Article
Immunology
Yuhua Shi, Qian Lv, Mengjie Zheng, Hongxiang Sun, Fushan Shi
Summary: INF39 is a specific inhibitor for NLRP3 inflammasome activation, without affecting other inflammasomes. It exerts its anti-inflammatory effect by inhibiting the interaction of NEK7-NLRP3 and other downstream events.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2021)
Article
Biochemistry & Molecular Biology
Yueke Lin, Xiaoting Lv, Caiyu Sun, Yanlin Sun, Min Yang, Dapeng Ma, Weiqiang Jing, Yunxue Zhao, Yeping Cheng, Haocheng Xuan, Lihui Han
Summary: This study reveals a novel regulatory mechanism of NLRP3 via TRIM50 and suggests that modulating TRIM50 might represent a therapeutic strategy for NLRP3-dependent pathologies.
Review
Immunology
Fang Hua, Lingli Shi, Peng Zhou
Summary: Inflammatory infiltration is a factor in the development of cardiovascular diseases (CVDs), and the NLRP3 inflammasome is involved in several types of CVDs. Inhibiting the activity of the NLRP3 inflammasome can hinder the progress of CVDs. This article summarizes 20 phenols and terpenoids for the treatment of CVDs based on the inhibition of the NLRP3 inflammasome, identifying salvianolic acid B, ellagic acid, oridonin, and triptolide as potential agents for future NLRP3 inflammasome inhibitors or lead compounds.
INFLAMMOPHARMACOLOGY
(2022)
Review
Immunology
Wanyi Huang, Ziqi Zhang, Yueyang Qiu, Yuan Gao, Yongqiang Fan, Qiang Wang, Qing Zhou
Summary: Implant surgery triggers inflammatory reactions that impact postoperative outcomes. The inflammasome has a crucial role in inflammation, inducing pyroptosis and producing interleukin-1 beta. The activation of the inflammasome in bone healing after implant surgery needs to be studied. Research has focused on metal-induced NLRP3 inflammasome activation due to the prominence of metals as implant materials. This review consolidates knowledge on NLRP3 inflammasome structures, activation mechanisms, and metal-induced NLRP3 inflammasome activation.
FRONTIERS IN IMMUNOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Yi Sun, Shuzhe Ding
Summary: The study investigates the link between diabetic cardiomyopathy (DCM) and NLRP3 inflammasome, indicating that NLRP3 inflammasome-mediated inflammatory response exacerbates DCM. Exercise training plays an important role in alleviating DCM.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Cell Biology
Na Lu, Weijia Cheng, Dongling Liu, Gang Liu, Can Cui, Chaoli Feng, Xianwei Wang
Summary: NLRP3 inflammasome is a crucial part of the body's immune system, and its overactivation has been linked to inflammatory responses and atherosclerosis. Therefore, finding specific inhibitors for NLRP3 inflammasome has become a potential target for clinical treatment.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Jie Shi, Yang Xia, Huihong Wang, Zhongjie Yi, Ruoruo Zhang, Xiufeng Zhang
Summary: This study identifies Piperlongumine (PL) as a natural inhibitor of Nod-like receptor family pyrin domain-containing protein-3 (NLRP3) inflammasome, which blocks NLRP3 activity by disrupting its assembly, thereby exerting anti-inflammatory effects.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Immunology
Saba Bakhshi, Saeedeh Shamsi
Summary: Evidence suggests that NLRP3 is involved in various inflammatory and autoimmune diseases, and inhibition of NLRP3 can be a useful treatment option. MCC950, a small molecule, can specifically inhibit NLRP3 and reduce the production of proinflammatory cytokines.
INTERNATIONAL IMMUNOPHARMACOLOGY
(2022)
Review
Immunology
Seungwha Paik, Jin Kyung Kim, Prashanta Silwal, Chihiro Sasakawa, Eun-Kyeong Jo
Summary: This review article discusses the molecular details of NLRP3 inflammasome activation, focusing on priming/licensing and assembly steps, as well as protein-protein interactions, posttranslational modifications, and spatiotemporal regulation of the NLRP3 inflammasome machinery. Multiple positive and/or negative regulatory pathways providing upstream signals for NLRP3 inflammasome complex assembly are also summarized, with the ultimate goal of developing methods for the prevention and treatment of NLRP3 inflammasome-related diseases.
CELLULAR & MOLECULAR IMMUNOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Sophie Coyle, Mohammed Naeem Khan, Melody Chemaly, Breedge Callaghan, Chelsey Doyle, Colin E. Willoughby, Sarah D. Atkinson, Meredith Gregory-Ksander, Victoria McGilligan
Summary: Glaucoma is a group of optic neuropathies characterized by the degeneration of retinal ganglion cells, with increased intraocular pressure and inflammation playing potential roles. Targeting the NLRP3 inflammasome as a therapeutic strategy may help protect vision in glaucoma patients.
Review
Pharmacology & Pharmacy
Pablo Pelegrin
Summary: ATP plays an essential role in cellular energetics and signaling. Extracellular ATP in inflammatory environments activates immune cells through P2X7 receptor, leading to the formation of inflammasomes and inflammatory cell death. Research on novel anti-inflammatory therapies targeting P2X7 receptor and NLRP3 pathway is ongoing.
BIOCHEMICAL PHARMACOLOGY
(2021)
Article
Chemistry, Multidisciplinary
Hao-yu Wang, Xi Lin, Guan-gen Huang, Rong Zhou, Shu-yue Lei, Jing Ren, Kai-rong Zhang, Chun-lan Feng, Yan-wei Wu, Wei Tang
Summary: This study shows that Atranorin, a secondary metabolite of lichen family, effectively inhibits NLRP3 inflammasome activation in macrophages and dendritic cells. It binds to ASC protein directly and restricts ASC oligomerization, leading to the suppression of cytokine secretion and cell pyroptosis. Atranorin exhibits therapeutic effects in various NLRP3 inflammasome-driven diseases.
ACTA PHARMACOLOGICA SINICA
(2023)
Article
Immunology
Asta Luciunaite, Indre Dalgediene, Rapolas Zilionis, Kristina Masalaite, Milda Norkiene, Andrius Sinkunas, Alma Gedvilaite, Indre Kucinskaite-Kodze, Aurelija Zvirbliene
Summary: This study investigates the effect of viral oligomeric proteins on the inflammatory response in macrophages. It finds that filamentous proteins do not induce inflammation, while spherical proteins mediate an inflammatory response and activate the NLRP3 inflammasome.
FRONTIERS IN IMMUNOLOGY
(2022)
Editorial Material
Cell Biology
Liqiu Wang, Jun Cui
Summary: NLRP3 senses pathogens and danger signals to initiate innate immune responses through forming inflammasomes. Dysregulation of NLRP3 inflammasomes contributes to various inflammatory disorders. Mechanisms that prevent sustained NLRP3 inflammasome activation, such as ZDHHC12-mediated palmitoylation and chaperone-mediated autophagy, have been identified. Gain-of-function variants of NLRP3 in autoinflammatory diseases lead to excessive NLRP3 inflammasome activation by impairing NLRP3 palmitoylation and chaperone-mediated autophagic degradation.
Review
Immunology
Panpan Chang, Hao Li, Hui Hu, Yongqing Li, Tianbing Wang
Summary: Autophagy plays a role in defending against harmful stimuli and degrading cellular components, while dysfunction in this process is linked to various diseases. Recent research has highlighted the crucial involvement of NLRP3 inflammasomes in the innate immune response, with a focus on their impact on cytokine secretion and pyroptosis. Additionally, the interplay between autophagy and NLRP3 inflammasome presents a complex relationship that affects host defenses and inflammation, although further understanding is needed.
FRONTIERS IN IMMUNOLOGY
(2021)
Article
Cardiac & Cardiovascular Systems
Marina Pascual Izco, Rafael Ramirez-Carracedo, Ignacio Hernandez Navarro, Alvaro Osorio Ruiz, Borja Castejon Navarro, Irene Cuadrado Berrocal, Carlota Largo Aramburu, Gonzalo Luis Alonso Salinas, Javier Diez, Marta Saura Redondo, Jose Luis Zamorano, Carlos Zaragoza, Marcelo Sanmartin
CARDIOLOGY JOURNAL
(2020)
Article
Chemistry, Medicinal
Laura Gonzalez-Cofrade, Irene Cuadrado, Angel Amesty, Ana Estevez-Braun, Beatriz de las Heras, Sonsoles Hortelano
Summary: The study demonstrates that DIH effectively inhibits NLRP3 inflammasome activation in macrophages, showing potential application in treating inflammation-related diseases.
Article
History
Beatriz de las Heras
Summary: Cinema is not just an art form, but also a tool for expressing emotions and conveying information. The avant-garde films of the interwar period were not only aesthetically groundbreaking, but also served as a means of expressing the desire for change in a collapsing modern society. Today, these films have become valuable sources of knowledge that allow us to explore and understand the history of that era.
Article
Chemistry, Medicinal
Irene Cuadrado, Sandra Oramas-Royo, Laura Gonzalez-Cofrade, Angel Amesty, Sonsoles Hortelano, Ana Estevez-Braun, Beatriz de las Heras
Summary: A series of new labdane conjugates were synthesized and showed cardioprotective effects against doxorubicin-induced cardiotoxicity by inhibiting oxidative stress-mediated signaling pathways and autophagy mediated by Akt activation.
DRUG DEVELOPMENT RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Laura Gonzalez-Cofrade, Jack P. Green, Irene Cuadrado, Angel Amesty, Sandra Oramas-Royo, David Brough, Ana Estevez-Braun, Sonsoles Hortelano, Beatriz de las Heras
Summary: This study evaluated the potential anti-inflammatory activity of phenolic and quinonemethide nor-triterpenes isolated from Maytenus retusa and their derivatives through inhibition of the NLRP3 inflammasome. Triterpenes 6 and 14 showed the highest anti-inflammatory activity by significantly reducing caspase-1 activity, IL-1 beta secretion, and pyroptosis. Further characterization confirmed their selective inhibition of NLRP3 inflammasome without affecting AIM2 or NLRC4 inflammasome activation.
BIOORGANIC CHEMISTRY
(2023)
Article
Plant Sciences
Pedro Martin-Acosta, Irene Cuadrado, Laura Gonzalez-Cofrade, Roberto Pestano, Sonsoles Hortelano, Beatriz de las Heras, Ana Estevez-Braun
Summary: A set of new dihydroquinoline embelin derivatives were synthesized from the reaction of natural benzoquinone embelin with anilines and aromatic aldehydes in the presence of AgOTf. The resulting compounds showed potential as cardioprotective agents, attenuating the cardiotoxicity effect of doxorubicin on oxidative stress and apoptosis. The best activities were achieved with quinoline-embelin derivatives having a 4-nitrophenyl group attached at the pyridine ring.
JOURNAL OF NATURAL PRODUCTS
(2023)
Article
Biology
Andrea Perez-Montero, Oscar Zaragoza, Alfonso Luque, Sonsoles Hortelano, Paloma Acebo
Summary: Lipid droplets (LD) are important lipid storage organelles with multiple biological functions. Fluorescence imaging is commonly used to visualize LD, but it can cause damage and alter organelle dynamics. This study presents a label-free method using 3D holotomographic microscopy to visualize LD accumulation in MH-S alveolar macrophages treated with oleic acid.
Meeting Abstract
Respiratory System
S. Barril, D. Castillo, P. Millan, A. Luque, P. Acebo, S. Hortelano
EUROPEAN RESPIRATORY JOURNAL
(2022)
Article
Pharmacology & Pharmacy
Paola Orlandi, Marta Banchi, Francesca Vaglini, Marco Carli, Stefano Aringhieri, Arianna Bandini, Carla Pardini, Cristina Viaggi, Michele Lai, Greta Ali, Alessandra Ottani, Eleonora Vandini, Patrizia Guidi, Margherita Bernardeschi, Veronica La Rocca, Giulio Francia, Gabriella Fontanini, Mauro Pistello, Giada Frenzilli, Daniela Giuliani, Marco Scarselli, Guido Bocci
Summary: This study investigates the role of MC4R in melanoma and the use of the selective antagonist ML in combination with vemurafenib. The results show that ML can inhibit melanoma cell proliferation and induce apoptosis through the inhibition of ERK1/2 phosphorylation and reduction of BCL-XL expression. The combination of vemurafenib and ML exhibits a synergistic effect in vitro and inhibits tumor growth in vivo without causing adverse effects.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Conor J. Bloxham, Katina D. Hulme, Fabrizio Fierro, Christian Fercher, Cassandra L. Pegg, Shannon L. O'Brien, Simon R. Foster, Kirsty R. Short, Sebastian G. B. Furness, Melissa E. Reichelt, Masha Y. Niv, Walter G. Thomas
Summary: Bitter taste receptors (T2Rs) are a type of G protein-coupled receptors that allow humans to detect aversive and toxic substances. This study characterized the functional properties of previously identified T2Rs in human cardiac tissues and their naturally occurring polymorphisms. The results showed differences in signaling among different T2R variants, and revealed a potential association between the T2R50 Tyr203 variant and cardiovascular disease.
BIOCHEMICAL PHARMACOLOGY
(2024)
Article
Pharmacology & Pharmacy
Lu Chen, Huanying Shi, Wenxin Zhang, Yongjun Zhu, Haifei Chen, Zimei Wu, Huijie Qi, Jiafeng Liu, Mingkang Zhong, Xiaojin Shi, Tianxiao Wang, Qunyi Li
Summary: This study demonstrates that Carfilzomib exhibits potent anti-tumor activity against esophageal squamous cell carcinoma (ESCC) by triggering mitochondrial apoptosis and reprogramming cellular metabolism. It has been identified that activating transcription factor 3 (ATF3) plays a crucial role as a cellular target in ESCC cells treated with Carfilzomib. Overexpression of ATF3 effectively counteracts the effects of Carfilzomib on ESCC cell proliferation, apoptosis, and metabolic reprogramming. Furthermore, ATF3 mediates the anti-tumor activity of Carfilzomib, suggesting its potential as a therapeutic agent for ESCC.
BIOCHEMICAL PHARMACOLOGY
(2024)
Review
Pharmacology & Pharmacy
Xing Zhang, Xiang Li, Ran Xia, Hong-Sheng Zhang
Summary: This review summarizes recent progress on the mechanisms of ferroptosis resistance in cancer and highlights the role of redox status and metabolism. Combination therapy for ferroptosis has great potential in treating resistant malignant tumors.
BIOCHEMICAL PHARMACOLOGY
(2024)
