Review
Biochemistry & Molecular Biology
Ines C. F. Fonseca, Miguel Castelo-Branco, Claudia Cavadas, Antero J. Abrunhosa
Summary: This article provides a systematic review of imaging biomarkers developed as PET tracers to study the functions and molecular mechanisms of the NPY receptor family.
Article
Endocrinology & Metabolism
Qiongyue Zhang, Qing Miao, Yehong Yang, Jiaying Lu, Huiwei Zhang, Yonghao Feng, Wei Wu, Xiaoming Zhu, Boni Xiang, Quanya Sun, Yihui Guan, Yiming Li, Chuantao Zuo, Hongying Ye
Summary: This study investigated the relationship between brain glucose metabolism and human BAT activity using PET/CT in healthy adults. The results showed that regional brain glucose metabolism is closely related to BAT activity, which may be mediated by NPY.
FRONTIERS IN ENDOCRINOLOGY
(2021)
Article
Oncology
Sydney A. Pascetta, Sarah M. Kirsh, Makenna Cameron, James Uniacke
Summary: In breast carcinomas, neuropeptide Y (NPY) acts on NPY1R and NPY5R, and their interaction is associated with enhanced migration and proliferation. Inhibiting NPY1R and NPY5R under hypoxia conditions greatly reduces signaling, proliferation, migration, invasion, and spheroid growth. In breast tumor tissue, NPY5R levels and colocalization with hypoxia correlate with advanced cancer, while NPY1R correlates with adverse outcomes.
Article
Multidisciplinary Sciences
Tyler S. Nelson, Ghanshyam P. Sinha, Diogo F. S. Santos, Peter Jukkola, Pranav Prasoon, Michelle K. Winter, Ken E. McCarson, Bret N. Smith, Bradley K. Taylor
Summary: Peripheral nerve injury enhances the excitability of Y1-INs in the spinal cord dorsal horn, leading to the development of allodynia and affective pain. Inhibition of Y1-INs or administration of Y1 agonists can alleviate allodynic symptoms. Conditional deletion of Npy1r in dorsal horn neurons prevents the anti-hyperalgesic effects of intrathecal Y1 agonists. These findings suggest that Y1-INs in the spinal cord are a promising target for the treatment of neuropathic pain.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2022)
Article
Clinical Neurology
Chunxiao Yang, Zihua Gong, Xiaochen Zhang, Shuai Miao, Bozhi Li, Wei Xie, Tao Wang, Xun Han, Liang Wang, Zhao Dong, Shengyuan Yu
Summary: This study aimed to investigate the role of neuropeptide Y (NPY) in migraine. The study found that the NPY signaling pathway was altered in patients with migraine, and injection of NPY in a mouse model could alleviate migraine symptoms. These findings may provide new insights into novel therapeutic targets for the treatment of migraine.
JOURNAL OF HEADACHE AND PAIN
(2023)
Article
Multidisciplinary Sciences
Ou Yamaguchi, Kyoichi Kaira, Ichiro Naruse, Yukihiro Umeda, Takeshi Honda, Satoshi Watanabe, Kosuke Ichikawa, Kazunari Tateishi, Norimitsu Kasahara, Tetsuya Higuchi, Kosuke Hashimoto, Shun Shinomiya, Yu Miura, Ayako Shiono, Atsuto Mouri, Hisao Imai, Kunihiko Iizuka, Tamotsu Ishizuka, Koichi Minato, Satoshi Suda, Hiroshi Kagamu, Keita Mori, Ichiei Kuji, Nobuhiko Seki
Summary: This study aimed to investigate the clinical relevance of F-18-FDG PET/CT compared to CT in predicting the response to PD-1 blockade in the early phase. The results showed that metabolic assessment by MTV or TLG was superior to morphological changes on CT for predicting the therapeutic response and survival.
SCIENTIFIC REPORTS
(2022)
Article
Chemistry, Organic
Aaron Schuell, Lisa Grothe, Eduardo Rodrigo, Thomas Erhard, Siegfried R. Waldvogel
Summary: A novel electrosynthetic approach for the synthesis of aryl dibenzothiophenium salts, including the metal-free, electrochemical formation of a C-S bond under ambient conditions, has been reported. The broad applicability of this method has been demonstrated with 14 examples, achieving isolated yields of up to 72%, including nitrogen-containing heterocycles. The resulting sulfonium salts can serve as precursors for the synthesis of [F-18]fluoroarenes found in PET tracer ligands.
Editorial Material
Oncology
Hannah M. Linden, David A. Mankoff
Summary: [F-18]fluoroestradiol (FES) PET is an FDA-approved imaging biomarker that predicts clinical benefit of endocrine therapy and measures target activity in drug development. A recent study showed that tumor heterogeneity of expression predicts clinical benefit, and serial FES monitoring can assess estrogen receptor blockade and posttreatment release.
CLINICAL CANCER RESEARCH
(2023)
Editorial Material
Hematology
Andrew Wirth, N. George Mikhaeel
Summary: This study demonstrates that in patients with DLBCL, those who are EOT PET-negative may be spared from radiotherapy, while selected patients with EOT PET-positive sites can achieve outcomes comparable to PET-negative patients when receiving selective treatment.
Article
Clinical Neurology
Emily A. Largent, Joshua D. Grill, Kyra O'Brien, David Wolk, Kristin Harkins, Jason Karlawish
Summary: Alzheimer's Disease (AD) is characterized by three pathologic processes: beta-amyloid, hyperphosphorylated tau, and neurodegeneration. Advances in measuring biomarkers of these processes have led to a growing interest in using AD biomarker tests in care and research. Therefore, a 5-step approach is proposed, including determining the appropriateness of testing, providing pretest education and consent, administering the test, disclosing the results, and follow-up for well-being.
Review
Biochemistry & Molecular Biology
Christophe van de Wiele, Sezgin Ustmert, Bart De Spiegeleer, Pieter-Jan De Jonghe, Mike Sathekge, Maes Alex
Summary: Various potential PET-apoptosis imaging radiopharmaceuticals have been developed to assess the response to cancer treatment. Some of these radiopharmaceuticals showed enhanced uptake in xenografted tumors in mice, but to varying degrees. Two validated radioligands showed favorable characteristics in healthy individuals, but did not significantly affect bone marrow. Further research is needed to evaluate the clinical value of these radiopharmaceuticals for apoptosis imaging in cancer patients.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Ivan Ho Shon, Thomas Hennessy, Jennifer Guille, Michael P. Gotsbacher, Angelina J. Lay, Bruce McBride, Rachel Codd, Philip J. Hogg
Summary: This study evaluates the biodistribution, radiation dosimetry, safety, and tumor uptake of the novel radiopharmaceutical GA-68 ([GA-68] GA-CDI) for imaging multiple forms of cell death. The results demonstrate that GA-68 ([GA-68] GA-CDI) is safe, has low radiation dosimetry, and excellent biodistribution and imaging characteristics. It shows potential advantages over previous radiopharmaceuticals for imaging cell death and has progressed to a proof-of-concept trial.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Review
Neurosciences
Aleksi Kokkonen, Emma A. Honkanen, Daniel T. Corp, Juho Joutsa
Summary: Deep brain stimulation (DBS) is an effective treatment for various brain disorders, but its mechanisms of action and detailed molecular effects still need further investigation.
Review
Chemistry, Inorganic & Nuclear
Sebastien Schmitt, Emmanuel Moreau
Summary: This article reviews all the radiolabeling conditions with chelators used since 2009, aiming to determine the most efficient conditions for the rapid development of future radiotracers. Additionally, it focuses on the limitations of this strategy, particularly in terms of automation.
COORDINATION CHEMISTRY REVIEWS
(2023)
Article
Biology
Benjamin Haenisch, Justine Y. Hansen, Boris C. Bernhardt, Simon B. Eickhoff, Juergen Dukart, Bratislav Misic, Sofie Louise Valk
Summary: This study investigates the role of neurotransmitter transporter and receptor molecules in the structure-function relationships in the human brain. Using positron-emission tomography imaging studies of 19 different neurotransmitter transporters and receptors, the researchers discovered three main spatial gradients of chemoarchitectural similarity in the cortical and subcortical regions of the brain. The findings show that the organization of the receptome shares similarities with functional and structural brain anatomy.
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)