Four new sesquiterpene lactones (3, 4, 6 and 7) and three known compounds, purpuride (1), berkedrimane B (2) and purpuride B (5), were isolated from the marine fungus, Talaromyces minioluteus (Penicillium minioluteum). New compounds were drimane sesquiterpenes conjugated with N-acetyl-l-valine, and their structures were elucidated by analysis of spectroscopic data, as well as by single crystal X-ray analysis. The isolated compounds could not inhibit the apoptosis-regulating enzyme, caspase-3, while three of the compounds (2, 3 and 7) exhibited weak cytotoxic activity.
P rostate cancer is the most commonly diagnosed cancer in men worldwide. Among men in the United State, prostate cancer is the third leading cause of death from malignancy. 1 According to American Cancer Society, about 1 man in 7 will be diagnosed with prostate cancer during his lifetime. 2 Prostate cancer develops mainly in older men. About 6 cases in 10 are diagnosed in men aged 65 or older, and it is rare before age 40. The average age at the time of diagnosis is about 66. Prostate cancer has high cure rate when detected early. Molecular Imaging technologies dramatically improve prostate cancer diagnosis and treatment. Although FDG is the most widely use PET tracer, using FDG for PET/CT imaging in prostate cancer is limited because a large fraction of prostate cancer shows limited FDG uptake. 3 In the past decade, alternative tracers for prostate cancer imaging are radiolabeled choline derivative such as 18 F-fluorocholine and 11 C-choline. They are used as PET tracers for staging and restaging of prostate cancer. 4 According to a meta-analyses report, in primary nodal imaging the specificity is as high as 95% but the sensitivity is very poor (49%). 5 Due to the lack of sensitive imaging for prostate cancer, more research has been focused on the development of new tracers that have better sensitivity and specificity. In recent years, targeting the prostate specific membrane antigen (PSMA) with 68 Ga-labeled and 18 F-labeled PET tracers has gained highest clinical impact. PSMA ligands PSMA is a type II transmembrane glycoprotein that is significantly (100-fold to 1000-fold) overexpressed in nearly all prostatic cancer cells compared with normal prostatic cells. 6-9 The level of PSMA expression rises with an increase in tumor grade, pathological stage and biochemical recurrence. PSMA PET/CT had a significant impact on the management of prostate cancer. A cohort study reported that radiotherapy management was changed for 50.8% when using 68 Ga-PSMA-11 PET/CT for radiotherapy planning. 10
Table of contentsOP03 Selective extraction of medically-related radionuclides from proton-irradiated thorium targetsV. Radchenko, J.W. Engle, C. Roy, J. Griswold, M.F. Nortier, E.R. Birnbaum, M. Brugh, S. Mirzadeh, K. D. John, M.E. FassbenderOP04 Comparison of [68Ga]FSC(succ-RGD)3 and [68Ga]NODAGA-RGD for PET imaging of αvβ3 integrin expressionChuangyan Zhai, Gerben M. Franssen, Milos Petrik, Peter Laverman, Clemens DecristoforoOP05 A new NPY-Y1R targeting peptide for breast cancer PET imagingAit-Mohand Samia, Dumulon-Perreault Véronique, Guérin BrigitteOP06 The influence of multivalency on CCK 2 receptor targetingD. Summer, A. Kroess, C. Rangger, H. Haas, P. Laverman, F. Gerben, E. von Guggenberg, C.DecristoforoOP07 SPECT Imaging of αvβ3 Expression by [99mTc(N)PNP43]- Bifunctional Chimeric RGD Peptide not Cross-Reacting with αvβ5Cristina Bolzati, Nicola Salvarese, Fiorenzo Refosco, Laura Meléndez-Alafort, Debora Carpanese, Antonio Rosato, Michele Saviano, Annarita Del Gatto, Daniela Comegna, Laura ZaccaroOP09 New dienophiles for the inverse-electron-demand Diels-Alder reaction and for pretargeted PET imagingEmilie Billaud, Muneer Ahamed, Frederik Cleeren, Elnaz Shahbazali, Tim Noël, Volker Hessel, Alfons Verbruggen and Guy BormansOP10 New complexing agent for Al18F-labelling of heat-sensitive biomolecules: Synthesis and preclinical evaluation of Al18F-RESCA1-HASCleeren F, Lecina J, Koole M, Verbruggen A and Bormans GOP11 A novel versatile precursor efficient for F-18 radiolabelling via click-chemistryB. Lugatoa, S. Stucchia, E.A. Turollaa, L. Giulianoa, S.Toddea, P. FerraboschibOP12 A general applicable method to quantify unidentified UV impurities in radiopharmaceuticalsR.P. Klok, M.P.J. Mooijer, N.H. Hendrikse, A.D. WindhorstOP13 Development of [18F]Fluoro-C-glycosides to radiolabel peptidesCollet C., Petry N., Chrétien F., Karcher G., Pellegrini-Moïse N., Lamandé-Langle S.OP14 A Microfluidic Approach for the 68Ga-labeling of PSMAHBED-CC and NODAGA-RGDSarah Pfaff, Cecile Philippe, Markus Mitterhauser, Marcus Hacker, Wolfgang WadsakOP16 Surprising reactivity of astatine in the nucleophilic substitution of aryliodonium salts: application to the radiolabeling of antibodiesFrançois Guérard, Yong-Sok Lee, Sébastien Gouard, Kwamena Baidoo, Cyrille Alliot, Michel Chérel, Martin W. Brechbiel, Jean-François GestinOP17 64Cu-NOTA-pertuzumab F(ab')2 fragments, a second-generation probe for PET imaging of the response of HER2-positive breast cancer to trastuzumab (Herceptin)Lam K, Chan C, Reilly RMOP18 Development of radiohalogenated analogues of a avb6-specific peptide for high LET particle emitter targeted radionuclide therapy of cancerSalomé Paillas, John Marshall, Jean-Pierre Pouget, Jane SosabowskiOP19 Ligand Specific Efficiency (LSE) as a guide in tracer optimizationEmmanuelle Briard, Yves P. Auberson, John Reilly, Mark Healy, David SykesOP23 The radiosynthesis of an 18F-labeled triglyceride, developed to visualize and quantify brown adipose tissue activityAndreas Paulus, Wouter van Marken Lichtenbelt,Felix Mottaghy,...
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