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105. Whole-body PET tracking of a d-dodecapeptide and its radiotheranostic potential for PD-L1 overexpressing tumors

Author

Hu, Kuan, primary, Wu, Wenyu, additional, Xie, Lin, additional, Geng, Hao, additional, Zhang, Yiding, additional, Hanyu, Masayuki, additional, Zhang, Lulu, additional, Liu, Yinghuan, additional, Nagatsu, Kotaro, additional, Suzuki, Hisashi, additional, Guo, Jialin, additional, Wu, Yundong, additional, Li, Zigang, additional, Wang, Feng, additional, and Zhang, Mingrong, additional

Published
2022
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107. Radiotheranostic Agent 64Cu-cyclam-RAFT-c(-RGDfK-)4 for Management of Peritoneal Metastasis in Ovarian Cancer

Author

Zhao-Hui, Jin, B Tsuji, Atsushi, Mélissa, Degardin, Sugyo, Aya, Obara, Satoshi, Wakizaka, Hidekatsu, Nagatsu, Kotaro, Hu, Kuan, Ming-Rong, Zhang, Dumy, Pascal, Boturyn, Didier, Higashi, Tatsuya, Atsushi, Tsuji, Aya, Sugyo, Satoshi, Obara, Hidekatsu, Wakizaka, Kotaro, Nagatsu, Kuan, Hu, Zhang, Ming-Rong, and Tatsuya, Higashi

Abstract

Ovarian cancer peritoneal metastases (OCPMs) are a pathophysiologically heterogeneous group of tumors that are rarely curable. αvβ3 integrin (αvβ3) is overexpressed on tumoral neovessels and frequently on ovarian cancer cells. Here, using two clinically relevant αvβ3-positive OCPM mouse models, we studied the theranostic potential of an αvβ3-specific radiopeptide, 64Cu-cyclam-RAFT-c(-RGDfK-)4 (64Cu-RaftRGD), and its intra- and intertumoral distribution in relation to the tumor microenvironment.

Published
2020

118. Novel Reversible-Binding PET Ligands for Imaging Monoacylglycerol Lipase Based on the Piperazinyl Azetidine Scaffold

Author

Rong, Jian, primary, Mori, Wakana, additional, Xia, Xiaotian, additional, Schafroth, Michael A., additional, Zhao, Chunyu, additional, Van, Richard S., additional, Yamasaki, Tomoteru, additional, Chen, Jiahui, additional, Xiao, Zhiwei, additional, Haider, Ahmed, additional, Ogasawara, Daisuke, additional, Hiraishi, Atsuto, additional, Shao, Tuo, additional, Zhang, Yiding, additional, Chen, Zhen, additional, Pang, Fuwen, additional, Hu, Kuan, additional, Xie, Lin, additional, Fujinaga, Masayuki, additional, Kumata, Katsushi, additional, Gou, Yuancheng, additional, Fang, Yang, additional, Gu, Shuyin, additional, Wei, Huiyi, additional, Bao, Liang, additional, Xu, Hao, additional, Collier, Thomas L., additional, Shao, Yihan, additional, Carson, Richard E., additional, Cravatt, Benjamin F., additional, Wang, Lu, additional, Zhang, Ming-Rong, additional, and Liang, Steven H., additional

Published
2021
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119. Design, Synthesis, and Evaluation of 18F‑Labeled Monoacylglycerol Lipase Inhibitors as Novel Positron Emission Tomography Probes

Author

Chen, Zhen, Mori, Wakana, Fu, Hualong, A. Schafroth, Michael, Hatori, Akiko, Shao, Tuo, Zhang, Genwei, S. Van, Richard, Zhang, Yiding, Hu, Kuan, Fujinaga, Masayuki, Ming-Rong, Zhang, Wakana, Mori, Akiko, Hatori, Kuan, Hu, Masayuki, Fujinaga, and Zhang, Ming-Rong

Abstract

Dysfunction of monoacylglycerol lipase (MAGL) is associated with several psychopathological disorders, including drug addiction and neurodegenerative diseases. Herein we design, synthesize, and evaluate several irreversible fluorine-containing MAGL inhibitors for positron emission tomography (PET) ligand development. Compound 6 (identified from a therapeutic agent) was advanced for 18F-labeling via a novel spirocyclic iodonium ylide (SCIDY) strategy, which demonstrated high brain permeability and excellent specific binding. This work supports further development of novel 18F-labeled MAGL PET probes.

Published
2019

120. Synthesis of quaternary succinimides promoted by Ferric Nitrate

Author

Chao Zheng, Cai-Ling Fan, Jun-Jie Wei, Xin-Qi Hao, Hu Kuan, Mao-Ping Song, and Jing-Lin Wang

Subjects
010405 organic chemistry, Chemistry, Organic Chemistry, 010402 general chemistry, 01 natural sciences, Biochemistry, Combinatorial chemistry, Toluene, 0104 chemical sciences, Succinimides, chemistry.chemical_compound, Nitrate, Drug Discovery, Pyridine, medicine, Ferric, Quaternary, medicine.drug
Abstract

An efficient protocol has been accomplished for the synthesis of quaternary α-aminosuccinimides in toluene medium involving 2-phenylimidazo[1, 2-a]pyridine in a one-pot reaction promoted by Ferric Nitrate at 120 °C. The protocol presented herein, is for the first time, via a novel transformation where Ferric Nitrate promotes imidazo[1,2-a]pyridine structural metamorphosis to the title compound quaternary succinimides. High compatibility, easy work-up, and excellent yields are the advantages of this protocol. The quaternary α-aminosuccinimides are expected to have great potential in synthesizing quaternary α-amino acids and applications in medicinal chemistry.

Published
2018

123. 211At-Labeled Polymer Nanoparticles for Targeted Radionuclide Therapy of Glucose-Dependent Insulinotropic Polypeptide Receptor (GIPR)-Overexpressed Cancer

Author

Shi, Xiumin, primary, Li, Qing, additional, Zhang, Lulu, additional, Hanyu, Masayuki, additional, Xie, Lin, additional, Hu, Kuan, additional, Nagatsu, Kotaro, additional, Zhang, Chuan, additional, Wu, Zhengcan, additional, Wang, Feng, additional, Zhang, Ming-Rong, additional, Yang, Kai, additional, and Zhu, Ran, additional

Published
2021
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125. Radiosynthesis and preclinical evaluation of a carbon-11 labeled PDE7 inhibitor for PET neuroimaging

Author

Xiao, Zhiwei, primary, Sun, Jiyun, additional, Fujinaga, Masayuki, additional, Wei, Huiyi, additional, Zhao, Chunyu, additional, Haider, Ahmed, additional, Van, Richard, additional, Yamasaki, Tomoteru, additional, Zhang, Yiding, additional, Rong, Jian, additional, Hu, Kuan, additional, Chen, Jiahui, additional, Leon, Erick Calderon, additional, Hiraishi, Atsuto, additional, Wei, Junjie, additional, Xu, Yi, additional, Shao, Yihan, additional, Zhang, Han-Ting, additional, Lloyd, KC Kent, additional, Wang, Lu, additional, Zhang, Ming-Rong, additional, and Liang, Steven, additional

Published
2021
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127. Development of a highly-specific 18F-labeled irreversible positron emission tomography tracer for monoacylglycerol lipase mapping

Author

Chen, Zhen, primary, Mori, Wakana, additional, Rong, Jian, additional, Schafroth, Michael A., additional, Shao, Tuo, additional, Van, Richard S., additional, Ogasawara, Daisuke, additional, Yamasaki, Tomoteru, additional, Hiraishi, Atsuto, additional, Hatori, Akiko, additional, Chen, Jiahui, additional, Zhang, Yiding, additional, Hu, Kuan, additional, Fujinaga, Masayuki, additional, Sun, Jiyun, additional, Yu, Qingzhen, additional, Collier, Thomas L., additional, Shao, Yihan, additional, Cravatt, Benjamin F., additional, Josephson, Lee, additional, Zhang, Ming-Rong, additional, and Liang, Steven H., additional

Published
2021
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132. Synthesis and preliminary evaluation of 4-hydroxy-6-(3-[11C]methoxyphenethyl)pyridazin-3(2H)-one, a 11C-labeled d-amino acid oxidase (DAAO) inhibitor for PET imaging

Author

Deng, Xiaoyun, Zhang, Yiding, Chen, Zhen, Kumata, Katsushi, Van, Richard, Rong, Jian, Shao, Tuo, Hatori, Akiko, Mori, Wakana, Yu, Qingzhen, Hu, Kuan, Fujinaga, Masayuki, Wey, Hsiao-Ying, Shao, Yihan, Josephson, Lee, Murtas, Giulia, Pollegioni, Loredano, Zhang, Ming-Rong, and Liang, Steven

Published
2020
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133. Synthesis and preliminary evaluation of 18F-labeled 1-(6,7-dimethyl-4-(methylamino)-1,3-dihydro-2H-pyrrolo[3,4-c]pyridin-2-yl)-2-(trans-2-(6-fluoropyridin-3-yl)cyclopropyl)ethan-1-one for imaging muscarinic acetylcholine receptor subtype 4

Author

Deng, Xiaoyun, Zhang, Yiding, Rong, Jian, Kumata, Katsushi, Shao, Tuo, Wang, Gangqiang, Hatori, Akiko, Mori, Wakana, Yu, Qingzhen, Hu, Kuan, Fujinaga, Masayuki, Shao, Yihan, Josephson, Lee, Sun, Shaofa, Zhang, Ming-Rong, and Liang, Steven

Published
2020
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141. A Novel Image Fusion Algorithm for Visible and PMMW Images based on Clustering and NSCT

Author

Xiong Jintao, Xie Weichao, Yang Jianyu, Fu Yanlong, Hu Kuan, and Zhong Zhibin

Subjects
Engineering (General). Civil engineering (General), TA1-2040
Abstract

Aiming at the fusion of visible and Passive Millimeter Wave (PMMW) images, a novel algorithm based on clustering and NSCT (Nonsubsampled Contourlet Transform) is proposed. It takes advantages of the particular ability of PMMW image in presenting metal target and uses the clustering algorithm for PMMW image to extract the potential target regions. In the process of fusion, NSCT is applied to both input images, and then the decomposition coefficients on different scale are combined using different rules. At last, the fusion image is obtained by taking the inverse NSCT of the fusion coefficients. Some methodologies are used to evaluate the fusion results. Experiments demonstrate the superiority of the proposed algorithm for metal target detection compared to wavelet transform and Laplace transform.

Published
2016
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142. WAVE2 Enhanced Hepatic Stellate Cells Activity in Colorectal Liver Metastases

Author

Tan,Fengbo, He,Dongren, Hu,Kuan, Wang,Dong, Zhang,Sai, Li,Juanni, Wang,Zhiming, and Tao,Yiming

Subjects
Cancer Management and Research
Abstract

Fengbo Tan,1,2 Dongren He,2 Kuan Hu,1,2 Dong Wang,2 Sai Zhang,3 Juanni Li,4 Zhiming Wang,1,2 Yiming Tao1 1Department of General Surgery Research, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of China; 2Department of General Surgery, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of China; 3Institute of Medical Sciences, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of China; 4Department of Pathology, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of ChinaCorrespondence: Yiming Tao Department of General SurgeryResearch, Xiangya Hospital, Central South University, Changsha, Hunan, People’s Republic of ChinaTel +86-731-8432-7191Fax +86-731-8975-3510Email yimingtao@csu.edu.cnBackground: Cancer cell migration, tumor angiogenesis, and activated hepatic stellate cells (a-HSCs) promote the development of colorectal liver metastases (CLM). Wiskott–Aldrich syndrome protein family verprolin-homologous protein 2 (WAVE2) has been associated with CLM, although the underlying molecular mechanisms remain unclear.Methods: In the current study, we evaluated the relationship between WAVE2 and CLM in 103 CLM patients who underwent liver resection. Immunohistochemistry (IHC) staining was performed to determine the association between WAVE2 protein expression and hepatic micro-metastasis in human CLM tissues. WAVE2 knockout was performed in hepatic stellate cells (HSC) to explore the function and signaling pathways of WAVE2 in colorectal cancer progression.Results: Significantly higher levels of WAVE2 were detected in portal-associated relative to sinusoid-associated micro-metastasis. A strong correlation was identified between WAVE2 levels and microvessel density (MVD) in hepatic metastasis. Similarly, expression of WAVE2 was closely associated with activation of HSCs. Mechanistically, WAVE2 regulated the progression of human CLM acts by regulating the growth factor β (TGF-β) and Hippo pathways via effector yes-associated protein (YAP1).Conclusion: Overall, our results demonstrated that WAVE2 participates in CLM tumor microenvironment, and can be a potential latent therapeutic target for CLM.Keywords: colorectal cancer, hepatic stellate cells, liver metastasis, WAVE2

Published
2020

144. Clouds and Convective Self-Aggregation in a Multimodel Ensemble of Radiative-Convective Equilibrium Simulations

Author

Wing, Allison A., Stauffer, Catherine L., Becker, Tobias, Reed, Kevin A., Ahn, Min Seop, Arnold, Nathan P., Bony, Sandrine, Branson, Mark, Bryan, George H., Chaboureau, Jean Pierre, De Roode, Stephan R., Gayatri, Kulkarni, Hohenegger, Cathy, Hu, Kuan, Jansson, Fredrik, Jones, Todd R., Khairoutdinov, Marat, Kim, Daehyun, Martin, Zane K., Matsugishi, Shuhei, Medeiros, Brian, Miura, Hiroaki, Moon, Yumin, Müller, Sebastian K., Ohno, Tomoki, Popp, Max, Prabhakaran, Thara, Randall, David, Rios-Berrios, Rosimar, Rochetin, Nicolas, Roehrig, Romain, Romps, David M., Ruppert, James H., Satoh, Masaki, Silvers, Levi G., Singh, Martin S., Stevens, Bjorn, Tomassini, Lorenzo, van Heerwaarden, Chiel C., Wang, Shuguang, Zhao, Ming, Wing, Allison A., Stauffer, Catherine L., Becker, Tobias, Reed, Kevin A., Ahn, Min Seop, Arnold, Nathan P., Bony, Sandrine, Branson, Mark, Bryan, George H., Chaboureau, Jean Pierre, De Roode, Stephan R., Gayatri, Kulkarni, Hohenegger, Cathy, Hu, Kuan, Jansson, Fredrik, Jones, Todd R., Khairoutdinov, Marat, Kim, Daehyun, Martin, Zane K., Matsugishi, Shuhei, Medeiros, Brian, Miura, Hiroaki, Moon, Yumin, Müller, Sebastian K., Ohno, Tomoki, Popp, Max, Prabhakaran, Thara, Randall, David, Rios-Berrios, Rosimar, Rochetin, Nicolas, Roehrig, Romain, Romps, David M., Ruppert, James H., Satoh, Masaki, Silvers, Levi G., Singh, Martin S., Stevens, Bjorn, Tomassini, Lorenzo, van Heerwaarden, Chiel C., Wang, Shuguang, and Zhao, Ming

Abstract

The Radiative-Convective Equilibrium Model Intercomparison Project (RCEMIP) is an intercomparison of multiple types of numerical models configured in radiative-convective equilibrium (RCE). RCE is an idealization of the tropical atmosphere that has long been used to study basic questions in climate science. Here, we employ RCE to investigate the role that clouds and convective activity play in determining cloud feedbacks, climate sensitivity, the state of convective aggregation, and the equilibrium climate. RCEMIP is unique among intercomparisons in its inclusion of a wide range of model types, including atmospheric general circulation models (GCMs), single column models (SCMs), cloud-resolving models (CRMs), large eddy simulations (LES), and global cloud-resolving models (GCRMs). The first results are presented from the RCEMIP ensemble of more than 30 models. While there are large differences across the RCEMIP ensemble in the representation of mean profiles of temperature, humidity, and cloudiness, in a majority of models anvil clouds rise, warm, and decrease in area coverage in response to an increase in sea surface temperature (SST). Nearly all models exhibit self-aggregation in large domains and agree that self-aggregation acts to dry and warm the troposphere, reduce high cloudiness, and increase cooling to space. The degree of self-aggregation exhibits no clear tendency with warming. There is a wide range of climate sensitivities, but models with parameterized convection tend to have lower climate sensitivities than models with explicit convection. In models with parameterized convection, aggregated simulations have lower climate sensitivities than unaggregated simulations.

Published
2020

148. Recent developments on PET radiotracers for TSPO and their applications in neuroimaging

Author

Zhang, Lingling, primary, Hu, Kuan, additional, Shao, Tuo, additional, Hou, Lu, additional, Zhang, Shaojuan, additional, Ye, Weijian, additional, Josephson, Lee, additional, Meyer, Jeffrey H., additional, Zhang, Ming-Rong, additional, Vasdev, Neil, additional, Wang, Jinghao, additional, Xu, Hao, additional, Wang, Lu, additional, and Liang, Steven H., additional

Published
2021
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150. Radiotheranostic Agent 64Cu-cyclam-RAFT-c(-RGDfK-)4 for Management of Peritoneal Metastasis in Ovarian Cancer

Author

Jin, Zhao-Hui, primary, Tsuji, Atsushi B., additional, Degardin, Mélissa, additional, Sugyo, Aya, additional, Obara, Satoshi, additional, Wakizaka, Hidekatsu, additional, Nagatsu, Kotaro, additional, Hu, Kuan, additional, Zhang, Ming-Rong, additional, Dumy, Pascal, additional, Boturyn, Didier, additional, and Higashi, Tatsuya, additional

Published
2020
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