Genomes and Genes
Summary: Naphthalene rings which contain two ketone moieties in any position. They can be substituted in any position except at the ketone groups.
Publications292 found, 100 shown here
- Shikonin circumvents cancer drug resistance by induction of a necroptotic deathWeidong Han
Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, 88 Jiefang Road, Hangzhou, Zhejiang, China
Mol Cancer Ther 6:1641-9. 2007..To our best knowledge, this is the first report to document the induction of necroptosis by a small molecular compound to circumvent cancer drug resistance...
- Shikonin extracted from medicinal Chinese herbs exerts anti-inflammatory effect via proteasome inhibitionLi Lu
Protein Modification and Degradation Lab, Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, PR China
Eur J Pharmacol 658:242-7. 2011..The novel finding about macrophage proteasome as a target of shikonin suggests that this medicinal compound has great potential to be developed into an anti-inflammatory agent...
- Plumbagin induces G2-M arrest and autophagy by inhibiting the AKT/mammalian target of rapamycin pathway in breast cancer cellsPo Lin Kuo
Cell Biology Laboratory, Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan 717, Taiwan
Mol Cancer Ther 5:3209-21. 2006..Taken together, these results imply a critical role for AKT inhibition in plumbagin-induced G2-M arrest and autophagy of human breast cancer cells...
- Novel multiple apoptotic mechanism of shikonin in human glioma cellsChing Hsein Chen
Department of Microbiology, Immunology and Biopharmaceuticals, College of Life Sciences, National Chiayi University, Chiayi, Taiwan, ROC
Ann Surg Oncol 19:3097-106. 2012..However, the anticancer mechanism of shikonin in human glioma cells is unclear at present. In the present study, we demonstrated that shikonin induces apoptosis in three human glioma cell lines: U87MG, Hs683, and M059K cells...
- Is nitric oxide decrease observed with naphthoquinones in LPS stimulated RAW 264.7 macrophages a beneficial property?Brígida R Pinho
REQUIMTE Laboratório de Farmacognosia, Departamento de Quimica, Faculdade de Farmacia, Universidade do Porto, Porto, Portugal
PLoS ONE 6:e24098. 2011..Several naphthoquinones (plumbagin, naphthazarin, juglone, menadione, diosquinone and 1,4-naphthoquinone), plus p-hydroquinone and p-..
- Selective inactivation of parvulin-like peptidyl-prolyl cis/trans isomerases by jugloneL Hennig
Max Planck Research Unit, Enzymology of Protein Folding, Halle Saale, Germany
Biochemistry 37:5953-60. 1998..Thus, partial unfolding of the active site of the parvulins was thought to be the cause of the deterioration of PPIase activity...
- A multi-center phase II evaluation of the small molecule survivin suppressor YM155 in patients with unresectable stage III or IV melanomaKarl D Lewis
University of Colorado Health Sciences Center, Aurora, CO, USA
Invest New Drugs 29:161-6. 2011..YM155 is a small molecule suppressant of survivin that has been shown in preclinical cell lines, xenograft models and phase I studies to have anti-tumor activity...
- Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) induces apoptosis and cell cycle arrest in A549 cells through p53 accumulation via c-Jun NH2-terminal kinase-mediated phosphorylation at serine 15 in vitro and in vivoYa Ling Hsu
Department of Biotechnology, Chia Nan University of Pharmacy and Science, Tainan, Taiwan
J Pharmacol Exp Ther 318:484-94. 2006..Taken together, these results suggest a critical role for JNK and p53 in plumbagin-induced G2/M arrest and apoptosis of human nonsmall cell lung cancer cells...
- The effects on Trypanosoma cruzi of novel synthetic naphthoquinones are mediated by mitochondrial dysfunctionRubem F S Menna-Barreto
Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 900, Brazil
Free Radic Biol Med 47:644-53. 2009..Our results indicate that the trypanocidal action of the naphthofuranquinones is associated with mitochondrial dysfunction, leading to increased reactive oxygen species generation and parasite death...
- Pharmacological stimulation of NADH oxidation ameliorates obesity and related phenotypes in miceJung Hwan Hwang
Department of Internal Medicine, Chungnam National University School of Medicine, Daejeon, Korea
Diabetes 58:965-74. 2009..We tried to determine whether pharmacological stimulation of NADH oxidation provides therapeutic effects in rodent models of metabolic syndrome...
- Natural products as antiparasitic drugsO Kayser
Freie Universitat Berlin, Institut fur Pharmazie, Pharmazeutische Biotechnologie, Kelchstrasse 31, 12169 Berlin, Germany
Parasitol Res 90:S55-62. 2003..Many novel lead structures, however, have severe chemico-physical drawbacks such as poor solubility. Here, innovative drug formulations and carrier systems might help, as discussed by the authors in another article of this series...
- YM155, a novel small-molecule survivin suppressant, induces regression of established human hormone-refractory prostate tumor xenograftsTakahito Nakahara
Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
Cancer Res 67:8014-21. 2007..Further extensive investigation of YM155 in many types of cancer, including HRPC, seems to be worthwhile to develop this novel therapeutic approach...
- Shikonin, a Chinese plant-derived naphthoquinone, induces apoptosis in hepatocellular carcinoma cells through reactive oxygen species: A potential new treatment for hepatocellular carcinomaKe Gong
College of Life Sciences, Wuhan University, Wuhan 430072, People s Republic of China
Free Radic Biol Med 51:2259-71. 2011..Taken together, our data show that shikonin, which may be a promising agent in the treatment of liver cancer, induced apoptosis in HCC cells through the ROS/Akt and RIP1/NF-κB pathways...
- Plumbagin inhibits invasion and migration of breast and gastric cancer cells by downregulating the expression of chemokine receptor CXCR4Kanjoormana Aryan Manu
Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore, Singapore 117597
Mol Cancer 10:107. 2011..Thus, novel agents that can downregulate the CXCR4/CXCL12 axis have therapeutic potential in inhibiting cancer metastasis...
- Plumbagin induces cell death through a copper-redox cycle mechanism in human cancer cellsS Nazeem
Department of Biochemistry, Faculty of Life Sciences, Aligarh Muslim University, Aligarh 202002, Uttar Pradesh, India
Mutagenesis 24:413-8. 2009....
- Cellular pharmacology studies of shikonin derivativesXin Chen
Laboratory of Molecular Immunoregulation, Division of Basic Sciences, National Cancer Institute Frederick, MD 21702 1201, USA
Phytother Res 16:199-209. 2002..This general inhibitory effect can account for the broad spectrum of shikonin biological and pharmacological activities...
- Phase I study of YM155, a novel survivin suppressant, in patients with advanced solid tumorsTaroh Satoh
Department of Medical Oncology, Kinki University School of Medicine, Osaka, Japan
Clin Cancer Res 15:3872-80. 2009..The aim of this study was to determine the maximum tolerated dose (MTD) and to assess the safety, pharmacokinetics, and antitumor activity of YM155 in patients with advanced refractory solid tumors...
- Antitumor effects of YM155, a novel survivin suppressant, against human aggressive non-Hodgkin lymphomaAya Kita
Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
Leuk Res 35:787-92. 2011..YM155 increased survival significantly versus rituximab in disseminated Ramos models. This study suggests that YM155 may represent an effective treatment for aggressive lymphomas...
- YM155, a novel survivin suppressant, enhances taxane-induced apoptosis and tumor regression in a human Calu 6 lung cancer xenograft modelTakahito Nakahara
Institute for Drug Discovery Research, Astellas Pharma Inc, Tsukuba shi, Ibaraki, Japan
Anticancer Drugs 22:454-62. 2011....
- Broad spectrum and potent antitumor activities of YM155, a novel small-molecule survivin suppressant, in a wide variety of human cancer cell lines and xenograft modelsTakahito Nakahara
Institute for Drug Discovery Research, Astellas Pharma, Inc, Tsukuba, Ibaraki, Japan
Cancer Sci 102:614-21. 2011..The broad and potent antitumor activity presented in the present study is indicative of the therapeutic potential of YM155 in the clinical setting...
- Anti-inflammatory effects of plumbagin are mediated by inhibition of NF-kappaB activation in lymphocytesRahul Checker
Radiation Biology and Health Sciences Division, Bhabha Atomic Research Centre, Mumbai 400085, India
Int Immunopharmacol 9:949-58. 2009..Further, plumbagin prevented Graft Versus Host Disease-induced mortality in mice. To our knowledge this is the first report showing the immunomodulatory effects of plumbagin in lymphocytes via modulation of NF-kappaB activation...
- Multicenter phase II trial of YM155, a small-molecule suppressor of survivin, in patients with advanced, refractory, non-small-cell lung cancerGiuseppe Giaccone
Vrije Universiteit Medical Center, Amsterdam, The Netherlands
J Clin Oncol 27:4481-6. 2009..To evaluate the antitumor activity and safety of YM155, a novel, small-molecule suppressor of survivin, as single-agent therapy in patients with previously treated, advanced non-small-cell lung cancer (NSCLC)...
- Phase I and pharmacokinetic study of YM155, a small-molecule inhibitor of survivinAnthony W Tolcher
Institute for Drug Development, Cancer Therapy and Research Center, San Antonio, TX, USA
J Clin Oncol 26:5198-203. 2008..To determine the maximum-tolerated dose (MTD) and assess the safety, pharmacokinetics, and preliminary evidence of antitumor activity of YM155, a small-molecule inhibitor of survivin...
- Plumbagin (5-hydroxy-2-methyl-1,4-naphthoquinone) suppresses NF-kappaB activation and NF-kappaB-regulated gene products through modulation of p65 and IkappaBalpha kinase activation, leading to potentiation of apoptosis induced by cytokine and chemotherapeSantosh K Sandur
Cytokine Research Laboratory, Department of Experimental Therapeutics, Unit 143, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
J Biol Chem 281:17023-33. 2006..This may explain its cell growth modulatory, anticarcinogenic, and radiosensitizing effects previously described...
- An NQO1- and PARP-1-mediated cell death pathway induced in non-small-cell lung cancer cells by beta-lapachoneErik A Bey
Department of Pharmacology, Laboratory of Molecular Stress Responses, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA
Proc Natl Acad Sci U S A 104:11832-7. 2007..beta-Lapachone killed cells in a tumorselective manner and is indicated for use against NQO1+ NSCLC cancers...
- Cytotoxic action of juglone and plumbagin: a mechanistic study using HaCaT keratinocytesJ Johnson Inbaraj
Laboratory of Pharmacology and Chemistry, National Institute of Environmental Health Sciences, National Institutes of Health, Research Triangle Park, North Carolina 27709, USA
Chem Res Toxicol 17:55-62. 2004..However, it is probable that the antifungal, antiviral, and antibacterial properties of these quinones are the result of redox cycling...
- Necrostatin-1 reverts shikonin-induced necroptosis to apoptosisWeidong Han
Cancer Institute, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310009, China
Apoptosis 14:674-86. 2009..To the best of our knowledge, this is the first study to document a conversion from necroptosis to apoptosis...
- Shikonin exerts antitumor activity via proteasome inhibition and cell death induction in vitro and in vivoHuanjie Yang
Department of Pathophysiology, Guangzhou Medical College, Guangzhou, Guangdong, People s Republic of China
Int J Cancer 124:2450-9. 2009..Our results indicate that the tumor proteasome is one of the cellular targets of shikonin and inhibition of the proteasome activity by shikonin contributes to its antitumor property...
- Beta-lapachone, a modulator of NAD metabolism, prevents health declines in aged miceJeong Sook Lee
Department of Biological Sciences, KAIST Korea Advanced Institute of Science and Technology, Daejeon, Korea
PLoS ONE 7:e47122. 2012..These results support the potentiation of NQO1 activity by a βL diet and could be an option for preventing age-related decline of muscle and brain functions...
- Beta-hydroxyisovalerylshikonin induces apoptosis in human leukemia cells by inhibiting the activity of a polo-like kinase 1 (PLK1)Yutaka Masuda
Laboratory of Biological Chemistry, School of Pharmaceutical Sciences, Showa University, Tokyo 142 8555, Japan
Oncogene 22:1012-23. 2003..These results suggest that suppression of the activity of PLK1 via inhibition of tyrosine kinase activity by beta-HIVS might play a critical role in the induction of apoptosis...
- Activation of NAD(P)H:quinone oxidoreductase 1 prevents arterial restenosis by suppressing vascular smooth muscle cell proliferationSun Yee Kim
Department of Internal Medicine, Kyungpook National University School of Medicine, Daegu, South Korea
Circ Res 104:842-50. 2009..These observations provide the molecular basis that pharmacological stimulation of NQO1 activity is a new therapy for the treatment of vascular restenosis and/or atherosclerosis which are caused by proliferation of VSMCs...
- Shikonin kills glioma cells through necroptosis mediated by RIP-1Chuanjiang Huang
Department of Neurosurgery, First Bethune Hospital of Jilin University, Changchun, China
PLoS ONE 8:e66326. 2013..Shikonin was reported to induce necroptosis in leukemia cells, but apoptosis in glioma cell lines. Thus, it is needed to clarify whether shikonin could cause necroptosis in glioma cells and investigate its underlying mechanisms...
- Natural and synthetic naphthoquinones active against Trypanosoma cruzi: an initial step towards new drugs for Chagas diseaseCristian O Salas
Facultad de Quimica, Pontificia Universidad Catolica de Chile, Casilla 306, Santiago 6094411, Chile
Curr Med Chem 18:144-61. 2011..An overview of a number of natural naphthoquinones tested against T. cruzi parasites is provided...
- Synthesis of a small library of 2-phenoxy-1,4-naphthoquinone and 2-phenoxy-1,4-anthraquinone derivatives bearing anti-trypanosomal and anti-leishmanial activityMaria Laura Bolognesi
Department of Pharmaceutical Sciences, Alma Mater Studiorum, Bologna University, Via Belmeloro 6, I 40126 Bologna, Italy
Bioorg Med Chem Lett 18:2272-6. 2008..28microM, and IC(50)=1.26microM, respectively)...
- Increased age reduces DAF-16 and SKN-1 signaling and the hormetic response of Caenorhabditis elegans to the xenobiotic jugloneAaron J Przybysz
Department of Pharmacology, Vanderbilt University, 1161 21st Avenue South, Nashville, TN 37232, USA
Mech Ageing Dev 130:357-69. 2009..Our studies provide a foundation for developing a molecular understanding of how age affects cytoprotective transcriptional pathways...
- A novel triazolic naphthofuranquinone induces autophagy in reservosomes and impairment of mitosis in Trypanosoma cruziM C Fernandes
Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, RJ 21040 360, Brazil
Parasitology 139:26-36. 2012..In folk medicine, natural products including naphthoquinones have been employed for the treatment of different parasitic diseases...
- Plumbagin inhibits tumour angiogenesis and tumour growth through the Ras signalling pathway following activation of the VEGF receptor-2Li Lai
Institute of Biomedical Sciences and School of Life Sciences, East China Normal University, 500 Dongchuan Road, Shanghai 200241, China
Br J Pharmacol 165:1084-96. 2012..Here, we sought to determine the biological effects of plumbagin on signalling mechanisms during tumour angiogenesis...
- Endoplasmic reticulum stress-induced JNK activation is a critical event leading to mitochondria-mediated cell death caused by β-lapachone treatmentHyemi Lee
Department of Microbiology, College of Medicine, Center for Advanced Medical Education by BK21 Project, Inha University, Incheon, Republic of Korea
PLoS ONE 6:e21533. 2011..Although β-lap has been reported to induce apoptosis in various cancer types in an NQO1-dependent manner, the signaling pathways by which β-lap causes apoptosis are poorly understood...
- Plumbagin induces apoptosis via the p53 pathway and generation of reactive oxygen species in human osteosarcoma cellsLinqiang Tian
Department of Orthopedics, Tongji Hospital, Tongji Medical College, Huazhong University of Science and Technology, Wuhan 430030, PR China
Mol Med Rep 5:126-32. 2012..To conclude, PL exerted anticancer activity on osteosarcoma cells by inducing pro-apoptotic signaling and modulating the intracellular ROS that causes induction of apoptosis. These effects may relate to the p53 status...
- A novel color change mechanism for breast cancer biomarker detection: naphthoquinones as specific ligands of human arylamine N-acetyltransferase 1Nicola Laurieri
Department of Pharmacology, University of Oxford, Oxford, United Kingdom
PLoS ONE 8:e70600. 2013..This represents a new mechanism for selective biomarker sensing and may be exploited as a general approach to the specific detection of biomarkers in disease. ..
- Involvement of reactive oxygen species, but not mitochondrial permeability transition in the apoptotic induction of human SK-Hep-1 hepatoma cells by shikoninChing Hsein Chen
Department of Medical Technology, Fooyin University, Ta Liao, Kaohsiung, Taiwan, ROC
Planta Med 69:1119-24. 2003..Taken together, we suggest that shikonin-induced apoptosis of SK-Hep-1 cells proceeds by an oxidative stress-mediated pathway...
- A shikonin derivative, beta-hydroxyisovalerylshikonin, is an ATP-non-competitive inhibitor of protein tyrosine kinasesKazuyasu Nakaya
School of Pharmaceutical Sciences, Showa University, Tokyo, Japan
Anticancer Drugs 14:683-93. 2003....
- Artemisinin-naphthoquine combination (ARCO) therapy for uncomplicated falciparum malaria in adults of Papua New Guinea: a preliminary report on safety and efficacyFrancis W Hombhanje
Faculty of Health Sciences, Divine Word University, Madang Province, Papua New Guinea
Malar J 8:196. 2009..A study was undertaken to assess the safety, efficacy and tolerability of ANQ combination in areas of multi-drug resistance to generate preliminary baseline data in adult population of Papua New Guinea...
- Multiple stressors in Caenorhabditis elegans induce stress hormesis and extended longevityJames R Cypser
Institute for Behavioral Genetics, University of Colorado, Boulder 80303, USA
J Gerontol A Biol Sci Med Sci 57:B109-14. 2002..In dose-response studies, induced thermotolerance paralleled the induced increase in life expectancy, which is consistent with a common origin...
- Selective induction of necrotic cell death in cancer cells by beta-lapachone through activation of DNA damage response pathwayXiangao Sun
Department of Therapeutic Biology, ArQule Biomedical Institute, Norwood, Massachusetts 02062, USA
Cell Cycle 5:2029-35. 2006..Our data suggest that selective necrotic cell death can be induced through activation of DNA damage response pathways, supporting the idea of selective necrotic cell death as a therapeutic strategy to eliminate cancer cells...
- Plumbagin-induced apoptosis of human breast cancer cells is mediated by inactivation of NF-kappaB and Bcl-2Aamir Ahmad
Department of Pathology, Barbara Ann Karmanos Cancer Center and Wayne State University School of Medicine, Detroit, Michigan 48201, USA
J Cell Biochem 105:1461-71. 2008....
- Prostate cancer radiosensitization through poly(ADP-Ribose) polymerase-1 hyperactivationYing Dong
Departments of Pharmacology, Radiation Oncology, Pathology, Biostatistics and Clinical Sciences, and Urology, Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, Dallas, TX 75390 8807, USA
Cancer Res 70:8088-96. 2010..Our findings offer a rationale for the clinical utilization of β-lap (Arq 501) as a radiosensitizer in prostate cancers that overexpress NQO1, offering a potentially synergistic targeting strategy to exploit PARP-1 hyperactivation...
- Calcium is a key signaling molecule in beta-lapachone-mediated cell deathC Tagliarino
Departments of Radiation Oncology and Pharmacology, Department of Anatomy, Case Western Reserve University, Cleveland, Ohio 44106-4942, USA
J Biol Chem 276:19150-9. 2001..Use of beta-Lap to trigger an apparently novel, calpain-like-mediated apoptotic cell death could be useful for breast and prostate cancer therapy...
- Alteration of the repressor activity of MarR, the negative regulator of the Escherichia coli marRAB locus, by multiple chemicals in vitroM N Alekshun
Center for Adaptation Genetics and Drug Resistance, Tufts University School of Medicine, Boston, Massachusetts 02111, USA
J Bacteriol 181:4669-72. 1999..It is proposed that these compounds can interact directly with MarR to affect its repressor activity...
- Induction of apoptosis by shikonin through a ROS/JNK-mediated process in Bcr/Abl-positive chronic myelogenous leukemia (CML) cellsXin Mao
1State Key Laboratory of Virology, College of Life Sciences, Wuhan University, Wuhan 430072, China
Cell Res 18:879-88. 2008..Our data also suggest that shikonin may be a promising agent for the treatment of CML, as a generator of ROS...
- Inhibition of Nox-4 activity by plumbagin, a plant-derived bioactive naphthoquinoneYaxian Ding
Department of Medicine, Case Western Reserve University and University Hospital of Cleveland, Cleveland, Ohio 44106, USA
J Pharm Pharmacol 57:111-6. 2005..Furthermore, plumbagin inhibited the superoxide production in Nox-4 transfected COS-7 cells. These results indicated that plumbagin directly interacted with Nox-4 and inhibited its activity...
- Plumbagin, a medicinal plant-derived naphthoquinone, is a novel inhibitor of the growth and invasion of hormone-refractory prostate cancerMoammir H Aziz
Department of Human Oncology, School of Medicine and Public Health, University of Wisconsin, Madison, Wisconsin 53792, USA
Cancer Res 68:9024-32. 2008..PL inhibits multiple molecular targets including PKCepsilon, a predictive biomarker of PCa aggressiveness. PL may be a novel agent for therapy of hormone-refractory PCa...
- The trypanocidal activity of naphthoquinones: a reviewAntonio Ventura Pinto
Núcleo de Pesquisas em Produtos Naturais, Centro de Ciencias da Saude, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil
Molecules 14:4570-90. 2009b>Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes...
- p53-mediated cell cycle arrest and apoptosis induced by shikonin via a caspase-9-dependent mechanism in human malignant melanoma A375-S2 cellsZhen Wu
Department of Phytochemistry, Shenyang Pharmaceutical University, P R China
J Pharmacol Sci 94:166-76. 2004..Apoptosis-inducing factor, another apoptotic protein of mitochondria, partially contributed to shikonin-induced release of cytochrome c. Taken together, shikonin-induced DNA damage activates p53 and caspase-9 pathways...
- Naturally-occurring shikonin analogues--a class of necroptotic inducers that circumvent cancer drug resistanceYanyan Xuan
Cancer Institute, The Key Laboratory of Cancer Prevention and Intervention, China National Ministry of Education, The Second Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang 310009, China
Cancer Lett 274:233-42. 2009..The results strengthen the previous findings that necroptotic induction could circumvent a broad spectrum of cancer drug resistance...
- Shikonin induces apoptosis through reactive oxygen species/extracellular signal-regulated kinase pathway in osteosarcoma cellsI Chang Chang
Institute of Medicine, Chung Shan Medical University, Taichung 40201, Taiwan
Biol Pharm Bull 33:816-24. 2010..Therefore, shikonin may be a promising chemotherapeutic agent for osteosarcoma treatment...
- Plumbagin induces reactive oxygen species, which mediate apoptosis in human cervical cancer cellsPriya Srinivas
Division of Cancer Biology, Rajiv Gandhi Centre for Biotechnology, Thiruvananthapuram, Kerala, India
Mol Carcinog 40:201-11. 2004....
- Cytochrome b mutations that modify the ubiquinol-binding pocket of the cytochrome bc1 complex and confer anti-malarial drug resistance in Saccharomyces cerevisiaeJacques J Kessl
Department of Biochemistry, Dartmouth Medical School, Hanover, New Hampshire 03755
J Biol Chem 280:17142-8. 2005..By modeling the variations in cytochrome b structure and atovaquone binding with the mutated bc1 complexes, we obtained the first quantitative explanation for the molecular basis of atovaquone resistance in malaria parasites...
- Caenorhabditis elegans lifespan extension caused by treatment with an orally active ROS-generator is dependent on DAF-16 and SIR-2.1Tanja Heidler
Department of Food and Nutrition, Molecular Nutrition Unit, Technical University of Munich, Am Forum 5, Freising, Germany
Biogerontology 11:183-95. 2010..1-dependent alterations in gene expression after a ROS challenge lead to a lifespan extension in C. elegans as long as the stressor concentration does not exceed the saturable protective capacity...
- Putative polyketide synthase and laccase genes for biosynthesis of aurofusarin in Gibberella zeaeJung Eun Kim
School of Agricultural Biotechnology and Center for Agricultural Biomaterials, Seoul National University, Seoul, Korea
Appl Environ Microbiol 71:1701-8. 2005..zeae. This information is the first information concerning the biosynthesis of these pigments by G. zeae and could help in studies of their toxicity in domesticated animals...
- Naphthoimidazoles promote different death phenotypes in Trypanosoma cruziR F S Menna-Barreto
Laboratorio de Biologia Celular, Instituto Oswaldo Cruz, Fundacao Oswaldo Cruz, Rio de Janeiro, Brazil
Parasitology 136:499-510. 2009..However, there are other pathways occurring concomitantly with variable intensities, justifying the need to detail the molecular features involved...
- Shikonin, an ingredient of Lithospermum erythrorhizon induced apoptosis in HL60 human premyelocytic leukemia cell lineY Yoon
Laboratory of Cancer Research, Korea Institute of Oriental Medicine, Seoul
Planta Med 65:532-5. 1999..The DNA fragmentation induced by shikonin was completely inhibited by the pretreatment of z-VAD-fmk, a specific inhibitor of caspase, clearly showing that the mode of cell death is apoptotic...
- Selective killing of cancer cells by beta -lapachone: direct checkpoint activation as a strategy against cancerYouzhi Li
Division of Gastroenterology, Beth Israel Deaconess Medical Center, Harvard Medical School, 330 Brookline Avenue, Boston, MA 02215, USA
Proc Natl Acad Sci U S A 100:2674-8. 2003..This study suggests direct checkpoint activation as a strategy against cancer...
- Calcium-dependent modulation of poly(ADP-ribose) polymerase-1 alters cellular metabolism and DNA repairMelissa S Bentle
Department of Pharmacology, Case Western Reserve University, Cleveland, Ohio 44106, USA
J Biol Chem 281:33684-96. 2006..Thus, Ca(2+) appears to be an important co-factor in PARP-1 hyperactivation after ROS-induced DNA damage, which alters cellular metabolism and DNA repair...
- Plumbagin induces cell cycle arrest and apoptosis through reactive oxygen species/c-Jun N-terminal kinase pathways in human melanoma A375.S2 cellsClay C C Wang
Department of Chemistry, University of Southern California, College of Letters, Arts, and Sciences, University Park Campus, Los Angeles, CA 90089, USA
Cancer Lett 259:82-98. 2008..Moreover, blocking ERK and JNK by specific inhibitors suppressed plumbagin-triggered mitochondrial apoptotic pathway. Taken together, these results imply a critical role for ROS and JNK in the plumbagin's anticancer activity...
- Suppression of human prostate cancer cell growth by beta-lapachone via down-regulation of pRB phosphorylation and induction of Cdk inhibitor p21(WAF1/CIP1)Yung Hyun Choi
Department of Biochemistry, College of Oriental Medicine, Dong Eui University and Research Center for Oriental Medicine, Pusan 614 052, Korea
J Biochem Mol Biol 36:223-9. 2003..Overall, our results demonstrate a combined mechanism that involves the inhibition of pRB phosphorylation and induction of p21 as targets for beta-lapachone. This may explain some of its anticancer effects...
- Alkannins and shikonins: a new class of wound healing agentsV P Papageorgiou
Laboratory of Organic Chemistry, Department of Chemical Engineering, Aristotle University of Thessaloniki, Greece
Curr Med Chem 15:3248-67. 2008..In this paper we review the findings and advances on the molecular and biological properties of A/S that promote wound healing...
- Shikonin induces programmed necrosis-like cell death through the formation of receptor interacting protein 1 and 3 complexSeungyeon Park
Department of Pharmacy, Keimyung University, 1095 Sindang dong, Dalseo Gu, Daegu 704 701, South Korea
Food Chem Toxicol 55:36-41. 2013..Here, it is highlighted that SKN as well as TNFα can directly mediate cell death via a pronecrotic complex, but ROS were generated via different routes depending on cell death-inducing agents...
- Plumbagin induces apoptosis in Her2-overexpressing breast cancer cells through the mitochondrial-mediated pathwayAnna Kawiak
Department of Biotechnology, Intercollegiate Faculty of Biotechnology, University of Gdansk and Medical University of Gdansk, Kladki 24, 80 822 Gdansk, Poland
J Nat Prod 75:747-51. 2012....
- Plumbagin, a plant derived natural agent inhibits the growth of pancreatic cancer cells in in vitro and in vivo via targeting EGFR, Stat3 and NF-κB signaling pathwaysBilal Bin Hafeez
Department of Human Oncology, Wisconsin Institute of Medical Research, Paul Carbone Comprehensive Cancer Center, School of Medicine and Public Health, University of Wisconsin, Madison, WI 53792, USA
Int J Cancer 131:2175-86. 2012..These results suggest that PL may be used as a novel therapeutic agent against human PC. Published 2012 Wiley-Liss, Inc. This article is a US Government work, and, as such, is in the public domain in the United States of America...
- Perspectives on medicinal properties of plumbagin and its analogsSubhash Padhye
Department of Pathology, Barbara Ann Karmanos Cancer Institute, Wayne State University School of Medicine, Hudson Webber Cancer Research Center, Detroit, Michigan 48201, USA
Med Res Rev 32:1131-58. 2012..This comprehensive review is an attempt to understand the chemistry of plumbagin and catalog its biological activities reported to date...
- Plumbagin inhibits osteoclastogenesis and reduces human breast cancer-induced osteolytic bone metastasis in mice through suppression of RANKL signalingBokyung Sung
Cytokine Research Laboratory, Department of Experimental Therapeutics, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
Mol Cancer Ther 11:350-9. 2012..Overall, our results indicate that plumbagin, a vitamin K analogue, is a potent inhibitor of osteoclastogenesis induced by tumor cells and of breast cancer-induced osteolytic metastasis through suppression of RANKL signaling...
- In vitro antimicrobial activity of a new series of 1,4-naphthoquinonesA Riffel
Departamento de Ciências dos Alimentos, Instituto de Ciências e Tecnologia de Alimentos, Universidade Federal do Rio Grande do Sul, Porto Alegre, RS, Brasil
Braz J Med Biol Res 35:811-8. 2002The antibacterial activity of a series of 1,4-naphthoquinones was demonstrated. Disk diffusion tests were carried out against several Gram-positive and Gram-negative bacteria...
- Novel o-naphthoquinones induce apoptosis of EL-4 T lymphoma cells through the increase of reactive oxygen speciesMaría Emilia Di Rosso
Centro de Estudios Farmacologicos y Botanicos CEFYBO, Facultad de Medicina, Universidad de Buenos Aires CONICET, Paraguay 2155, piso 16, C1121ABG Buenos Aires, Argentina
Toxicol In Vitro 27:2094-104. 2013....
- Inhibition of mycobacterial growth by plumbagin derivativesRitta Mathew
Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India
Chem Biol Drug Des 76:34-42. 2010..smegmatis. Structural modifications of these molecules can further be improved upon to generate new molecules against mycobacteria...
- Plumbagin inhibits TPA-induced MMP-2 and u-PA expressions by reducing binding activities of NF-kappaB and AP-1 via ERK signaling pathway in A549 human lung cancer cellsJiunn Min Shieh
Department of Pulmonary Medicine, Chi Mei Medical Center, Tainan 710, Taiwan
Mol Cell Biochem 335:181-93. 2010..Presented data reveals that plumbagin is a novel, effective, anti-metastatic agent that functions by down-regulating MMP-2 and u-PA gene expressions...
- Strategies for the synthesis of bioactive pyran naphthoquinonesVitor Francisco Ferreira
Universidade Federal Fluminense, Instituto de Quimica, Departamento de Quimica Organica, CEG, Campus do Valonguinho, 24020 141 Niterói, Rio de Janeiro, Brazil
Org Biomol Chem 8:4793-802. 2010Taking into account the numerous reports in the literature related to pyran naphthoquinones in searching for new pharmacologically promising molecules against different therapeutic targets, this review intends to explore the synthetic ..
- A chemical genetic screen for modulators of asymmetrical 2,2'-dimeric naphthoquinones cytotoxicity in yeastAshkan Emadi
Department of Internal Medicine and Oncology, Johns Hopkins School of Medicine, Baltimore, Maryland, USA
PLoS ONE 5:e10846. 2010Dimeric naphthoquinones (BiQ) were originally synthesized as a new class of HIV integrase inhibitors but have shown integrase-independent cytotoxicity in acute lymphoblastic leukemia cell lines suggesting their use as potential anti-..
- The biosynthetic pathway for aurofusarin in Fusarium graminearum reveals a close link between the naphthoquinones and naphthopyronesRasmus J N Frandsen
Department of Ecology, The Royal Veterinary and Agricultural University, DK 1871 Frederiksberg C, Copenhagen, Denmark
Mol Microbiol 61:1069-80. 2006..This links the biosynthesis of naphthopyrones and naphthoquinones together...
- Design, synthesis and biological evaluation of novel nitrogen and sulfur containing hetero-1,4-naphthoquinones as potent antifungal and antibacterial agentsVishnu K Tandon
Department of Chemistry, University of Lucknow, Lucknow, India
Eur J Med Chem 44:3130-7. 2009A series of 2-Arylamino-3-chloro-1,4-naphthoquinones (3), 2-Amino-3-arylsulfanyl-1,4-naphthoquinones (5), 2-Arylamino-3-arylsulfanyl-1,4-naphthoquinones (6), Dihydrobenzo[f]naphtho[2,3-b][1,4]thiazepine-6,11-diones (9) (via Pictet-..
- Differential functional genomic effects of anti-inflammatory phytocompounds on immune signalingShao Chih Chiu
Graduate Institute of Immunology, China Medical University, 91 Hsueh Shih Rd, Taichung 40402, Taiwan
BMC Genomics 11:513. 2010....
- Antimicrobial activities of naphthazarins from Arnebia euchromaChien Chang Shen
National Research Institute of Chinese Medicine, Taipei 112, Taiwan
J Nat Prod 65:1857-62. 2002..6-5.4 microg/mL (CD(50)). Our results indicate that the ester derivatives of alkannin are potential candidates of anti-MRSA and anti-VRE agents with antitumor activity...
- Efficacy of oral single dose therapy with artemisinin-naphthoquine phosphate in uncomplicated falciparum malariaThein Tun
Department of Medical Research Upper Myanmar, Anisakhan, Pyin Oo Lwin 05062, Mandalay Division, Myanmar
Acta Trop 111:275-8. 2009..The drug was well tolerated and no adverse reactions were detected in the patients. Since it is a single dose therapy, health workers can administer the drug as directly observed treatment...
- Atovaquone-proguanil versus mefloquine for malaria prophylaxis in nonimmune travelers: results from a randomized, double-blind studyD Overbosch
Harbor Hospital and Institute of Tropical Medicine, Rotterdam, The Netherlands
Clin Infect Dis 33:1015-21. 2001..No confirmed diagnoses of malaria occurred in either group. Atovaquone-proguanil was better tolerated than was mefloquine, and it was similarly effective for malaria prophylaxis in nonimmune travelers...
- Initial response and cellular protection through the Keap1/Nrf2 system during the exposure of primary mouse hepatocytes to 1,2-naphthoquinoneTakashi Miura
Doctoral Programs in Medical Sciences, Graduate School of Comprehensive Human Sciences, Graduate School of Life and Environmental Sciences, University of Tsukuba, 1 1 1 Tennodai, Tsukuba, Ibaraki, Japan
Chem Res Toxicol 24:559-67. 2011..These findings suggest that the Keap1/Nrf2 system is essential for the prevention of cell damage resulting from exposure to 1,2-NQ...
- Causal prophylactic efficacy of atovaquone-proguanil (Malarone) in a human challenge modelJ D Berman
Walter Reed Army Institute of Research, Silver Spring, MD 20910, USA
Trans R Soc Trop Med Hyg 95:429-32. 2001..No atovaquone-proguanil volunteer acquired malaria. Atovaquone-proguanil is the first licensed antimalarial agent that kills P. falciparum in the liver and that may be discontinued 7 days after the last exposure...
- In vitro antifungal activity of naphthoquinone derivativesKenroh Sasaki
Tohoku Pharmaceutical University, Sendai, Japan
Biol Pharm Bull 25:669-70. 2002..krusei compared with the standard. Against the filamentous fungus, Trichosporon cutaneum, all naphthoquinones were found to have a range of activity with lower potency than standard...
- Shikonin derivatives inhibited LPS-induced NOS in RAW 264.7 cells via downregulation of MAPK/NF-kappaB signalingYu Wen Cheng
School of Pharmacy, Taipei Medical University, Taipei, Taiwan, Republic of China
J Ethnopharmacol 120:264-71. 2008..In the present study, the effect and the underline molecular mechanism of shikonin derivatives isolated from root extracts of Lithospermum euchroma on lipopolysaccharide (LPS)-induced inflammatory response were investigated...
- Design of anti-parasitic and anti-fungal hydroxy-naphthoquinones that are less susceptible to drug resistanceLouise M Hughes
Department of Biochemistry, Dartmouth Medical School, 7200 Vail, Hanover, NH 03755, USA
Mol Biochem Parasitol 177:12-9. 2011..fungi and overcome drug resistance, we have synthesized and tested the inhibitory activity of novel hydroxy-naphthoquinones against blood stage P. falciparum and liver stage P...
- Chemical inducers of heat shock proteins derived from medicinal plants and cytoprotective genes responseKanwal Ahmed
Division of Gastrointestinal Pathophysiology, Institute of Natural Medicine, University of Toyama, Toyama, Japan
Int J Hyperthermia 28:1-8. 2012..In short, the detailed mechanisms of Hsp70 induction by shikonin is not fully understood, Nrf2 and its target genes might be involved in the Hsp70 up-regulation in U937 cells...
- Targeted BIRC5 silencing using YM155 causes cell death in neuroblastoma cells with low ABCB1 expressionFieke Lamers
Department of Oncogenomics, Academic Medical Center, University of Amsterdam, Meibergdreef 15, PO Box 22700, 1105 AZ Amsterdam, The Netherlands
Eur J Cancer 48:763-71. 2012..Therefore YM155 is a promising novel compound for treatment of neuroblastoma with low ABCB1 expression...
- Plumbagin inhibits proliferative and inflammatory responses of T cells independent of ROS generation but by modulating intracellular thiolsRahul Checker
Radiation Biology and Health Sciences Division, Bio Medical Group, Bhabha Atomic Research Centre, Mumbai 400085, Maharashtra, India
J Cell Biochem 110:1082-93. 2010..Our results for the first time show that antiproliferative effects of plumbagin are mediated by modulation of cellular redox. These results provide a rationale for application of thiol-depleting agents as anti-inflammatory drugs...
- Tabebuia avellanedae naphthoquinones: activity against methicillin-resistant staphylococcal strains, cytotoxic activity and in vivo dermal irritability analysisEliezer Menezes Pereira
Instituto de Microbiologia Prof, Paulo de Góes, Universidade Federal do Rio de Janeiro, Rio de Janeiro, Brazil
Ann Clin Microbiol Antimicrob 5:5. 2006..In addition, its mechanism of action was also analyzed...
- Marked anti-tumour activity of the combination of YM155, a novel survivin suppressant, and platinum-based drugsT Iwasa
Department of Medical Oncology, Kinki University School of Medicine, 377 2 Ohno Higashi, Osaka Sayama, Osaka 589 8511, Japan
Br J Cancer 103:36-42. 2010..We have now investigated the effects of the combination of YM155, a novel small-molecule inhibitor of survivin expression, and platinum compounds (cisplatin and carboplatin) on human non-small cell lung cancer (NSCLC) cell lines...
- Activity of 7-methyljuglone derivatives against Mycobacterium tuberculosis and as subversive substrates for mycothiol disulfide reductaseAnita Mahapatra
Department of Botany, Faculty of Natural and Agricultural Sciences, University of Pretoria, Pretoria 0002, South Africa
Bioorg Med Chem 15:7638-46. 2007..g. other disulfide reductases)...
- Inhibition of tumor necrosis factor-alpha through selective blockade of Pre-mRNA splicing by shikoninShao Chih Chiu
Graduate Institute of Life Sciences, National Defense Medical Center and Agricultural Biotechnology Research Center, Academia Sinica, Taipei, Taiwan, ROC
Mol Pharmacol 71:1640-5. 2007....
- Studies on terpenoids produced by actinomycetes. 5-dimethylallylindole-3-carboxylic Acid and A80915G-8"-acid produced by marine-derived Streptomyces sp. MS239Keiichiro Motohashi
Faculty of Applied Biosciences, Tokyo University of Agriculture, Sakuragaoka, Setagaya Ku, Tokyo, Japan
J Antibiot (Tokyo) 61:75-80. 2008..MS239, two new terpenoids named 5-dimethylallylindole-3-carboxylic acid and A80915G-8''-acid were isolated and their structures were determined mainly by NMR analyses...
- Growth inhibition and induction of apoptosis in human oral squamous cell carcinoma Tca-8113 cell lines by Shikonin was partly through the inactivation of NF-kappaB pathwayRuan Min
Department of Oral and Maxillofacial Surgery, Affiliated No 9 People s Hospital, College of Medicine, Shanghai Jiao Tong University, Shanghai 200011, PRC
Phytother Res 22:407-15. 2008..Pharmacological inhibition of the NF-kappaB activity by Shikonin might be a powerful treatment option for OSCC in which activation of NF-kappaB plays a critical role in tumor growth and progression...
- Topoisomerase inhibitors as anti-arthritic agentsJ K Jackson
Faculty of Pharmaceutical Sciences, University of British Columbia, Vancouver, B C, V6T 1Z3, Canada
Inflamm Res 57:126-34. 2008..The objective of this study was to investigate a variety of structurally unrelated anticancer topoisomerase inhibiting agents as inhibitors of aspects of these disease processes involved in RA...
- Genotoxicity of plumbagin and its effects on catechol and NQNO-induced DNA damage in mouse lymphoma cellsJemal Demma
Department of Pharmaceutical Biosciences, Uppsala University, Division of Toxicology, Box 594, BMC, SE 751 24 Uppsala, Sweden
Toxicol In Vitro 23:266-71. 2009..The fact that non-DNA damaging concentrations of plumbagin diminished the DNA damage induced by catechol, provides further support for the idea that plumbagin may act as an antioxidative agent at low concentrations...
- Efficacy of beta-lapachone in pancreatic cancer treatment: exploiting the novel, therapeutic target NQO1Matthew Ough
Department of Surgery, University of Iowa College of Medicine, Iowa City, Iowa 52242, USA
Cancer Biol Ther 4:95-102. 2005....
- Novel Mechanisms of Quinone ToxicityDavid Ross; Fiscal Year: 2013DESCRIPTION (provided by applicant): Both benzoquinones and naphthoquinones have been found to perturb protein handling and degradation in a variety of cellular systems...
- The Mechanism of Plumbagin-induced Stress Resistance and Lifespan ExtensionSUZANNE ELIZABETH BEREZOVSKY; Fiscal Year: 2013..Plumbagin induces stress resistance at micromolar concentrations, about 0.1% the level required for other naphthoquinones to produce the same effect...
- PLANT TUMOR INHIBITORSDavid Kingston; Fiscal Year: 1980..The synthesis of some modified naphthoquinones as potential anticancer agents will also be carried out as a small portion of this project.
- Enabling Technologies for Combinatorial ChemistryK Nicolaou; Fiscal Year: 2005..abstract_text> ..
- TOTAL SYNTHESIS OF NATURAL PRODUCTSK Nicolaou; Fiscal Year: 2002..3] sigmatropic rearrangement and a radical based ring closure to form the bicyclic skeleton. ..
- TOTAL SYNTHESIS OF AZADIRACHTINK Nicolaou; Fiscal Year: 2008..The proposed work is expected to impact the general areas of pharmaceutical and agricultural research, and infectious diseases in particular, through discoveries in synthetic organic chemistry and chemical biology. ..
- SYNTHESIS OF ANTICANCER AGENTSK C Nicolaou; Fiscal Year: 2010..abstract_text> ..
- TOTAL SYNTHESIS OF APOPTOLIDINK Nicolaou; Fiscal Year: 2004..The proposed work is expected to have significant impact in the area of cancer chemotherapy and should provide enabling technologies and tools for biology and medicine. ..
- Sterol Metabolism in PneumocystisEDNA KANESHIRO; Fiscal Year: 2009....
- Synthesis of Macrolides, Steroids, Cyclopentanoids, etc.BARRY TROST; Fiscal Year: 2009..These new synthetic methods apply to many structural types beyond those illustrated and constitutes a significant to gain access to complex molecular targets more easily. ..
- NINTH INTERNATIONAL WORKSHOPS ON OPPORTUNISTIC PEOTISTS (IWOP-9)EDNA KANESHIRO; Fiscal Year: 2006..As in several IWOP meetings in the past, the 2006 Workshops will be held jointly with the annual meetings of the International Society of Protistologists ( formerly Society of Protozoologists). ..
- Pneumocystis Biochemistry: UbiquinonesEDNA KANESHIRO; Fiscal Year: 2002..carinii CoQ biosynthesis and growth in axenic cultures, and (4) develop atovaquone-resistant P. carinii populations to evaluate CoQ synthesis in sensitive and resistant organisms. ..
- A Molecular MotorT Kelly; Fiscal Year: 2004..The project should expand the understanding of chemically directed and controlled movement, which is a topic central to the understanding of biological systems. ..
- THE SYNTHESIS OF LACTONAMYCIN AND ANALOGST Kelly; Fiscal Year: 2003..To test, in collaboration with Pfizer Inc., analogs and synthetic intermediates for antibiotic, anticancer and other biological activities. ..
- Reduction of Alkylating Quinones and NitroarenesANTONIO ALEGRIA; Fiscal Year: 2003..Undergraduate students will participate in this project, thus improving their qualifications to pursue biomedical research careers. ..
- A Therapeutic Target for MicrosporidiosisLouis Weiss; Fiscal Year: 2007..In addition, the approaches and methods developed in this R21 should also prove useful for studies on methionine aminopeptidases as therapeutic targets in other pathogenic protists. [unreadable] [unreadable] [unreadable]..
- CHEMICAL DIVERSITY LIBRARIES FROM MEDICINAL PLANTS (RMI)Kuo Hsiung Lee; Fiscal Year: 2007..unreadable] [unreadable]..
- Second International Workshop on Microsporidia from Vertebrate and Invertebrate HLouis Weiss; Fiscal Year: 2007..Overall, the goal of this[unreadable] congress is to foster the exchange of information between these diverse groups of[unreadable] scientists leading to advances in research on these emergent pathogens. ..
- Peroxiredoxin 1 in radiotherapy of lung cancerYoung Mee Park; Fiscal Year: 2007..abstract_text> ..
- BIOCHEMICAL REGULATORS OF BLEOMYCIN INDUCED TUMORSJOHN LAZO; Fiscal Year: 2001..The Specific Aims are to: 1) develop cells and mice deficient in BH, 2) develop cells and mice that overexpress BH, 3) isolate and characterize potential proteins that interact with BH and, 4) analyze the regulation of BH expression. ..
- LUNG INJURY BY NAPHTHALENESAlan Buckpitt; Fiscal Year: 2009..These studies are expected to identify appropriate biomarker targets and metabolic proteins where polymorphisms could be important in altering individual susceptibility. ..
- TOXOPLASMA ENCEPHALITIS IN AIDS: BRADYZOITE REGULATIONLouis Weiss; Fiscal Year: 2009....
- SYNTHESIS OF CHLOROPEPTINS, GP120 CD4 BINDING INHIBITORSAMOS SMITH; Fiscal Year: 2001..abstract_text> ..
- PLANT ANTITUMOR AGENTSKuo Hsiung Lee; Fiscal Year: 2009....
- TRANSMISSION OF PNEUMOCYSTIS INFECTIONMelanie Cushion; Fiscal Year: 2001..These studies will result in a clearer understanding of the biology leading to infection with Pc and will provide a rational basis for clinical management and therapeutic intervention. ..
- In Vitro High Throughput Screening Assay for MKP-3(RMI)JOHN LAZO; Fiscal Year: 2005..Nonetheless, no potent or selective small molecule inhibitors of this protein phosphatase have been identified. This proposal will provide sufficient reagents to permit a high throughput screening of 100,000 compounds ..
- Pittsburgh Molecular Libraries Screening Center(RMI)JOHN LAZO; Fiscal Year: 2008..unreadable] [unreadable]..
- CDNA MICROARRAY TO DETECT CELLULAR RESPONSES TO MIXTURESAlan Buckpitt; Fiscal Year: 2001..By examining library clones, these studies may identify new genes whose regulation is altered by chemical exposure. ..
- Alkynyliodonium Salts and Derived Diyls in SynthesisKen Feldman; Fiscal Year: 2009..abstract_text> ..
- New Methodology for Indole Alkaloid SynthesesKen S Feldman; Fiscal Year: 2010..The use of a new variant of the Pummerer reaction to control both oxidation level and reaction site within the indole nucleus forms the basis of this chemistry. ..
- ACQUISITION OF MIRCOARRAY SPOTTER, READER, SOFTWAREAlan Buckpitt; Fiscal Year: 2001..abstract_text> ..
- NMR systems : 2 Bruker Avance 500 ConsolesAMOS SMITH; Fiscal Year: 2006..The areas of public health research include, among others, cancer, infectious diseases, neurodegenerative diseases such as Alzheimer's disease, and heart and cardiovascular disease. [unreadable] [unreadable] [unreadable]..
- Natural Product Leads for Drug DevelopmentKATHLYN PARKER; Fiscal Year: 2009..Molecular modeling will allow the design of candidates for more active drugs. Candidates will be evaluated in the squalene synthase assay. Collaborations for the medicinal chemistry components of the project have been arranged. ..
- PNEUMOCYSTIS GENOME PROJECTMelanie Cushion; Fiscal Year: 2004..Thus, there is but a single aim to this proposal: 1. To finish sequencing the genome of pneumocystis carinii and provide a completed assembly. ..
- International Congress on MicrosporidiosisLouis Weiss; Fiscal Year: 2004..Overall, the goal of this congress is to foster the exchange of information between these diverse groups of scientists leading to advances in research on these emergent pathogens. ..
- STRATEGIES AND METHODS IN SYNTHESIS OF NATURAL PRODUCTSKATHLYN PARKER; Fiscal Year: 2003..During the period which corresponds to this proposal, we plan to apply our new methodology to the synthesis of deacetylravidomycin and kidamycin, representatives of the remaining two major classes. ..
- MECHANISM, SPECIFICITY & REGULATION: CDC25 PHOSPHATASESJohannes Rudolph; Fiscal Year: 2004..Thus, this research will greatly expand the knowledge of cell cycle transitions, their control on a molecular basis, and their role in oncogenesis. ..
- Design and Synthesis of HIV-1 Protease InhibitorsAMOS SMITH; Fiscal Year: 2004....
- Chemical Complementation Assay for MKP-3 (RMI)JOHN LAZO; Fiscal Year: 2005..This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds. ..
- Microsporidiosis:A Therapeutic TargetLouis Weiss; Fiscal Year: 2003....
- In Vitro High Throughput Screening Assay for MKP-1(RMI)JOHN LAZO; Fiscal Year: 2005..No potent or selective small molecule inhibitors of this protein phosphatase are known. This proposal will provide sufficient reagents to permit a high throughput screening of 100,000 compounds. ..
- Chemical Complementation Assay for MKP-1 (RMI)JOHN LAZO; Fiscal Year: 2005..This proposal will provide sufficient reagents, including cells and DMA transfection vectors, to permit the high throughput screening of 100,000 compounds. ..
- New Approaches for Development of PcP TherapyMelanie Cushion; Fiscal Year: 2006..Finally, they will select the most efficacious combinations of agents and evaluate their effects on gene expression again using the macroarray approach. ..
- P450 MEDIATED LUNG TOXICITYAlan Buckpitt; Fiscal Year: 2002....
- SYNTHESIS OF SPONGISTATIN ANTITUMOR AGENTSAMOS SMITH; Fiscal Year: 2007..abstract_text> ..
- Eighth International Workshops on Opportunistic ProtistsMelanie Cushion; Fiscal Year: 2003..Mead's and Cushion's ancestors include native Americans; Marciano-Cabral is Hispanic; Kaneshiro has Pacific-Asian ancestry; Lindsay, Weiss are white. Lindsay is a physically handicapped individual. ..
- Bleomycin Hydrolase and Alzheimer's DiseaseJOHN LAZO; Fiscal Year: 2004..These studies should provide new mechanistic information concerning the pathogenesis of AD as well as reagents for future therapeutic studies. ..
- Cyanohydrin based fluorescent substrates of sEH (RMI)Christophe Morisseau; Fiscal Year: 2004..This will be done by screening the combinatorial libraries from the "NIH Roadmap", libraries contracted from commercial vendors, and more defined libraries generated in house. ..
- PHYSIOLOGICALLY ACTIVE NATURAL PRODUCTSDouglass Taber; Fiscal Year: 2007..In the course of these investigations, new molecular reactivity will be developed that will substantially shorten current routes to polycyclic natural products and drug candidates. ..
- Tissue Transglutaminase in Neurologic InjuryTHUNG SHEN LAI; Fiscal Year: 2007..The inhibitors will be used to investigate the role of TTG in the pathogenesis of expanded polyQ diseases. Current proposal will lead to new therapy for HD and other neurologic disorders. [unreadable] [unreadable] [unreadable]..
- Chemical and Biological Studies on Biaryl PhenolicsKen Feldman; Fiscal Year: 2005..The search for selective 20S proteosome inhibitors among the Ntn-type proteases will be advanced by these investigations. ..