Theresa Shapiro

Summary

Affiliation: Johns Hopkins University
Country: USA

Publications

  1. ncbi request reprint Chemoprotective glucosinolates and isothiocyanates of broccoli sprouts: metabolism and excretion in humans
    T 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
  2. pmc Activity of indenoisoquinolines against African trypanosomes
    Rahul 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
  3. doi request reprint A mitochondrial topoisomerase IA essential for late theta structure resolution in African trypanosomes
    Jane 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
  4. ncbi request reprint Distinct genes encode type II Topoisomerases for the nucleus and mitochondrion in the protozoan parasite Trypanosoma brucei
    Tomasz 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
  5. ncbi request reprint Molecular mechanisms of resistance in antimalarial chemotherapy: the unmet challenge
    Ravit 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
  6. pmc Newly identified antibacterial compounds are topoisomerase poisons in African trypanosomes
    Sonya 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
  7. doi request reprint Malaria-infected mice are cured by oral administration of new artemisinin derivatives
    Gary 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
  8. ncbi request reprint Orally active, water-soluble antimalarial 3-aryltrioxanes: short synthesis and preclinical efficacy testing in rodents
    Gary 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
  9. ncbi request reprint Malaria-infected mice are cured by a single dose of novel artemisinin derivatives
    Gary 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
  10. ncbi request reprint Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy
    Gary 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

Research Grants

  1. TOPOISOMERASE II--TARGET FOR ANT-TRYPANOSOMAL THERAPY
    Theresa Shapiro; Fiscal Year: 1993
  2. CLINICAL PHARMACOLOGY TRAINING PROGRAM
    Theresa Shapiro; Fiscal Year: 2007
  3. Topoisomerases: Target for Antitrypanosomal Therapy
    Theresa Shapiro; Fiscal Year: 2006
  4. TOPOISOMERASES--TARGET FOR ANTITRYPANOSOMAL THERAPY
    Theresa Shapiro; Fiscal Year: 2002

Collaborators

Detail Information

Publications22

  1. ncbi request reprint Chemoprotective glucosinolates and isothiocyanates of broccoli sprouts: metabolism and excretion in humans
    T 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...
  2. pmc Activity of indenoisoquinolines against African trypanosomes
    Rahul 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...
  3. doi request reprint A mitochondrial topoisomerase IA essential for late theta structure resolution in African trypanosomes
    Jane 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...
  4. ncbi request reprint Distinct genes encode type II Topoisomerases for the nucleus and mitochondrion in the protozoan parasite Trypanosoma brucei
    Tomasz 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
    ....
  5. ncbi request reprint Molecular mechanisms of resistance in antimalarial chemotherapy: the unmet challenge
    Ravit 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...
  6. pmc Newly identified antibacterial compounds are topoisomerase poisons in African trypanosomes
    Sonya 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...
  7. doi request reprint Malaria-infected mice are cured by oral administration of new artemisinin derivatives
    Gary 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...
  8. ncbi request reprint Orally active, water-soluble antimalarial 3-aryltrioxanes: short synthesis and preclinical efficacy testing in rodents
    Gary 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...
  9. ncbi request reprint Malaria-infected mice are cured by a single dose of novel artemisinin derivatives
    Gary 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...
  10. ncbi request reprint Orally active, antimalarial, anticancer, artemisinin-derived trioxane dimers with high stability and efficacy
    Gary 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
    ....
  11. ncbi request reprint RNA interference of Trypanosoma brucei topoisomerase IB: both subunits are essential
    Rahul 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...
  12. ncbi request reprint Anticancer and antimalarial efficacy and safety of artemisinin-derived trioxane dimers in rodents
    Gary 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...
  13. pmc Antitrypanosomal activities of fluoroquinolones with pyrrolidinyl substitutions
    Elizabeth 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...
  14. pmc 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 dose
    Lauren 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
    ....
  15. ncbi request reprint Second generation, orally active, antimalarial, artemisinin-derived trioxane dimers with high stability, efficacy, and anticancer activity
    Ik Hyeon Paik
    Department of Chemistry, The Johns Hopkins University, Baltimore, Maryland 21218 2685, USA
    J Med Chem 49:2731-4. 2006
    ....
  16. pmc Phase I/II evaluation of the prophylactic antimalarial activity of pafuramidine in healthy volunteers challenged with Plasmodium falciparum sporozoites
    Myaing 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...
  17. doi request reprint Fumagillin and fumarranol interact with P. falciparum methionine aminopeptidase 2 and inhibit malaria parasite growth in vitro and in vivo
    Xiaochun 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...
  18. pmc Malaria-infected mice are cured by a single oral dose of new dimeric trioxane sulfones which are also selectively and powerfully cytotoxic to cancer cells
    Andrew 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...
  19. ncbi request reprint New chemical and biological aspects of artemisinin-derived trioxane dimers
    Gary 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...
  20. pmc An unusual type IB topoisomerase from African trypanosomes
    Annette 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...
  21. ncbi request reprint Antimalarial chemotherapeutic peroxides: artemisinin, yingzhaosu A and related compounds
    Kristina 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...
  22. ncbi request reprint A short synthesis and biological evaluation of potent and nontoxic antimalarial bridged bicyclic beta-sulfonyl-endoperoxides
    Mario 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 Grants17

  1. TOPOISOMERASE II--TARGET FOR ANT-TRYPANOSOMAL THERAPY
    Theresa Shapiro; Fiscal Year: 1993
    ..It is hoped that they will also provide a rational basis for much-needed new anti-trypanosomal chemotherapy...
  2. CLINICAL PHARMACOLOGY TRAINING PROGRAM
    Theresa 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. ..
  3. Topoisomerases: Target for Antitrypanosomal Therapy
    Theresa 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. ..
  4. TOPOISOMERASES--TARGET FOR ANTITRYPANOSOMAL THERAPY
    Theresa 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. ..