Julie L Eiseman

Summary

Affiliation: University of Pittsburgh
Country: USA

Publications

  1. ncbi request reprint Selective inhibition of MCF-7(piGST) breast tumors using glutathione transferase-derived 2-methylene-cycloalkenones
    Erin Joseph
    Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, Baltimore, MD 21250, USA
    J Med Chem 48:6549-52. 2005
  2. ncbi request reprint Evaluation of plasma insulin-like growth factor binding protein 2 and Her-2 extracellular domain as biomarkers for 17-allylamino-17-demethoxygeldanamycin treatment of adult patients with advanced solid tumors
    Julie L Eiseman
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213 1863, USA
    Clin Cancer Res 13:2121-7. 2007
  3. ncbi request reprint Distribution of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) uracil in mice bearing colorectal cancer xenografts: rationale for therapeutic use and as a positron emission tomography probe for thymidylate synthase
    Julie L Eiseman
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213 1863, USA
    Clin Cancer Res 10:6669-76. 2004
  4. ncbi request reprint Pharmacokinetics and pharmacodynamics of 17-demethoxy 17-[[(2-dimethylamino)ethyl]amino]geldanamycin (17DMAG, NSC 707545) in C.B-17 SCID mice bearing MDA-MB-231 human breast cancer xenografts
    Julie L Eiseman
    Department of Pharmacology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 55:21-32. 2005
  5. doi request reprint Pharmacokinetics and tissue distribution of inositol hexaphosphate in C.B17 SCID mice bearing human breast cancer xenografts
    Julie Eiseman
    Molecular Therapeutics and Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Metabolism 60:1465-74. 2011
  6. pmc Improved synthesis of 6-epi-dictyostatin and antitumor efficacy in mice bearing MDA-MB231 human breast cancer xenografts
    Julie L Eiseman
    Department of Pharmacology and Chemical Biology and University of Pittsburgh Cancer Institute, G 27 b Research Pavilion, Hillman Cancer Center, 5117 Centre Avenue, Pittsburgh, Pennsylvania 15213 1862, USA
    J Med Chem 51:6650-3. 2008
  7. ncbi request reprint Systemic and tumor disposition of platinum after administration of cisplatin or STEALTH liposomal-cisplatin formulations (SPI-077 and SPI-077 B103) in a preclinical tumor model of melanoma
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 53:329-36. 2004
  8. pmc Plasma pharmacokinetics and oral bioavailability of 3,4,5,6-tetrahydrouridine, a cytidine deaminase inhibitor, in mice
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 62:457-64. 2008
  9. ncbi request reprint Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284)
    Jianxia Guo
    Departments of Pharmacology, University of Pittsburgh Cancer Institute, University of Pittsburgh, Pittsburgh, PA, 15261, USA
    Anticancer Res 27:3067-73. 2007
  10. ncbi request reprint Tumor, tissue, and plasma pharmacokinetic studies and antitumor response studies of docetaxel in combination with 9-nitrocamptothecin in mice bearing SKOV-3 human ovarian xenografts
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 62:417-26. 2008

Collaborators

Detail Information

Publications43

  1. ncbi request reprint Selective inhibition of MCF-7(piGST) breast tumors using glutathione transferase-derived 2-methylene-cycloalkenones
    Erin Joseph
    Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, Baltimore, MD 21250, USA
    J Med Chem 48:6549-52. 2005
    ..The COMCs are a potentially important new class of prodrugs, which can specifically target multi-drug-resistant tumors overexpressing hGSTP1-1...
  2. ncbi request reprint Evaluation of plasma insulin-like growth factor binding protein 2 and Her-2 extracellular domain as biomarkers for 17-allylamino-17-demethoxygeldanamycin treatment of adult patients with advanced solid tumors
    Julie L Eiseman
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213 1863, USA
    Clin Cancer Res 13:2121-7. 2007
    ..Pretreatment plasma samples were also obtained from 12 healthy volunteers. Plasma IGFBP-2 and Her-2 ECD concentrations were quantitated by ELISA...
  3. ncbi request reprint Distribution of 1-(2-deoxy-2-fluoro-beta-D-arabinofuranosyl) uracil in mice bearing colorectal cancer xenografts: rationale for therapeutic use and as a positron emission tomography probe for thymidylate synthase
    Julie L Eiseman
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213 1863, USA
    Clin Cancer Res 10:6669-76. 2004
    ..These studies were designed to evaluate FAU as a potential therapeutic and diagnostic probe...
  4. ncbi request reprint Pharmacokinetics and pharmacodynamics of 17-demethoxy 17-[[(2-dimethylamino)ethyl]amino]geldanamycin (17DMAG, NSC 707545) in C.B-17 SCID mice bearing MDA-MB-231 human breast cancer xenografts
    Julie L Eiseman
    Department of Pharmacology, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 55:21-32. 2005
    ..v. delivery to mice; and (2) correlated tumor and normal tissue 17DMAG concentrations with alterations in heat shock protein 90 (HSP90) and selected HSP90-chaperoned proteins...
  5. doi request reprint Pharmacokinetics and tissue distribution of inositol hexaphosphate in C.B17 SCID mice bearing human breast cancer xenografts
    Julie Eiseman
    Molecular Therapeutics and Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Metabolism 60:1465-74. 2011
    ..After both IV and PO administration, exogenous IP(6) was rapidly dephosphorylated to inositol; however, alterations in endogenous IPs were not examined...
  6. pmc Improved synthesis of 6-epi-dictyostatin and antitumor efficacy in mice bearing MDA-MB231 human breast cancer xenografts
    Julie L Eiseman
    Department of Pharmacology and Chemical Biology and University of Pittsburgh Cancer Institute, G 27 b Research Pavilion, Hillman Cancer Center, 5117 Centre Avenue, Pittsburgh, Pennsylvania 15213 1862, USA
    J Med Chem 51:6650-3. 2008
    ..Here we describe a new total synthesis that produced more than 30 mg of 6- epi-dictyostatin. The compound was found to have potent antitumor activity in SCID mice bearing MDA-MB231 human breast cancer xenografts...
  7. ncbi request reprint Systemic and tumor disposition of platinum after administration of cisplatin or STEALTH liposomal-cisplatin formulations (SPI-077 and SPI-077 B103) in a preclinical tumor model of melanoma
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 53:329-36. 2004
    ..Thus, we evaluated the disposition of encapsulated and released Pt in plasma and tumors after administration of STEALTH liposomal and nonliposomal cisplatin...
  8. pmc Plasma pharmacokinetics and oral bioavailability of 3,4,5,6-tetrahydrouridine, a cytidine deaminase inhibitor, in mice
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 62:457-64. 2008
    ..This suggests the feasibility of using THU to decrease elimination and first-pass metabolism of cytidine analogues by CD. THU pharmacokinetics are now being evaluated in humans...
  9. ncbi request reprint Pharmacology and antitumor activity of a quinolinedione Cdc25 phosphatase inhibitor DA3003-1 (NSC 663284)
    Jianxia Guo
    Departments of Pharmacology, University of Pittsburgh Cancer Institute, University of Pittsburgh, Pittsburgh, PA, 15261, USA
    Anticancer Res 27:3067-73. 2007
    ..These studies suggest that the minimal antitumor activity of DA3003-1 in mice may be due to its rapid metabolism...
  10. ncbi request reprint Tumor, tissue, and plasma pharmacokinetic studies and antitumor response studies of docetaxel in combination with 9-nitrocamptothecin in mice bearing SKOV-3 human ovarian xenografts
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 62:417-26. 2008
    ....
  11. pmc Efficacy, pharmacokinetics, tisssue distribution, and metabolism of the Myc-Max disruptor, 10058-F4 [Z,E]-5-[4-ethylbenzylidine]-2-thioxothiazolidin-4-one, in mice
    Jianxia Guo
    Hillman Cancer Center, The University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 63:615-25. 2009
    ..In vitro studies indicate the thioxothiazolidinone, 10058-F4, inhibits c-Myc/Max dimerization. In this study, we report the efficacy, pharmacokinetics and metabolism of this novel protein-protein disruptor in mice...
  12. ncbi request reprint Relationship between plasma exposure of 9-nitrocamptothecin and its 9-aminocamptothecin metabolite and antitumor response in mice bearing human colon carcinoma xenografts
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pennsylvania 15213 1863, USA
    Clin Cancer Res 11:4867-74. 2005
    ..These results suggest that the intermittent schedule of 9-nitrocamptothecin may be an active regimen in patients with colorectal carcinoma...
  13. pmc Plasma pharmacokinetics and oral bioavailability of the 3,4,5,6-tetrahydrouridine (THU) prodrug, triacetyl-THU (taTHU), in mice
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Hillman Research Pavilion, Room G27D, 5117 Centre Avenue, Pittsburgh, PA 5213 1863, USA
    Cancer Chemother Pharmacol 67:421-30. 2011
    ..Therefore, we characterized THU pharmacokinetics after the administration to mice of the more lipophilic pro-drug triacetyl-THU (taTHU)...
  14. ncbi request reprint A mass balance and disposition study of the DNA methyltransferase inhibitor zebularine (NSC 309132) and three of its metabolites in mice
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, 5117 Centre Avenue, Pittsburgh, PA 15213, USA
    Clin Cancer Res 12:5826-33. 2006
    ..To elucidate the in vivo metabolic fate of zebularine (NSC 309132), a DNA methyltransferase inhibitor proposed for clinical evaluation in the treatment of cancer...
  15. doi request reprint Plasma and tissue disposition of non-liposomal DB-67 and liposomal DB-67 in C.B-17 SCID mice
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA, 15213, USA
    Invest New Drugs 26:399-406. 2008
    ..We evaluated the tissue and plasma disposition of DB-67 lactone and hydroxy acid after administration of non-liposomal (NL) and liposomal (L) DB-67 in severe combined immunodeficient (SCID) mice...
  16. ncbi request reprint Plasma, tumor, and tissue disposition of STEALTH liposomal CKD-602 (S-CKD602) and nonliposomal CKD-602 in mice bearing A375 human melanoma xenografts
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania, USA
    Clin Cancer Res 13:7217-23. 2007
    ..For STEALTH liposomal formulations of anticancer agents to achieve antitumor effects, the active drug must be released into the tumor extracellular fluid (ECF)...
  17. doi request reprint Modulation of gemcitabine (2',2'-difluoro-2'-deoxycytidine) pharmacokinetics, metabolism, and bioavailability in mice by 3,4,5,6-tetrahydrouridine
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Room G 27d, Hillman Research Pavilion, 5117 Centre Avenue, Pittsburgh, PA 15213 1863, USA
    Clin Cancer Res 14:3529-35. 2008
    ..3,4,5,6-Tetrahydrouridine (THU) is a potent CD inhibitor with a 20% oral bioavailability. We investigated the ability of THU to decrease elimination and first-pass effect by CD, thereby enabling oral dosing of dFdC...
  18. ncbi request reprint Phase I and pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin in adult patients with refractory advanced cancers
    Ramesh K Ramanathan
    Division of Hematology Oncology, Department of Medicine, University of Pittsburgh School of Medicine, Pittsburgh, PA 15232, USA
    Clin Cancer Res 13:1769-74. 2007
    ..The primary objective was to establish the dose-limiting toxicity (DLT) and recommended phase II dose of 17-(allylamino)-17-demethoxygeldanamycin (17AAG) given twice a week...
  19. pmc In vitro cytotoxicity, pharmacokinetics, tissue distribution, and metabolism of small-molecule protein kinase D inhibitors, kb-NB142-70 and kb-NB165-09, in mice bearing human cancer xenografts
    Jianxia Guo
    Molecular Therapeutics and Drug Discovery, The University of Pittsburgh Cancer Institute, Hillman Cancer Center, 5117 Centre Ave, Room G27b, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 71:331-44. 2013
    ..Therefore, PKD inhibitors may have therapeutic potential. We evaluated the in vitro cytotoxicity of two PKD inhibitors, kb-NB142-70 and its methoxy analogue, kb-NB165-09, and examined their in vivo efficacy and pharmacokinetics...
  20. ncbi request reprint Noninvasive and nondestructive optical spectroscopic measurement of motexafin gadolinium in mouse tissues: comparison to high-performance liquid chromatography
    Stephen C Kanick
    Department of Chemical Engineering, University of Pittsburgh, School of Engineering, Pittsburgh, PA 15261, USA
    J Photochem Photobiol B 88:90-104. 2007
    ..900 and 1.185, respectively; however, the variability was significant (r(2)=0.477 and 0.269). The clinical utility of the OPS to quantitate MGd concentrations remains to be validated...
  21. pmc In vitro cytotoxicity and in vivo efficacy, pharmacokinetics, and metabolism of 10074-G5, a novel small-molecule inhibitor of c-Myc/Max dimerization
    Dana M Clausen
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania 15213, USA
    J Pharmacol Exp Ther 335:715-27. 2010
    ..Our identification of 10074-G5 metabolites in mice will help design new, more metabolically stable small-molecule inhibitors of c-Myc...
  22. doi request reprint Pharmacokinetic modeling of motexafin gadolinium disposition in mouse tissues using optical pharmacokinetic system measurements
    Stephen C Kanick
    Department of Chemical Engineering, University of Pittsburgh School of Engineering, Pittsburgh, PA 15261, USA
    Photodiagnosis Photodyn Ther 5:276-84. 2008
    ..The PK modeling techniques presented here are extensible to other optically active compounds and, potentially, to the development of patient-specific treatment schedules...
  23. ncbi request reprint Quantitative determination of the cytidine deaminase inhibitor tetrahydrouridine (THU) in mouse plasma by liquid chromatography/electrospray ionization tandem mass spectrometry
    Robert A Parise
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    Rapid Commun Mass Spectrom 21:1991-7. 2007
    ..This assay is currently being used to quantitate THU in ongoing pharmacokinetic studies. In addition, the assay is expected to be a useful tool in any future studies involving co-administration of THU with cytidine analogues...
  24. ncbi request reprint Plasma pharmacokinetics, oral bioavailability, and interspecies scaling of the DNA methyltransferase inhibitor, zebularine
    Julianne L Holleran
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, Pennsylvania, USA
    Clin Cancer Res 11:3862-8. 2005
    ..Zebularine is a DNA methyltransferase inhibitor proposed for clinical evaluation...
  25. ncbi request reprint Inter- and intratumoral disposition of platinum in solid tumors after administration of cisplatin
    William C Zamboni
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, Pennsylvania 15213, USA
    Clin Cancer Res 8:2992-9. 2002
    ..There was no relationship between Factor VIII expression and Pt exposure in tumors. The variable penetration of Pt from plasma into tumor ECF may be associated with variable response of tumors...
  26. ncbi request reprint Control-relevant modeling of the antitumor effects of 9-nitrocamptothecin in SCID mice bearing HT29 human colon xenografts
    John M Harrold
    Department of Chemical and Petroleum Engineering, University of Pittsburgh School of Engineering, Pittsburgh, PA 15261, USA
    J Pharmacokinet Pharmacodyn 32:65-83. 2005
    ..This methodology could then be used to aid the clinician in selecting dose levels and schedules, and extension to patient tailored treatment may eventually be feasible with this approach...
  27. ncbi request reprint Phase I pharmacokinetic-pharmacodynamic study of 17-(allylamino)-17-demethoxygeldanamycin (17AAG, NSC 330507), a novel inhibitor of heat shock protein 90, in patients with refractory advanced cancers
    Ramesh K Ramanathan
    Molecular Therapeutics Drug Discovery Program, Biostatistics Department, Graduate School of Public Health, and Biostatistics Facility, University of Pittsburgh Cancer Institute, PA 15232, USA
    Clin Cancer Res 11:3385-91. 2005
    ..We did a phase I study of 17AAG to establish the dose-limiting toxicity and maximum tolerated dose and to characterize 17AAG pharmacokinetics and pharmacodynamics...
  28. ncbi request reprint Quantitative determination of zebularine (NSC 309132), a DNA methyltransferase inhibitor, and three metabolites in murine plasma by high-performance liquid chromatography coupled with on-line radioactivity detection
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    J Chromatogr B Analyt Technol Biomed Life Sci 831:147-55. 2006
    ..5-50 microg/mL for uridine, 1.0-10 microg/mL for uracil and 0.5-5.0 microg/mL for dihydrouracil. This assay is being used to quantitate zebularine and its metabolites in ongoing pharmacokinetic studies of zebularine...
  29. ncbi request reprint Pharmacokinetics, metabolism, and oral bioavailability of the DNA methyltransferase inhibitor 5-fluoro-2'-deoxycytidine in mice
    Jan H Beumer
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, PA 15213 1863, USA
    Clin Cancer Res 12:7483-91. 2006
    ..However, the full effects of THU on FdCyd metabolism and pharmacokinetics are unknown. We aimed to characterize the pharmacokinetics, metabolism, and bioavailability of FdCyd with and without THU in mice...
  30. pmc Liquid chromatography-tandem mass spectrometric assay for the quantitation in human plasma of the novel indenoisoquinoline topoisomerase I inhibitors, NSC 743400 and NSC 725776
    Julianne L Holleran
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, 5117 Centre Avenue, Pittsburgh, PA 15213, USA
    J Pharm Biomed Anal 52:714-20. 2010
    ..Protein binding in human plasma as assessed by equilibrium dialysis showed both indenoisoquinolines to be more than 98% protein bound...
  31. ncbi request reprint Phase I and pharmacokinetic study of the novel redox-active agent, motexafin gadolinium, with concurrent radiation therapy in patients with locally advanced pancreatic or biliary cancers
    Ramesh K Ramanathan
    Division of Hematology Oncology, Department of Medicine, University of Pittsburgh School of Medicine, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 57:465-74. 2006
    ..The pharmacokinetics of MGd were also evaluated...
  32. doi request reprint Nonlinear model predictive control for dosing daily anticancer agents using a novel saturating-rate cell-cycle model
    Jeffry A Florian
    Department of Chemical and Petroleum Engineering, University of Pittsburgh School of Engineering, Pittsburgh, PA, USA
    Comput Biol Med 38:339-47. 2008
    ..Overall, the NMPC algorithm is suitable for dosing chemotherapeutics with regular administration schedules and may be adapted for regularly administered chemotherapeutics other than tamoxifen...
  33. ncbi request reprint Pharmacokinetics, tissue distribution, and metabolism of 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (NSC 707545) in CD2F1 mice and Fischer 344 rats
    Merrill J Egorin
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, PA 15213, USA
    Cancer Chemother Pharmacol 49:7-19. 2002
    ..p. and oral delivery; (3) characterize the biliary excretion of 17DMAG after i.v. delivery to rats; and (4) characterize, if possible, any metabolites of 17DMAG observed in plasma, tissue, urine, or bile...
  34. pmc Formation of active products of benzaldehyde dimethane sulfonate (NSC 281612, DMS612) in human blood and plasma and their activity against renal cell carcinoma lines
    Robert A Parise
    Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15213, USA
    Cancer Chemother Pharmacol 71:73-83. 2013
    ..The information gained from these experiments will be instrumental in the evaluation of the pharmacology of BEN in ongoing human trials...
  35. doi request reprint The relationship of phthalocyanine 4 (pc 4) concentrations measured noninvasively to outcome of pc 4 photodynamic therapy in mice
    Lihua Bai
    Department of Pharmacology and Chemical Biology, University of Pittsburgh School of Medicine, Pittsburgh, PA, USA
    Photochem Photobiol 85:1011-9. 2009
    ..86). In excised tumors, OPS-measured Pc 4 concentrations were similar to the HPLC-measured concentrations. Thus, OPS measurements of photosensitizer concentrations can be used to assist in the scheduling of Pc 4-PDT...
  36. ncbi request reprint In vitro metabolism of the phosphatidylinositol 3-kinase inhibitor, wortmannin, by carbonyl reductase
    Julianne L Holleran
    University of Pittsburgh Cancer Institute, Room G27E, Hillman Research Pavilion, 5117 Centre Avenue, Pittsburgh, PA 15213 1863
    Drug Metab Dispos 32:490-6. 2004
    ..Metabolism of wortmannin to 17-OH-wortmannin has mechanistic, and possibly toxicologic, implications because 17-OH-wortmannin is 10-fold more potent an inhibitor of phosphatidylinositol 3-kinase than is wortmannin...
  37. pmc Liquid chromatography-mass spectrometric assay for quantitation of the short-chain fatty acid, 2,2-dimethylbutyrate (NSC 741804), in rat plasma
    Robert A Parise
    Molecular Therapeutics Drug Discovery Program, University of Pittsburgh Cancer Institute, Pittsburgh, PA 15213, USA
    J Chromatogr B Analyt Technol Biomed Life Sci 862:168-74. 2008
    ..The assay was accurate (97-107%) and precise (3.4-6.2%) between 100 and 10,000ng/mL. Recovery from plasma was >62%. Plasma freeze-thaw and room temperature stability were acceptable...
  38. pmc Inducible silencing of protein kinase D3 inhibits secretion of tumor-promoting factors in prostate cancer
    Courtney R LaValle
    Department of Pharmacology and Chemical Biology, University of Pittsburgh, Pittsburgh, Pennsylvania 15261, USA
    Mol Cancer Ther 11:1389-99. 2012
    ..These data validate PKD3 as a promising therapeutic target in prostate cancer and shed light on the role of secreted tumor-promoting factors in prostate cancer progression...
  39. ncbi request reprint Preclinical toxicity of a geldanamycin analog, 17-(dimethylaminoethylamino)-17-demethoxygeldanamycin (17-DMAG), in rats and dogs: potential clinical relevance
    Elizabeth R Glaze
    Toxicology and Pharmacology Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute, Executive Plaza North, Room 8040, Rockville, MD 20852, USA
    Cancer Chemother Pharmacol 56:637-47. 2005
    ..In addition, 17-DMAG undergoes only limited metabolism compared to 17-AAG. The present results are from preclinical toxicity studies evaluating 17-DMAG in rats and dogs...
  40. ncbi request reprint N-(2-hydroxypropyl)methacrylamide copolymers of a glutathione (GSH)-activated glyoxalase i inhibitor and DNA alkylating agent: synthesis, reaction kinetics with GSH, and in vitro antitumor activities
    Zhe Bin Zheng
    Department of Chemistry and Biochemistry, University of Maryland, Baltimore, Maryland 21250, USA
    Bioconjug Chem 16:598-607. 2005
    ..This prodrug strategy should be applicable to a range of different GSH-based antitumor agents...
  41. ncbi request reprint Biliary excretion of 17-(allylamino)-17-demethoxygeldanamycin (NSC 330507) and metabolites by Fischer 344 rats
    Steven M Musser
    Instrumentation and Biophysics Branch, Center for Food Safety and Applied Nutrition, Food and Drug Administration, College Park, MD 20740, USA
    Cancer Chemother Pharmacol 52:139-46. 2003
    ..Studies were performed to define the biliary excretion of 17AAG after i.v. delivery to rats, and to characterize the metabolites of 17AAG observed in rat bile...
  42. ncbi request reprint Physiologically-based pharmacokinetics and molecular pharmacodynamics of 17-(allylamino)-17-demethoxygeldanamycin and its active metabolite in tumor-bearing mice
    Lu Xu
    Department of Biomedical Engineering, University of Southern California, University Park, Los Angeles, CA 90089, USA
    J Pharmacokinet Pharmacodyn 30:185-219. 2003
    ..In modeling pharmacokmetics and pharmacodynamics, Bayesian inference was employed to estimate the kinetic, physiological and molecular parameters when prior information was available...
  43. ncbi request reprint Molecular basis of the antitumor activities of 2-crotonyloxymethyl-2-cycloalkenones
    Erin Joseph
    Department of Chemistry and Biochemistry, University of Maryland, Baltimore County, Baltimore, Maryland 21250, USA
    J Med Chem 46:194-6. 2003
    ..041 microM) and its five- and seven-membered ring homologues. Antitumor activity probably results from a reactive intermediate that forms during conjugation of the COMCs with intracellular GSH...