spectrom 18:1901-10. 2004
    ..agent, 1-(3-[3-(4-cyanobenzyl)-3H-imidazol-4-yl]-propyl)-3-(6-methoxypyridin-3-yl)-1-(2-trifluoromethylbenzyl)thiourea (YH3945), was investigated in rats...
  78. ncbi Effects of SEA0400 and KB-R7943 on Na+/Ca2+ exchange current and L-type Ca2+ current in canine ventricular cardiomyocytes
    Péter Birinyi
    Department of Physiology, University Medical School of Debrecen, P O Box 22, 4012, Debrecen, Hungary
    Naunyn Schmiedebergs Arch Pharmacol 372:63-70. 2005
    ..At concentrations higher than 1 microM, however, I(Ca) is progressively suppressed by the compound...
  79. ncbi Structure-activity relationship studies of salubrinal lead to its active biotinylated derivative
    Kai Long
    State Key Laboratory of Bioorganic and Natural Products Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 354 Fenglin Road, Shanghai 200032, China
    Bioorg Med Chem Lett 15:3849-52. 2005
    ..Based on the SAR results, salubrinal was converted into a biotinylated derivative which retains activity and can be used as a biological tool for target identification...
  80. ncbi Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicin
    Dong Wook Kang
    Research Institute of Pharmaceutical Sciences, College of Pharmacy, Seoul National University, Seoul 151 742, Republic of Korea
    Bioorg Med Chem Lett 17:214-9. 2007
    ..Compounds 23c and 31b were found to be potent full antagonists with K(i) (as functional antagonist)=23.1 and 30.3 nM in rTRPV1/CHO system, respectively...
  81. ncbi Therapeutic potential of novel Na+-Ca2+ exchange inhibitors in attenuating ischemia-reperfusion injury
    Candace Lee
    Institute of Cardiovascular Sciences, St Boniface General Hospital Research Centre, Department of Physiology, Faculty of Medicine, University of Manitoba, Winnipeg, Canada
    Can J Cardiol 21:509-16. 2005
    ..Novel NCX inhibitors discovered in recent years have shown great promise in attenuating ischemia-reperfusion injury...
  82. ncbi Protection of ischemic rat spinal cord white matter: Dual action of KB-R7943 on Na+/Ca2+ exchange and L-type Ca2+ channels
    M Ouardouz
    Ottawa Health Research Institute, Division of Neuroscience, University of Ottawa, Ottawa, ON, Canada K1Y 4K9
    Neuropharmacology 48:566-75. 2005
    ....
  83. ncbi SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic models
    T Matsuda
    Laboratory of Medicinal Pharmacology, Graduate School of Pharmaceutical Sciences, Osaka University, Suita, Osaka, Japan
    J Pharmacol Exp Ther 298:249-56. 2001
    ..These results indicate that SEA0400 is the most potent and selective inhibitor of NCX, and suggest that the compound may exert protective effects on postischemic brain damage...
  84. ncbi Superoxide, H2O2, and iron are required for TNF-alpha-induced MCP-1 gene expression in endothelial cells: role of Rac1 and NADPH oxidase
    Xi Lin Chen
    Athero Genics, Inc, 8995 Westside Parkway, Alpharetta, GA 30004, USA
    Am J Physiol Heart Circ Physiol 286:H1001-7. 2004
    ..These data suggest that ROS such as superoxide and H(2)O(2) derived from Rac1-activated NADPH oxidase mediate TNF-alpha-induced MCP-1 expression in endothelial cells...
  85. ncbi Use of thiourea to increase the solubility of membrane proteins in two-dimensional electrophoresis
    T Rabilloud
    CEA Laboratoire de Bioénergétique Cellulaire et Pathologique, UA 2019 DBMS BECP, Grenoble, France
    Electrophoresis 19:758-60. 1998
    ..It is shown here that the use of thiourea, previously described for focusing in immobilized pH gradients, can be extended to conventional isoelectric ..
  86. ncbi Blockade of NMDA channels in acutely isolated rat hippocampal neurons by the Na+/Ca2+ exchange inhibitor KB-R7943
    A I Sobolevsky
    Institute of General Pathology and Pathophysiology, Moscow, Russian Federation
    Neuropharmacology 38:1235-42. 1999
    ..26-0.41. The blocking action of KB-R7943 on NMDA channels did not depend either on ASP or glycine concentrations which indicated that the binding sites for KB-R7943 and those for the agonist and the coagonist did not overlap...
  87. ncbi Protein alkylation in the presence/absence of thiourea in proteome analysis: a matrix assisted laser desorption/ionization-time of flight-mass spectrometry investigation
    M Galvani
    GlaxoWellcome SpA, Medicines Research Center, Verona, Italy
    Electrophoresis 22:2066-74. 2001
    ..dimension), it is here reported that one component of the sample solubilization cocktail adopted recently (namely thiourea) strongly quenches such alkylation process (as typically carried out with iodoacetamide, IAA)...
  88. doi Effects of neuronal nitric oxide synthase on human coronary artery diameter and blood flow in vivo
    Michael Seddon
    King s College London British Heart Foundation Centre, Cardiovascular Division, Department of Cardiology, London, UK
    Circulation 119:2656-62. 2009
    ..Here, we investigated the in vivo effects of an nNOS-selective inhibitor, S-methyl-L-thiocitrulline (SMTC), on the human coronary circulation and on flow-mediated dilatation in the forearm...
  89. ncbi Inhibition of Na+/Ca2+ exchange by KB-R7943: transport mode selectivity and antiarrhythmic consequences
    C L Elias
    Institute of Cardiovascular Sciences, St. Boniface General Hospital Research Centre, University of Manitoba, Winnipeg, Manitoba, Canada
    Am J Physiol Heart Circ Physiol 281:H1334-45. 2001
    ..The observed electrophysiological profile of KB-R7943 and its protective effects on ischemia-reperfusion-induced ventricular arrhythmias support the notion of a prominent role of Ca2+ entry via reverse Na+/Ca2+ exchange in this process...
  90. ncbi Improving typeability of multiple bacterial species using pulsed-field gel electrophoresis and thiourea
    Suzane Silbert
    Laboratório Especial de Microbiologia Clínica, Disciplina de Doencas Infecciosas e Parasitarias, Universidade Federal de Sao Paulo, Rua Leandro Dupret, 188 CEP, Sao Paulo, Brazil
    Diagn Microbiol Infect Dis 47:619-21. 2003
    ..Previous reports suggest that the addition of thiourea in the gel buffer can improved the typeability for some species...
  91. ncbi Structure-activity relationships in platinum-acridinylthiourea conjugates: effect of the thiourea nonleaving group on drug stability, nucleobase affinity, and in vitro cytotoxicity
    Margaret C Ackley
    Department of Chemistry, Wake Forest University, P O Box 7486 Reynolda Station, Winston Salem, NC 27109, USA
    J Biol Inorg Chem 9:453-61. 2004
    ..To establish structure-activity relationships within this class of compounds, systematic changes were made to the thiourea nonleaving group, which links the intercalator to platinum...
  92. ncbi Thiourea derivatives and their nickel(II) and platinum(II) complexes: antifungal activity
    Rafael del Campo
    Departamento de Quimica Inorganica, Facultad de Farmacia, Campus Miguel de Unamuno, Universidad de Salamanca, 37007, Salamanca, Spain
    J Inorg Biochem 89:74-82. 2002
    We have synthesized two thiourea derivatives of methyl anthranilate (1, 2) and their complexes with nickel (3) and platinum(II) (4). We have also prepared the complexes of nickel(II) with two benzoylthiourea derivatives (5, 6)...
  93. ncbi Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials
    I Kucukguzel
    Department of Pharmaceutical Chemistry, Marmara University, Faculty of Pharmacy, Haydarpasa 81010, Istanbul, Turkey
    Bioorg Med Chem Lett 11:1703-7. 2001
    ..tuberculosis H37Rv at varying degrees. Compound 21 was identified as the most potent derivative of the 1-22 series by an MIC value of 6.25 microg/mL and selectivity index of 1.6...
  94. ncbi Quantitative fluorescence measurement of cardiac Na+/Ca2+ exchanger inhibition by kinetic analysis in stably transfected HEK293 cells
    Iyuki Namekata
    Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences, Funabashi, Chiba, Japan
    J Pharmacol Sci 101:356-60. 2006
    ....
  95. ncbi Inhibition by SEA0400, a selective inhibitor of Na+/Ca2+ exchanger, of Na+ -dependent Ca2+ uptake and catecholamine release in bovine adrenal chromaffin cells
    Shin Soma
    Department of Pharmacology, The Nippon Dental University School of Life Dentistry at Niigata, Japan
    J Pharmacol Sci 102:88-95. 2006
    ..From these results, it is concluded that unlike KB-R7943, SEA0400 has a potent and selective action on NCX in bovine adrenal chromaffin cells...
  96. ncbi Single alpha-domain constructs of the Na+/Ca2+ exchanger, NCLX, oligomerize to form a functional exchanger
    Raz Palty
    Department of Physiology, Zlotowski Center for Neuroscience, Faculty of Health Sciences, Ben Gurion University of the Negev, Beer Sheva 84105, Israel
    Biochemistry 45:11856-66. 2006
    ..Such organization may give rise to transport activity with distinct kinetic parameters and physiological roles...
  97. ncbi The influence of sodium-calcium exchange inhibitors on rabbit lens ion balance and transparency
    Shigeo Tamiya
    Department of Ophthalmology and Visual Sciences, University of Louisville, School of Medicine, Louisville, KY 40202, USA
    Exp Eye Res 83:1089-95. 2006
    ..The ability of bepridil to cause significant changes in lens transparency and electrolyte content points to an important role for NCX-meditated calcium export in the lens...
  98. ncbi Angiotensin II-stimulated Ca2+ entry mechanisms in afferent arterioles: role of transient receptor potential canonical channels and reverse Na+/Ca2+ exchange
    Susan K Fellner
    Department of Cell and Molecular Physiology, University of North Carolina at Chapel Hill, Chapel Hill, NC 27599, USA
    Am J Physiol Renal Physiol 294:F212-9. 2008
    ..KB-R7943 decreased the peak [Ca(2+)](i) response to ANG II by 48% and to FFA by 38%. We conclude that TRPC6 and reverse-mode NCX may be important Ca(2+) entry pathways in afferent arterioles...
  99. ncbi On the source of Ca(2+) activating the tonic component of contraction of myocytes of guinea pig heart
    K Emanuel
    Department of Clinical Physiology, Medical Centre of Postgraduate Education, Marymoncka 99, 01-813, Warsaw, Poland
    Cardiovasc Res 52:76-83. 2001
    ..Rather, it is activated by Ca(2+) released from the sarcoplasmic reticulum. However, kinetics and mechanism of release seem to be quite different from those of Ca(2+) fraction activating the phasic component of contraction...
  100. doi An increase of late sodium current induces delayed afterdepolarizations and sustained triggered activity in atrial myocytes
    Yejia Song
    Division of Cardiovascular Medicine, University of Florida, 1600 SW Archer Road, Gainesville, FL 32610 0277, USA
    Am J Physiol Heart Circ Physiol 294:H2031-9. 2008
    ..The data reveal that an increase of late I(Na) is a novel mechanism for initiation of atrial arrhythmic activity...
  101. ncbi Gender influences [Ca(2+)](i) during metabolic inhibition in myocytes overexpressing the Na(+)-Ca(2+) exchanger
    K Sugishita
    Division of Cardiology, University of Utah Health Sciences Center, Salt Lake City, Utah 84132, USA
    Circulation 104:2101-6. 2001
    ..This gender difference appears to be mediated in part by an inhibitory effect of estrogen on the rise in [Na(+)](i), an NCX modifier, during MI...

Research Grants100

  1. Mode of Action of Thiorcarlide in Mycobacterium Tuberculosis
    Mary Jackson; Fiscal Year: 2010
    Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis (M. tb)...
  2. MICROVASCULAR TRANSPORT IN THE RENAL MEDULLA
    THOMAS PALLONE; Fiscal Year: 2002
    ..Residual osmotic water permeability of AQP1 -/- will be examined for sensitivity to pCMBS and thiourea. The Arrhenius activation energy of remaining pathways will also be determined...
  3. ASSEMBLY OF THE HERPES SIMPLEX VIRUS CAPSID
    Jay Brown; Fiscal Year: 2006
    ..and portal proteins; (3) determine the mechanism of action of WAY-150138, a small molecule (a substituted thiourea) that inhibits HSV-1 growth in cell culture by blocking DNA encapsidation; and (4) use sensitivity to trypsin ..
  4. Identification of Desaturase Targets
    Mary Jackson; Fiscal Year: 2007
    DESCRIPTION (provided by the applicant): Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis...
  5. Identification of Desaturase Targets
    Patrick Brennan; Fiscal Year: 2006
    DESCRIPTION (provided by the applicant): Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis...
  6. Mechanisms of Positive Energy Balance in PROP Nontasters
    Kathleen Keller; Fiscal Year: 2007
    Inherited differences in human's ability to taste bitter thiourea compounds, specifically phenylthiocarbamide (PTC) and 6-n-propylthiouracil (PROP), have been studied since 1931. 70% of adults and children in the U.S...
  7. Thiourea-Catalyzed Nucleophilic Desymmetrization of Meso-Cyclopropanes
    KRISTINE NOLIN; Fiscal Year: 2007
    ..This proposal outlines the development of stereoselective 1,5-functionalization of carbonyls through thiourea catalyzed desymmetrizations of meso-cyclopropanes by nucleophilic ring opening...
  8. Catalytic Asymmetric Synthesis of Piperidene Derivatives
    SARAH REISMAN; Fiscal Year: 2007
    ..Recent work in the Jacobsen laboratory has shown that chiral thiourea catalysts can activate N-alkylimines and N-acyliminium ions towards a number of asymmetric processes...
  9. Biomimetic Synthesis of Complex Natural Products
    John A Porco; Fiscal Year: 2010
    ..Jacobsen and coworkers (Harvard University) will seek to identify chiral thiourea photocatalysts for asymmetric photocycloadditions...
  10. Varicella-zoster virus DNA encapsidation proteins
    Robert Visalli; Fiscal Year: 2005
    ..Recently, a series of alpha-methylbenzyl thiourea compounds were described with specific anti-VZV activity...
  11. PHI-443: Novel Non-Spermicidal Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..an integrated effort involving synthesis, docking studies, and biological evaluation, we identified a thiophene thiourea non-nucleoside inhibitor (N'-[2-(2-thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea [PHI-443]) with ..
  12. PHI 346: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2003
    ..Our lead compound, N-[2-(1-cyclohexenyl)ethyl]-N'-[2-(5-bromopyridyl)]-thiourea (PHI-346), was the most potent, non-cytotoxic, dual-function anti-HIV agent against NNI-sensitive, NNI-resistant, ..
  13. Stampidine: A Novel Broad-Spectrum Anti-HIV Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ..Specific Aims 1 and 2 may provide the foundation for the clinical development of STAMP in Phase II studies as a safe, effective broad-spectrum anti-HIV microbicide without conception-inhibiting functions. ..
  14. NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITY
    OSMOND D CRUZ; Fiscal Year: 2001
    ..The preclinical data on in vivo efficacies of WHI-05 and WHI-07 will be essential to further explore the utility of these novel drugs for clinical studies in human patients. ..
  15. Vanadocenes as a New Class of Spermicidal Drugs
    OSMOND D CRUZ; Fiscal Year: 2007
    ....
  16. Phase II SBIR: WHI-07: A Novel Dual-Function Microbicide
    OSMOND D CRUZ; Fiscal Year: 2005
    ....
  17. FLP-102: Rationally Engineered Antiviral Protein
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The preclinical data on FLP-102 will be essential to further explore the utility of this novel recombinant PAP mutant for Phase II. ..
  18. METVAN: A Novel Anticancer Agent
    OSMOND D CRUZ; Fiscal Year: 2003
    ..The knowledge gained from these studies described under Specific Aims 1-2 is expected to facilitate the design of innovative treatment regimens employing METVAN for metastatic breast cancer and brain tumor patients. ..
  19. Development of At-211-Labeled Reagents for Therapy of Metastatic Prostate Cancer
    DANIEL SCOTT WILBUR; Fiscal Year: 2010
    ..The proposed research will develop new and unique At-211-labeled reagents that have the potential to dramatically improve the five-year survival of prostate cancer patients with metastatic disease. ..
  20. Development of Reagents for Labeling with At-211
    DANIEL WILBUR; Fiscal Year: 2007
    ..abstract_text> ..
  21. MEDICAL SCIENTIST TRAINING PROGRAM
    MYLES AKABAS; Fiscal Year: 2007
    ....
  22. PLASTICITY AT A CRAYFISH NEUROMUSCULAR SYNAPSE
    Jen Wei Lin; Fiscal Year: 1999
    ..Changes in calcium cooperativity add a new facet to our thinking of synaptic plasticity. ..
  23. Malaria PfCRT Transporter: Structure, Function, Sorting
    MYLES AKABAS; Fiscal Year: 2006
    ..It is the current lack of such an assay and the fact that this is a high risk search that has motivated us to apply for an R21 grant, which is exploratory in nature, rather than an RO1. ..
  24. Small GTPases and Lung Endothelial Apoptosis
    Sharon Rounds; Fiscal Year: 2009
    ..In addition, understanding of apoptosis may provide clues to treatment of lung diseases dependent upon abnormal endothelial proliferation, such as Pulmonary Arterial Hypertension and cancer. ..
  25. FOCAL ADHESION COMPLEXES AND LUNG ENDOTHELIAL APOPTOSIS
    Sharon Rounds; Fiscal Year: 2004
    ..Understanding of endothelial apoptosis will allow development of means of regulating vascular injury and repair. ..
  26. SHORT TERM TRAINING FOR MINORITY STUDENTS
    Sharon Rounds; Fiscal Year: 2006
    ..We present results of our previous experience showing that of students trained thus far, 45 percent have gone on to MD, PhD, or MD/PhD training programs. ..
  27. Small GTPases and Lung Endothelial Apoptosis
    Sharon Rounds; Fiscal Year: 2007
    ..In addition, understanding of apoptosis may provide clues to treatment of lung diseases dependent upon abnormal endothelial proliferation, such as Pulmonary Arterial Hypertension and cancer. ..
  28. Short-Term Training Program to Increase Diversity in Health-Related Research
    Sharon Rounds; Fiscal Year: 2007
    ..We present results of our previous experience, showing that 51% of students in the past 10 years have gone on to advanced degree programs in biomedical related fields. ..
  29. HIV GAG PRECURSOR PROTEIN INTERACTIONS
    Eric Barklis; Fiscal Year: 2002
    ....
  30. Analysis of Sin Nombre virus inhibition in lung cells
    Eric Barklis; Fiscal Year: 2005
    ..We believe that these exploratory studies have a high probability of leading to more efficient treatment of hantavirus-mediated pulmonary failure. ..
  31. AUTOREGULATION OF GLOMERULAR FILTRATION RATE
    Roland Blantz; Fiscal Year: 2009
    ..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..
  32. AUTOREGULATION OF GLOMERULAR FILTRATION RATE
    Roland Blantz; Fiscal Year: 2009
    ..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..
  33. AUTOREGULATION OF GLOMERULAR FILTRATION RATE
    Roland Blantz; Fiscal Year: 2007
    ..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..