ArticleJournal of medicinal chemistry2019
Design, Synthesis, and Evaluation of Reversible and Irreversible Monoacylglycerol Lipase Positron Emission Tomography (PET) Tracers Using a "Tail Switching" Strategy on a Piperazinyl Azetidine Skeleton.
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Article in Journal of medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
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20 citing papers in PubMed, 45 citations in OpenAlex.
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Authors and funding
34 authors at 6 institutions in 4 countries.
Zhen ChenDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0002-6289-4332
Wakana MoriDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Xiaoyun DengDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Ran ChengDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Daisuke OgasawaraThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology , The Scripps Research Institute , SR107 10550 North Torrey Pines Road , La Jolla , California 92037 , United States.
Genwei ZhangDepartment of Chemistry and Biochemistry , University of Oklahoma , Norman , Oklahoma 73019 , United States.
Michael A SchafrothThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology , The Scripps Research Institute , SR107 10550 North Torrey Pines Road , La Jolla , California 92037 , United States.ORCID 0000-0002-5864-6766
Kenneth DahlDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Hualong FuDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Akiko HatoriDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Tuo ShaoDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Yiding ZhangDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Tomoteru YamasakiDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Xiaofei ZhangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Jian RongDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Qingzhen YuDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Kuan HuDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Masayuki FujinagaDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Lin XieDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Katsushi KumataDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.
Yuancheng GouChemShuttle, Inc. , 1699 Huishan Blvd. , Wuxi , Jiangsu 214174 , China.
Jingjin ChenChemShuttle, Inc. , 1699 Huishan Blvd. , Wuxi , Jiangsu 214174 , China.
Shuyin GuChemShuttle, Inc. , 1699 Huishan Blvd. , Wuxi , Jiangsu 214174 , China.
Liang BaoChemShuttle, Inc. , 1699 Huishan Blvd. , Wuxi , Jiangsu 214174 , China.
Lu WangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Thomas Lee CollierDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Neil VasdevDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0002-2087-5125
Yihan ShaoDepartment of Chemistry and Biochemistry , University of Oklahoma , Norman , Oklahoma 73019 , United States.ORCID 0000-0001-9337-341X
Jun-An MaDepartment of Chemistry, School of Science , Tianjin University , 92 Weijin Road , Nankai District, Tianjin 300072 , China.ORCID 0000-0002-3902-6799
Benjamin F CravattThe Skaggs Institute for Chemical Biology and Department of Chemical Physiology , The Scripps Research Institute , SR107 10550 North Torrey Pines Road , La Jolla , California 92037 , United States.ORCID 0000-0001-5330-3492
Christopher FowlerDepartment of Pharmacology and Clinical Neuroscience , Umeå University , SE-901 87 Umeå , Sweden.
Lee JosephsonDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.
Ming-Rong ZhangDepartment of Radiopharmaceuticals Development, National Institute of Radiological Sciences , National Institutes for Quantum and Radiological Science and Technology , Chiba 263-8555 , Japan.ORCID 0000-0002-3001-9605
Steven H LiangDivision of Nuclear Medicine and Molecular Imaging, Massachusetts General Hospital & Department of Radiology , Harvard Medical School , Boston , Massachusetts 02114 , United States.ORCID 0000-0003-1413-6315
Harvard University · USNational Institutes for Quantum Science and Technology · JPScripps Research Institute · USUniversity of Oklahoma · USTianjin University · CNUmeå University · SE
Funding
CHEMOPROTEOMIC METHODS FOR SERINE HYDROLASE INHIBITOR DEVELOPMENTR01DA033760 · NIDA · SCRIPPS RESEARCH INSTITUTE, THE · PI CRAVATT, BENJAMIN F, SCAMPAVIA, LOUIS DANIEL · 2012 to 2021
$5.1MNeuro-PET Radiotracer Discovery for Imaging Glycogen Synthase Kinase-3R01AG054473 · NIA · MASSACHUSETTS GENERAL HOSPITAL · PI VASDEV, NEIL · 2017 to 2020
$1.7MNew PET tracers for neuroimaging of FAAH in endocannabinoid signalingK01DA038000 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2014 to 2018
$927kNovel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR33DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2019 to 2021
$851kNovel PET Tracers for Imaging Monoacylglycerol Lipase in Endocannabinoid SignalingR21DA043507 · NIDA · MASSACHUSETTS GENERAL HOSPITAL · PI LIANG, STEVEN H · 2017 to 2018
$425kNIA NIH HHS R01 AG054473NIDA NIH HHS K01 DA038000NIDA NIH HHS R01 DA033760NIDA NIH HHS R21 DA043507NIDA NIH HHS R33 DA043507
Abstract
Monoacylglycerol lipase (MAGL) is a serine hydrolase that degrades 2-arachidonoylglycerol (2-AG) in the endocannabinoid system (eCB). Selective inhibition of MAGL has emerged as a potential therapeutic approach for the treatment of diverse pathological conditions, including chronic pain, inflammation, cancer, and neurodegeneration. Herein, we disclose a novel array of reversible and irreversible MAGL inhibitors by means of "tail switching" on a piperazinyl azetidine scaffold. We developed a lead irreversible-binding MAGL inhibitor 8 and reversible-binding compounds 17 and 37, which are amenable for radiolabeling with
Indexed as
Drug DesignAnimalsAzetidinesDose-Response Relationship, DrugEnzyme InhibitorsMiceMice, KnockoutMolecular Docking SimulationMonoacylglycerol LipasesPiperazinesPositron-Emission TomographyProof of Concept StudyRadioligand AssayRadiopharmaceuticalsRatsRats, Sprague-DawleyazetidineAzetidinesEnzyme InhibitorsMonoacylglycerol LipasesPiperazinesRadiopharmaceuticals
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