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Preparation, Characterization, and Radiolabeling of Anti‐HER2 scFv With Technetium Tricarbonyl and Stability Studies J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-03-15 Negar Bozorgchami, Maryam Ahmadzadeh, Dara Hatamabadi, Abdolreza Yazdani, Soraya Shahhosseini, Elham Mohit
Breast cancer is the most common diagnosed cancer, and the second cause of cancer death among women, worldwide. HER2 overexpression occurred in approximately 15% to 20% of breast cancers. Invasive biopsy method has been used for detection of HER2 overexpression. HER2‐targeted imaging via an appropriate radionuclide is a promising method for sensitive and accurate identification of HER2+ primary and
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Synthesis of Stable Isotope, Tritiated, and Carbon‐14 Labeled Balcinrenone J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-03-05 Jonas Bergare, Christopher Bailey, Henrik Sörensen, Gunnar Grönberg, Karl Broberg, Monica Berglund, Tudor Grecu, Carolina Sanchez, Hans Emtenäs, Ryan A. Bragg, Charles S. Elmore
As part of a medicinal chemistry program aimed at discovering a mineralocorticoid receptor modulator for treatment of kidney and cardiovascular indications, multiple labeled versions of the lead compound, balcinrenone (AZD9977), were prepared. Four stable isotope labeled versions of the compound were prepared for clinical bioanalysis and biological investigations. Three of these stable isotope labeled
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-03-04
No abstract is available for this article.
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Automated radiosynthesis of mGluR5 PET tracer [18F]FPEB from aryl-chloro precursor and validation for clinical application J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-02-19 Mahabuba Jahan, Arsalan Amir, Arindam Das, Jacob Kihlström, Sangram Nag
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Formulation of patient dose of [177Lu]Lu-Trastuzumab using in-house developed freeze-dried kit: A path forward for clinical translation J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-02-11 Jeyachitra Amirdhanayagam, Mohini Guleria, Rohit Sharma, Naveen Kumar, Archana Mukherjee, Tapas Das
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Tritium and deuterium labelling of a kainate receptor antagonist and evaluation as a radioligand J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-02-08 Paulina Chałupnik, Aleš Marek, Marie Emilie Leiticia Hovah, Darryl S. Pickering, Piero Temperini, Stephanie Donbosco, Ewa Szymańska, Tommy N. Johansen
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-02-12
No abstract is available for this article.
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Automated radiolabeling and handling of 177Lu- and 225Ac-PSMA-617 using a robotic pipettor J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-31 Shin Hye Ahn, Anthony P. Belanger
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Synthesis of [3H]Org24598 using in-house prepared [3H]MeI J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-14 Michal Kriegelstein, Gabriela Nováková, Aleš Marek
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-14
No abstract is available for this article.
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18F-Fluorination of a supported 2-(aryl-di-tert-butylsilyl)-N-methyl-imidazole for indirect 18F-labeling of a VHH single-variable domain J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-15 Marine Steffann, Guillaume Bluet, Sébastien Roy, Catherine Aubert, Eric Fouquet, Philippe Hermange
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Preparation of [1′-13C]citric acid as a probe in a breath test to evaluate tricarboxylic acid cycle flux J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-03 Hidemichi Mitome, Mieko Takenishi, Kumiko Ono, Naoyuki Kawagoe, Tsunehiko Imai, Yosuke Sasaki, Yoshihisa Urita, Kazuki Akira
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A facile synthesis of precursor for the σ-1 receptor PET radioligand [18F]FTC-146 and its radiofluorination J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2024-01-03 Anna Marešová, Michal Jurášek, Pavel B. Drašar, Bohumil Dolenský, Elena A. Prokudina, Vladimir Shalgunov, Matthias M. Herth, Paul Cumming, Alexander Popkov
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Open-source flow setup for rapid and efficient [18F]fluoride drying for automation of PET tracer syntheses J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-28 Florian Menzel, Jonathan Cotton, Thomas Ziegler, Andreas Maurer, Jochen M. Neumaier
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Development of radiotracers for riboflavin transporter 3 imaging in diseases—A brief overview J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-22 Jindian Li, Xianzhong Zhang
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Validation of a good manufacturing practice procedure for the production of [11C]AZD4747, a CNS penetrant KRASG12c inhibitor J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-20 Miguel A. Cortés González, Antonia A. Högnäsbacka, Christer Halldin, Magnus Schou
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Automated radiosynthesis of [18F]CETO, a PET radiotracer for imaging adrenal glands, on Synthra RNplus J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-20 Matthew Hird, Joseph J. Russell, Lei Li Corrigan, Istvan Boros, Patrik Nordeman, Gunnar Antoni, Mark Gurnell, Franklin I. Aigbirhio
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[11C]CO2 BOP fixation with amines to access 11C-labeled ureas for PET imaging J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-10 Coralie M. Bonnemaire, Albert D. Windhorst, Romano Orru, Eelco Ruijter, Danielle J. Vugts
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14C-radiolabeling of a new steroidal antiandrogen with a C-18 angular methyl extension J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-08 Jean-Yves Sancéau
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-07
No abstract is available for this article.
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Synthesis and spectroscopic characterization of 13C4-labeled 4-cyano-2-oxobutyraldehyde semicarbazone: A metabolite of nitrofurazone J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-12-03 Anuradha Singh, David J. Smith, Gary D. Strahan, Steven J. Lehotay
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Synthesis of trifold-labeled versatile reagent [3,5-13C2,4-15 N]4-phenyl-1,2,4-triazoline-3,5-dione J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-20 Frederic Bourgeois, Ulrich Höller, Thomas Netscher
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Novel synthesis of 11C-labeled imidazolines via Pd(0)-mediated 11C-carbomethoxylation using [11C]CO and arylborons J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-13 Hideki Ishii, Katsuyuki Minegishi, Kotaro Nagatsu, Nobuki Nengaki, Ming-Rong Zhang
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-14
No abstract is available for this article.
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Facile synthesis of 14C-nitrofurazone from 14C-urea J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-08 Anuradha Singh, David J. Smith
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Photocatalyzed radiosynthesis of 11C-phenylacetic acids J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-08 Maxime Munch, Braeden A. Mair, Myriam Adi, Benjamin H. Rotstein
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Preparation and evaluation of radiolabeled acetaminosalol microspheres: A new potential selective radiotracer for ulcerative colitis early diagnosis J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-07 O. A. El-Kawy, H. A. Shweeta, M. R. Abdelgawad
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A simplified protocol for the automated production of 2-[18F]fluoro-3-[2-((S)-3-pyrrolinyl)methoxy]pyridine ([18F]nifene) on an IBA Synthera® module J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-11-05 Mohammed Bhuiyan, Jeffrey Souris, Anna Kucharski, Richard Freifelder, Jogeshwar Mukherjee, Chin-Tu Chen
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Site-specifically radiolabeled nanobodies for imaging blood-brain barrier penetration and targeting in the brain J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-10-24 Yingbo Li, Junfeng Wang
Nanobodies (Nbs) hold significant potential in molecular imaging due to their unique characteristics. However, there are challenges to overcome when it comes to brain imaging. To address these obstacles, collaborative efforts and interdisciplinary research are needed. This article aims to raise awareness and encourage collaboration among researchers from various fields to find solutions for effective
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Synthesis and preclinical evaluation of a selective MET kinase positron emission tomography tracer J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-10-22 Vegard Torp Lien, Emily Hauge, Syed Nuruddin, Jo Klaveness, Dag Erlend Olberg
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-10-03
No abstract is available for this article.
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Total synthesis of [13C2]-labeled phytosiderophores of the mugineic and avenic acid families J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-26 Nicolas Kratena, Markus Draskovits, Nina Biedermann, Eva Oburger, Christian Stanetty
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A practical protocol for large-scale copper-mediated radioiodination of organoboronic precursors: Radiosynthesis of [123I]KX-1 for Auger radiotherapy J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-21 Dong Zhou, Wenhua Chu, Jinbin Xu
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Stable isotope synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-20 Bachir Latli, Matt J. Hrapchak, Maxim Chevliakov, Lalith P. Samankumara, Rogelio P. Frutos, Heewon Lee
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Preliminary PET imaging of [11C]evobrutinib in mouse models of colorectal cancer, SARS-CoV-2, and lung damage: Radiosynthesis via base-aided palladium-NiXantphos-mediated 11C-carbonylation J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-10 Amanda J. Boyle, Anton Lindberg, Junchao Tong, Dongxu Zhai, Fang Liu, Neil Vasdev
Evobrutinib is a second-generation, highly selective, irreversible Bruton's tyrosine kinase (BTK) inhibitor that has shown efficacy in the autoimmune diseases arthritis and multiple sclerosis. Its development as a positron emission tomography (PET) radiotracer has potential for in vivo imaging of BTK in various disease models including several cancers, severe acute respiratory syndrome-coronavirus-2
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-11
No abstract is available for this article.
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[68Ga]Ga-PentixaFor: Development of a fully automated in hospital production on the Trasis miniAllinOne synthesizer J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-09-07 Julien Costes, Kilian Casasagrande, Constance Dubegny, Juan Castillo, Jens Kaufman, Julien Masset, Charles Vriamont, Corentin Warnier, Alain Faivre-Chauvet, Judith Anna Delage
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Development of 11C-labeled CRANAD-102 for positron emission tomography imaging of soluble Aβ-species J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-31 Markus Staudt, Vladimir Shalgunov, Maiken Nedergaard, Matthias M. Herth
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An improved synthesis of [18F]VAT and its precursor J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-24 Bao Hu, Hari K. Akula, Doyoung Noh, Yiu Fung Mui, Mark Slifstein, Ramin Parsey, Wenchao Qu
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Automated production of 11C-labeled carboxylic acids and esters via “in-loop” 11C-carbonylation using GE FX synthesis modules J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-22 Tanpreet Kaur, Jay S. Wright, Bradford D. Henderson, Jonathan Godinez, Xia Shao, Peter J. H. Scott
An in-loop 11C-carbonylation process for the radiosynthesis of 11C-carboxylic acids and esters from halide precursors has been developed. The reaction proceeds at room temperature under mild conditions and enables 11C-carbonylation of both electron deficient and electron rich (hetero)aromatic halides to provide 11C-carboxylic acids and esters in good to excellent radiochemical yields, high radiochemical
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Luminescence enhancement by deuterium J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-16 Crist N. Filer
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-09
No abstract is available for this article.
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Enzymatic synthesis of halogen derivatives of L-phenylalanine and phenylpyruvic acid stereoselectively labeled with hydrogen isotopes in the side chain J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-08-02 Katarzyna Pałka, Katarzyna Podsadni, Małgorzata Pająk
Halogenated, labeled with deuterium, tritium or doubly labeled with deuterium and tritium in the 3S position of the side chain isotopomers of L-phenylalanine and phenylpyruvic acid were synthesized. Isotopomers of halogenated L-phenylalanine were obtained by addition of ammonia from isotopically enriched buffer solution to the halogenated derivative of (E)-cinnamic acid catalyzed by phenylalanine ammonia
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Carbon 14 and stable isotope synthesis of two potent and selective phosphodiesterase type 4 inhibitors J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-07-24 Bachir Latli, Matt J. Hrapchak, Thomas G. Tampone, Rogelio P. Frutos, Heewon Lee
(R)-2-(4-(Benzo[d]oxazol-2-yl)piperazin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (1) and (R)-2-(4-(4-chlorophenoxy)piperidin-1-yl)-4-((tetrahydro-2H-pyran-4-yl)amino)-6,7-dihydrothieno[3,2-d]pyrimidine 5-oxide (2) are two potent and selective inhibitors of phosphodiesterase type 4 (PDE4). In this manuscript, we report the detailed synthesis of these two compounds
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Featured Cover J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-07-20
The cover image is based on different strategies covered within this issue used for crossing the blood brain barrier.
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-07-20
No abstract is available for this article.
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Blood Brain Barrier - tactics and attributes in developing successful neuroimaging agents. J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-07-06 Selena Milicevic Sephton,Stephen Thompson
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Development of an economical method to synthesize O-(2-[18F]fluoroethyl)-L-tyrosine (18FFET) J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-07-06 Aishwarya Kumar, Raman Kumar Joshi, Riptee Thakur, Dinesh Kumar, Chandana Nagaraj, Pardeep Kumar
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Carbon 14 synthesis of glycine transporter 1 inhibitor Iclepertin (BI 425809) and its major metabolites J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-06-29 Bachir Latli, Matt J. Hrapchak, Rogelio P. Frutos, Heewon Lee, Jinhua J. Song
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-06-19
No abstract is available for this article.
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Mild and selective hydrogen–deuterium exchange for aromatic hydrogen of amines J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-06-19 Zetryana Puteri Tachrim, Manami Hashinoki, Zeping Wang, Zhang Wen, Zhuang Zihan, Makoto Hashimoto
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Applications of radiolabeled antibodies in neuroscience and neuro-oncology J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-06-15 Ryan J. Pakula, Peter J. H. Scott
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Development and physicochemical characterization of a biodegradable microspheres formulation loaded with samarium-153 and doxorubicin for chemo-radioembolization of liver tumours J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-06-07 Asseel Hisham Alregib, Hun Yee Tan, Yin How Wong, Azahari Kasbollah, Eng Hwa Wong, Basri Johan Jeet Abdullah, Alan Christopher Perkins, Chai Hong Yeong
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Synthesis and evaluation of 111In-labeled tetrapeptide-based compounds as single-photon emission computed tomography imaging probes targeting granzyme B J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-05-29 Nobuki Kazuta, Hiroyuki Watanabe, Masahiro Ono
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Issue Information J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-05-15
No abstract is available for this article.
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Efficient synthesis of carbon-14 labeled metabolites of the strobilurin fungicide mandestrobin using biomimetic iron-porphyrin catalyzed oxidation J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-05-13 Shuichi Murata, Motohiro Kurosawa, Takuo Fujisawa
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Small-scale two-dimensional liquid chromatography for a preparative re-purification of a highly labile tritium-labeled compound J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-05-05 Martin Sandvoss, Christian Klaus, Remo Weck, Volker Derdau, Matthias Schiell
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The inverse electron demand Diels–Alder cycloaddition with carbon-11 and fluorine-18: A gateway to pretargeted imaging across the blood–brain barrier J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-05-05 Simon H. Zientek, Stephen Thompson, Selena Milicevic Sephton, Franklin I. Aigbirhio
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Automated radiosynthesis of 1-(2-[18F]fluoroethyl)-L-tryptophan ([18F]FETrp) for positron emission tomography (PET) imaging of cancer in humans J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-04-28 Huailei Jiang, Yan Guo, Hancheng Cai, Nerissa Viola, Anthony Frank Shields, Otto Muzik, Csaba Juhasz
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Nitrilase mediated mild hydrolysis of a carbon-14 nitrile for the radiosynthesis of 4-(7-hydroxycarbamoyl-[1-14C-heptanoyl]-oxy)-benzoic acid methyl ester, [14C]-SHP-141: A novel class I/II histone deacetylase (HDAC) inhibitor J. Label. Comp. Radiopharm. (IF 1.8) Pub Date : 2023-04-25 Sean L. Kitson, William Watters, Thomas S. Moody, Todd Chappell, Ralph Mazitschek