[11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors
[Display omitted] Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer’s disea...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2022-06, Vol.65, p.128704-128704, Article 128704 |
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| container_title | Bioorganic & medicinal chemistry letters |
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| creator | Ogata, Aya Ji, Bin Yamada, Takashi Hattori, Saori Abe, Junichiro Ikenuma, Hiroshi Ichise, Masanori Koyama, Hiroko Suzuki, Masaaki Kato, Takashi Ito, Kengo Kimura, Yasuyuki |
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Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer’s disease. In this study, we developed [11C]NCGG401, a positron emission tomography (PET) ligand, targeting for CSF1R as an imaging biomarker for microglial pathophysiology in Alzheimer’s disease. NCGG401 showed a high potency to inhibit human CSF1R kinase activity and a high binding affinity to human CSF1R. PET imaging with [11C]NCGG401 in healthy rats showed a good brain permeability. Furthermore, the specific binding component was determined by postmortem autoradiography in rat brain and human hippocampal sections. The knowledge of the characteristics of [11C]NCCC401, our initial CSF1R compound, we have obtained may be useful for further development and optimization of CSF1R radioligands for PET imaging of microglia. |
| doi_str_mv | 10.1016/j.bmcl.2022.128704 |
| format | Article |
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Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer’s disease. In this study, we developed [11C]NCGG401, a positron emission tomography (PET) ligand, targeting for CSF1R as an imaging biomarker for microglial pathophysiology in Alzheimer’s disease. NCGG401 showed a high potency to inhibit human CSF1R kinase activity and a high binding affinity to human CSF1R. PET imaging with [11C]NCGG401 in healthy rats showed a good brain permeability. Furthermore, the specific binding component was determined by postmortem autoradiography in rat brain and human hippocampal sections. The knowledge of the characteristics of [11C]NCCC401, our initial CSF1R compound, we have obtained may be useful for further development and optimization of CSF1R radioligands for PET imaging of microglia.</description><identifier>ISSN: 0960-894X</identifier><identifier>EISSN: 1464-3405</identifier><identifier>DOI: 10.1016/j.bmcl.2022.128704</identifier><identifier>PMID: 35351586</identifier><language>eng</language><publisher>England: Elsevier Ltd</publisher><subject>Alzheimer Disease - metabolism ; Alzheimer’s disease ; Animals ; Brain - diagnostic imaging ; Brain - metabolism ; Colony-stimulating factor 1 receptor ; Disease Models, Animal ; Ligands ; Macrophage Colony-Stimulating Factor - metabolism ; Microglia ; Microglia - metabolism ; Positron emission tomography ; Positron-Emission Tomography - methods ; Rats ; Receptor, Macrophage Colony-Stimulating Factor - metabolism ; Receptors, Granulocyte-Macrophage Colony-Stimulating Factor</subject><ispartof>Bioorganic & medicinal chemistry letters, 2022-06, Vol.65, p.128704-128704, Article 128704</ispartof><rights>2022 Elsevier Ltd</rights><rights>Copyright © 2022 Elsevier Ltd. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c271t-95f5f93397d8b27e08eef3e74481085fa0cac9edf9a6bf1367ff655142a069ef3</citedby><cites>FETCH-LOGICAL-c271t-95f5f93397d8b27e08eef3e74481085fa0cac9edf9a6bf1367ff655142a069ef3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.bmcl.2022.128704$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3548,27923,27924,45994</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/35351586$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ogata, Aya</creatorcontrib><creatorcontrib>Ji, Bin</creatorcontrib><creatorcontrib>Yamada, Takashi</creatorcontrib><creatorcontrib>Hattori, Saori</creatorcontrib><creatorcontrib>Abe, Junichiro</creatorcontrib><creatorcontrib>Ikenuma, Hiroshi</creatorcontrib><creatorcontrib>Ichise, Masanori</creatorcontrib><creatorcontrib>Koyama, Hiroko</creatorcontrib><creatorcontrib>Suzuki, Masaaki</creatorcontrib><creatorcontrib>Kato, Takashi</creatorcontrib><creatorcontrib>Ito, Kengo</creatorcontrib><creatorcontrib>Kimura, Yasuyuki</creatorcontrib><title>[11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors</title><title>Bioorganic & medicinal chemistry letters</title><addtitle>Bioorg Med Chem Lett</addtitle><description>[Display omitted]
Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer’s disease. In this study, we developed [11C]NCGG401, a positron emission tomography (PET) ligand, targeting for CSF1R as an imaging biomarker for microglial pathophysiology in Alzheimer’s disease. NCGG401 showed a high potency to inhibit human CSF1R kinase activity and a high binding affinity to human CSF1R. PET imaging with [11C]NCGG401 in healthy rats showed a good brain permeability. Furthermore, the specific binding component was determined by postmortem autoradiography in rat brain and human hippocampal sections. The knowledge of the characteristics of [11C]NCCC401, our initial CSF1R compound, we have obtained may be useful for further development and optimization of CSF1R radioligands for PET imaging of microglia.</description><subject>Alzheimer Disease - metabolism</subject><subject>Alzheimer’s disease</subject><subject>Animals</subject><subject>Brain - diagnostic imaging</subject><subject>Brain - metabolism</subject><subject>Colony-stimulating factor 1 receptor</subject><subject>Disease Models, Animal</subject><subject>Ligands</subject><subject>Macrophage Colony-Stimulating Factor - metabolism</subject><subject>Microglia</subject><subject>Microglia - metabolism</subject><subject>Positron emission tomography</subject><subject>Positron-Emission Tomography - methods</subject><subject>Rats</subject><subject>Receptor, Macrophage Colony-Stimulating Factor - metabolism</subject><subject>Receptors, Granulocyte-Macrophage Colony-Stimulating Factor</subject><issn>0960-894X</issn><issn>1464-3405</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2022</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kMFKAzEQhoMotlZfwIPk6MGtSTbJ7oIXKbUKRT20IIiENDspKbubutkW-vamtHr0NMPw_T_Mh9A1JUNKqLxfDRe1qYaMMDakLM8IP0F9yiVPUk7EKeqTQpIkL_hHD12EsCKEcsL5OeqlIhVU5LKP5p-Ujr5eR5MJJ_QOa9z4LVT4fTzDlVvqpsTWt9jVeumaJfYWG1_5ZodD5-pNpbv91WrTRYjiFgys4xou0ZnVVYCr4xyg-dN4NnpOpm-Tl9HjNDEso11SCCtskaZFVuYLlgHJAWwKGec5JbmwmhhtCihtoeXC0lRm1kohKGeayCKiA3R76F23_nsDoVO1CwaqSjfgN0ExyQXPYo5FlB1Q0_oQWrBq3ca32p2iRO11qpXa61R7neqgM4Zujv2bRQ3lX-TXXwQeDgDEL7cOWhWMg8ZA6aKMTpXe_df_A2sZhC8</recordid><startdate>20220601</startdate><enddate>20220601</enddate><creator>Ogata, Aya</creator><creator>Ji, Bin</creator><creator>Yamada, Takashi</creator><creator>Hattori, Saori</creator><creator>Abe, Junichiro</creator><creator>Ikenuma, Hiroshi</creator><creator>Ichise, Masanori</creator><creator>Koyama, Hiroko</creator><creator>Suzuki, Masaaki</creator><creator>Kato, Takashi</creator><creator>Ito, Kengo</creator><creator>Kimura, Yasuyuki</creator><general>Elsevier Ltd</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>20220601</creationdate><title>[11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors</title><author>Ogata, Aya ; Ji, Bin ; Yamada, Takashi ; Hattori, Saori ; Abe, Junichiro ; Ikenuma, Hiroshi ; Ichise, Masanori ; Koyama, Hiroko ; Suzuki, Masaaki ; Kato, Takashi ; Ito, Kengo ; Kimura, Yasuyuki</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c271t-95f5f93397d8b27e08eef3e74481085fa0cac9edf9a6bf1367ff655142a069ef3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2022</creationdate><topic>Alzheimer Disease - metabolism</topic><topic>Alzheimer’s disease</topic><topic>Animals</topic><topic>Brain - diagnostic imaging</topic><topic>Brain - metabolism</topic><topic>Colony-stimulating factor 1 receptor</topic><topic>Disease Models, Animal</topic><topic>Ligands</topic><topic>Macrophage Colony-Stimulating Factor - metabolism</topic><topic>Microglia</topic><topic>Microglia - metabolism</topic><topic>Positron emission tomography</topic><topic>Positron-Emission Tomography - methods</topic><topic>Rats</topic><topic>Receptor, Macrophage Colony-Stimulating Factor - metabolism</topic><topic>Receptors, Granulocyte-Macrophage Colony-Stimulating Factor</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ogata, Aya</creatorcontrib><creatorcontrib>Ji, Bin</creatorcontrib><creatorcontrib>Yamada, Takashi</creatorcontrib><creatorcontrib>Hattori, Saori</creatorcontrib><creatorcontrib>Abe, Junichiro</creatorcontrib><creatorcontrib>Ikenuma, Hiroshi</creatorcontrib><creatorcontrib>Ichise, Masanori</creatorcontrib><creatorcontrib>Koyama, Hiroko</creatorcontrib><creatorcontrib>Suzuki, Masaaki</creatorcontrib><creatorcontrib>Kato, Takashi</creatorcontrib><creatorcontrib>Ito, Kengo</creatorcontrib><creatorcontrib>Kimura, Yasuyuki</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic & medicinal chemistry letters</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ogata, Aya</au><au>Ji, Bin</au><au>Yamada, Takashi</au><au>Hattori, Saori</au><au>Abe, Junichiro</au><au>Ikenuma, Hiroshi</au><au>Ichise, Masanori</au><au>Koyama, Hiroko</au><au>Suzuki, Masaaki</au><au>Kato, Takashi</au><au>Ito, Kengo</au><au>Kimura, Yasuyuki</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>[11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors</atitle><jtitle>Bioorganic & medicinal chemistry letters</jtitle><addtitle>Bioorg Med Chem Lett</addtitle><date>2022-06-01</date><risdate>2022</risdate><volume>65</volume><spage>128704</spage><epage>128704</epage><pages>128704-128704</pages><artnum>128704</artnum><issn>0960-894X</issn><eissn>1464-3405</eissn><abstract>[Display omitted]
Colony-stimulating factor 1 receptors (CSF1R) are expressed exclusively on microglia in the central nervous system. The receptors regulate immune responses by controlling the survival and activity of microglia and are intricately involved in the pathophysiology of Alzheimer’s disease. In this study, we developed [11C]NCGG401, a positron emission tomography (PET) ligand, targeting for CSF1R as an imaging biomarker for microglial pathophysiology in Alzheimer’s disease. NCGG401 showed a high potency to inhibit human CSF1R kinase activity and a high binding affinity to human CSF1R. PET imaging with [11C]NCGG401 in healthy rats showed a good brain permeability. Furthermore, the specific binding component was determined by postmortem autoradiography in rat brain and human hippocampal sections. The knowledge of the characteristics of [11C]NCCC401, our initial CSF1R compound, we have obtained may be useful for further development and optimization of CSF1R radioligands for PET imaging of microglia.</abstract><cop>England</cop><pub>Elsevier Ltd</pub><pmid>35351586</pmid><doi>10.1016/j.bmcl.2022.128704</doi><tpages>1</tpages></addata></record> |
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| subjects | Alzheimer Disease - metabolism Alzheimer’s disease Animals Brain - diagnostic imaging Brain - metabolism Colony-stimulating factor 1 receptor Disease Models, Animal Ligands Macrophage Colony-Stimulating Factor - metabolism Microglia Microglia - metabolism Positron emission tomography Positron-Emission Tomography - methods Rats Receptor, Macrophage Colony-Stimulating Factor - metabolism Receptors, Granulocyte-Macrophage Colony-Stimulating Factor |
| title | [11C]NCGG401, a novel PET ligand for imaging of colony stimulating factor 1 receptors |
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