Genomes and Genes
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.
Publications260 found, 100 shown here
- A selective inhibitor of eIF2alpha dephosphorylation protects cells from ER stressMichael 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...
- The plasma membrane Na+/Ca2+ exchange inhibitor KB-R7943 is also a potent inhibitor of the mitochondrial Ca2+ uniporterJ 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. 2007The 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...
- Synthesis, spectroscopic properties and antipathogenic activity of new thiourea derivativesCarmen 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 ..
- Synthesis and antiviral activities of chiral thiourea derivatives containing an alpha-aminophosphonate moietyMei 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.
- (Bis)urea and (bis)thiourea inhibitors of lysine-specific demethylase 1 as epigenetic modulatorsShiv 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...
- Attractive noncovalent interactions in asymmetric catalysis: links between enzymes and small molecule catalystsRobert 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...
- Deficiency of αB crystallin augments ER stress-induced apoptosis by enhancing mitochondrial dysfunctionGuorui 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...
- Na+-Ca2+ exchanger contributes to Ca2+ extrusion in ATP-stimulated endothelium of intact rat aortaRoberto 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...
- Synergistic apoptosis induction in leukemic cells by the phosphatase inhibitor salubrinal and proteasome inhibitorsHannes C A Drexler
Department of Vascular Cell Biology, Max Planck Institute for Molecular Biomedicine, Muenster, Germany
PLoS ONE 4:e4161. 2009....
- MreB drives de novo rod morphogenesis in Caulobacter crescentus via remodeling of the cell wallConstantin 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...
- Sex differences in the effects of inherited bitter thiourea sensitivity on body weight in 4-6-year-old childrenKathleen 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...
- 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 receptorLei 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, ..
- Isothioureas: potent inhibitors of nitric oxide synthases with variable isoform selectivityG J Southan
William Harvey Research Institute, St Bartholomew s Hospital Medical College, London
Br J Pharmacol 114:510-6. 1995....
- Induction of autophagic cell death by a novel molecule is increased by hypoxiaMarco 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...
- Studies on the anti-proliferative effects of novel DNA-intercalating bipyridyl-thiourea-Pt(II) complexes against cisplatin-sensitive and -resistant human ovarian cancer cellsGaetano 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. 2008Six 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''..
- Enantioselective thiourea-catalyzed cationic polycyclizationsRobert R Knowles
Department of Chemistry and Chemical Biology, Harvard University, Cambridge, Massachusetts 02138, USA
J Am Chem Soc 132:5030-2. 2010A new thiourea catalyst is reported for the enantioselective cationic polycyclization of hydroxylactams...
- Selective inhibition of eukaryotic translation initiation factor 2 alpha dephosphorylation potentiates fatty acid-induced endoplasmic reticulum stress and causes pancreatic beta-cell dysfunction and apoptosisMiriam 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...
- Mechanism of amido-thiourea catalyzed enantioselective imine hydrocyanation: transition state stabilization via multiple non-covalent interactionsStephan J Zuend
Harvard University, Department of Chemistry and Chemical Biology, Cambridge, Massachusetts 02138, USA
J Am Chem Soc 131:15358-74. 2009An experimental and computational investigation of amido-thiourea promoted imine hydrocyanation has revealed a new and unexpected mechanism of catalysis...
- Antifungal efficacy of chitosan and its thiourea derivatives upon the growth of some sugar-beet pathogensM Eweis
Department of Botany, Faculty of Science, Cairo University, Cairo, Egypt
Int J Biol Macromol 38:1-8. 2006Chitosan (CS) was modified by reaction with benzoyl thiocyanate to give a thiourea derivative (TUCS)...
- N-D-aldopentofuranosyl-N'-[p-(isoamyloxy)phenyl]-thiourea derivatives: potential anti-TB therapeutic agentsAvraham 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. 2008Thiocarlide (THC; N,N'-bis[p-(isoamyloxy)phenyl]-thiourea; also known as isoxyl) has been used in the past as anti-tuberculosis agent...
- Acetylcholine-induced asynchronous calcium waves in intact human bronchial muscle bundleJiazhen 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...
- Osteoporosis regulation by salubrinal through eIF2α mediated differentiation of osteoclast and osteoblastLong 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...
- Novel class of thiourea compounds that inhibit herpes simplex virus type 1 DNA cleavage and encapsidation: resistance maps to the UL6 geneM van Zeijl
Department of Molecular Biology Virology, Wyeth Ayerst Research, Pearl River, New York 10965, USA
J Virol 74:9054-61. 2000In our search for novel inhibitors of herpes simplex virus type 1 (HSV-1), a new class of thiourea inhibitors was discovered...
- Human mitochondrial thymidine kinase is selectively inhibited by 3'-thiourea derivatives of beta-thymidine: identification of residues crucial for both inhibition and catalytic activityJan Balzarini
Rega Institute for Medical Research, Katholieke Universiteit Leuven, Leuven, Belgium
Mol Pharmacol 75:1127-36. 2009Substituted 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, ..
- Differential branchial and renal handling of urea, acetamide and thiourea in the gulf toadfish Opsanus beta: evidence for two transportersM 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...
- Salubrinal promotes healing of surgical wounds in rat femursPing 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...
- Salubrinal attenuates β-amyloid-induced neuronal death and microglial activation by inhibition of the NF-κB pathwayXiumei 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...
- Adsorption of platinum(IV) and palladium(II) from aqueous solution by thiourea-modified chitosan microspheresLimin 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. 2009The chitosan microparticles were prepared using the inverse phase emulsion dispersion method and modified with thiourea (TCS)...
- Characteristics of equilibrium, kinetics studies for adsorption of Hg(II), Cu(II), and Ni(II) ions by thiourea-modified magnetic chitosan microspheresLimin 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. 2009Magnetic chitosan microspheres were prepared and chemically modified with thiourea (TMCS) for adsorption of metal ions...
- Rational design and 3D-pharmacophore mapping of 5'-thiourea-substituted alpha-thymidine analogues as mycobacterial TMPK inhibitorsCarolina 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...
- 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 miceFaizul Azam
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Seventh October, Misurata, Libya
Eur J Med Chem 44:3889-97. 2009A series of 3-phenyl/ethyl-2-thioxo-2,3-dihydrothiazolo[4,5-d]pyrimidin-7-yl urea and thiourea derivatives were designed and synthesized...
- Recovery of silver (I) using a thiourea-modified chitosan resinLin 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...
- Evaluation of nitrification-inhibition measurementsK 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-..
- (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)...
- KB-R7943, an inhibitor of the reverse Na+ /Ca2+ exchanger, blocks N-methyl-D-aspartate receptor and inhibits mitochondrial complex ITatiana 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...
- Comparative gene transfer between cationic and thiourea lipoplexesMarie 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.
- Specific inhibition of human cytomegalovirus glycoprotein B-mediated fusion by a novel thiourea small moleculeThomas 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...
- Bifunctional primary amine-thiourea-TfOH (BPAT·TfOH) as a chiral phase-transfer catalyst: the asymmetric synthesis of dihydropyrimidinesYangyun Wang
State Key Laboratory and Institute of Elemento Organic Chemistry, Nankai University, Tianjin, 300071, China
Org Biomol Chem 9:3050-4. 2011An 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...
- 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) complexesCristina 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...
- Involvement of Na(+)/Ca(2+) exchanger in endothelial NO production and endothelium-dependent relaxationJean 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...
- Functional differences of Na+/Ca2+ exchanger expression in Ca2+ transport system of smooth muscle of guinea pig stomachYasushi 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...
- Structure-activity relationship study of the bacterial actin-like protein MreB inhibitors: effects of substitution of benzyl group in S-benzylisothioureaNoritaka 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...
- The dimethylthiourea-induced attenuation of cisplatin nephrotoxicity is associated with the augmented induction of heat shock proteinsTakayuki 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...
- Pharmacology of KB-R7943: a Na+-Ca2+ exchange inhibitorMd 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....
- Highly enantio- and diastereoselective Mannich reactions of glycine Schiff bases with in situ generated N-Boc-imines catalyzed by a cinchona alkaloid thioureaHaile 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 ..
- Direction-independent block of bi-directional Na+/Ca2+ exchange current by KB-R7943 in guinea-pig cardiac myocytesJ 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...
- Free radicals generated in yeast by the Salmonella test-negative carcinogens benzene, urethane, thiourea and auramine OR 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...
- Effect of SEA0400, a novel inhibitor of sodium-calcium exchanger, on myocardial ionic currentsHikaru 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...
- Fundamental importance of Na+-Ca2+ exchange for the pacemaking mechanism in guinea-pig sino-atrial nodeLuke Sanders
University Department of Pharmacology, Mansfield Road, Oxford OX1 3QT, UK
J Physiol 571:639-49. 2006....
- The thioamides methimazole and thiourea inhibit growth of M. avium Subspecies paratuberculosis in cultureRobert 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...
- Docking and 3D QSAR study of thiourea analogs as potent inhibitors of influenza virus neuraminidaseJiaying Sun
College of Bioengineering, Chongqing University, Chongqing 400044, China
J Mol Model 16:1809-18. 2010Surflex-Dock was applied to study interactions between 30 thiourea analogs and neuraminidase (NA)...
- Development and application of Na+/Ca2+ exchange inhibitorsTakahiro 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...
- Rational design of 5'-thiourea-substituted alpha-thymidine analogues as thymidine monophosphate kinase inhibitors capable of inhibiting mycobacterial growthIneke 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 ..
- Calcium dynamics and vasomotion in rat mesenteric arteriesAlexander Schuster
Cellular Biophysics and Biomechanics Laboratory, Swiss Federal Institute of Technology, Lausanne, Switzerland
J Cardiovasc Pharmacol 43:539-48. 2004....
- Store-refilling involves both L-type calcium channels and reverse-mode sodium-calcium exchange in airway smooth muscleS 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...
- Asymmetric cooperative catalysis of strong Brønsted acid-promoted reactions using chiral ureasHao 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...
- MreB actin-mediated segregation of a specific region of a bacterial chromosomeZemer 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...
- Synthesis and biological evaluation of pyrazole derivatives containing thiourea skeleton as anticancer agentsPeng 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...
- Effects of S-(3,4-dichlorobenzyl) isothiourea on different cellular events in the cyanobacterium Anabaena sp. strain PCC 7120Xuan 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...
- A22 disrupts the bacterial actin cytoskeleton by directly binding and inducing a low-affinity state in MreBG 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...
- A new entry to cascade organocatalysis: reactions of stable sulfur ylides and nitroolefins sequentially catalyzed by thiourea and DMAPLiang 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...
- Cytotoxicity of a series of mono- and di-substituted thiourea in freshly isolated rat hepatocytes: a preliminary structure-toxicity relationship studyR C Onderwater
Leiden Amsterdam Center for Drug Research, Division of Molecular Toxicology, Vrije Universiteit, Amsterdam, The Netherlands
Toxicology 125:117-29. 1998The cytotoxicity of a series of 12 mono- and 4 di-substituted thiourea containing compounds in freshly isolated rat hepatocytes was investigated...
- Thiourea toxicity in mouse C3H/10T1/2 cells expressing human flavin-dependent monooxygenase 3P 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 ..
- Label-free capacitive immunosensor for microcystin-LR using self-assembled thiourea monolayer incorporated with Ag nanoparticles on gold electrodeSuchera 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...
- Potentiometric detection of mercury(II) ions using a carbon paste electrode modified with substituted thiourea-functionalized highly ordered nanoporous silicaMehran Javanbakht
Department of Chemistry, Amirkabir University of Technology, Tehran, Iran
Anal Sci 25:789-94. 2009A potentiometric sensor is reported for the mercury(II) detection, which uses substituted thiourea-functionalized nanoporous silica (FTU-LUS-1) as the sensitive material...
- Mononuclear ferrocenophane structural motifs with two thiourea arms acting as a dual binding site for anions and cationsFrancisco Otón
Departamento de Quimica Organica, Facultad de Quimica, Campus de Espinardo, Universidad de Murcia, E 30100 Murcia, Spain
Inorg Chem 48:1566-76. 2009The 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...
- Functional coupling between the Na+/Ca2+ exchanger and nonselective cation channels during histamine stimulation in guinea pig tracheal smooth musclePaola 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...
- Ca(2+) signaling by TRPC3 involves Na(+) entry and local coupling to the Na(+)/Ca(2+) exchangerChristian 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...
- Modulation of genotoxic effects in asbestos-exposed primary human mesothelial cells by radical scavengers, metal chelators and a glutathione precursorIna 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...
- The reverse mode of the Na(+)/Ca(2+) exchanger provides a source of Ca(2+) for store refilling following agonist-induced Ca(2+) mobilizationSimon 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...
- Neuronal nitric oxide synthase regulates basal microvascular tone in humans in vivoMichael 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...
- Ataxia telangiectasia mutated and p21CIP1 modulate cell survival of drug-induced senescent tumor cells: implications for chemotherapyElvira 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...
- 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 agentsIlkay 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...
- Small molecule-based reversible reprogramming of cellular lifespanJaejoon 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...
- Influence of erythrocytes on the hepatic distribution kinetics of urea and thioureaSelma Sahin
Hacettepe University, Faculty of Pharmacy, Ankara, Turkey
Eur J Pharm Sci 31:180-9. 2007The role of erythrocyte on the hepatic distribution kinetics of urea and thiourea was investigated in the in situ isolated perfused rat liver...
- A pharmacoproteomic approach implicates eukaryotic elongation factor 2 kinase in ER stress-induced cell deathM 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...
- 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 compoundJaeick 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...
- Effects of SEA0400 and KB-R7943 on Na+/Ca2+ exchange current and L-type Ca2+ current in canine ventricular cardiomyocytesPéter 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...
- Structure-activity relationship studies of salubrinal lead to its active biotinylated derivativeKai 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...
- Halogenation of 4-hydroxy-3-methoxybenzyl thiourea TRPV1 agonists showed enhanced antagonism to capsaicinDong 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...
- Therapeutic potential of novel Na+-Ca2+ exchange inhibitors in attenuating ischemia-reperfusion injuryCandace 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...
- Protection of ischemic rat spinal cord white matter: Dual action of KB-R7943 on Na+/Ca2+ exchange and L-type Ca2+ channelsM Ouardouz
Ottawa Health Research Institute, Division of Neuroscience, University of Ottawa, Ottawa, ON, Canada K1Y 4K9
Neuropharmacology 48:566-75. 2005....
- SEA0400, a novel and selective inhibitor of the Na+-Ca2+ exchanger, attenuates reperfusion injury in the in vitro and in vivo cerebral ischemic modelsT 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...
- Superoxide, H2O2, and iron are required for TNF-alpha-induced MCP-1 gene expression in endothelial cells: role of Rac1 and NADPH oxidaseXi 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...
- Use of thiourea to increase the solubility of membrane proteins in two-dimensional electrophoresisT 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 ..
- Blockade of NMDA channels in acutely isolated rat hippocampal neurons by the Na+/Ca2+ exchange inhibitor KB-R7943A 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...
- Protein alkylation in the presence/absence of thiourea in proteome analysis: a matrix assisted laser desorption/ionization-time of flight-mass spectrometry investigationM 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)...
- Effects of neuronal nitric oxide synthase on human coronary artery diameter and blood flow in vivoMichael 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...
- Inhibition of Na+/Ca2+ exchange by KB-R7943: transport mode selectivity and antiarrhythmic consequencesC 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...
- Improving typeability of multiple bacterial species using pulsed-field gel electrophoresis and thioureaSuzane 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...
- Structure-activity relationships in platinum-acridinylthiourea conjugates: effect of the thiourea nonleaving group on drug stability, nucleobase affinity, and in vitro cytotoxicityMargaret 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...
- Thiourea derivatives and their nickel(II) and platinum(II) complexes: antifungal activityRafael 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. 2002We 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)...
- Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterialsI 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...
- Quantitative fluorescence measurement of cardiac Na+/Ca2+ exchanger inhibition by kinetic analysis in stably transfected HEK293 cellsIyuki Namekata
Department of Pharmacology, Toho University Faculty of Pharmaceutical Sciences, Funabashi, Chiba, Japan
J Pharmacol Sci 101:356-60. 2006....
- Inhibition by SEA0400, a selective inhibitor of Na+/Ca2+ exchanger, of Na+ -dependent Ca2+ uptake and catecholamine release in bovine adrenal chromaffin cellsShin 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...
- Single alpha-domain constructs of the Na+/Ca2+ exchanger, NCLX, oligomerize to form a functional exchangerRaz 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...
- The influence of sodium-calcium exchange inhibitors on rabbit lens ion balance and transparencyShigeo 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...
- Angiotensin II-stimulated Ca2+ entry mechanisms in afferent arterioles: role of transient receptor potential canonical channels and reverse Na+/Ca2+ exchangeSusan 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...
- On the source of Ca(2+) activating the tonic component of contraction of myocytes of guinea pig heartK 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...
- An increase of late sodium current induces delayed afterdepolarizations and sustained triggered activity in atrial myocytesYejia 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...
- Gender influences [Ca(2+)](i) during metabolic inhibition in myocytes overexpressing the Na(+)-Ca(2+) exchangerK 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...
- Mode of Action of Thiorcarlide in Mycobacterium TuberculosisMary Jackson; Fiscal Year: 2010Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis (M. tb)...
- MICROVASCULAR TRANSPORT IN THE RENAL MEDULLATHOMAS 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...
- ASSEMBLY OF THE HERPES SIMPLEX VIRUS CAPSIDJay 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 ..
- Identification of Desaturase TargetsMary Jackson; Fiscal Year: 2007DESCRIPTION (provided by the applicant): Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis...
- Identification of Desaturase TargetsPatrick Brennan; Fiscal Year: 2006DESCRIPTION (provided by the applicant): Thiocarlide (THC), a thiourea, inhibits the synthesis of mycolic acids and fatty acids in Mycobacterium tuberculosis...
- Mechanisms of Positive Energy Balance in PROP NontastersKathleen Keller; Fiscal Year: 2007Inherited 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...
- Thiourea-Catalyzed Nucleophilic Desymmetrization of Meso-CyclopropanesKRISTINE 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...
- Catalytic Asymmetric Synthesis of Piperidene DerivativesSARAH 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...
- Biomimetic Synthesis of Complex Natural ProductsJohn A Porco; Fiscal Year: 2010..Jacobsen and coworkers (Harvard University) will seek to identify chiral thiourea photocatalysts for asymmetric photocycloadditions...
- Varicella-zoster virus DNA encapsidation proteinsRobert Visalli; Fiscal Year: 2005..Recently, a series of alpha-methylbenzyl thiourea compounds were described with specific anti-VZV activity...
- PHI-443: Novel Non-Spermicidal Anti-HIV MicrobicideOSMOND 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 ..
- PHI 346: A Novel Dual-Function MicrobicideOSMOND 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, ..
- Stampidine: A Novel Broad-Spectrum Anti-HIV MicrobicideOSMOND 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. ..
- NOVEL CONTRACEPTIVES WITH ANTI-HIV ACTIVITYOSMOND 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. ..
- Vanadocenes as a New Class of Spermicidal DrugsOSMOND D CRUZ; Fiscal Year: 2007....
- Phase II SBIR: WHI-07: A Novel Dual-Function MicrobicideOSMOND D CRUZ; Fiscal Year: 2005....
- FLP-102: Rationally Engineered Antiviral ProteinOSMOND 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. ..
- METVAN: A Novel Anticancer AgentOSMOND 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. ..
- Development of At-211-Labeled Reagents for Therapy of Metastatic Prostate CancerDANIEL 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. ..
- Development of Reagents for Labeling with At-211DANIEL WILBUR; Fiscal Year: 2007..abstract_text> ..
- MEDICAL SCIENTIST TRAINING PROGRAMMYLES AKABAS; Fiscal Year: 2007....
- PLASTICITY AT A CRAYFISH NEUROMUSCULAR SYNAPSEJen Wei Lin; Fiscal Year: 1999..Changes in calcium cooperativity add a new facet to our thinking of synaptic plasticity. ..
- Malaria PfCRT Transporter: Structure, Function, SortingMYLES 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. ..
- Small GTPases and Lung Endothelial ApoptosisSharon 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. ..
- FOCAL ADHESION COMPLEXES AND LUNG ENDOTHELIAL APOPTOSISSharon Rounds; Fiscal Year: 2004..Understanding of endothelial apoptosis will allow development of means of regulating vascular injury and repair. ..
- SHORT TERM TRAINING FOR MINORITY STUDENTSSharon 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. ..
- Small GTPases and Lung Endothelial ApoptosisSharon 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. ..
- Short-Term Training Program to Increase Diversity in Health-Related ResearchSharon 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. ..
- HIV GAG PRECURSOR PROTEIN INTERACTIONSEric Barklis; Fiscal Year: 2002....
- Analysis of Sin Nombre virus inhibition in lung cellsEric 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. ..
- AUTOREGULATION OF GLOMERULAR FILTRATION RATERoland Blantz; Fiscal Year: 2009..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..
- AUTOREGULATION OF GLOMERULAR FILTRATION RATERoland Blantz; Fiscal Year: 2009..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..
- AUTOREGULATION OF GLOMERULAR FILTRATION RATERoland Blantz; Fiscal Year: 2007..These studies will also define the role of purinergic (ATP) and adenosine mediated TGF during all 3 phases of TGF. ..