Rakesh Kumar

Summary

Affiliation: University of Alberta
Country: Canada

Publications

  1. ncbi request reprint Synthesis and antiviral activity of novel 5-(1-cyanamido-2-haloethyl) and 5-(1-hydroxy(or methoxy)-2-azidoethyl) analogues of uracil nucleosides
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, AB, Canada T6G 2H7
    J Med Chem 44:3531-8. 2001
  2. ncbi request reprint 5-(1-Substituted) alkyl pyrimidine nucleosides as antiviral (herpes) agents
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Curr Med Chem 11:2749-66. 2004
  3. ncbi request reprint Novel treatment options for hepatitis B virus infection
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, T6G 2H7, Canada
    Curr Opin Investig Drugs 5:171-8. 2004
  4. ncbi request reprint Synthesis and enzymatic transformations of 5-halo-6-methoxy-5,6-dihydro derivatives of 5-[1-methoxy-2-halo (or 2,2-dihalo)ethyl]-2'-deoxyuridines as potential herpes simplex virus inhibitors
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Alta, T6G 2H7 Canada
    J Enzyme Inhib Med Chem 18:273-8. 2003
  5. ncbi request reprint Design and synthesis of novel 5-substituted acyclic pyrimidine nucleosides as potent and selective inhibitors of hepatitis B virus
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Alberta, Canada T6G 2H7
    J Med Chem 45:2032-40. 2002
  6. ncbi request reprint Synthesis and biological investigations of 5-substituted pyrimidine nucleosides coupled to a dihydropyridine/pyridinium salt redox chemical delivery system
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton T6G 2H7, AB, Canada
    Arch Pharm (Weinheim) 334:351-6. 2001
  7. ncbi request reprint Novel 5-vinyl pyrimidine nucleosides with potent anti-hepatitis B virus activity
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Canada T6G 2H7
    Bioorg Med Chem Lett 11:2917-20. 2001
  8. ncbi request reprint Effect of various pyrimidines possessing the 1-[(2-hydroxy-1-(hydroxymethyl)ethoxy)methyl] moiety, able to mimic natural 2'-deoxyribose, on wild-type and mutant hepatitis B virus replication
    Rakesh Kumar
    Department of Laboratory Medicine and Pathology, 1 41 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    J Med Chem 49:3693-700. 2006
  9. ncbi request reprint Synthesis and antiviral activity of novel acyclic nucleoside analogues of 5-(1-azido-2-haloethyl)uracils
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton T6G 2H7, Canada
    J Med Chem 44:4225-9. 2001
  10. ncbi request reprint 5-Bromo (or chloro)-6-azido-5,6-dihydro-2' -deoxyuridine and -thymidine derivatives with potent antiviral activity
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Canada T6G 2H7
    Bioorg Med Chem Lett 12:275-8. 2002

Collaborators

Detail Information

Publications92

  1. ncbi request reprint Synthesis and antiviral activity of novel 5-(1-cyanamido-2-haloethyl) and 5-(1-hydroxy(or methoxy)-2-azidoethyl) analogues of uracil nucleosides
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, AB, Canada T6G 2H7
    J Med Chem 44:3531-8. 2001
    ..6-6.6 microM). All compounds investigated exhibited low host cell toxicity to several stationary and proliferating host cell lines as well as mitogen-stimulated proliferating human T lymphocytes...
  2. ncbi request reprint 5-(1-Substituted) alkyl pyrimidine nucleosides as antiviral (herpes) agents
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Curr Med Chem 11:2749-66. 2004
    ..In this article the work on design, synthesis and structure activity relationships of several 5-[(1-substituted) alkyl (or vinyl)] pyrimidine nucleoside derivatives as potential inhibitors of herpes viruses is reviewed...
  3. ncbi request reprint Novel treatment options for hepatitis B virus infection
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, T6G 2H7, Canada
    Curr Opin Investig Drugs 5:171-8. 2004
    ....
  4. ncbi request reprint Synthesis and enzymatic transformations of 5-halo-6-methoxy-5,6-dihydro derivatives of 5-[1-methoxy-2-halo (or 2,2-dihalo)ethyl]-2'-deoxyuridines as potential herpes simplex virus inhibitors
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Alta, T6G 2H7 Canada
    J Enzyme Inhib Med Chem 18:273-8. 2003
    ..The compounds (3-12) themselves were found to be non-inhibitory against herpes simplex virus type-1 (HSV-1), likely due in part to their inability to undergo conversion to parent compounds in cell culture medium...
  5. ncbi request reprint Design and synthesis of novel 5-substituted acyclic pyrimidine nucleosides as potent and selective inhibitors of hepatitis B virus
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Alberta, Canada T6G 2H7
    J Med Chem 45:2032-40. 2002
    ..All of the compounds investigated did not show any detectable toxicity to several stationary and proliferating host cell lines or to mitogen stimulated proliferating human T lymphocytes, up to the highest concentration tested...
  6. ncbi request reprint Synthesis and biological investigations of 5-substituted pyrimidine nucleosides coupled to a dihydropyridine/pyridinium salt redox chemical delivery system
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton T6G 2H7, AB, Canada
    Arch Pharm (Weinheim) 334:351-6. 2001
    ....
  7. ncbi request reprint Novel 5-vinyl pyrimidine nucleosides with potent anti-hepatitis B virus activity
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Canada T6G 2H7
    Bioorg Med Chem Lett 11:2917-20. 2001
    ..Compounds 6 and 7 were potent inhibitors of DHBV in cell culture, in contrast, all of the compounds described were devoid of activity against TK(+) HSV-1 and TK(-) HSV-1...
  8. ncbi request reprint Effect of various pyrimidines possessing the 1-[(2-hydroxy-1-(hydroxymethyl)ethoxy)methyl] moiety, able to mimic natural 2'-deoxyribose, on wild-type and mutant hepatitis B virus replication
    Rakesh Kumar
    Department of Laboratory Medicine and Pathology, 1 41 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    J Med Chem 49:3693-700. 2006
    ....
  9. ncbi request reprint Synthesis and antiviral activity of novel acyclic nucleoside analogues of 5-(1-azido-2-haloethyl)uracils
    R Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton T6G 2H7, Canada
    J Med Chem 44:4225-9. 2001
    ..31-1.55 microM) and HCMV (EC(50) = 3.1 microM). None of the compounds investigated showed any detectable toxicity to several stationary and proliferating host cells...
  10. ncbi request reprint 5-Bromo (or chloro)-6-azido-5,6-dihydro-2' -deoxyuridine and -thymidine derivatives with potent antiviral activity
    Rakesh Kumar
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Canada T6G 2H7
    Bioorg Med Chem Lett 12:275-8. 2002
    ..Compounds 4 and 5 exhibited a broad spectrum of antiherpes activity against (HSV-1, HSV-2, HCMV, and VZV)...
  11. doi request reprint Antiviral activity of various 1-(2'-deoxy-β-D-lyxofuranosyl), 1-(2'-fluoro-β-D-xylofuranosyl), 1-(3'-fluoro-β-D-arabinofuranosyl), and 2'-fluoro-2',3'-didehydro-2',3'-dideoxyribose pyrimidine nucleoside analogues against duck hepatitis B virus (DHBV) and
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, Dentistry, University of Alberta, Edmonton, Alberta, Canada T6G 2H7
    J Med Chem 53:7156-66. 2010
    ..1 μM. In contrast, 50% inhibition could not be achieved by lamivudine at 44 μM concentration in the drug-resistant strain. The compounds investigated did not show cytotoxicity to host cells up to the highest concentrations tested...
  12. doi request reprint Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors
    Neeraj Shakya
    Department of Laboratory Medicine and Pathology, 7 28 Heritage Medical Research Centre, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem 20:4088-97. 2012
    ..No cellular toxicity of 13 or 21 was observed up to the highest concentration tested (CC(50)>100 μg/mL). These observations offer promise for a new drug treatment regimen to augment and complement the current chemotherapy of TB...
  13. doi request reprint Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada
    J Med Chem 53:6180-7. 2010
    ..These data indicated that there is a significant potential in this class of compounds...
  14. ncbi request reprint Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides
    Dinesh Rai
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, University of Alberta, Edmonton, AB, T6G 2H7, Canada
    J Med Chem 50:4766-74. 2007
    ..bovis and M. tuberculosis, and M. avium, respectively...
  15. ncbi request reprint Inhibition of hepatitis B virus (HBV) replication by pyrimidines bearing an acyclic moiety: effect on wild-type and mutant HBV
    Wassila Semaine
    Department of Laboratory Medicine and Pathology, 1 41 Medical Sciences Building, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada
    J Med Chem 49:2049-54. 2006
    ..We herein report the capability of acyclic pyrimidine nucleosides to inhibit the replication of both wild-type and drug-resistant mutant HBV...
  16. ncbi request reprint Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs
    Monika Johar
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    J Med Chem 50:3696-705. 2007
    ..tuberculosis H37Rv at similar concentrations. Some of these analogs also revealed in vitro antimicrobial effect against several other gram-positive pathogens...
  17. ncbi request reprint Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria
    Dinesh Rai
    Department of Laboratory Medicine and Pathology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta T6G 2H7, Canada
    J Med Chem 48:7012-7. 2005
    ..The investigated nucleosides are recognized here for the first time to be potent inhibitors of mycobacteria. This class of compounds could be of interest for lead optimization as antimycobacterial agents...
  18. doi request reprint A new class of pyrimidine nucleosides: inhibitors of hepatitis B and C viruses
    Neeraj Shakya
    Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, AB, Canada
    Bioorg Med Chem Lett 22:6475-80. 2012
    ..The activity exhibited by a single agent towards both hepatitis viruses and no detectable in vitro cytotoxicity make this new class of compounds of interest...
  19. doi request reprint In vitro activation and differentiation of naïve CD4+ and CD8+ T cells into HCV core- and NS3-specific armed effector cells: a new role for CD4+ T cells
    Deepa K Krishnadas
    Department of Surgery, University of Alberta, Edmonton, Alta T6G 2S2, Canada
    Cell Immunol 259:141-9. 2009
    ..This is the first study demonstrating the activation of GrB+CD4+ T cells against antigen(s) derived from HCV. Our study suggests a novel role of CD4+ T cells in immunity against HCV...
  20. doi request reprint HCV-core and NS3 antigens play disparate role in inducing regulatory or effector T cells in vivo: Implications for viral persistence or clearance
    Deepa K Krishnadas
    Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada
    Vaccine 28:2104-14. 2010
    ....
  21. doi request reprint Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem Lett 22:1091-4. 2012
    ..Among these compounds, 3'-azido-5-ethyl-2',3'-dideoxyuridine (3) was found to have significant antimycobacterial activities against M. bovis (MIC(50)=1μg/mL), M. tuberculosis (MIC(50)=10μg/mL) and M. avium (MIC(50)=10μg/mL)...
  22. doi request reprint 3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis
    Neeraj Shakya
    Department of Laboratory Medicine and Pathology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada
    J Med Chem 53:4130-40. 2010
    ..Overall, these encouraging results substantiate the potential of this new class of compounds as promising antituberculosis agents...
  23. ncbi request reprint Studies on acyclic pyrimidines as inhibitors of mycobacteria
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 41 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem 15:2045-53. 2007
    ....
  24. doi request reprint Synthesis and in vitro antiviral activities of 3'-fluoro (or chloro) and 2',3'-difluoro 2',3'-dideoxynucleoside analogs against hepatitis B and C viruses
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem 18:7542-7. 2010
    ..The 5-hydroxymethyl-3'-fluoro-2',3'-dideoxyuridine (4) and 1-(3-chloro-2,3-dideoxy-β-d-erythro-pentofuranosyl)-5-fluorouracil (19) provided the most inhibition of both viruses without cytotoxicity...
  25. doi request reprint Immunomodulation by hepatitis C virus-derived proteins: targeting human dendritic cells by multiple mechanisms
    Deepa K Krishnadas
    Department of Surgery, University of Alberta, Heritage Medical Research Centre, Edmonton, Canada
    Int Immunol 22:491-502. 2010
    ..These studies delineate important mechanisms by which initial DC dysfunction can establish contributing to chronicity. Our data are in agreement with earlier observations that DCs are impaired in HCV infected people...
  26. doi request reprint Antiviral activity of 2,3'-anhydro and related pyrimidine nucleosides against hepatitis B virus
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem Lett 20:6790-3. 2010
    ..The nucleoside 18 also demonstrated significant anti-HBV activity against DHBV with an EC(50) value of 2.5 μg/mL, however, it was less active against HBV in 2.2.15 cells (EC(50) = > 10 μg/mL)...
  27. doi request reprint Immunization with Recombinant Adenoviral Vectors Expressing HCV Core or F Proteins Leads to T Cells with Reduced Effector Molecules Granzyme B and IFN-γ: A Potential New Strategy for Immune Evasion in HCV Infection
    Subodh Kumar Samrat
    1 Department of Surgery, University of Alberta, Edmonton, Canada
    Viral Immunol 28:309-24. 2015
    ..These studies are important in the investigation of prophylactic vaccine and immunotherapy strategies for HCV infection...
  28. pmc Heterologous Immunity between Adenoviruses and Hepatitis C Virus: A New Paradigm in HCV Immunity and Vaccines
    Shakti Singh
    Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada
    PLoS ONE 11:e0146404. 2016
    ..This intrinsic property of adenovirus vectors to cross-prime HCV immunity can also be exploited to develop a prophylactic and/or therapeutic vaccine against HCV. ..
  29. doi request reprint Recombinant adenoviral vector expressing HCV NS4 induces protective immune responses in a mouse model of Vaccinia-HCV virus infection: a dose and route conundrum
    Shakti Singh
    Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada
    Vaccine 32:2712-21. 2014
    ..Our results demonstrate that recombinant adenovirus vector can induce both humoral and cellular protective immunity against HCV-NS4 antigen, and that immunity is intricately controlled by route and dose of immunizing vector. ..
  30. ncbi request reprint In vitro anti-mycobacterial activities of various 2'-deoxyuridine, 2'-arabinouridine and 2'-arabinofluoro-2'-deoxyuridine analogues: synthesis and biological studies
    Naveen C Srivastav
    Department of Laboratory Medicine and Pathology, University of Alberta, Edmonton, Canada
    Med Chem 2:287-93. 2006
    ..avium (MIC50 = 1-10 microg/mL range); 5-(1-azidovinyl)-2'-deoxyuridine being the most active (MIC50 = 1-5 microg/mL range). The nature of C-5 substituents appeared to be a determinant of anti-mycobacterial activity...
  31. doi request reprint Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents
    Saurabh Garg
    Department of Laboratory Medicine and Pathology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB T6G 2H7, Canada
    Bioorg Med Chem 24:5521-5533. 2016
    ..No in vitro cytotoxicity of the test compounds was observed up to the highest concentration tested (CC50>300μg/mL)...
  32. doi request reprint 4'-Substituted pyrimidine nucleosides lacking 5'-hydroxyl function as potential anti-HCV agents
    Neeraj Shakya
    Department of Laboratory Medicine and Pathology, 7 28 Heritage Medical Research Centre, University of Alberta, Edmonton, AB T6G 2S2, Canada
    Bioorg Med Chem Lett 24:1407-9. 2014
    ..9 μM). Further, the most active analog, 12, was found to interact synergistically with ribavirin to inhibit HCV RNA replication...
  33. ncbi request reprint Synthesis and in vitro anti-mycobacterial activity of 5-substituted pyrimidine nucleosides
    Monika Johar
    Department of Laboratory Medicine and Pathology, 1 71 Medical Sciences Building, University of Alberta, Edmonton, AB, Canada T6G 2H7
    Bioorg Med Chem 13:6663-71. 2005
    ..This new class of inhibitors could serve as useful compounds for the design and study of new anti-tuberculosis agents...
  34. doi request reprint Novel lipopeptides of ESAT-6 induce strong protective immunity against Mycobacterium tuberculosis: Routes of immunization and TLR agonists critically impact vaccine's efficacy
    Nancy Gupta
    Department of Laboratory Medicine and Pathology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB, Canada
    Vaccine 34:5677-5688. 2016
    ..These findings demonstrate the promise of synthetic lipopeptides as the basis of a subunit vaccine for TB...
  35. doi request reprint Co-incubation with core proteins of HBV and HCV leads to modulation of human dendritic cells
    Amogh Agrawal
    1 Department of Medical Microbiology and Immunology, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Canada
    Viral Immunol 27:412-7. 2014
    ..These results reveal an important mechanism by which HBV and HCV synergistically induce immune tolerance early in infection that may be instrumental in establishing chronic, persistent infections...
  36. ncbi request reprint Evaluation of 5-[1-(2-halo(or nitro)ethoxy-2-iodoethyl)]-2'-deoxyuridines as inhibitors of herpes simplex virus
    Dinesh Rai
    Department of Medical Microbiology and Immunology, Faculty of Medicine, University of Alberta, Edmonton, Canada T6G 2H7
    J Enzyme Inhib Med Chem 18:41-5. 2003
    ..The compounds 3-10 were either weak or non-inhibitory to HSV-1 replication. All compounds investigated exhibited low host cell cytotoxicity...
  37. pmc Chemotherapeutic interventions against tuberculosis
    Neeraj Shakya
    Department of Laboratory Medicine and Pathology, 728 Heritage Medical Research Center, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB T6G 2S2, Canada
    Pharmaceuticals (Basel) 5:690-718. 2012
    ..This review article presents an account of the existing chemotherapeutics and highlights the therapeutic potential of emerging molecules that are at different stages of development for the management of tuberculosis disease. ..
  38. pmc Alternate reading frame protein (F protein) of hepatitis C virus: paradoxical effects of activation and apoptosis on human dendritic cells lead to stimulation of T cells
    Subodh Kumar Samrat
    Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta, Canada
    PLoS ONE 9:e86567. 2014
    ..Taken together, our findings suggest important aspects of F protein in modulating DC function and stimulating T cell responses in humans. ..
  39. ncbi request reprint Priming and stimulation of hepatitis C virus-specific CD4+ and CD8+ T cells against HCV antigens NS4, NS5a or NS5b from HCV-naive individuals: implications for prophylactic vaccine
    Wen Li
    Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, Alberta T6G 2S2, Canada
    Int Immunol 20:89-104. 2008
    ..These studies have significant implications in designing vaccines for HCV infection in both prophylactic and therapeutic settings...
  40. pmc Symbiotic chemo- and immuno-therapy for hepatitis B and C viruses
    Babita Agrawal
    Babita Agrawal, Department of Surgery, Faculty of Medicine and Dentistry, University of Alberta, Edmonton, AB T6G 2R3, Canada
    World J Gastroenterol 22:5623-6. 2016
    ..Moreover, a synergy of, chemo- and immuno-therapeutic strategies will be necessary to eradicate HBV or HCV from a host. ..
  41. pmc Filamin A regulates focal adhesion disassembly and suppresses breast cancer cell migration and invasion
    Yingjie Xu
    Lady Davis Institute for Medical Research, Jewish General Hospital, Faculty of Medicine, McGill University, Montreal, Quebec H3T 1E2, Canada
    J Exp Med 207:2421-37. 2010
    ..These results document a regulation of FA dynamics by FLNa in breast cancer cells...
  42. ncbi request reprint Comparison of the interaction of uridine, cytidine, and other pyrimidine nucleoside analogues with recombinant human equilibrative nucleoside transporter 2 (hENT2) produced in Saccharomyces cerevisiae
    Mark F Vickers
    Department of Oncology, University of Alberta, Cross Cancer Institute, Edmonton, Canada
    Biochem Cell Biol 80:639-44. 2002
    ..hENT2 displayed a lower ability, compared with hENT1, to interact with cytidine and cytidine analogues, suggesting a low tolerance for the presence of the amino group at the 4 position of the base...
  43. ncbi request reprint Suppression of epidermal growth factor receptor, mitogen-activated protein kinase, and Pak1 pathways and invasiveness of human cutaneous squamous cancer cells by the tyrosine kinase inhibitor ZD1839 (Iressa)
    Christopher J Barnes
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Mol Cancer Ther 2:345-51. 2003
    ....
  44. ncbi request reprint Cell cycle-dependent phosphorylation of the RUNX2 transcription factor by cdc2 regulates endothelial cell proliferation
    Meng Qiao
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, MD 21201, USA
    J Biol Chem 281:7118-28. 2006
    ....
  45. ncbi request reprint Higher efficacy of sequential therapy with interferon-alpha and lamivudine combination compared to lamivudine monotherapy in HBeAg positive chronic hepatitis B patients
    Shiv Kumar Sarin
    Department of Gastroenterology, G B Pant Hospital, Affiliated to the University of Delhi, India
    Am J Gastroenterol 100:2463-71. 2005
    ..A sequential combination may have better therapeutic effects by sustained viral suppression combined with immunomodulation...
  46. ncbi request reprint Insulin-like growth factor receptor as a therapeutic target in head and neck cancer
    Christopher J Barnes
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 13:4291-9. 2007
    ..The present study was undertaken to determine the effects of anti-IGF-IR therapeutic targeting on cell signaling and cancer cell phenotypes in squamous cell carcinomas of the head and neck (SCCHN)...
  47. pmc Metastasis-associated protein 1 interacts with NRIF3, an estrogen-inducible nuclear receptor coregulator
    Amjad H Talukder
    Departments of Molecular and Cellular Oncology, University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Mol Cell Biol 24:6581-91. 2004
    ..These findings suggest that NRIF3, an MTA1-interacting protein, is an estrogen-inducible gene and that regulatory interactions between MTA1 and NRIF3 might be important in modulating the sensitivity of breast cancer cells to estrogen...
  48. ncbi request reprint The role of adapter protein Shc in estrogen non-genomic action
    Zhenguo Zhang
    Department of Internal Medicine, University of Virginia School of Medicine, Charlottesville, VA 22903, USA
    Steroids 69:523-9. 2004
    ..In this review, the role of Shc in mediating estrogen effects on MAP Kinase regulation, cell growth and anti-apoptosis will be discussed. The possible role of PI3-kinase in estrogen rapid action is also reviewed in brief...
  49. ncbi request reprint Insulin-like growth factor-1 regulates endogenous RUNX2 activity in endothelial cells through a phosphatidylinositol 3-kinase/ERK-dependent and Akt-independent signaling pathway
    Meng Qiao
    Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, USA
    J Biol Chem 279:42709-18. 2004
    ..These results indicate that the angiogenic growth factor, IGF-1, can regulate RUNX2 DNA binding through sequential activation of the PI3K/Pak1 and ERK1/2 signaling cascade...
  50. pmc The HER4/4ICD estrogen receptor coactivator and BH3-only protein is an effector of tamoxifen-induced apoptosis
    Anjali Naresh
    Department of Molecular and Cellular Biology, Tulane University Health Sciences Center, New Orleans, Louisiana
    Cancer Res 68:6387-95. 2008
    ....
  51. doi request reprint Characterization of an Akt kinase inhibitor with potent pharmacodynamic and antitumor activity
    Nelson Rhodes
    Oncology Biology, GlaxoSmithKline, Collegeville, PA 19426, USA
    Cancer Res 68:2366-74. 2008
    ..Immunohistochemical analysis of tumor xenografts after repeat dosing with GSK690693 showed reductions in phosphorylated Akt substrates in vivo. These results support further evaluation of GSK690693 as an anticancer agent...
  52. ncbi request reprint PET in anti-cancer drug development and therapy
    Rakesh Kumar
    Department of Nuclear Medicine, All India Institute of Medical Sciences, New Delhi 110029, India
    Recent Pat Anticancer Drug Discov 2:259-63. 2007
    ..In addition, PET-CT improves characterization of equivocal lesions and decreases interobserver variability. The most important recent patents concerning role of PET in drug development have been presented...
  53. pmc The effect of anti-VEGF therapy on immature myeloid cell and dendritic cells in cancer patients
    Takuya Osada
    Duke University Medical Center, Box 3233, Durham, NC 27710, USA
    Cancer Immunol Immunother 57:1115-24. 2008
    ..These data suggest that DC differentiation is negatively associated with VEGF levels and may be one explanation for impaired anticancer immunity, especially in patients with advanced malignancies...
  54. ncbi request reprint Dynein light chain 1, a p21-activated kinase 1-interacting substrate, promotes cancerous phenotypes
    Ratna K Vadlamudi
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    Cancer Cell 5:575-85. 2004
    ..DLC1 protein level is elevated in more than 90% of human breast tumors. The regulation of cell survival functions by Pak1-DLC1 interaction represents a novel mechanism by which a signaling kinase might regulate the cancerous phenotypes...
  55. ncbi request reprint Estrogen receptor activation at serine 305 is sufficient to upregulate cyclin D1 in breast cancer cells
    Seetharaman Balasenthil
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, 1515 Holcombe Boulevard, Houston, TX 77030, USA
    FEBS Lett 567:243-7. 2004
    ....
  56. ncbi request reprint Human epidermal growth factor receptor 2 status modulates subcellular localization of and interaction with estrogen receptor alpha in breast cancer cells
    Zhibo Yang
    Department of Molecular and Cellular Oncology, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 10:3621-8. 2004
    ..ER hormone responsiveness is widely believed to be influenced by enhanced cross-talk of ER with overexpressed human epidermal growth factor receptor 2 (HER2), and a subgroup of ER-positive tumors coexpress high HER2...
  57. ncbi request reprint Adaptive hypersensitivity to estrogen: mechanism for sequential responses to hormonal therapy in breast cancer
    Richard J Santen
    Department of Medicine, University of Virginia Health Sciences System, Charlottesville, Virginia, USA
    Clin Cancer Res 10:337S-45S. 2004
    ....
  58. ncbi request reprint p21-activated kinase-1 signaling mediates cyclin D1 expression in mammary epithelial and cancer cells
    Seetharaman Balasenthil
    Department of Molecular and Cellular Oncology, University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 279:1422-8. 2004
    ....
  59. ncbi request reprint HER2 regulation of peroxisome proliferator-activated receptor gamma (PPARgamma) expression and sensitivity of breast cancer cells to PPARgamma ligand therapy
    Zhibo Yang
    Department of Molecular, Breast Medical Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 9:3198-203. 2003
    ..In summary, these findings show for the first time that HER2 up-regulates PPARgamma expression and modulates the sensitivity of breast cancer cells to PPARgamma ligand therapy...
  60. ncbi request reprint GW654652, the pan-inhibitor of VEGF receptors, blocks the growth and migration of multiple myeloma cells in the bone marrow microenvironment
    Klaus Podar
    Department of Medical Oncology, Jerome Lipper Multiple Myeloma Center, Harvard Medical School, Boston, MA 02115, USA
    Blood 103:3474-9. 2004
    ....
  61. ncbi request reprint Antihuman epidermal growth factor receptor 2 antibody herceptin inhibits autocrine motility factor (AMF) expression and potentiates antitumor effects of AMF inhibitors
    Amjad H Talukder
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 8:3285-9. 2002
    ..Accordingly, the combination of AMF inhibitor with HCT can potentiate the growth-inhibitory and anti-invasive action of HCT in breast cancer cells...
  62. ncbi request reprint Expression and transactivating functions of the bZIP transcription factor GADD153 in mammary epithelial cells
    Amjad H Talukder
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas, TX 77030, USA
    Oncogene 21:4289-300. 2002
    ....
  63. ncbi request reprint The epidermal growth factor receptor tyrosine kinase inhibitor ZD1839 (Iressa) suppresses c-Src and Pak1 pathways and invasiveness of human cancer cells
    Zhibo Yang
    Department of Molecular and Cellular Oncology, The University of Texas, M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 10:658-67. 2004
    ....
  64. ncbi request reprint Metastatic tumor antigen 1 short form (MTA1s) associates with casein kinase I-gamma2, an estrogen-responsive kinase
    Sandip K Mishra
    Department of Molecular and Cellular Oncology, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA
    Oncogene 23:4422-9. 2004
    ....
  65. pmc MicroRNA-7, a homeobox D10 target, inhibits p21-activated kinase 1 and regulates its functions
    Sirigiri Divijendra Natha Reddy
    Department of Molecular and Cellular Oncology, The University of Texas MD Anderson Cancer Center, Baylor College of Medicine, Houston, Texas 77030, USA
    Cancer Res 68:8195-200. 2008
    ....
  66. ncbi request reprint Delivery of cytoplasmic proteins to autophagosomes
    Kazufumi Ohshiro
    Molecular and Cellular Oncology, The University of Texas MD Anderson Cancer Center, Houston, Texas 77030, USA
    Autophagy 4:104-6. 2008
    ....
  67. ncbi request reprint Solution structure and antiestrogenic activity of the unique C-terminal, NR-box motif-containing region of MTA1s
    Rajesh R Singh
    Department of Molecular and Cellular Oncology and Experimental Therapeutics, University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 281:25612-21. 2006
    ..In brief, the characterization of structure and antiestrogenic activity of MTA1s peptide highlight its therapeutic potential...
  68. ncbi request reprint Growth factor regulation of a 26S proteasomal subunit in breast cancer
    Christopher J Barnes
    Department of Molecular and Cellular Oncology, University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Clin Cancer Res 11:2868-74. 2005
    ..We sought to gain insight into the mechanisms of heregulin-beta1 (HRG) action on breast epithelial cells by identifying and characterizing HRG-regulated proteins...
  69. ncbi request reprint Essential role of KIBRA in co-activator function of dynein light chain 1 in mammalian cells
    Suresh K Rayala
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    J Biol Chem 281:19092-9. 2006
    ..Together these findings indicate that DLC1-KIBRA interaction is essential for ER transactivation in breast cancer cells...
  70. pmc Metastasis-associated protein 2 is a repressor of estrogen receptor alpha whose overexpression leads to estrogen-independent growth of human breast cancer cells
    Yukun Cui
    Department of Medicine, Baylor College of Medicine, One Baylor Plaza, BCM 600, Houston, Texas 77030, USA
    Mol Endocrinol 20:2020-35. 2006
    ..We hypothesize that MTA2 is a repressor of ERalpha activity and that it could represent a new therapeutic target of ERalpha action in human breast tumors...
  71. ncbi request reprint Design, synthesis and evaluation of carbazole derivatives as PPAR alpha/gamma dual agonists and antioxidants
    Rakesh Kumar
    Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S A S Nagar 160 062, India
    Bioorg Med Chem 13:4279-90. 2005
    ..While most compounds showed good antioxidant activity, some compounds were identified as potential PPAR alpha/gamma dual agonists as well. Compounds 10a and 16 were found to be active in animal studies...
  72. ncbi request reprint Commentary: targeting colorectal cancer through molecular biology
    Rakesh Kumar
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, 77030, USA
    Semin Oncol 32:S37-9. 2005
    ..Optimal therapeutic strategies to inhibit cancer cell motility, invasiveness, and angiogenesis may involve combinations of growth factor receptor inhibitors, COX-2 inhibitors, and urokinase inhibitors...
  73. ncbi request reprint Estrogen and tamoxifen induce cytoskeletal remodeling and migration in endometrial cancer cells
    Filippo Acconcia
    University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Endocrinology 147:1203-12. 2006
    ..This new information may serve as the foundation for the development of new clinical therapeutic strategies...
  74. ncbi request reprint Stage-specific expression of dynein light chain-1 and its interacting kinase, p21-activated kinase-1, in rodent testes: implications in spermiogenesis
    Rui An Wang
    Department of Molecular and Cellular Oncology UT MD Anderson Cancer Center, Houston, TX 77030, USA
    J Histochem Cytochem 53:1235-43. 2005
    ..Further, Pak1 may also play a role in spermiogenesis by regulating DLC1 phosphorylation and, consequently, its function...
  75. ncbi request reprint Marine water quality assessment at Mumbai West Coast
    S S Dhage
    NEERI, Mumbai Zonal Laboratory, 89 B, Dr A B Road, Worli, Mumbai 18, India
    Environ Int 32:149-58. 2006
    ..This paper presents observations of the coastal studies at Mumbai and the impact zone of Worli outfall...
  76. pmc Functional implications of altered subcellular localization of PELP1 in breast cancer cells
    Ratna K Vadlamudi
    Department of Molecular and Cellular Oncology, University of Texas M D Anderson Cancer Center, Houston, Texas 77030, USA
    Cancer Res 65:7724-32. 2005
    ....
  77. pmc Proline-, glutamic acid-, and leucine-rich protein-1 is essential in growth factor regulation of signal transducers and activators of transcription 3 activation
    Bramanandam Manavathi
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas, USA
    Cancer Res 65:5571-7. 2005
    ..Such regulatory interactions of PELP1 may have important functional implications in the cross-talk of estrogen receptor and growth factor signaling...
  78. ncbi request reprint Chronic morphine exposure causes pronounced virus replication in cerebral compartment and accelerated onset of AIDS in SIV/SHIV-infected Indian rhesus macaques
    Rakesh Kumar
    Laboratory of Viral Immunology, AIDS Research Program and Department of Microbiology, Ponce School of Medicine, Ponce, PR 00732, Puerto Rico
    Virology 354:192-206. 2006
    ..Three morphine-exposed macaques (euthanized at weeks 18, 19 and 20) did not develop cellular or humoral immune responses, whereas the other 3 morphine-exposed and 3 control macaques developed both cellular and humoral immune responses...
  79. ncbi request reprint Inhibition of VEGF receptors significantly impairs mammary cancer growth in C3(1)/Tag transgenic mice through antiangiogenic and non-antiangiogenic mechanisms
    Jung im Huh
    Laboratory of Cell Regulation and Carcinogenesis, National Cancer Institute, National Institutes of Health, Bethesda, MD 20892, USA
    Oncogene 24:790-800. 2005
    ....
  80. ncbi request reprint Increased expression of tissue transglutaminase in pancreatic ductal adenocarcinoma and its implications in drug resistance and metastasis
    Amit Verma
    Department of Experimental Therapeutics, The University of Texas M D Anderson Cancer Center, Houston, TX 77030, USA
    Cancer Res 66:10525-33. 2006
    ..These results show for the first time that elevated expression of TG2 can induce constitutive activation of FAK and thus may contribute to the development of drug resistance and invasive phenotypes in PDAC...
  81. ncbi request reprint Higher frequency of Yq microdeletions in sperm DNA as compared to DNA isolated from blood
    Rima Dada
    Laboratory for Molecular Reproduction and Genetics, Anatomy Department, All India Institute of Medical Sciences AIIMS, New Delhi 29, India
    Asian J Androl 9:720-2. 2007
    ..To determine if Yq microdeletion frequency and loci of deletion are similar in two tissues (blood and sperm) of different embryological origin...
  82. ncbi request reprint Potential role of a novel transcriptional coactivator PELP1 in histone H1 displacement in cancer cells
    Sujit S Nair
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, Texas 77030 4009, USA
    Cancer Res 64:6416-23. 2004
    ..Our results provide novel insights about the transcription regulation of PELP1 and suggest that PELP1 participates in chromatin remodeling activity via displacement of histone 1 in cancer cells...
  83. ncbi request reprint Pharmacokinetic-pharmacodynamic correlation from mouse to human with pazopanib, a multikinase angiogenesis inhibitor with potent antitumor and antiangiogenic activity
    Rakesh Kumar
    Oncology Biology, GlaxoSmithKline, 1250 South Collegeville Road, UP1450, Collegeville, PA 19426, USA
    Mol Cancer Ther 6:2012-21. 2007
    ..Furthermore, the steady-state concentration of pazopanib determined from preclinical activity showed a strong correlation with the pharmacodynamic effects and antitumor activity in the phase I clinical trial...
  84. ncbi request reprint 18F-FDG PET for evaluation of the treatment response in patients with gastrointestinal tract lymphomas
    Rakesh Kumar
    Division of Nuclear Medicine, Department of Radiology, Hospital of the University of Pennsylvania, Philadelphia, Pennsylvania 19104, USA
    J Nucl Med 45:1796-803. 2004
    ..This study was undertaken to investigate the usefulness of (18)F-FDG PET in monitoring the response to the treatment of lymphomas in this setting...
  85. ncbi request reprint Design and synthesis of 6-methyl-2-oxo-1,2,3,4-tetrahydro-pyrimidine-5-carboxylic acid derivatives as PPARgamma activators
    Rakesh Kumar
    Department of Pharmaceutical Technology, National Institute of Pharmaceutical Education and Research, Sector 67, S A S Nagar, Punjab 160 062, India
    Bioorg Med Chem Lett 17:4613-8. 2007
    ..The FlexX docking and radioligand binding affinity of some promising compounds of this series is comparable to that of thiazolidinedione based antidiabetic drugs currently in clinical use...
  86. pmc Oncogenic potential of the nuclear receptor coregulator proline-, glutamic acid-, leucine-rich protein 1/modulator of the nongenomic actions of the estrogen receptor
    Rajib Rajhans
    Department of Obstetrics and Gynecology and San Antonio Cancer Institute, University of Texas Health Science Center at San Antonio, San Antonio, Texas 78229 3900, USA
    Cancer Res 67:5505-12. 2007
    ..Our data suggest that PELP1 is a potential oncogene, that its expression is deregulated during cancer progression, and that PELP1 may play a role in oncogenesis...
  87. ncbi request reprint Assessment of therapy response in malignant tumours with 18F-fluorothymidine
    Rakesh Kumar
    Eur J Nucl Med Mol Imaging 34:1334-8. 2007
  88. pmc Deregulation of estrogen receptor coactivator proline-, glutamic acid-, and leucine-rich protein-1/modulator of nongenomic activity of estrogen receptor in human endometrial tumors
    Ratna K Vadlamudi
    Department of Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, USA
    J Clin Endocrinol Metab 89:6130-8. 2004
    ..In addition, PELP1 and ERbeta were localized predominantly in the cytoplasm of high-grade endometrial tumors. Our results suggest that PELP1 plays an essential role in the proliferation of cancerous endometrial cells...
  89. pmc Proline-, glutamic acid-, and leucine-rich protein-1/modulator of nongenomic activity of estrogen receptor enhances androgen receptor functions through LIM-only coactivator, four-and-a-half LIM-only protein 2
    Sujit S Nair
    Department of Obstetrics and Gynecology, University of Texas Health Science Center, Floyd Curl Drive, San Antonio, Texas 78229 3900, USA
    Mol Endocrinol 21:613-24. 2007
    ..Our results suggest that PELP1 functions as a molecular adaptor, coupling FHL2 with nuclear receptors, and PELP1-FHL2 interactions may have a role in prostate cancer progression...
  90. ncbi request reprint An inherent role of integrin-linked kinase-estrogen receptor alpha interaction in cell migration
    Filippo Acconcia
    Departments of Molecular and Cellular Oncology and Molecular Therapeutics, The University of Texas M D Anderson Cancer Center, Houston, TX, USA
    Cancer Res 66:11030-8. 2006
    ..Thus, status of ILK signaling may be an important modifier of ER signaling in breast cancer cells and this pathway could be exploited for therapeutic intervention in breast cancer cells...
  91. ncbi request reprint Ciz1, a Novel DNA-binding coactivator of the estrogen receptor alpha, confers hypersensitivity to estrogen action
    Petra den Hollander
    Molecular and Cellular Oncology, The University of Texas M D Anderson Cancer Center, Houston, TX, USA
    Cancer Res 66:11021-9. 2006
    ..These findings revealed the inherent role of Ciz1, a novel DNA binding and ER coactivator, in amplifying estrogenic responses and promoting breast cancer tumorigenesis...
  92. ncbi request reprint Increased viral replication in simian immunodeficiency virus/simian-HIV-infected macaques with self-administering model of chronic alcohol consumption
    Rakesh Kumar
    Laboratory of Viral Immunology, Department of Microbiology, Ponce School of Medicine, San Juan, PR
    J Acquir Immune Defic Syndr 39:386-90. 2005
    ..The extent of CD4 cell loss in the alcohol group was significantly higher than that in the control animals at week 1 after infection...