Genomes and Genes
Summary: Sulfur-containing compounds also known as thioketones of general formula R2C=S.
- Jia Z, Zhu H, Misra H, Li Y. Potent induction of total cellular GSH and NQO1 as well as mitochondrial GSH by 3H-1,2-dithiole-3-thione in SH-SY5Y neuroblastoma cells and primary human neurons: protection against neurocytotoxicity elicited by dopamine, 6-hydroxydopamine, 4-hydroxy. Brain Res. 2008;1197:159-69 pubmed publisher
- Gaval Cruz M, Schroeder J, Liles L, Javors M, Weinshenker D. Effects of disulfiram and dopamine beta-hydroxylase knockout on cocaine-induced seizures. Pharmacol Biochem Behav. 2008;89:556-62 pubmed publisher..These results suggest that disulfiram enhances CIS via two distinct mechanisms: it both increases CIS frequency by inhibiting DBH and increases CIS frequency in a DBH-independent manner...
- Dupré A, Boyer Chatenet L, Sattler R, Modi A, Lee J, Nicolette M, et al. A forward chemical genetic screen reveals an inhibitor of the Mre11-Rad50-Nbs1 complex. Nat Chem Biol. 2008;4:119-25 pubmed publisher..Consistent with its ability to target the MRN complex, mirin abolishes the G2/M checkpoint and homology-dependent repair in mammalian cells...
- Nadar V, Ketschek A, Myers K, Gallo G, Baas P. Kinesin-5 is essential for growth-cone turning. Curr Biol. 2008;18:1972-7 pubmed publisher..We propose that kinesin-5 permits MTs to selectively invade one side of the growth cone by opposing their entry into the other side. ..
- Schroeder J, Cooper D, Schank J, Lyle M, Gaval Cruz M, Ogbonmwan Y, et al. Disulfiram attenuates drug-primed reinstatement of cocaine seeking via inhibition of dopamine ?-hydroxylase. Neuropsychopharmacology. 2010;35:2440-9 pubmed publisher..Our results suggest that disulfiram's efficacy in the treatment of cocaine addiction is associated with the inhibition of DBH and interference with the ability of environmental stimuli to trigger relapse...
- Kollu S, Bakhoum S, Compton D. Interplay of microtubule dynamics and sliding during bipolar spindle formation in mammalian cells. Curr Biol. 2009;19:2108-13 pubmed publisher..Thus, the temporal requirement for microtubule sliding generated by Eg5 activity during bipolar spindle assembly in mammalian cells is regulated by changes in the dynamic behavior of microtubules during mitosis. ..
- Rello Varona S, Vitale I, Kepp O, Senovilla L, Jemaà M, Metivier D, et al. Preferential killing of tetraploid tumor cells by targeting the mitotic kinesin Eg5. Cell Cycle. 2009;8:1030-5 pubmed..In conclusion, tetraploid cells are particular vulnerable to undergo mitotic catastrophe after genetic or pharmacological inhibition of Eg5. ..
- Paonessa J, Munday C, Mhawech Fauceglia P, Munday R, Zhang Y. 5,6-Dihydrocyclopenta[c][1,2]-dithiole-3(4H)-thione is a promising cancer chemopreventive agent in the urinary bladder. Chem Biol Interact. 2009;180:119-26 pubmed publisher..In conclusion, CPDT potently and preferentially induces Phase 2 enzymes in the bladder epithelium and Nrf2 is its key mediator. ..
- El Emam A, Al Tamimi A, Al Omar M, Alrashood K, Habib E. Synthesis and antimicrobial activity of novel 5-(1-adamantyl)-2-aminomethyl-4-substituted-1,2,4-triazoline-3-thiones. Eur J Med Chem. 2013;68:96-102 pubmed publisher..None of the newly synthesized compounds were proved to possess marked activity against C. albicans. ..
- Zhang Y, Munday R. Dithiolethiones for cancer chemoprevention: where do we stand?. Mol Cancer Ther. 2008;7:3470-9 pubmed publisher..Further investigation of these compounds may lead to development of effective and safe agents for cancer prevention in humans. ..
- Paonessa J, Ding Y, Randall K, Munday R, Argoti D, Vouros P, et al. Identification of an unintended consequence of Nrf2-directed cytoprotection against a key tobacco carcinogen plus a counteracting chemopreventive intervention. Cancer Res. 2011;71:3904-11 pubmed publisher..Thus, CPDT exemplifies a counteracting solution to the dilemma posed by Nrf2. ..
- Spadaro F, Ramoni C, Mezzanzanica D, Miotti S, Alberti P, Cecchetti S, et al. Phosphatidylcholine-specific phospholipase C activation in epithelial ovarian cancer cells. Cancer Res. 2008;68:6541-9 pubmed publisher..These findings warrant further investigations on the role of PC-PLC and on the effects of its inhibition on the pathways responsible for constitutive EOC cell stimulation and cell proliferation. ..
- Liu C, Wang J. Copper(II) sulfamate: an efficient catalyst for the one-pot synthesis of 3,4-dihydropyrimidine-2(1H)-ones and thiones. Molecules. 2009;14:763-70 pubmed publisher..Compared to the classical Biginelli reaction conditions, the present method has the advantages of good yields, short reaction times and experimental simplicity. ..
- Zhang Y, Xu W. Progress on kinesin spindle protein inhibitors as anti-cancer agents. Anticancer Agents Med Chem. 2008;8:698-704 pubmed..Accordingly, more and more interest has been focused on the development of high effective and selective KSPi. This review will focus on some kinds of KSPi on the basis of introducing structure and function of KSP. ..
- Kaur J, Sundar S, Singh N. Molecular docking, structure-activity relationship and biological evaluation of the anticancer drug monastrol as a pteridine reductase inhibitor in a clinical isolate of Leishmania donovani. J Antimicrob Chemother. 2010;65:1742-8 pubmed publisher..To our knowledge, this is the first report presenting monastrol as a potent oral antileishmanial. ..
- Wang N, Sun C, Huo S, Zhang Y, Zhao J, Zhang S, et al. Cooperation of phosphatidylcholine-specific phospholipase C and basic fibroblast growth factor in the neural differentiation of mesenchymal stem cells in vitro. Int J Biochem Cell Biol. 2008;40:294-306 pubmed..Moreover, basic fibroblast growth factor could contribute to rescuing the differentiated cells from death through decreasing overly high mitochondrial membrane potentials and reactive oxygen species levels. ..
- Bhatia M, Sidhapuriwala J, Sparatore A, Moore P. Treatment with H2S-releasing diclofenac protects mice against acute pancreatitis-associated lung injury. Shock. 2008;29:84-8 pubmed..These results suggest the usefulness of H(2)S-releasing nonsteroidal anti-inflammatory drugs as potential treatments for pancreatitis-associated lung injury. ..
- Sidhapuriwala J, Li L, Sparatore A, Bhatia M, Moore P. Effect of S-diclofenac, a novel hydrogen sulfide releasing derivative, on carrageenan-induced hindpaw oedema formation in the rat. Eur J Pharmacol. 2007;569:149-54 pubmed..It is proposed that the enhanced anti-inflammatory effect of S-diclofenac relates to its ability to release H(2)S at the inflamed site. These data provide evidence for an anti-inflammatory effect of H(2)S. ..
- Manandhar S, Cho J, Kim J, Kensler T, Kwak M. Induction of Nrf2-regulated genes by 3H-1, 2-dithiole-3-thione through the ERK signaling pathway in murine keratinocytes. Eur J Pharmacol. 2007;577:17-27 pubmed
- Koparir M, Orek C, Parlak A, Söylemez A, Koparir P, Karatepe M, et al. Synthesis and biological activities of some novel aminomethyl derivatives of 4-substituted-5-(2-thienyl)-2,4-dihydro-3H-1,2,4-triazole-3-thiones. Eur J Med Chem. 2013;63:340-6 pubmed publisher..Some of the compounds were found to exhibit significant antimicrobial and antioxidant activity. ..
- Ghani U, Ullah N. New potent inhibitors of tyrosinase: novel clues to binding of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides to the dicopper active site. Bioorg Med Chem. 2010;18:4042-8 pubmed publisherA series of 1,3,4-thiadiazole-2(3H)-thiones, 1,3,4-oxadiazole-2(3H)-thiones, 4-amino-1,2,4-triazole-5(4H)-thiones, and substituted hydrazides were tailored and synthesized as new potent inhibitors of tyrosinase...
- Dong J, Sulik K, Chen S. Nrf2-mediated transcriptional induction of antioxidant response in mouse embryos exposed to ethanol in vivo: implications for the prevention of fetal alcohol spectrum disorders. Antioxid Redox Signal. 2008;10:2023-33 pubmed publisher..In addition, the potency of D3T in inducing antioxidants as well as in diminishing ethanol-induced apoptosis suggests that further exploration of the antiteratogenic effect of this compound will be fruitful. ..
- Canman J, Cameron L, Maddox P, Straight A, Tirnauer J, Mitchison T, et al. Determining the position of the cell division plane. Nature. 2003;424:1074-8 pubmed..Our data are consistent with a model in which chromosomes supply microtubules with factors that promote microtubule stability and furrowing. ..
- Lampson M, Renduchitala K, Khodjakov A, Kapoor T. Correcting improper chromosome-spindle attachments during cell division. Nat Cell Biol. 2004;6:232-7 pubmed..Our results provide direct evidence for a mechanism required for the maintenance of genome integrity during cell division. ..
- Singh A, Radeff J, Kunnel J, Stern P. Phosphatidylcholine-specific phospholipase C inhibitor, tricyclodecan-9-yl xanthogenate (D609), increases phospholipase D-mediated phosphatidylcholine hydrolysis in UMR-106 osteoblastic osteosarcoma cells. Biochim Biophys Acta. 2000;1487:201-8 pubmed..The studies reveal a novel action of this inhibitor on signaling in osteoblastic cells which might influence downstream responses. ..
- Vijapurkar U, Wang W, Herbst R. Potentiation of kinesin spindle protein inhibitor-induced cell death by modulation of mitochondrial and death receptor apoptotic pathways. Cancer Res. 2007;67:237-45 pubmed..This study has elucidated cellular responses induced by KSP inhibitors, and the results provide insights for a more effective cancer treatment with these agents. ..
- Kapoor T, Mitchison T. Eg5 is static in bipolar spindles relative to tubulin: evidence for a static spindle matrix. J Cell Biol. 2001;154:1125-33 pubmed..We discuss alternative interpretations of the Eg5 dynamics we observe, ideas for the biochemical nature of a spindle matrix, and implications for Eg5 function. ..
- Brier S, Lemaire D, DeBonis S, Forest E, Kozielski F. Identification of the protein binding region of S-trityl-L-cysteine, a new potent inhibitor of the mitotic kinesin Eg5. Biochemistry. 2004;43:13072-82 pubmed..It is likely that S-trityl-l-cysteine and monastrol inhibit HsEg5 by a similar mechanism. The common inhibitor binding region appears to represent a "hot spot" for HsEg5 that could be exploited for further inhibitor screening. ..
- Even Ram S, Doyle A, Conti M, Matsumoto K, Adelstein R, Yamada K. Myosin IIA regulates cell motility and actomyosin-microtubule crosstalk. Nat Cell Biol. 2007;9:299-309 pubmed..We conclude that myosin IIA negatively regulates cell migration and suggest that it maintains a balance between the actomyosin and microtubule systems by regulating microtubule dynamics. ..
- Kwak M, Egner P, Dolan P, Ramos Gomez M, Groopman J, Itoh K, et al. Role of phase 2 enzyme induction in chemoprotection by dithiolethiones. Mutat Res. 2001;480-481:305-15 pubmed..induction has led to the recognition or isolation of novel, potent chemopreventive agents such as 1,2-dithiole-3-thiones, terpenoids and the isothiocyanate sulforaphane...
- Maliga Z, Kapoor T, Mitchison T. Evidence that monastrol is an allosteric inhibitor of the mitotic kinesin Eg5. Chem Biol. 2002;9:989-96 pubmed..Future structural studies should help in designing more potent Eg5 inhibitors for possible use as anticancer drugs and cell biological reagents. ..
- Katiyar D, Tiwari V, Tripathi R, Srivastava A, Chaturvedi V, Srivastava R, et al. Synthesis and antimycobacterial activity of 3,5-disubstituted thiadiazine thiones. Bioorg Med Chem. 2003;11:4369-75 pubmedA series of 3,5-disubstituted thiadiazine thiones (4-24) have been synthesized by reaction of primary amines with carbon disulphide followed by cyclocondensation of the resulting intermediate with formaldehyde and primary amines or amino ..
- Li L, Rossoni G, Sparatore A, Lee L, Del Soldato P, Moore P. Anti-inflammatory and gastrointestinal effects of a novel diclofenac derivative. Free Radic Biol Med. 2007;42:706-19 pubmed..Administration of S-diclofenac (47.2 micromol/kg, i.p.) to conscious rats significantly increased plasma H2S concentration (at 45 min and 6 h). We propose that H2S release from S-diclofenac in vivo contributes to the observed effects. ..
- Khodjakov A, Copenagle L, Gordon M, Compton D, Kapoor T. Minus-end capture of preformed kinetochore fibers contributes to spindle morphogenesis. J Cell Biol. 2003;160:671-83 pubmed..We propose that the capture and incorporation of preformed K-fibers complements the microtubule plus-end capture mechanism and contributes to spindle formation in vertebrates. ..
- Benbrook D, Kamelle S, Guruswamy S, Lightfoot S, Rutledge T, Gould N, et al. Flexible heteroarotinoids (Flex-Hets) exhibit improved therapeutic ratios as anti-cancer agents over retinoic acid receptor agonists. Invest New Drugs. 2005;23:417-28 pubmed..In conclusion, Flex-Hets exhibit improved therapeutic ratios for multiple cancer types over RAR and/or RXR agonists. ..
- Gartner M, Sunder Plassmann N, Seiler J, Utz M, Vernos I, Surrey T, et al. Development and biological evaluation of potent and specific inhibitors of mitotic Kinesin Eg5. Chembiochem. 2005;6:1173-7 pubmed
- Mayer T, Kapoor T, Haggarty S, King R, Schreiber S, Mitchison T. Small molecule inhibitor of mitotic spindle bipolarity identified in a phenotype-based screen. Science. 1999;286:971-4 pubmed..All previously known small molecules that specifically affect the mitotic machinery target tubulin. Monastrol will therefore be a particularly useful tool for studying mitotic mechanisms. ..
- Crevel I, Alonso M, Cross R. Monastrol stabilises an attached low-friction mode of Eg5. Curr Biol. 2004;14:R411-2 pubmed
- Cochran J, Gilbert S. ATPase mechanism of Eg5 in the absence of microtubules: insight into microtubule activation and allosteric inhibition by monastrol. Biochemistry. 2005;44:16633-48 pubmed
- Hasegawa T, Yamada K, Kosemura S, Yamamura S, Hasegawa K. Phototropic stimulation induces the conversion of glucosinolate to phototropism-regulating substances of radish hypocotyls. Phytochemistry. 2000;54:275-9 pubmed..These results suggest that phototropic stimulation promotes myrosinase activity in the illuminated side of radish hypocotyls, releasing bioactive MTBI from inactive MTBG and simultaneously producing bioactive raphanusanins. ..
- Rusan N, Tulu U, Fagerstrom C, Wadsworth P. Reorganization of the microtubule array in prophase/prometaphase requires cytoplasmic dynein-dependent microtubule transport. J Cell Biol. 2002;158:997-1003 pubmed..The data demonstrate that dynamic astral Mts search the cytoplasm for other Mts, as well as chromosomes, in mitotic cells. ..
- Ramoni C, Spadaro F, Barletta B, Dupuis M, Podo F. Phosphatidylcholine-specific phospholipase C in mitogen-stimulated fibroblasts. Exp Cell Res. 2004;299:370-82 pubmed..These effects were associated with a D609-induced long-lasting cell cycle block in Go. ..
- Munday R, Munday C. Induction of phase II enzymes by 3H-1,2-dithiole-3-thione: dose-response study in rats. Carcinogenesis. 2004;25:1721-5 pubmed..The inductive potency of D3T makes it a most promising candidate for use as a chemoprotective agent. ..
- Yoon S, Choi J, Huh J, Hwang O, Lee H, Hong H, et al. Monastrol, a selective inhibitor of the mitotic kinesin Eg5, induces a distinctive growth profile of dendrites and axons in primary cortical neuron cultures. Cell Motil Cytoskeleton. 2005;60:181-90 pubmed..Taken together, we conclude that Eg5 acts distinctively on dendrites and axons in neurons and suggest a putative model of how Eg5 works distinctively on dendrites and axons. ..
- Kwak M, Itoh K, Yamamoto M, Sutter T, Kensler T. Role of transcription factor Nrf2 in the induction of hepatic phase 2 and antioxidative enzymes in vivo by the cancer chemoprotective agent, 3H-1, 2-dimethiole-3-thione. Mol Med. 2001;7:135-45 pubmed..Knowledge of the factors controlling the specificity of actions of enzyme inducers will be exceedingly helpful in the design and isolation of more efficient and selective chemoprotective agents. ..
- Haque S, Hasaka T, Brooks A, Lobanov P, Baas P. Monastrol, a prototype anti-cancer drug that inhibits a mitotic kinesin, induces rapid bursts of axonal outgrowth from cultured postmitotic neurons. Cell Motil Cytoskeleton. 2004;58:10-6 pubmed..The comparatively modest toxic effects on the neurons over time are a hopeful sign for clinicians interested in using anti-Eg5 drugs for cancer therapy. ..
- Kwak M, Itoh K, Yamamoto M, Kensler T. Enhanced expression of the transcription factor Nrf2 by cancer chemopreventive agents: role of antioxidant response element-like sequences in the nrf2 promoter. Mol Cell Biol. 2002;22:2883-92 pubmed
- Ramoni C, Spadaro F, Menegon M, Podo F. Cellular localization and functional role of phosphatidylcholine-specific phospholipase C in NK cells. J Immunol. 2001;167:2642-50 pubmed..These newly detected mechanisms of PC-PLC translocation and function support an essential role of this enzyme in regulated granule exocytosis and NK-mediated cytotoxicity. ..
- Chun K, Benbrook D, Berlin K, Hong W, Lotan R. The synthetic heteroarotinoid SHetA2 induces apoptosis in squamous carcinoma cells through a receptor-independent and mitochondria-dependent pathway. Cancer Res. 2003;63:3826-32 pubmed..Further investigation of the potential of SHetA2 in prevention and therapy of HNSCC is warranted also because of much lower toxicities compared with receptor active retinoids. ..
- Zhang Y, Hua Y, Benbrook D, Covey J, Dai G, Liu Z, et al. High performance liquid chromatographic analysis and preclinical pharmacokinetics of the heteroarotinoid antitumor agent, SHetA2. Cancer Chemother Pharmacol. 2006;58:561-9 pubmed..A highly sensitive HPLC/UV method for the quantification of SHetA2 in plasma has been developed to support pharmacokinetics of SHetA2 in the mouse. Pharmacokinetic behaviors of this drug appear to be favorable for future development. ..