Article
Chemistry, Medicinal
Carlotta Granchi, Giulia Bononi, Rebecca Ferrisi, Eleonora Gori, Giulia Mantini, Sandra Glasmacher, Giulio Poli, Stefano Palazzolo, Isabella Caligiuri, Flavio Rizzolio, Vincenzo Canzonieri, Tiziana Perin, Juerg Gertsch, Andrea Sodi, Elisa Giovannetti, Marco Macchia, Filippo Minutolo, Tiziano Tuccinardi, Andrea Chicca
Summary: The manuscript expands and optimizes the class of benzoylpiperidine-based MAGL inhibitors, which selectively inhibit MAGL against other components of the endocannabinoid system. Experimental results demonstrate the potential use of these compounds as anticancer agents.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Giulia Bononi, Giacomo Tonarini, Giulio Poli, Ivana Barravecchia, Isabella Caligiuri, Marco Macchia, Flavio Rizzolio, Gian Carlo Demontis, Filippo Minutolo, Carlotta Granchi, Tiziano Tuccinardi
Summary: Research has shown that the enzyme monoacylglycerol lipase (MAGL) is involved in various pathological conditions, encouraging the development of new MAGL modulators. Newly developed compounds exhibit potential anticancer activity.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Medicinal
Giulia Bononi, Giulio Poli, Flavio Rizzolio, Tiziano Tuccinardi, Marco Macchia, Filippo Minutolo, Carlotta Granchi
Summary: This review discusses patents related to new MAGL inhibitors and their potential therapeutic applications published since 2018. In the years 2018-2020, several known chemical scaffolds of MAGL inhibitors have been further optimized and developed, along with the identification of new chemical classes as MAGL inhibitors. The focus on MAGL-specific PET ligands in scientific publications and efforts from pharmaceutical companies and academic groups demonstrate the rapid growth in this research area.
EXPERT OPINION ON THERAPEUTIC PATENTS
(2021)
Article
Radiology, Nuclear Medicine & Medical Imaging
Keisuke Takahata, Chie Seki, Yasuyuki Kimura, Manabu Kubota, Masanori Ichise, Yasunori Sano, Yasuharu Yamamoto, Kenji Tagai, Hitoshi Shimada, Soichiro Kitamura, Kiwamu Matsuoka, Hironobu Endo, Hitoshi Shinotoh, Kazunori Kawamura, Ming-Rong Zhang, Yuhei Takado, Makoto Higuchi
Summary: This study demonstrates the first visualization of MAGL in the human brain using the novel PET ligand F-18-T-401. The results confirm the reliability of F-18-T-401-PET for quantification and stability analysis of MAGL in vivo.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
(2022)
Article
Gastroenterology & Hepatology
Manon Allaire, Rola Al Sayegh, Morgane Mabire, Adel Hammoutene, Matthieu Siebert, Charles Caer, Mathilde Cadoux, Jinghong Wan, Aida Habib, Maude Le Gall, Pierre de la Grange, Herve Guillou, Catherine Postic, Valerie Paradis, Sophie Lotersztajn, Helene Gilgenkrantz
Summary: This study investigates the role of monoacylglycerol lipase (MAGL) in liver regeneration. Using in vitro and in vivo models, the researchers found that MAGL expression in hepatocytes and macrophages has a significant impact on the liver regeneration process. Inhibition of MAGL leads to reduced hepatocyte proliferation and delays liver regeneration.
Article
Multidisciplinary Sciences
Rantaro Kamimura, Mohammad Zakir Hossain, Kojiro Takahashi, Isao Saito, Junichi Kitagawa
Summary: The study demonstrated that preventing the degradation of endocannabinoid 2-AG may help alleviate neuropathic orofacial pain by suppressing microglial reactivity in the trigeminal spinal subnucleus caudalis (Vc) under neuropathic pain conditions.
Article
Biochemistry & Molecular Biology
Tuo Shao, Zhen Chen, Ran Cheng, Lee Collier, Lee Josephson, Raymond T. Chung, Steven H. Liang
Summary: Hepatocellular carcinoma (HCC) is a prevalent liver malignancy with poor prognosis. This study aimed to visualize the expression and activity of hepatic monoacylglycerol lipase (MAGL) in HCC cells and patients' samples using positron emission tomography (PET) imaging. The results showed higher MAGL expression levels in HCC cells compared to normal liver cells. Additionally, HCC patients also exhibited increased uptake of the MAGL radio-ligand, suggesting its potential as an effective PET ligand for HCC diagnosis.
BIOORGANIC CHEMISTRY
(2022)
Article
Pharmacology & Pharmacy
Muhammad Adeel, Gloria Saorin, Giacomo Boccalon, Andrea Augusto Sfriso, Salvatore Parisi, Isabella Moro, Stefano Palazzolo, Isabella Caligiuri, Carlotta Granchi, Giuseppe Corona, Maja Cemazar, Vincenzo Canzonieri, Tiziano Tuccinardi, Flavio Rizzolio
Summary: The MAGL inhibitor MAGL23 was formulated into nanocrystals coated with albumin to improve solubility and maintain potency in cancer cell lines. The system showed enhanced therapeutic window and favorable biodistribution in in vivo studies.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Article
Cell Biology
Xiaohong Ma, Min Xia, Lina Wei, Kui Guo, Rui Sun, Yao Liu, Chunping Qiu, Jie Jiang
Summary: This study found that MGLL is highly expressed in progesterone resistant endometrial adenocarcinoma samples. Overexpression of MGLL promotes tumor growth, metastasis, and progesterone resistance, while silencing MGLL inhibits tumor growth, metastasis, and reverses progesterone resistance.
CELL DEATH & DISEASE
(2022)
Article
Pharmacology & Pharmacy
Mei Yu, Chris Gordon, Keith Studholme, Mariam Hassan, Faisal Sadar, Ayesha Khan, James Nicholson, David E. Komatsu, Martin Kaczocha
Summary: This study examines the expression of monoacylglycerol lipase (MAGL) and cyclooxygenase-2 (COX-2) in knee osteochondral tissue of patients with osteoarthritis (OA). The results show that MAGL is expressed throughout arthritic cartilage and subchondral bone, and there is potential crosstalk between MAGL and COX-2. This crosstalk may play a role in the development and maintenance of OA pain.
CANNABIS AND CANNABINOID RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Ran Cheng, Masayuki Fujinaga, Jing Yang, Jian Rong, Ahmed Haider, Daisuke Ogasawara, Richard S. Van, Tuo Shao, Zhen Chen, Xiaofei Zhang, Erick R. Calderon Leon, Yiding Zhang, Wakana Mori, Katsushi Kumata, Tomoteru Yamasaki, Lin Xie, Shaofa Sun, Lu Wang, Chongzhao Ran, Yihan Shao, Benjamin Cravatt, Lee Josephson, Ming-Rong Zhang, Steven H. Liang
Summary: MAGL is a key enzyme involved in regulating endocannabinoid balance by degrading 2-AG, and selective inhibition of it may have therapeutic implications for various pathologies. A reversible and peripheral-specific radiofluorinated MAGL PET ligand has been developed, showing exceptional specificity and selectivity in BAT, providing a non-invasive imaging tool for studying the role of BAT in ECS-related pathologies.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Biochemistry & Molecular Biology
Feifan Zhang, Dong Yang, Jingchen Li, Cuilian Du, Xinran Sun, Wanru Li, Fengwei Liu, Yiwei Yang, Yuhong Li, Lei Fu, Rena Li, Claire Xi Zhang
Summary: This study reveals the function of synaptotagmin-11 (Syt11) in microglial immune responses. Syt11 inhibits cytokine release through interactions with vps10p-tail-interactor-1a (vti1a) and vti1b.
JOURNAL OF NEUROCHEMISTRY
(2023)
Article
Endocrinology & Metabolism
Yasushi Hattori, Chie Seki, Jun Maeda, Yuji Nagai, Kazunobu Aoyama, Ming-Rong Zhang, Takafumi Minamimoto, Tatsuki Koike, Makoto Higuchi
Summary: The study established an analytical method to quantify MAGL availability and occupancy by an exogenous inhibitor in rhesus monkey brains using [F-18]T-401-PET. Pretreatment of monkeys with JW642 resulted in a dose-dependent reduction of [F-18]T-401 retentions in the brain and V-T. Lassen's graphical analysis indicated a V-ND of 0.69 mL/cm(3) and a plasma JW642 concentration of 126 ng/mL for inhibiting specific binding by 50%.
JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM
(2022)
Review
Neurosciences
Shivanshu Bajaj, Shreshta Jain, Preeti Vyas, Sandhya Bawa, Divya Vohora
Summary: Alzheimer's disease is a neurodegenerative disease with potential therapeutic targets in the endocannabinoid system. Inhibitors of monoacylglycerol (MAGL) and fatty acid amide hydrolase (FAAH) possess multi-faceted properties for the treatment of Alzheimer's disease.
BRAIN RESEARCH BULLETIN
(2021)
Article
Chemistry, Multidisciplinary
Shiuan-Haur Su, Yujing Song, Michael W. Newstead, Tao Cai, MengXi Wu, Andrew Stephens, Benjamin H. Singer, Katsuo Kurabayashi
Summary: The digital Phenoplate (dPP) is an integrated platform that allows ultra-sensitive measurement of cellular cytokine secretory profiles, making it suitable for high precision and high throughput characterization of cellular phenotypes.
Article
Biochemistry & Molecular Biology
Soojung Hahn, Gyuri Kim, Sang-Man Jin, Jae Hyeon Kim
Summary: This study utilized three-dimensional intestinal organoids to investigate the effects of metformin on inflammatory bowel disease (IBD) and found that metformin can enhance intestinal barrier function and reduce levels of inflammatory cytokines.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
V. V. Sudarev, M. S. Gette, S. V. Bazhenov, O. M. Tilinova, E. V. Zinovev, I. V. Manukhov, A. I. Kuklin, Yu. L. Ryzhykau, A. V. Vlasov
Summary: This study investigated the self-assembly processes of ferritin-based protein complexes and obtained structurally characterized oligomeric states. These results provide new potential and opportunities for the application of ferritin in various fields.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Yalda Sabaghi, Farnaz Pourfarzad, Leila Zolghadr, Azita Bahrami, Tahereh Shojazadeh, Alireza Farasat, Nematollah Gheibi
Summary: p-Coumaric acid (p-CA) is a plant compound with anti-cancer activities. This study designed a nano-liposomal carrier containing p-CA to enhance its effectiveness against melanoma cells. The findings showed that the liposomal form of p-CA had a greater impact on the cells. Kinetic modeling indicated that the best fitting model was zero-order.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
M. D. Nazmul Hasan, Md Mahfuzur Rahman, Al Asmaul Husna, Nobuhiro Nozaki, Osamu Yamato, Naoki Miura
Summary: This study investigated the expression of ncRNAs other than miRNAs in different histologic subtypes of canine mammary gland tumors (MGT). Three aberrantly expressed ncRNAs were identified as potential biomarkers for differentiating MGT subtypes. YRNA and tRFs expression levels were found to be decreased in metastatic compared to primary MGT cell lines.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Seine A. Shintani
Summary: In this study, the researchers used signal analysis to study the instantaneous amplitude and phase of sarcomeric oscillations in skeletal muscle. They identified two types of oscillations, sarcomeric oscillations and sarcosynced oscillations, and visualized their behavior during propagating waves. The researchers discovered the presence of sarcomeric defect holes and sarcomeric collision holes, which are important indicators for understanding the oscillation properties of sarcomeres. This finding has important implications for improving our understanding of muscle function and its regulatory mechanisms.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Shuanglin Zhang, Yuzhong Jia, Guolan Ma, Yanyan Yang, Zhenzhen Cao, Antao Luo, Zefu Zhang, Shihan Li, Jie Wen, Hanfeng Liu, Jihua Ma
Summary: Bupleurum is an antiarrhythmic agent that may exert its effects by inhibiting L-type calcium channels.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Tomotaka Ohkubo, Yasuhiko Matsumoto, Hiroaki Sasaki, Kaoru Kinoshita, Yuki Ogasawara, Takashi Sugita
Summary: This study found that Citrobacter koseri inhibits the growth of Staphylococcus epidermidis, disrupting the balance between S. epidermidis and Staphylococcus aureus, and exacerbating inflammation in atopic dermatitis.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Toshifumi Asano, Philipp Sasse, Takao Nakata
Summary: A Cre recombination-based fluorescent reporter system was developed to monitor cell-cell fusion. The system successfully detected the formation of multinuclear myotubes and placental syncytiotrophoblast. This tool could facilitate the study of cell-to-cell fusion.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Ke Shi, Yunlong Shan, Xiao Sun, Kuida Chen, Qiong Luo, Qiang Xu
Summary: This study found that low expression of TP53INP2 is associated with poor survival in colorectal cancer (CRC) patients. As the malignancy of CRC progresses, TP53INP2 expression gradually decreases. Knockdown of TP53INP2 promotes CRC cell proliferation and tumor growth. Mechanistically, TP53INP2 deficiency decreases phosphorylation of beta-catenin, leading to increased accumulation and enhanced nuclear translocation and transcriptional activity. Additionally, TP53INP2 sequesters TIM50, inhibiting its activation of beta-catenin. In conclusion, downregulation of TP53INP2 promotes CRC progression by activating beta-catenin.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Martina Rossi, Fabio Tomaselli, Alejandro Hochkoeppler
Summary: Oligomeric enzymes are known for their higher catalytic rates compared to monomeric enzymes, but the extent of additivity in their activity is still not well understood. This study used tetrameric rabbit lactate dehydrogenase as a model to examine the kinetics of its catalytic action. Surprisingly, when the concentration of the limiting reactant exceeded that of a single subunit, there was a significant slowdown in the enzyme's conformational rearrangements.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Amin Sahraei, Mohammad Javad Shamsoddini, Fakhrossadat Mohammadi, Leila Hassani
Summary: This study explored the inhibitory effects of gallium curcumin, indium curcumin, and vanadyl curcumin on the amyloid fibrillation of hen egg white lysozyme, as well as the binding interactions of these metal complexes with the enzyme. The results showed that indium curcumin and vanadyl curcumin exhibited higher binding affinities and stronger inhibitory effects on amyloid fibrillation compared to gallium curcumin.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Takahiro Sasaki, Yoshiki Kuse, Shinsuke Nakamura, Masamitsu Shimazawa
Summary: PGRN deficiency plays a significant role in cardiac remodeling and arrhythmias post-myocardial infarction (MI), potentially by promoting metabolic abnormalities in macrophages.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Hongwei Zhao, Yiqiang Li, Yibo Zhang, Chi Zhang
Summary: Electrical brain stimulation technology is commonly used to treat brain neurological disorders, but it can cause side effects. This study investigated the impact of electric fields on nerve fibers and revealed the possible origin of side effects. The findings provide guidance for selecting electrical parameters in clinical stimulation therapy.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Julia S. Scott, Lake-Ee Quek, Andrew J. Hoy, Johannes V. Swinnen, Zeyad D. Nassar, Lisa M. Butler
Summary: The fatty acid elongation enzyme ELOVL5 plays a critical role in promoting metastasis in prostate cancer. Knocking down ELOVL5 leads to the accumulation of malonyl-CoA, which inhibits fatty acid oxidation in mitochondria. This study highlights the importance of fatty acid elongation in regulating cell viability and provides a potential target for prostate cancer treatment.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)
Article
Biochemistry & Molecular Biology
Zan Zhou, Wen-jun Jiang, Li Li, Jun-qiang Si
Summary: This study investigates the effect of noise exposure on cognitive function in mice and explores the underlying molecular mechanisms. The findings suggest that noise exposure leads to increased inflammation, increased phosphorylation of Tau protein, and decreased levels of postsynaptic density protein, resulting in cognitive impairment.
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS
(2024)