In silico design of novel probes for the atypical opioid receptor MRGPRX2

Lansu, Katherine, Karpiak, Joel, Liu, Jing, Huang, Xi-Ping, McCorvy, John D, Kroeze, Wesley K, Che, Tao, Nagase, Hiroshi, Carroll, Frank I, Jin, Jian, Shoichet, Brian K, Roth, Bryan L·2017·Nature Chemical Biology

DOI 10.1038/nchembio.2334

Cited by (298)

Items 101–200 of 298

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In silico fragment-based drug design with SEED
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Mast Cell Degranulation and Fibroblast Activation in the Morphine-induced Spinal Mass
Tony L. Yaksh, Kelly A. Eddinger, Shinichi Kokubu, Zhenping Wang, Anna DiNardo, Roshni Ramachandran, Yuelian Zhu, Yajun He, Fieke Weren, Daphne Quang et al. · 2019 · Anesthesiology
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Aleksandra Dondalska, Elin Rönnberg, Haisha Ma, Sandra Axberg Pålsson, Elín Ingibjörg Magnúsdóttir, Tianle Gao, Lucille Adam, Ethan A. Lerner, Gunnar P. Nilsson, Malin Charlotta Lagerström et al. · 2020 · Frontiers in Immunology
Evaluation of Therapies for Peripheral and Neuraxial Opioid-induced Pruritus based on Molecular and Cellular Discoveries
Eileen K. Nguyen, Grace Lim, Sarah E. Ross · 2021 · Anesthesiology
Mas-Related G Protein–Coupled Receptor-X2 and Its Role in Non-immunoglobulin E–Mediated Drug Hypersensitivity
Chalatip Chompunud Na Ayudhya, Hydar Ali · 2022 · Immunology and Allergy Clinics of North America
Opioid toxicity: histamine, hypersensitivity, and MRGPRX2
Brian A. Baldo, Nghia H. Pham · 2022 · Archives of Toxicology
Phenothiazine antipsychotics exhibit dual properties in pseudo-allergic reactions: Activating MRGPRX2 and inhibiting the H1 receptor
Yajing Hou, Delu Che, Di Wei, Cheng Wang, Yitong Xie, Kaining Zhang, Jiao Cao, Jia Fu, Nan Zhou, Huaizhen He · 2019 · Molecular Immunology
A Mast Cell–Specific Receptor Is Critical for Granuloma Induced by Intrathecal Morphine Infusion
Tao Zhang, Rui Liu, Delu Che, Priyanka Pundir, Nan Wang, Shengli Han, Jiao Cao, Yanni Lv, Haiyan Dong, Fang Fang et al. · 2019 · The Journal of Immunology
Ligands and Signaling of Mas-Related G Protein-Coupled Receptor-X2 in Mast Cell Activation
Yan‐ni Mi, Na-Na Ping, Yong‐Xiao Cao · 2020 · Reviews of physiology, biochemistry and pharmacology
P17 induces chemotaxis and differentiation of monocytes via MRGPRX2-mediated mast cell–line activation
Karthi Duraisamy, Kailash Singh, Mukesh Kumar, Benjamin Lefranc, Elsa Bonnafé, Michel Treilhou, Jérôme Leprince, Bkc Chow · 2021 · Journal of Allergy and Clinical Immunology
Allergic and other adverse reactions to drugs used in anesthesia and surgery
Brian A. Baldo · 2023 · Anesthesiology and Perioperative Science
The Polyanalgesic Consensus Conference (PACC)®: Updates on Clinical Pharmacology and Comorbidity Management in Intrathecal Drug Delivery for Cancer Pain
Timothy Ray Deer, Salim Michel Hayek, Jay S. Grider, Jason E. Pope, Shane E. Brogan, Amitabh Gulati, Jonathan Michael Hagedorn, Natalie H. Strand, Jennifer M. Hah, Tony L. Yaksh et al. · 2024 · Neuromodulation Technology at the Neural Interface
Association between mutated Mas-related G protein-coupled receptor-X2 and rocuronium-induced intraoperative anaphylaxis
Yasuyuki Suzuki, Shuang Liu, Fumito Kadoya, Yasushi Takasaki, Toshihiro Yorozuya, Masaki Mogi · 2020 · British Journal of Anaesthesia
MRGPRX2 activation in mast cells by neuromuscular blocking agents and other agonists: Modulation by sugammadex
Nithya A. Fernandopulle, Stephanie S Zhang, Paul Soeding, Graham A. Mackay · 2020 · Clinical & Experimental Allergy
Structure-Based Design of a Chemical Probe Set for the 5-HT 5A Serotonin Receptor
Anat Levit Kaplan, Ryan T. Strachan, João M. Bráz, Veronica Craik, Samuel T. Slocum, Thomas J. Mangano, Vanessa Amabo, Henry R. O’Donnell, Parnian Lak, Allan I. Basbaum et al. · 2022 · Journal of Medicinal Chemistry
Recent Trends and Applications of Molecular Modeling in GPCR–Ligand Recognition and Structure-Based Drug Design
Xiaojing Yuan, Yechun Xu · 2018 · International Journal of Molecular Sciences
Murepavadin, a Small Molecule Host Defense Peptide Mimetic, Activates Mast Cells via MRGPRX2 and MrgprB2
Aetas Amponnawarat, Chalatip Chompunud Na Ayudhya, Hydar Ali · 2021 · Frontiers in Immunology
β-arrestin-1 and β-arrestin-2 Restrain MRGPRX2-Triggered Degranulation and ERK1/2 Activation in Human Skin Mast Cells
Zhao Wang, Zhuoran Li, Gürkan Bal, Kristin Franke, Torsten Zuberbier, Magda Babina · 2022 · Frontiers in Allergy
Basophil Activation Experiments in Immediate Drug Hypersensitivity: More Than a Diagnostic Aid
Didier Gaston Ebo, Jessy Elst, Athina Ludovica Van Gasse, Leander P. De Puysseleyr, Margaretha Antje Faber, Margo Maria Hagendorens, Cristobalina Mayorga, Christel H. Mertens, Chris H. Bridts, Luc S. De Clerck et al. · 2020 · Methods in molecular biology
Clinical Practice Guidelines for Diagnosis and Management of Hypersensitivity Reactions to Quinolones
Inmaculada Doña, Natalia Blanca‐López, Cosmin Boteanu, Begoña Cueva Oliver, Javier Fernández, Pablo Gajate, M. C Garcia-Aviles, Ignacio García-Núñez, Teófilo Lobera, Esther Moreno et al. · 2021 · Journal of Investigational Allergology and Clinical Immunology
How to get rid of itching
Ashley Vander Does, Teresa Ju, Noreen Mohsin, Divya Chopra, Gil Yosipovitch · 2023 · Pharmacology & Therapeutics
Computational Chemistry for the Identification of Lead Compounds for Radiotracer Development
Chia‐Ju Hsieh, Sam G. Giannakoulias, E. James Petersson, Robert H. Mach · 2023 · Pharmaceuticals
Analysis of Mrgprb2 Receptor-Evoked Ca2+ Signaling in Bone Marrow Derived (BMMC) and Peritoneal (PMC) Mast Cells of TRPC-Deficient Mice
Volodymyr Tsvilovskyy, Alejandra Solis-Lopez, Julia Almering, Christin Richter, Lutz Birnbaumer, Alexander Dietrich, Marc Freichel · 2020 · Frontiers in Immunology
Targeted stabilization of Munc18‐1 function via pharmacological chaperones
Debra Abramov, Noah Guy Lewis Guiberson, Andrew Daab, Yoonmi Na, Gregory A. Petsko, Manu Sharma, Jacqueline Burré · 2020 · EMBO Molecular Medicine
Quercetin Attenuates MRGPRX2-Mediated Mast Cell Degranulation via the MyD88/IKK/NF-κB and PI3K/AKT/ Rac1/Cdc42 Pathway
Chenrui Zhao, Yuanyuan Ding, Yihan Huang, Chao Wang, Bin Guo, Tao Zhang · 2024 · Journal of Inflammation Research
Proinflammatory chemokine CXCL14 activates MAS-related G protein-coupled receptor MRGPRX2 and its putative mouse ortholog MRGPRB2
Ghazl Al Hamwi, Vigneshwaran Namasivayam, Beatriz Bueschbell, Robin Gedschold, Stefan Gölz, Christa Elisabeth Müller · 2024 · Communications Biology
Anti-pseudo-allergy effect of isoliquiritigenin is MRGPRX2-dependent
Yajing Hou, Delu Che, Pengyu Ma, Tingting Zhao, Yingnan Zeng, Nan Wang · 2018 · Immunology Letters
MRGPRX2 activation as a rapid, high-throughput mechanistic-based approach for detecting peptide-mediated human mast cell degranulation liabilities
Marc A. Lafleur, Jonathan A. Werner, Madeline M. Fort, Edward K. Lobenhofer, Mercedesz Balázs, Ana Goyos · 2020 · Journal of Immunotoxicology
Minireview: Mas-related G protein-coupled receptor X2 activation by therapeutic drugs
Benjamin D. McNeil · 2021 · Neuroscience Letters
A high expression Mas-related G protein coupled receptor X2 cell membrane chromatography coupled with liquid chromatography and mass spectrometry method for screening potential anaphylactoid components in kudiezi injection
Yuanyuan Lin, Yanni Lv, Jia Fu, Qianqian Jia, Shengli Han · 2018 · Journal of Pharmaceutical and Biomedical Analysis
A mast-cell-specific receptor mediates Iopamidol induced immediate IgE-independent anaphylactoid reactions
Wenjun Jiang, Shiling Hu, Delu Che, Hongli An, Rui Liu · 2019 · International Immunopharmacology
Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor D Induces Release of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling
Rohit Arora, Kenny M. Van Theemsche, Samuel Van Remoortel, Dirk J. Snyders, Alain J. Labro, Jean‐Pierre Timmermans · 2021 · International Journal of Molecular Sciences
Definition of fatty acid transport protein-2 (FATP2) structure facilitates identification of small molecule inhibitors for the treatment of diabetic complications
Mukesh Kumar, Robert J. Gaivin, Shenaz Khan, Yuriy Federov, Drew Adams, Weiyang Zhao, Hsueh‐Yun Lee, Xinghong Dai, Chris Godfrey Dealwis, Jeffrey R. Schelling · 2023 · International Journal of Biological Macromolecules
Itch receptor MRGPRX4 interacts with the receptor activity–modifying proteins
Kotliar, Ilana B., Ceraudo, Emilie, Kemelmakher-Liben, Kevin, Oren, Deena A., Lorenzen, Emily, Dodig-Crnković, Tea, Horioka-Duplix, Mizuho, Huber, Thomas, Schwenk, Jochen M., Sakmar, Thomas P. · 2023 · Journal of Biological Chemistry
Characterization of Effect of Repeated Bolus or Continuous Intrathecal Infusion of Morphine on Spinal Mass Formation in the Dog
Keith R. Hildebrand, Linda M. Page, Tina M. Billstrom, Joanne Steinauer, Kelly A. Eddinger, Shervin Arjomand, Tony L. Yaksh · 2019 · Neuromodulation Technology at the Neural Interface
Kaempferol ameliorates secretagogue-induced pseudo-allergic reactions via inhibiting intracellular calcium fluctuation
Jiao Cao, Yuejin Wang, Shiling Hu, Yuanyuan Ding, Qianqian Jia, Jing Zhu, Hongli An · 2020 · Journal of Pharmacy and Pharmacology
From Synapse to Function: A Perspective on the Role of Neuroproteomics in Elucidating Mechanisms of Drug Addiction
Luis A. Natividad, Matthew W. Buczynski, Daniel B. McClatchy, John R. Yates · 2018 · Proteomes
Subnanomolar MAS-related G protein-coupled receptor-X2/B2 antagonists with efficacy in human mast cells and disease models
Ghazl Al Hamwi, Mohamad Wessam Alnouri, Sven Verdonck, Piotr Leonczak, Shaswati Chaki, Stefan Frischbutter, Pavel Kolkhir, Michaela Matthey, Constantin Kopp, Marek Bednarski et al. · 2025 · Signal Transduction and Targeted Therapy
Effects of Dietary Components on Mast Cells: Possible Use as Nutraceuticals for Allergies?
Sina Kaag, Axel Lorentz · 2023 · Cells
Clinical Manifestations and Diagnostic Evaluation of Opioid Allergy Labels – A Review
Jerry P. Kalangara, Sudheer Potru, Merin Elizabeth Kuruvilla · 2019 · Journal of Pain & Palliative Care Pharmacotherapy
Endogenous opiates and behavior: 2017
Richard J. Bodnar · 2019 · Peptides
Possible involvement of the μ opioid receptor in the antinociception induced by sinomenine on formalin-induced nociceptive behavior in mice
Takaaki Komatsu, Soh Katsuyama, Fumihide Takano, Takemasa Okamura, Chikai Sakurada, Minoru Tsuzuki, Kakuyou Ogawa, Atsuhito Kubota, Osamu Morinaga, Kenji Tabata et al. · 2019 · Neuroscience Letters
The anti‐anaphylactoid effects of Piperine through regulating MAS‐related G protein‐coupled receptor X2 activation
Chuchu Qiao, Shiling Hu, Delu Che, Jue Wang, Jiapan Gao, Ruiping Ma, Wenjun Jiang, Tao Zhang, Rui Liu · 2020 · Phytotherapy Research
Peripheral blood cultured mast cells: Phenotypic and functional outcomes of different culture protocols
Jessy Elst, Vito Sabato, Marie‐Line M. van der Poorten, Margaretha Antje Faber, Athina Ludovica Van Gasse, Leander P. De Puysseleyr, Chris H. Bridts, Christel H. Mertens, Michel Van Houdt, Marcus Maurer et al. · 2021 · Journal of Immunological Methods
Structure-guided design of partial agonists at an opioid receptor
Balázs R. Varga, Sarah M. Bernhard, Amal El Daibani, Saheem A. Zaidi, Jordy Homing Lam, Jhoan Sebastian Aguilar, Kevin Appourchaux, Antonina L. Nazarova, Alexa Kouvelis, Ryosuke Shinouchi et al. · 2025 · Nature Communications
Current and future therapeutics targeting mast cells in disease
William P. M. Worrall, Laurent Lionel Reber · 2025 · Pharmacology & Therapeutics
Peripheral endomorphins drive mechanical alloknesis under the enzymatic control of CD26/DPPIV
Eriko Komiya, Mitsutoshi Tominaga, Ryo Hatano, Yuji Kamikubo, Sumika Toyama, Hakushun Sakairi, Kotaro Honda, Takumi Itoh, Yayoi Kamata, Munehiro Tsurumachi et al. · 2021 · Journal of Allergy and Clinical Immunology
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Qianqian Jia, Yanni Lv, Chenyang Miao, Jingting Feng, Yifan Ding, Tongpei Zhou, Shengli Han, Langchong He · 2023 · Talanta
Isosalvianolic acid C-induced pseudo-allergic reactions via the mast cell specific receptor MRGPRX2
Yuanyuan Lin, Jue Wang, Yajing Hou, Jia Fu, Di Wei, Qianqian Jia, Yanni Lv, Cheng Wang, Shengli Han, Langchong He · 2019 · International Immunopharmacology
The Mas-related G protein–coupled receptor d (Mrgprd) mediates pain hypersensitivity in painful diabetic neuropathy
Dale George, Nirupa D. Jayaraj, Paola Pacifico, Dongjun Ren, Nikhil Sriram, Rachel E. Miller, Anne‐Marie Malfait, Richard J. Miller, Daniela Maria Menichella · 2023 · Pain
MRGPRX4 in Cholestatic Pruritus
Huasheng Yu, Kirk J. Wangensteen, Tong Deng, Yulong Li, Wenqin Luo · 2021 · Seminars in Liver Disease
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Revisiting the role of MRGPRX2 on hypersensitivity reactions to neuromuscular blocking drugs
Hydar Ali · 2021 · Current Opinion in Immunology
Immediate Hypersensitivity to Fluoroquinolones: A Cohort Assessing Cross-Reactivity
Sara F Azimi, Vincent Mainella, Meghan N. Jeffres · 2022 · Open Forum Infectious Diseases
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Sreeparna Majumdar, Yi-Ting Chiu, Julie E. Pickett, Bryan L. Roth · 2023 · Drug Discovery Today
Dictamnine is an effective anti‐anaphylactoid compound acting via the MrgX2 receptor located on mast cells
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Action of substance P and PAMP(9-20) on different excitation sites of MRGPRX2 induces differences in mast cell activation
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S P H Alexander, Jim Battey, Helen E. Benson, Richard V. Benya, Tom I. Bonner, Anthony P. Davenport, Satoru Eguchi, Anthony J. Harmar, Nicholas D. Holliday, Robert T. Jensen et al. · 2019 · IUPHAR/BPS Guide to Pharmacology CITE
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Lei Lu, Shammy Raj, Narcy G Arizmendi, Jie Ding, Gary Eitzen, Peter O. Kwan, Marianna Kulka, Larry D. Unsworth · 2021 · Acta Biomaterialia
Association between mutated Mas-related G protein-coupled receptor-X2 and rocuronium-induced intraoperative anaphylaxis. Comment on Br J Anaesth 2020; 125: e446–e448
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Adverse Reactions to Illicit Drugs (Marijuana, Opioids, Cocaine) and Alcohol
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p-Phenylenediamine induces immediate contact allergy and non-histaminergic itch via MRGPRX2
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Class A Orphans (version 2020.5) in the IUPHAR/BPS Guide to Pharmacology Database
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Mutations of MRGPRX2, drug sensitivity, and genetic markers related to disease
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Development of an environmentally sensitive fluorescent peptide probe for MrgX2 and application in ligand screening of peptide antibiotics
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MRGPRX2 is critical for clozapine induced pseudo-allergic reactions
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