Zhude Tu

Summary

Affiliation: Washington University School of Medicine
Country: USA

Publications

  1. pmc Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups
    Zhude Tu
    Department of Radiology, Washington University, St Louis, MO 63110, United States
    Bioorg Med Chem 20:4422-9. 2012
  2. pmc Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain
    Zhude Tu
    Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Bioorg Med Chem 19:1666-73. 2011
  3. pmc Carbon-11 labeled papaverine as a PET tracer for imaging PDE10A: radiosynthesis, in vitro and in vivo evaluation
    Zhude Tu
    Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Nucl Med Biol 37:509-16. 2010
  4. pmc Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Med Chem 52:1358-69. 2009
  5. ncbi request reprint Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Med Chem 50:3194-204. 2007
  6. pmc Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: a positron emission tomography study
    Robert H Mach
    Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, Missouri 63110, USA
    Synapse 65:724-32. 2011
  7. pmc [3H]4-(dimethylamino)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl) butyl)benzamide: a selective radioligand for dopamine D(3) receptors. II. Quantitative analysis of dopamine D(3) and D(2) receptor density ratio in the caudate-putamen
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri 63110, USA
    Synapse 64:449-59. 2010
  8. pmc Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Neuroimage 71:168-74. 2013
  9. ncbi request reprint Synthesis and in vivo evaluation of 2 high-affinity 76Br-labeled sigma2-receptor ligands
    Douglas J Rowland
    Department of Radiology, Washington University in St Louis, Saint Louis, Missouri, USA
    J Nucl Med 47:1041-8. 2006
  10. pmc Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 South Kingshighway Blvd, St Louis, MO 63110, USA
    Appl Radiat Isot 68:2268-73. 2010

Collaborators

Detail Information

Publications34

  1. pmc Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups
    Zhude Tu
    Department of Radiology, Washington University, St Louis, MO 63110, United States
    Bioorg Med Chem 20:4422-9. 2012
    ..2 nM, VAChT/σ(1)=1500, VAChT/σ(2)=2030). These four compounds can be radiosynthesized with C-11 or F-18 to validate their possibilities of serving as PET probes for quantifying the levels of VAChT in vivo...
  2. pmc Radiosynthesis and in vivo evaluation of [11C]MP-10 as a PET probe for imaging PDE10A in rodent and non-human primate brain
    Zhude Tu
    Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Bioorg Med Chem 19:1666-73. 2011
    ..MicroPET studies of [(11)C]MP-10 in monkeys displayed selective uptake in striatum. However, a radiolabeled metabolite capable of penetrating the blood-brain-barrier may limit the clinical utility of [(11)C]MP-10 as a PDE10A PET tracer...
  3. pmc Carbon-11 labeled papaverine as a PET tracer for imaging PDE10A: radiosynthesis, in vitro and in vivo evaluation
    Zhude Tu
    Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Nucl Med Biol 37:509-16. 2010
    ..Analogs of papaverine having a higher potency for inhibiting PDE10A and improved pharmacokinetic properties will be necessary for imaging this enzyme with PET...
  4. pmc Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Med Chem 52:1358-69. 2009
    ..88 at 30 min postinjection (p.i.). MicroPET imaging of macaques demonstrated a 2.1 ratio of (-)-[(18)F]9e in putamen versus cerebellum at 2 h p.i. (-)-[(18)F]9e has potential to be a PET tracer for clinical imaging of the VAChT...
  5. ncbi request reprint Fluorine-18-labeled benzamide analogues for imaging the sigma2 receptor status of solid tumors with positron emission tomography
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
    J Med Chem 50:3194-204. 2007
    ....
  6. pmc Endogenous dopamine (DA) competes with the binding of a radiolabeled D₃ receptor partial agonist in vivo: a positron emission tomography study
    Robert H Mach
    Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, Missouri 63110, USA
    Synapse 65:724-32. 2011
    ..These data indicate that there is a high level of competition between [¹⁸F]5 and endogenous dopamine for D₃ receptors in vivo...
  7. pmc [3H]4-(dimethylamino)-N-(4-(4-(2-methoxyphenyl)piperazin-1-yl) butyl)benzamide: a selective radioligand for dopamine D(3) receptors. II. Quantitative analysis of dopamine D(3) and D(2) receptor density ratio in the caudate-putamen
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, Saint Louis, Missouri 63110, USA
    Synapse 64:449-59. 2010
    ..A mathematical model for calculating the absolute densities of dopamine D(2) and D(3) receptors based on the in vitro receptor binding data of [3H]WC-10 and [3H]raclopride was developed...
  8. pmc Positron emission tomography imaging of dopamine D2 receptors using a highly selective radiolabeled D2 receptor partial agonist
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Neuroimage 71:168-74. 2013
    ..d-Amphetamine challenge studies indicate that there is a significant displacement of [(11)C]SV-III-130 by d-Amphetamine-induced increases in synaptic dopamine levels...
  9. ncbi request reprint Synthesis and in vivo evaluation of 2 high-affinity 76Br-labeled sigma2-receptor ligands
    Douglas J Rowland
    Department of Radiology, Washington University in St Louis, Saint Louis, Missouri, USA
    J Nucl Med 47:1041-8. 2006
    ..These are 5-bromo-N-(4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl)-2,3-dimethoxybenzamide (compound (1)) and 5-bromo-N-(2-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)ethyl)-2-methoxybenzamide (compound (2))...
  10. pmc Radiosynthesis and biological evaluation of a promising sigma(2)-receptor ligand radiolabeled with fluorine-18 or iodine-125 as a PET/SPECT probe for imaging breast cancer
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 South Kingshighway Blvd, St Louis, MO 63110, USA
    Appl Radiat Isot 68:2268-73. 2010
    ....
  11. pmc [(3)H]4-(Dimethylamino)-N-[4-(4-(2-methoxyphenyl)piperazin- 1-yl)butyl]benzamide, a selective radioligand for dopamine D(3) receptors. I. In vitro characterization
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, USA
    Synapse 63:717-28. 2009
    ..In vitro autoradiography studies of rat and monkey brains show that [(3)H]WC-10 labeled D(3) sites in the striatal region...
  12. pmc Effect of cyclosporin A on the uptake of D3-selective PET radiotracers in rat brain
    Zhude Tu
    Department of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Nucl Med Biol 38:725-39. 2011
    ..Four benzamide analogs having a high affinity and selectivity for D(3) versus D(2) receptors were radiolabeled with (11)C or (18)F for in vivo evaluation...
  13. pmc Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter
    Junfeng Li
    Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St Louis, MO 63110, USA
    J Med Chem 56:6216-33. 2013
    ..The data revealed that (-)-[(11)C]24b has highest binding in striatum and has favorable pharmacokinetics in the brain. ..
  14. pmc Synthesis and pharmacological evaluation of fluorine-containing D₃ dopamine receptor ligands
    Zhude Tu
    Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, United States
    J Med Chem 54:1555-64. 2011
    ..17 nM for D(3), 163-fold selectivity for D(3) vs D(2) receptors), represents a candidate fluorine-18 radiotracer for in vivo PET imaging studies on the regulation of D(3) receptor expression...
  15. pmc Binding of the radioligand SIL23 to α-synuclein fibrils in Parkinson disease brain tissue establishes feasibility and screening approaches for developing a Parkinson disease imaging agent
    Devika P Bagchi
    Department of Neurology, Washington University School of Medicine, St Louis, MO, USA
    PLoS ONE 8:e55031. 2013
    ....
  16. pmc Synthesis, radiolabeling and initial in vivo evaluation of [(11)C]KSM-01 for imaging PPAR-α receptors
    Kiran Kumar Solingapuram Sai
    Division of Radiological Sciences, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Bioorg Med Chem Lett 22:6233-6. 2012
    ..5-fold greater radiotracer uptake in the heart of transgenic mice compared to the wild-type littermates. These results demonstrate the potential utility of PPAR-α agonists as PET radiopharmaceuticals...
  17. pmc Synthesis and in vitro biological evaluation of carbonyl group-containing analogues for σ1 receptors
    Wei Wang
    Department of Radiology, Washington University School of Medicine, St Louis, Missouri 63110, United States
    J Med Chem 54:5362-72. 2011
    ..All four of these most promising compounds (14a, 14b, 14c, and 14e) can be radiosynthesized with fluorine-18 or carbon-11, which will allow further evaluation of their properties as PET probes for imaging σ(1) receptor in vivo...
  18. ncbi request reprint Synthesis and characterization of selective dopamine D2 receptor antagonists
    Suwanna Vangveravong
    Division of Radiological Sciences, Washington University School of Medicine, Mallinckrodt Institute of Radiology, St Louis, MO 63110, USA
    Bioorg Med Chem 14:815-25. 2006
    ....
  19. doi request reprint Functional assays to define agonists and antagonists of the sigma-2 receptor
    Chenbo Zeng
    Department of Radiology, Division of Radiological Sciences, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA Electronic address
    Anal Biochem 448:68-74. 2014
    ..The establishment of functional assays for defining sigma-2 agonists and antagonists will facilitate functional characterization of sigma-2 receptor ligands and sigma-2 receptors. ..
  20. pmc Synthesis and evaluation of 15-(4-(2-[¹⁸F]Fluoroethoxy)phenyl)pentadecanoic acid: a potential PET tracer for studying myocardial fatty acid metabolism
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, Missouri 63110, USA
    Bioconjug Chem 21:2313-9. 2010
    ..0030 ± 0.0005 vs 0.0006 ± 0.00013, P < 0.01). These initial studies suggest that [¹⁸F]7 could be a potentially useful clinical PET tracer to assess abnormal myocardial fatty acid metabolism...
  21. pmc Identification of the PGRMC1 protein complex as the putative sigma-2 receptor binding site
    Jinbin Xu
    Division of Radiological Sciences, Department of Radiology, Mail Box 8225, Washington University School of Medicine, 510 S Kingshighway Boulevard, St Louis, Missouri 63110, USA
    Nat Commun 2:380. 2011
    ..The identification of the putative sigma-2 receptor-binding site as PGRMC1 should stimulate the development of unique imaging agents and cancer therapeutics that target the sigma-2 receptor/PGRMC1 complex...
  22. ncbi request reprint [3H]N-[4-(3,4-dihydro-6,7-dimethoxyisoquinolin-2(1H)-yl)butyl]-2-methoxy-5-methylbenzamide: a novel sigma-2 receptor probe
    Jinbin Xu
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Eur J Pharmacol 525:8-17. 2005
    ..The pharmacologic profile of [3H]RHM-1 was in agreement with that of [3H]DTG. The results of this study indicate that [3H]RHM-1 is a useful ligand for studying sigma2 receptors in vitro...
  23. pmc Synthesis and in vitro evaluation of new analogues as inhibitors for phosphodiesterase 10A
    Zhanbin Zhang
    Mallinckrodt Institute of Radiology, Washington University School of Medicine, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Eur J Med Chem 46:3986-95. 2011
    ..To identify high potent PDE10A inhibitor, further optimization of the structures of these analogues is necessary...
  24. pmc Automated radiosynthesis of [11C]morphine for clinical investigation
    Jinda Fan
    Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Blvd St Louis, MO 63110, USA
    Appl Radiat Isot 69:431-5. 2011
    ..Radiosynthesis took 45 min with a radiochemical yield ranging from 45% to 50% and specific activity ranging from 20 to 26 Ci/μmol (decay corrected to end-of-bombardment); radiochemical and chemical purities were >95% (n=28)...
  25. ncbi request reprint Characterization of a novel iodinated sigma-2 receptor ligand as a cell proliferation marker
    Catherine Hou
    Department of Radiology, University of Pennsylvania, Philadelphia, PA 19104, USA
    Nucl Med Biol 33:203-9. 2006
    ..Further modification of the ligand and the imaging parameters will be needed to improve the signal for in vivo detection...
  26. ncbi request reprint Synthesis and in vivo evaluation of [11C]PJ34, a potential radiotracer for imaging the role of PARP-1 in necrosis
    Zhude Tu
    Division of Radiological Sciences, Washington University School of Medicine, St Louis, MO 63110, USA
    Nucl Med Biol 32:437-43. 2005
    ..These data indicate that [(11)C]PJ34 may be a useful radiotracer for imaging tissues undergoing cellular death via necrosis...
  27. ncbi request reprint Carbon-11 labeled sigma2 receptor ligands for imaging breast cancer
    Zhude Tu
    Mallinckrodt Institute of Radiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Nucl Med Biol 32:423-30. 2005
    ..Consequently, [(11)C]2 is a potential radiotracer for imaging the proliferative status of breast tumors in vivo with PET...
  28. pmc Chemical and enzyme-assisted syntheses of norbuprenorphine-3-β-D-glucuronide
    Jinda Fan
    Department of Radiology, Washington University in St Louis, 660 S Euclid Avenue, St Louis, Missouri 63110, United States
    Bioconjug Chem 22:752-8. 2011
    ..The fractional yield of the enzyme-assisted synthesis was greater than that of the chemical synthesis (67% vs 5.3%), but due to larger reaction volumes, the chemical synthesis afforded greater amounts of total 1...
  29. ncbi request reprint N-benzylisatin sulfonamide analogues as potent caspase-3 inhibitors: synthesis, in vitro activity, and molecular modeling studies
    Wenhua Chu
    Division of Radiological Sciences, Washington University School of Medicine, 510 South Kingshighway Boulevard, St Louis, Missouri 63110, USA
    J Med Chem 48:7637-47. 2005
    ....
  30. pmc Synthesis and in vitro evaluation of α-synuclein ligands
    Lihai Yu
    Department of Radiology, Washington University School of Medicine, 510 South Kingshighway Boulevard, St Louis, MO 63110, USA
    Bioorg Med Chem 20:4625-34. 2012
    ..Further optimization of the structure of these analogues may yield compounds with high affinity and selectivity for aggregated α-synuclein...
  31. pmc Quantitative receptor-based imaging of tumor proliferation with the sigma-2 ligand [(18)F]ISO-1
    Kooresh I Shoghi
    Department of Radiology, Washington University School of Medicine, St Louis, Missouri, United States of America Department of Biomedical Engineering, Washington University School of Medicine, St Louis, Missouri, United States of America Division of Biology and Biomedical Sciences, Washington University School of Medicine, St Louis, Missouri, United States of America
    PLoS ONE 8:e74188. 2013
    ..Our data suggest that PET studies of [(18)F]ISO-1 provide a measure of both the proliferative status and tumor growth rate, which would be valuable in designing an appropriate treatment strategy. ..
  32. pmc The novel sigma-2 receptor ligand SW43 stabilizes pancreas cancer progression in combination with gemcitabine
    John R Hornick
    Department of Surgery, Washington University School of Medicine, S, Euclid Avenue, St Louis, MO, USA
    Mol Cancer 9:298. 2010
    ..In this study, we investigated the role of the novel sigma-2 receptor ligand SW43 to induce apoptosis and augment standard chemotherapy...
  33. doi request reprint Preclinical evaluation of the novel monoclonal antibody H6-11 for prostate cancer imaging
    Hongjun Jin
    Department of Radiology, Washington University School of Medicine, 510 S Kingshighway Boulevard, St Louis, Missouri 63110, United States
    Mol Pharm 10:3655-64. 2013
    ..By 120 h postinjection, the tumors were still evident, although the liver showed significant clearance. These studies suggest that the mAb H6-11 may be a useful tool to detect prostate cancer in vitro and in vivo...
  34. ncbi request reprint Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands
    Wenhua Chu
    Department of Radiology, Division of Radiological Sciences, Washington University School of Medicine, Campus Box 8225, 510 S Kingshighway Blvd, St Louis, MO 63110, USA
    Bioorg Med Chem 13:77-87. 2005
    ....