Article
Oncology
Yang Chen, Jingya Han, Yan Zhao, Xinming Zhao, Mengmeng Zhao, Jingmian Zhang, Jianfang Wang
Summary: This study proposes an imaging method for assessing FGFR1 expression, utilizing [18F]F-FGFR1 as a peptide probe. In vitro and in vivo experiments demonstrate that [18F]F-FGFR1 shows high stability, affinity, specificity, and good imaging capacity in FGFR1-overexpressing tumors.
FRONTIERS IN ONCOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Natalia Porebska, Agata Knapik, Marta Pozniak, Mateusz Adam Krzyscik, Malgorzata Zakrzewska, Jacek Otlewski, Lukasz Opalinski
Summary: FGFR1 is considered an attractive molecular target for anticancer therapies due to its overexpression in various tumor types. By genetically fusing FGF1 to GFPp, a set of GFPp_FGF1 oligomers with improved receptor binding were generated, leading to the development of a stable and highly specific 3xGFPp_FGF1E_LPET_MMAE cytotoxic conjugate. This conjugate exhibited nanomolar affinity for FGFR1 and demonstrated efficient internalization into cancer cells with high FGFR1 expression, showing potential for imaging and targeted therapy of FGFR1-overproducing cancers.
Article
Chemistry, Multidisciplinary
Yi-kuan Wu, Zheng-nan Ren, Sheng-long Zhu, Yun-zhou Wu, Gang Wang, Hao Zhang, Wei Chen, Zhao He, Xian-long Ye, Qi-xiao Zhai
Summary: Sulforaphane may ameliorate lipid metabolism disorders in NAFLD mice by upregulating the FGF21/FGFR1 pathway, making it a promising intervention to treat or relieve NAFLD.
ACTA PHARMACOLOGICA SINICA
(2022)
Article
Cell Biology
Xiuqin Jia, Ming Xin, Juanjuan Xu, Xindong Xiang, Xuan Li, Yuhan Jiao, Lulin Wang, Jingjing Jiang, Feng Pang, Xianzhen Zhang, Jian Zhang
Summary: In this study, the FGFRs inhibitor FIIN-2 was found to inhibit the proliferation, colony formation, and migration of platinum-resistant LUAD cells while inducing mitochondria-mediated apoptosis. Furthermore, FIIN-2 was shown to enhance autophagy flux in these cells, suggesting its potential as a treatment strategy for LUAD, especially in combination with autophagy inhibitors.
CELL DEATH & DISEASE
(2022)
Article
Genetics & Heredity
Shengru Wang, Xiran Chai, Zihui Yan, Sen Zhao, Yang Yang, Xiaoxin Li, Yuchen Niu, Guanfeng Lin, Zhe Su, Zhihong Wu, Terry Jianguo Zhang, Nan Wu
Summary: The FGFR1 variants identified in this study resulted in only mild disruption to protein function, causing milder skeletal and cardiac phenotypes compared to previous reports.
Article
Oncology
Nawal Alshahrany, Ayesha Begum, Dorit Siebzehnrubl, Ana Jimenez-Pascual, Florian A. Siebzehnrubl
Summary: Glioblastoma, the most lethal brain cancer in adults, is characterized by heterogeneity, therapy resistance, and infiltration. The fibroblast growth factor receptor 1 (FGFR1) signaling pathway plays a role in therapy resistance and cancer stemness. FGFR1 has been found to be associated with poorer survival and tumor invasion in glioblastoma.
Article
Biochemistry & Molecular Biology
Chunsik Lee, Rongyuan Chen, Guangli Sun, Xialin Liu, Xianchai Lin, Chang He, Liying Xing, Lixian Liu, Lasse D. Jensen, Anil Kumar, Harald F. Langer, Xiangrong Ren, Jianing Zhang, Lijuan Huang, Xiangke Yin, JongKyong Kim, Juanhua Zhu, Guanqun Huang, Jiani Li, Weiwei Lu, Wei Chen, Juanxi Liu, Jiaxin Hu, Qihang Sun, Weisi Lu, Lekun Fang, Shasha Wang, Haiqing Kuang, Yihan Zhang, Geng Tian, Jia Mi, Bi-Ang Kang, Masashi Narazaki, Aaron Prodeus, Luc Schoonjans, David M. Ornitz, Jean Gariepy, Guy Eelen, Mieke Dewerchin, Yunlong Yang, Jing-Song Ou, Antonio Mora, Jin Yao, Chen Zhao, Yizhi Liu, Peter Carmeliet, Yihai Cao, Xuri Li
Summary: Although the angiogenic effect of VEGF-B is not well understood, inhibitors of VEGF-B are being used in the treatment of neovascular diseases. In this study, we reveal a previously unrecognized function of VEGF-B as an endogenous inhibitor of angiogenesis by inhibiting the FGF2/FGFR1 pathway. We found that VEGF-B binds to FGFR1, induces FGFR1/VEGFR1 complex formation, suppresses FGF2-induced Erk activation, and inhibits FGF2-driven angiogenesis and tumor growth.
SIGNAL TRANSDUCTION AND TARGETED THERAPY
(2023)
Article
Chemistry, Multidisciplinary
Yu Gu, Songtao Lai, Yang Dong, Hao Fu, Liwei Song, Tianxiang Chen, Yourong Duan, Zhen Zhang
Summary: The study reveals activation of autophagy and FGFR1 signaling pathways in AZD9291 resistant NSCLC, and demonstrates that the pH-sensitive shell-core nanoparticles CP@NP-cRGD can effectively reverse resistance by inducing apoptosis, G0/G1 phase arrest, and downregulation of p-ERK1/2. The coloaded CQ and PD173074 nanoparticle has shown tumor targeting abilities, low toxicity and promising antitumor effects in mouse models, providing a potential novel approach for overcoming AZD9291 resistance in clinical settings.
Article
Biochemistry & Molecular Biology
Lucia Fadiga, Mariana Lavrador, Nuno Vicente, Luisa Barros, Catarina Goncalves, Asma Al-Naama, Luis R. Saraiva, Manuel C. Lemos
Summary: A novel missense mutation in the FGFR1 gene associated with CHH has been identified, expanding the mutational spectrum of this gene and contributing to the understanding of the pathogenesis of CHH.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Review
Oncology
Milind Javle, Gentry King, Kristen Spencer, Mitesh J. Borad
Summary: This review summarizes the preclinical and clinical development of futibatinib, an irreversible FGFR1-4 inhibitor, which has shown promising activity against advanced, refractory cancers with FGFR aberrations. Future directions include exploring mechanisms of resistance and combination therapy approaches.
Article
Oncology
Yunping Hu, Yong Lu, Fei Xing, Wesley Hsu
Summary: This study reveals a mechanism of immune escape in lung cancer, showing that activation of the transcription factor brachyury leads to upregulation of PD-L1, inhibiting T cell proliferation and infiltration. Blocking the FGFR1/MAPK pathway reverses immune suppression and enhances the therapeutic response to anti-PD-1 treatment.
Article
Pharmacology & Pharmacy
Yunhui Xu, Krista L. Denning, Yongke Lu
Summary: FGF21 is mainly regulated by PPARα in liver, providing protection against ALD. While liver-specific FGFR1 abrogation had no effect on ALD, adipose tissues highly express FGFR1. In mice experiments, WY-14,643 inhibits alcoholic fatty liver through FGFR1-dependent regulation of adipose tissue mass and fat mobilization to the liver.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Oncology
Mengdie Hu, Shujun Zhang
Summary: The expression of FGFR1 and FGFR2 may be involved in the development of laryngeal squamous cell carcinoma. There is a moderate positive correlation between FGFR1 and FGFR2 expression in laryngeal SCC. The expressions of FGFR1 and FGFR2 are not associated with tumor characteristics.
TRANSLATIONAL CANCER RESEARCH
(2022)
Article
Pharmacology & Pharmacy
Noof Aloufi, Yoon Namkung, Hussein Traboulsi, Emily T. Wilson, Stephane A. Laporte, Barbara L. F. Kaplan, Matthew K. Ross, Parameswaran Nair, David H. Eidelman, Carolyn J. Baglole
Summary: Cannabis is a commonly used illicit product globally and the second most popular smoking plant after tobacco. This study developed a standardized protocol for generating cannabis smoke extract (CaSE) and investigated its impact on cellular mechanisms in vitro. The results showed that CaSE contains cannabinoids and induces an inflammatory response in human lung fibroblasts.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Medicine, Research & Experimental
Zhang Yang, Shun-Qing Liang, Maria Saliakoura, Haitang Yang, Eric Vassella, Georgia Konstantinidou, Mario Tschan, Balazs Hegedus, Liang Zhao, Yanyun Gao, Duo Xu, Haibin Deng, Thomas M. Marti, Gregor J. Kocher, Wenxiang Wang, Ralph A. Schmid, Ren-Wang Peng
Summary: By combining FGFR1 and PLK1 inhibitors, synergistic cytotoxicity can be achieved in KRAS-mutant tumors, inducing cell death. This treatment induces apoptosis by upregulating ROS and activating the JNK/p38 pathway, while enhancing sensitivity of tumor cells to inhibitors by inhibiting autophagy.
EMBO MOLECULAR MEDICINE
(2021)
Article
Clinical Neurology
Antonio Flores-Burgess, Carmelo Millon, Belen Gago, Laura Garcia-Duran, Noelia Cantero-Garcia, Araceli Puigcerver, Jose Angel Narvaez, Kjell Fuxe, Luis Santin, Zaida Diaz-Cabiale
Summary: The study revealed that GAL(1-15) enhances the antidepressant effects of FLX in a depression animal model, potentially mediated through 5-HT1AR. This opens up the possibility of using a combination of GAL(1-15) and FLX as a novel treatment strategy for depression.
INTERNATIONAL JOURNAL OF NEUROPSYCHOPHARMACOLOGY
(2022)
Editorial Material
Pharmacology & Pharmacy
Dasiel O. Borroto-Escuela, Luca Ferraro, Kjell Fuxe
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Pharmacology & Pharmacy
Dasiel O. Borroto-Escuela, Ramon Fores, Mariana Pita, Miguel A. Barbancho, Pablo Zamorano-Gonzalez, Natalia Garcia Casares, Kjell Fuxe, Manuel Narvaez
Summary: This study assesses the effects of GALR2 and NPYY1R agonists coadministration on sustained memory and hippocampal cell proliferation, suggesting the potential therapeutic benefits for dementia conditions and memory deficits.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Cell Biology
Domenico Nuzzo, Monica Frinchi, Costanza Giardina, Miriana Scordino, Mariachiara Zuccarini, Chiara De Simone, Marta Di Carlo, Natale Belluardo, Giuseppa Mudo, Valentina Di Liberto
Summary: Alzheimer's disease is a multifactorial and age-related neurodegenerative disorder. Its pathogenesis is associated with senile plaques, neurofibrillary tangles, oxidative stress, and neuroinflammation. Current therapies have limited effectiveness, and research on disease-modifying treatments is ongoing. Previous studies have shown that Oxo, a muscarinic acetylcholine receptor agonist, has neurotrophic effects and can modulate oxidative stress and neuroinflammation in the brain. This study investigated the neuroprotective effects of Oxo in an in vitro model of AD, and found that it enhanced cell survival, neurite length, and counteracted DNA fragmentation caused by A beta(1-42) peptide. Oxo treatment also blocked oxidative stress and mitochondrial impairment associated with A beta(1-42) exposure. These results suggest that Oxo could potentially be a novel multi-target drug for treating AD.
CELLULAR AND MOLECULAR NEUROBIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Anna Andrioli, Paolo Francesco Fabene, Giuseppa Mudo, Vincenza Barresi, Valentina Di Liberto, Monica Frinchi, Marina Bentivoglio, Daniele Filippo Condorelli
Summary: This study investigated the expression of neuronal Cx36 and astrocytic Cx30 and Cx43 mRNAs in the brain of rats after pilocarpine-induced status epilepticus (SE). The results showed a significant decrease in Cx43 and Cx30 mRNA levels 24 hours after SE onset in certain brain regions, indicating a potential protective response of neuroglial networks to SE-induced acute damage.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Cell Biology
Jose Erik Alvarez-Contino, Estela Diaz-Sanchez, Marina Mirchandani-Duque, Jose Andres Sanchez-Perez, Miguel A. Barbancho, Alexander Lopez-Salas, Natalia Garcia-Casares, Kjell Fuxe, Dasiel O. Borroto-Escuela, Manuel Narvaez
Summary: This study found that intranasal infusion of GALR2 and Y1R agonists promotes neuroblast proliferation and induces the expression of the neurotrophic factor BDNF in the ventral hippocampus, resulting in antidepressant effects. These effects may be mediated by increased formation of Y1R-GALR2 heteroreceptor complexes. These findings may provide a new approach for the development of novel therapies for major depressive disorder.
JOURNAL OF CELLULAR PHYSIOLOGY
(2023)
Article
Biochemistry & Molecular Biology
Patrizia Ambrogini, Davide Lattanzi, Marica Pagliarini, Michael Di Palma, Stefano Sartini, Riccardo Cuppini, Kjell Fuxe, Dasiel Oscar Borroto-Escuela
Summary: This study investigates the effects of 5HT1AR-FGFR1 complex activation on hippocampal pyramidal neurons and midbrain dorsal raphe serotonergic neurons using an electrophysiological approach. The results show that in normal rats, FGFR1 agonist-induced allosteric action counteracts the ability of 5HT1AR to open GIRK channels, leading to increased neuronal firing. However, in a depression rat model, the change in 5HT1AR caused by FGFR1 does not affect the GIRK channels, except in CA2 neurons. Therefore, the reduced inhibitory ability of FGFR1 on 5HT1AR-mediated GIRK channel opening may be associated with depression.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Biochemistry & Molecular Biology
Miriana Scordino, Monica Frinchi, Giulia Urone, Domenico Nuzzo, Giuseppa Mudo, Valentina Di Liberto
Summary: The differentiation of neural progenitors involves complex regulatory mechanisms that can be modulated by signals such as HSP70 and SOD1. These regulatory mechanisms are crucial for understanding stem cell and cancer research and therapy. In this study, the expression of HSP70 and SOD1 was found to play a role in promoting cell survival and protecting against oxidative stress-induced damage during the differentiation process of SH-SY5Y cells.
Article
Pediatrics
Francisco Manuel Morales-Rodriguez, Juan Pedro Martinez-Ramon, Manuel Alejandro Narvaez Pelaez, Catalda Corvasce
Summary: This research analyzed the sources of school anxiety, coping strategies, and social skills in Italian secondary school students using an artificial neural network. The results showed that cognitive avoidance and behavioral avoidance coping strategies, together with a lack of social skills, contributed the most to school anxiety scores.
Review
Clinical Neurology
Daniel Fonseca-Barriendos, Christian Lizette Frias-Soria, Daniel Perez-Perez, Rosenda Gomez-Lopez, Dasiel O. Borroto Escuela, Luisa Rocha
Summary: Epilepsy affects over 50 million people globally, with one-third suffering from drug-resistant epilepsy (DRE). The therapeutic target hypothesis explains DRE to some extent, but new research suggests that various conditions, such as epigenetic mechanisms and protein-protein interactions, may result in alterations of drug targets, presenting new avenues for controlling DRE.
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)
