Research Topics
Genomes and Genes | Theresa ShapiroSummaryAffiliation: Johns Hopkins University Country: USA Publications
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Publications
Chemoprotective glucosinolates and isothiocyanates of broccoli sprouts: metabolism and excretion in humansT A Shapiro
Department of Pharmacology and Molecular Sciences, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
Cancer Epidemiol Biomarkers Prev 10:501-8. 2001..These findings will assist in the design of dosing regimens for clinical studies of broccoli sprout efficacy...
Activity of indenoisoquinolines against African trypanosomesRahul P Bakshi
Department of Medicine, Division of Clinical Pharmacology, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
Antimicrob Agents Chemother 53:123-8. 2009..The indenoisoquinolines provide a promising lead for the development of drugs against sleeping sickness...
A mitochondrial topoisomerase IA essential for late theta structure resolution in African trypanosomesJane R Scocca
Division of Clinical Pharmacology, Department of Medicine and of Pharmacology, The Johns Hopkins University School of Medicine, Baltimore, MD, USA
Mol Microbiol 67:820-9. 2008..With no close orthologue in humans it also offers a target for the rational development of selectively toxic new antiprotozoal therapies...- Distinct genes encode type II Topoisomerases for the nucleus and mitochondrion in the protozoan parasite Trypanosoma bruceiTomasz Kulikowicz
Division of Clinical Pharmacology, Department of Medicine, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
J Biol Chem 281:3048-56. 2006.... - Molecular mechanisms of resistance in antimalarial chemotherapy: the unmet challengeRavit Arav-Boger
Division of Infectious Diseases, Department of Pediatrics, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
Annu Rev Pharmacol Toxicol 45:565-85. 2005..Efforts to circumvent resistance range from the use of combination therapy with existing agents to laboratory studies directed toward discovering novel targets and therapies... - Newly identified antibacterial compounds are topoisomerase poisons in African trypanosomesSonya C Tang
Department of Medicine, The Johns Hopkins University School of Medicine, 301 Hunterian Building, 725 North Wolfe Street, Baltimore, MD 21205, USA
Antimicrob Agents Chemother 54:620-6. 2010..Both compounds are planar aromatic polycyclic structures that intercalate into and unwind DNA. These findings reinforce the utility of topoisomerase IImt as a target for development of new drugs for African sleeping sickness... - Malaria-infected mice are cured by oral administration of new artemisinin derivativesGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 51:1035-42. 2008..7-13.7, and this effect is comparable to that of the fully synthetic trioxolane drug development candidate OZ277, which is in phase II clinical trials... - Orally active, water-soluble antimalarial 3-aryltrioxanes: short synthesis and preclinical efficacy testing in rodentsGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 45:3824-8. 2002..4 than is artelinic acid (1), a leading semisynthetic, herb-derived antimalarial trioxane drug candidate... - Malaria-infected mice are cured by a single dose of novel artemisinin derivativesGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins Malaria Research Institute, Johns Hopkins University, Baltimore, Maryland 21218, USA
J Med Chem 50:2516-9. 2007..Four of these trioxane dimers cure malaria-infected mice after only a single subcutaneous dose, and two other dimers cure after three oral doses... - Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacyGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 46:1060-5. 2003.... - RNA interference of Trypanosoma brucei topoisomerase IB: both subunits are essentialRahul P Bakshi
Division of Clinical Pharmacology, Department of Medicine, Johns Hopkins University School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA
Mol Biochem Parasitol 136:249-55. 2004..These findings underscore the essential nature of type IB topoisomerase activity in Trypanosoma brucei and its suitability as a target for rational drug design... - Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodentsGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 N Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 47:1299-301. 2004..In the transgenic adenocarcinoma of mouse prostate model, some of the trioxane dimers had potent anticancer activity... - Antitrypanosomal activities of fluoroquinolones with pyrrolidinyl substitutionsElizabeth Nenortas
Departments of Medicine and of Pharmacology and Molecular Sciences, The Johns Hopkins University, Baltimore, Maryland 21205, USA
Antimicrob Agents Chemother 47:3015-7. 2003..These compounds trap protein-DNA complexes and inhibit nucleic acid biosynthesis in trypanosomes, characteristics of topoisomerase II inhibition... - Malaria-infected mice live until at least day 30 after a new monomeric trioxane combined with mefloquine are administered together in a single low oral doseLauren E Woodard
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 52:7458-62. 2009.... - Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activityIk-Hyeon Paik
Department of Chemistry, The Johns Hopkins University, Baltimore, Maryland 21218-2685, USA
J Med Chem 49:2731-4. 2006.... - Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoitesMyaing M Nyunt
Department of Medicine, The Johns Hopkins University School of Medicine, Baltimore, Maryland 21205, USA
Am J Trop Med Hyg 80:528-35. 2009..We conclude that a single dose of 100 mg pafuramidine does not adequately protect non-immune individuals against P. falciparum and shows no clinically or statistically significant evidence of causal prophylactic activity... - Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivoXiaochun Chen
Department of Pharmacology and Molecular Sciences, Johns Hopkins School of Medicine, 725 North Wolfe Street, Baltimore, MD 21205, USA
Chem Biol 16:193-202. 2009..These findings suggest that PfMetAP2 is a viable target, and fumarranol is a promising lead compound for the development of novel antimalarial agents... - Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cellsAndrew S Rosenthal
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, 3400 North Charles Street, Baltimore, Maryland 21218 2685, USA
J Med Chem 52:1198-203. 2009..Both dimers 4c and 4b were potently and selectively cytotoxic toward five cancer cell lines... - New chemical and biological aspects of artemisinin-derived trioxane dimersGary H Posner
Department of Chemistry, School of Arts and Sciences, The Johns Hopkins University, Baltimore, MD 21218, USA
Bioorg Med Chem 10:227-32. 2002..Each dimer was evaluated in vitro for antimalarial, antiproliferative, and antitumor activities; ketone dimers and, more than fluorinated dimers and, are promising for chemotherapy of both malaria and cancer... - An unusual type IB topoisomerase from African trypanosomesAnnette L Bodley
Division of Clinical Pharmacology, Department of Medicine, Johns Hopkins University School of Medicine, Baltimore, MD 21205, USA
Proc Natl Acad Sci U S A 100:7539-44. 2003..It also provides another basis for the design of selectively toxic drug candidates... - Antimalarial chemotherapeutic peroxides: artemisinin, yingzhaosu A and related compoundsKristina Borstnik
Department of Chemistry, The Johns Hopkins University, 3400 North Charles Street, Baltimore, MD 21218-2685, USA
Int J Parasitol 32:1661-7. 2002..This review summarises recent achievements in this area of peroxide drug development for malaria chemotherapy... - A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxidesMario D Bachi
Department of Organic Chemistry, The Weizmann Institute of Science, Rehovot 76100, Israel
J Med Chem 46:2516-33. 2003..NS. In view of the nontoxicity of beta-sulfonyl peroxides 39a, 46a, and 46b in mice, at high dosing, these compounds are regarded as promising antimalarial drug candidates...
Research Grants
- TOPOISOMERASE II--TARGET FOR ANT-TRYPANOSOMAL THERAPYTheresa Shapiro; Fiscal Year: 1993..It is hoped that they will also provide a rational basis for much-needed new anti-trypanosomal chemotherapy...
- CLINICAL PHARMACOLOGY TRAINING PROGRAMTheresa Shapiro; Fiscal Year: 2007..Graduates from this program will have the skills and knowledge to undertake an independent career that features research in both basic and clinical pharmacology. ..
- Topoisomerases: Target for Antitrypanosomal TherapyTheresa Shapiro; Fiscal Year: 2006..Compounds that appear most promising will be evaluated in mice. These studies take a multi-faceted, rational, and tangible approach to the development of much-needed new anti-trypanosomal chemotherapy. ..
- TOPOISOMERASES--TARGET FOR ANTITRYPANOSOMAL THERAPYTheresa Shapiro; Fiscal Year: 2002..Inhibitors that appear most promising will be evaluated in mice. This work will increase our understanding of these critical enzymes in trypanosomal metabolism, and it offers some hope for the development of much-needed new therapy. ..