Article
Biochemistry & Molecular Biology
Jing Hu, Mengkang Gao, Yang Zhang, Yusui Wang, Zhenrui Qiao, Weiya Zhang, Qiang Wang, Lin Yan, Hai Qian
Summary: In this study, three series of new piperazine urea TRPV1 antagonists were designed, synthesized, and evaluated, among which compound 5ac showed excellent TRPV1 antagonistic activity, good bioavailability, and no hyperthermia side effects. The molecular docking study revealed that compound 5ac interacted well with the amino acid residues on rTRPV1 through hydrophobic interaction, making it an efficient TRPV1 antagonist and a potential candidate for analgesic drug development.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Tatsuya Kida, Nobuaki Takahashi, Masayuki X. Mori, Jiacheng H. Sun, Hideto Oota, Kosuke Nishino, Takashi Okauchi, Yuta Ochi, Daisuke Kano, Ukihide Tateishi, Yasuyoshi Watanabe, Yilong Cui, Yasuo Mori, Hisashi Doi
Summary: TRPV1-targeted compounds were synthesized by modifying the structure of SB366791, and higher antagonistic activities were achieved by avoiding amide-iminol tautomerization. Additionally, explorative PET imaging trials were conducted using labeled derivatives, providing a basis for further applications.
RSC MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Arpad Szallasi
Summary: Today's sedentary lifestyle and poor dietary habits contribute to the increasing prevalence of hypertension, a major risk factor for stroke. Recent research suggests that the activation of TRPV1 receptor by capsaicin, a compound found in chili peppers, can lower blood pressure and potentially be a therapeutic target for hypertensive patients. However, the mechanism of action of capsaicin on blood pressure regulation is more complex than previously understood. Further studies are needed to explore the potential benefits of TRPV1-targeting drugs in treating hypertension.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Chemistry, Medicinal
Jin Mi Kang, Sun Ok Kwon, Jihyae Ann, Sunho Lee, Changhoon Kim, Nayeon Do, Jin Ju Jeong, Peter M. Blumberg, Heejin Ha, Thi Ngoc Lan Vu, Sanghee Yoon, Sun Choi, Robert Frank-Foltyn, Bernhard Lesch, Gregor Bahrenberg, Hannelore Stockhausen, Thomas Christoph, Jeewoo Lee
Summary: The series of 117 2-(halogenated phenyl) acetamide and propanamide analogs were investigated as TRPV1 antagonists, with halogenated phenyl A-region analogs showing a broad functional profile. Antagonists 28 and 92 exhibited potent antagonism against capsaicin for hTRPV1, with antagonist 92 displaying promising analgesic activity in vivo. Molecular modeling of compound 92 suggested that the two fluoro groups in the A-region interacted hydrophobically with the receptor.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Medicinal
Yue Qiao, Yang Zhang, Zhenrui Qiao, Wenya He, Yingda Chen, Depu Song, Guohao Wang, Ning Guo, Lulian Shao, Zhiyong Tian, Qiang Wang, Lin Yan, Hai Qian
Summary: In this study, novel molecules based on the key pharmacophore structures of classic TRPV1 ligands were designed and synthesized, and a potent TRPV1 antagonist with excellent central nervous system penetration and bioavailability was identified. The findings provide a valuable lead for the development of novel TRPV1 antagonists.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Medicine, Research & Experimental
Koki Nagaoka, Takuya Nagashima, Nozomi Asaoka, Hiroki Yamamoto, Chihiro Toda, Gen Kayanuma, Soni Siswanto, Yasuhiro Funahashi, Keisuke Kuroda, Kozo Kaibuchi, Yasuo Mori, Kazuki Nagayasu, Hisashi Shirakawa, Shuji Kaneko
Summary: It was discovered that acetaminophen was able to prevent adverse movement symptoms induced by antipsychotic drugs, and this effect was achieved by activating TRPV1 channels to increase the activity of indirect pathway neurons.
Article
Physiology
Laura Gabriela Nisembaum, Guillaume Loentgen, Thibaut L'Honore, Patrick Martin, Charles-Hubert Paulin, Michael Fuentes, Karine Escoubeyrou, Maria Jesus Delgado, Laurence Besseau, Jack Falcon
Summary: Fish rely on external temperature and photoperiod to regulate their metabolism, physiology, and behavior. Recent studies have found that TRPV1 and TRPV4 channels play a role in regulating melatonin production in Atlantic salmon, possibly in response to temperature changes.
FRONTIERS IN PHYSIOLOGY
(2022)
Article
Immunology
Jeremie Joffre, Erika Wong, Samira Lawton, Elliot Lloyd, Nina Nguyen, Fengyun Xu, Cristina Sempio, Lester Kobzik, Ivana Zlatanova, Mark Schumacher, Jost Klawitter, Hua Su, Katalin Rabl, Kevin Wilhelmsen, Che-Chung Yeh, Judith Hellman
Summary: This study reveals that OLDA has potent anti-inflammatory effects by activating the neuronal TRPV1 and modulating the systemic inflammatory response induced by endotoxemia and infection through a multicellular network.
JOURNAL OF NEUROINFLAMMATION
(2022)
Article
Oncology
Sofia A. Omari, Dominic P. Geraghty, Alhossain A. Khalafallah, Pooja Venkat, Yvette M. Shegog, Scott J. Ragg, Charles E. de Bock, Murray J. Adams
Summary: The ectopic overexpression of TRPV1 has been detected in various solid cancers, and here we show that it is also increased in hematological malignancies. We provide an optimized flow cytometry method to assess TRPV1 protein expression in cell lines and patient samples, and found that TRPV1 is overexpressed in acute monocytic leukemia and multiple myeloma. TRPV1 expression was also observed in B-cell non-Hodgkin's lymphoma, multiple myeloma, and other hematological malignancies.
Article
Medicine, Research & Experimental
Ben Katz, Rachel Zaguri, Simon Edvardson, Channa Maayan, Orly Elpeleg, Shaya Lev, Elyad Davidson, Maximilian Peters, Shlomit Kfir-Erenfeld, Esther Berger, Shifa Ghazalin, Alexander M. Binshtok, Baruch Minke
Summary: This study provides direct evidence in humans for pain-related functional changes linked to TRPV1, a potential target in the development of pain relievers. Two individuals carrying a homozygous missense mutation in TRPV1 demonstrated insensitivity to heat stimulation, elevated pain thresholds, and abnormal responses to a TRPA1 channel activator. These findings highlight the importance of TRPV1 in pain modulation and may contribute to the development of novel pain therapies.
JOURNAL OF CLINICAL INVESTIGATION
(2023)
Article
Multidisciplinary Sciences
Tina Blazevic, Cosmin I. Ciotu, Markus Gold-Binder, Elke H. Heiss, Michael J. M. Fischer, Verena M. Dirsch
Summary: Capsaicin, an active compound of chili peppers, can inhibit platelet-derived growth factor-induced proliferation in primary rat vascular smooth muscle cells (VSMCs), possibly through a role of TRPV1. However, commercially available antibodies were ineffective in detecting TRPV1 expression. Moreover, TRPV1 agonists did not increase intracellular calcium levels in VSMCs. RT-qPCR results showed low TRPV1 expression in VSMCs, suggesting the absence of canonical TRPV1 channel activity.
Article
Neurosciences
Wenting Ma, Matthew R. Sapio, Allison P. Manalo, Dragan Maric, Mary Kate Dougherty, Taichi Goto, Andrew J. Mannes, Michael J. Iadarola
Summary: Primary afferent neurons in the dorsal root ganglia (DRG) play a crucial role in transmitting peripheral nociceptive signals and regulating analgesic control. The coexpression of Trpv1 and Oprm1 in these neurons may explain the remarkable efficacy of opioid drugs administered at the level of the DRG-spinal synapse.
FRONTIERS IN MOLECULAR NEUROSCIENCE
(2022)
Article
Pharmacology & Pharmacy
Ankush M. Korishettar, Yoshinori Nishijima, Zhihao Wang, Yangjing Xie, Juan Fang, David A. Wilcox, David X. Zhang
Summary: TRPV1 channels are expressed in the human vasculature and affect vascular tone of human arterioles when activated. Their vasomotor function is modulated by endothelin-1, partly mediated by protein kinase C.
BRITISH JOURNAL OF PHARMACOLOGY
(2021)
Article
Zoology
Jing Wen, Tingbei Bo, Zhijun Zhao, Dehua Wang
Summary: The study found that TRPV1 and PKA are involved in behavioral thermoregulation in Mongolian gerbils. Activation of TRPV1 with capsaicin resulted in the gerbils exhibiting a preference for lower temperatures and a significant decrease in food intake and non-shivering thermogenesis.
INTEGRATIVE ZOOLOGY
(2022)
Review
Neurosciences
Rodrigo C. Meza, Carlos Ancaten-Gonzalez, Chiayu Q. Chiu, Andres E. Chavez
Summary: This article discusses the roles of TRPV1 in both central and peripheral systems, exploring its regulation of synaptic function and potential therapeutic applications.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2022)
Article
Biochemistry & Molecular Biology
Sarah Hanzen, Katarina Vielfort, Junsheng Yang, Friederike Roger, Veronica Andersson, Sara Zamarbide-Fores, Rebecca Andersson, Lisa Malm, Gael Palais, Benoit Biteau, Beidong Liu, Michel B. Toledano, Mikael Molin, Thomas Nystrom
Review
Biochemistry & Molecular Biology
Pauraic Mc Carron, Aisling Crowley, Denis O'Shea, Malachy McCann, Orla Howe, Mary Hunt, Michael Devereux
CURRENT MEDICINAL CHEMISTRY
(2018)
Review
Biochemistry & Molecular Biology
Mary C. Hunt, Veronika Tillander, Stefan E. H. Alexson
Article
Biochemistry & Molecular Biology
Veronika Tillander, Elisabet Arvidsson Nordstrom, Jenny Reilly, Malgorzata Strozyk, Paul P. Van Veldhoven, Mary C. Hunt, Stefan E. H. Alexson
CELLULAR AND MOLECULAR LIFE SCIENCES
(2014)
Article
Cell Biology
Katarina Vielfort, Niklas Soderholm, Linda Weyler, Daniel Vare, Sonja Lofmark, Helena Aro
JOURNAL OF CELL SCIENCE
(2013)
Article
Multidisciplinary Sciences
Katarina Vielfort, Linda Weyler, Niklas Soderholm, Mattias Engelbrecht, Sonja Lofmark, Helena Aro
Article
Multidisciplinary Sciences
Linda Weyler, Mattias Engelbrecht, Manuel Mata Forsberg, Karl Brehwens, Daniel Vare, Katarina Vielfort, Andrzej Wojcik, Helena Aro
Article
Endocrinology & Metabolism
Annika Ohlsson, Mary Hunt, Anna Wedell, Ulrika von Dobeln
JOURNAL OF INHERITED METABOLIC DISEASE
(2019)
Article
Microbiology
Anna Clara M. Galdino, Livia Viganor, Alexandre A. de Castro, Elaine F. F. da Cunha, Thais P. Mello, Larissa M. Mattos, Marcos D. Pereira, Mary C. Hunt, Megan O'Shaughnessy, Orla Howe, Michael Devereux, Malachy McCann, Teodorico C. Ramalho, Marta H. Branquinha, Andre L. S. Santos
FRONTIERS IN MICROBIOLOGY
(2019)
Article
Multidisciplinary Sciences
Kimberly Filcek, Katarina Vielfort, Samada Muraleedharan, Johan Henriksson, Raphael H. Valdivia, Patrik M. Bavoil, Barbara S. Sixt
Article
Genetics & Heredity
Rebecca Andersson, Anna Maria Eisele-Burger, Sarah Hanzen, Katarina Vielfort, David Oling, Frederik Eisele, Gustav Johansson, Tobias Gustafsson, Kristian Kvint, Thomas Nystrom
Summary: Hsp70 proteins are crucial chaperones in the cellular protein quality control network, with Ssa1 and Ssa2 deficiency in yeast leading to reduced cellular reproduction and accelerated aging. Overproduction of Ssa4 in cells lacking Ssa1/2 can rescue growth, mitigate aggregate formation, and promote protein degradation, indicating the importance of Hsp70 activity for cellular fitness and longevity.
Article
Microbiology
Carlos Nunez-Otero, Wael Bahnan, Katarina Vielfort, Jim Silver, Pardeep Singh, Haitham Elbir, Fredrik Almqvist, Sven Bergstrom, Asa Gylfe
Summary: Chlamydia trachomatis is a strict intracellular bacterium causing sexually transmitted infections and eye infections. 2-Pyridone amides, like KSK213, are potent inhibitors of Chlamydia infectivity, specifically targeting C. trachomatis. The resistance mechanism to KSK213 involves amino acid substitutions in RNA helicase and RNase III, indicating inhibition of transcriptional machinery as the mode of action.
ANTIMICROBIAL AGENTS AND CHEMOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Martina Kulen, Carlos Nunez-Otero, Andrew G. Cairns, Jim Silver, Anders E. G. Lindgren, Emma Wede, Pardeep Singh, Katarina Vielfort, Wael Bahnan, James A. D. Good, Richard Svensson, Sven Bergstrom, Asa Gylfe, Fredrik Almqvist
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)