1,468
Views
60
CrossRef citations to date
0
Altmetric
Review

Recent progress in the development of Toll-like receptor (TLR) antagonists

&
Pages 719-730 | Received 10 Mar 2016, Accepted 29 Apr 2016, Published online: 18 May 2016

Keep up to date with the latest research on this topic with citation updates for this article.

Read on this site (2)

Fitria Salim, Hendra Gunawan, Oki Suwarsa & Endang Sutedja. (2023) Increased Expression of Toll-Like Receptor (TLR) 2 and TLR6 on Peripheral Blood Monocytes by Induction of Staphylococcal Enterotoxin B During Exacerbation of Atopic Dermatitis Patients. Clinical, Cosmetic and Investigational Dermatology 16, pages 301-307.
Read now
Madeleine E. Kieffer, Akash M. Patel, Scott A. Hollingsworth & W. Michael Seganish. (2020) Small molecule agonists of toll-like receptors 7 and 8: a patent review 2014 – 2020. Expert Opinion on Therapeutic Patents 30:11, pages 825-845.
Read now

Articles from other publishers (58)

Soyeon Lee, Jiyoung Seo, Young Hun Kim, Hyeon Jin Ju, Shina Kim, Yun Bae Ji, Hai Bang Lee, Han Su Kim, Sangdun Choi & Moon Suk Kim. (2023) Enhanced intra-articular therapy for rheumatoid arthritis using click-crosslinked hyaluronic acid hydrogels loaded with toll-like receptor antagonizing peptides. Acta Biomaterialia 172, pages 188-205.
Crossref
Shuang Liang, Jianjun Yao, Dan Liu, Lang Rao, Xiaoyuan Chen & Zhaohui Wang. (2023) Harnessing Nanomaterials for Cancer Sonodynamic Immunotherapy. Advanced Materials 35:33.
Crossref
Junjie Yang, Yue Pan, Xiaoshan Zeng, Shuwen Liu, Zhipeng Chen & Kui Cheng. (2023) Discovery of novel aporphine alkaloid derivative as potent TLR2 antagonist reversing macrophage polarization and neutrophil infiltration against acute inflammation. Acta Pharmaceutica Sinica B.
Crossref
Jiayu Wang, Jifa Zhang, Jiaxing Wang, Xinyue Hu, Liang Ouyang & Yuxi Wang. (2023) Small-Molecule Modulators Targeting Toll-like Receptors for Potential Anticancer Therapeutics. Journal of Medicinal Chemistry 66:10, pages 6437-6462.
Crossref
Qian Zhao, Liyun Zhu, Sunan Wang, Yongsheng Gao & Fei Jin. (2023) Molecular mechanism of the anti-inflammatory effects of plant essential oils: A systematic review. Journal of Ethnopharmacology 301, pages 115829.
Crossref
Shuo LI, Guifang FAN, Xiaojiaoyang LI, Yajie CAI & Runping LIU. (2023) Modulation of type I interferon signaling by natural products in the treatment of immune-related diseases. Chinese Journal of Natural Medicines 21:1, pages 3-18.
Crossref
Wenbin Dai, Longhai Long, Xiaoqiang Wang, Sen Li & Houping Xu. (2022) Phytochemicals targeting Toll-like receptors 4 (TLR4) in inflammatory bowel disease. Chinese Medicine 17:1.
Crossref
Run Zheng & Jian Ma. (2022) Immunotherapeutic Implications of Toll-like Receptors Activation in Tumor Microenvironment. Pharmaceutics 14:11, pages 2285.
Crossref
Yu Chen, Hui Chen, Xiao-Chen Li, Wen-Li Mi, Yu-Xia Chu, Yan-Qing Wang & Qi-Liang Mao-Ying. (2022) Neuronal toll like receptor 9 contributes to complete Freund’s adjuvant-induced inflammatory pain in mice. Frontiers in Molecular Neuroscience 15.
Crossref
Chen Tian-qi, Deng Yan-fang, Wang Yan-yan & Zhang Yong-hui. (2022) Butyrolactone I attenuates inflammation in murine NASH by inhibiting the NF-κB signaling pathway. Biochemical and Biophysical Research Communications 626, pages 167-174.
Crossref
Abdul Manan, Rameez Hassan Pirzada, Muhammad Haseeb & Sangdun Choi. (2022) Toll-like Receptor Mediation in SARS-CoV-2: A Therapeutic Approach. International Journal of Molecular Sciences 23:18, pages 10716.
Crossref
Ge Huang, Dan Yao, Xiaoli Yan, Mingyu Zheng, Ping Yan, Xiaoxia Chen & Dan Wang. (2022) Emerging role of toll-like receptors signaling and its regulators in preterm birth: a narrative review. Archives of Gynecology and Obstetrics 308:2, pages 319-339.
Crossref
Zixuan Xu, Wenting Hao, Daxiang Xu, Yan He, Ziyi Yan, Fenfen Sun, Xiangyang Li, Xiaoying Yang, Yinghua Yu, Renxian Tang, Kuiyang Zheng & Wei Pan. (2022) Polyene Phosphatidylcholine Interacting with TLR-2 Prevents the Synovial Inflammation via Inactivation of MAPK and NF-κB Pathways. Inflammation 45:4, pages 1507-1519.
Crossref
Chunying Zhuang, Riken Chen, Zhenzhen Zheng, Jianmin Lu & Cheng Hong. (2022) Toll-Like Receptor 3 in Cardiovascular Diseases. Heart, Lung and Circulation 31:7, pages e93-e109.
Crossref
Ximei Nie, Yuqi Zhao, Hao Xu, Zhengxiao Han, Xing Zhang, Bingzhi Li, Xin Huang, Jiachun Ge & Qian Ren. (2022) Toll-crustin signaling pathway is activated in the Eriocheir sinensis with hepatopancreatic necrosis disease (HPND). Aquaculture 552, pages 738032.
Crossref
Etrusca Brogi, Federico Coccolini & Francesco Forfori. 2022. Postinjury Multiple Organ Failure. Postinjury Multiple Organ Failure 9 31 .
Danyang Li & Minghua Wu. (2021) Pattern recognition receptors in health and diseases. Signal Transduction and Targeted Therapy 6:1.
Crossref
Biswajit Kundu, Deblina Raychaudhuri, Ayan Mukherjee, Bishnu Prasad Sinha, Dipika Sarkar, Purbita Bandopadhyay, Sourav Pal, Nirmal Das, Debdeep Dey, Kantubhukta Ramarao, Kasireddy Nagireddy, Dipyaman Ganguly & Arindam Talukdar. (2021) Systematic Optimization of Potent and Orally Bioavailable Purine Scaffold as a Dual Inhibitor of Toll-Like Receptors 7 and 9. Journal of Medicinal Chemistry 64:13, pages 9279-9301.
Crossref
Dhruv Varshney, Sherry Yue Qiu, Tyler P. Graf & Kevin J. McHugh. (2021) Employing Drug Delivery Strategies to Overcome Challenges Using TLR7/8 Agonists for Cancer Immunotherapy. The AAPS Journal 23:4.
Crossref
Saghar Pahlavanneshan, Ali Sayadmanesh, Hamidreza Ebrahimiyan & Mohsen Basiri. (2021) Toll-Like Receptor-Based Strategies for Cancer Immunotherapy. Journal of Immunology Research 2021, pages 1-14.
Crossref
Jing Wang, Huiru Wu, Xinli Liu, Huiyu Jia & Hong Lu. (2021) Effect of LPS on Cytokine Secretion from Peripheral Blood Monocytes in Juvenile Idiopathic Arthritis-Associated Uveitis Patients with Positive Antinuclear Antibody. Journal of Immunology Research 2021, pages 1-8.
Crossref
Srinivasa Reddy Natala, Agata Habas, Emily M. Stocking, Andrew Orry, Diana L. Price, Martin B. Gill, Douglas W. Bonhaus, Ruben Abagyan & Wolfgang Wrasidlo. (2021) Structure based design and synthesis of novel Toll-like Receptor 2 (TLR 2) lipid antagonists. Bioorganic & Medicinal Chemistry Letters 40, pages 127861.
Crossref
Rui Zhao, Sushan Luo & Chongbo Zhao. (2021) The role of innate immunity in myasthenia gravis. Autoimmunity Reviews 20:5, pages 102800.
Crossref
Haixiang Shen, Jin Liu, Shiming Chen, Xueyou Ma, Yufan Ying, Jiangfeng Li, Weiyu Wang, Xiao Wang & Liping Xie. (2021) Prognostic Value of Tumor-Associated Macrophages in Clear Cell Renal Cell Carcinoma: A Systematic Review and Meta-Analysis. Frontiers in Oncology 11.
Crossref
Francesco Nucera, Federica Lo Bello, Sj S. Shen, Paolo Ruggeri, Irene Coppolino, Antonino Di Stefano, Cristiana Stellato, Vincenzo Casolaro, Phil M. Hansbro, Ian M. Adcock & Gaetano Caramori. (2021) Role of Atypical Chemokines and Chemokine Receptors Pathways in the Pathogenesis of COPD. Current Medicinal Chemistry 28:13, pages 2577-2653.
Crossref
Nicolás M. S. Gálvez, Catalina A. Andrade, Gaspar A. Pacheco, Jorge A. Soto, Vicente Stranger, Thomas Rivera, Abel E. Vásquez & Alexis M. Kalergis. (2021) Host Components That Modulate the Disease Caused by hMPV. Viruses 13:3, pages 519.
Crossref
Amit Kumar Ram, Gavin Wright & Balasubramaniyan Vairappan. 2021. Liver Pathology. Liver Pathology.
Haiyuan Xing, Ruiyan Li, Yun'an Qing, Boda Ying & Yanguo Qin. (2021) Biomaterial-based osteoimmunomodulatory strategies via the TLR4-NF-κB signaling pathway: A review. Applied Materials Today 22, pages 100969.
Crossref
Robert Root-Bernstein. (2021) Innate Receptor Activation Patterns Involving TLR and NLR Synergisms in COVID-19, ALI/ARDS and Sepsis Cytokine Storms: A Review and Model Making Novel Predictions and Therapeutic Suggestions. International Journal of Molecular Sciences 22:4, pages 2108.
Crossref
Nan Cheng, Xuexia Bai, Yuxin Shu, Owais Ahmad & Pingping Shen. (2021) Targeting tumor-associated macrophages as an antitumor strategy. Biochemical Pharmacology 183, pages 114354.
Crossref
Ali Keshavarz, Atieh Pourbagheri‐Sigaroodi, Parisa Zafari, Nader Bagheri, Seyed H. Ghaffari & Davood Bashash. (2020) Toll‐like receptors (TLRs) in cancer; with an extensive focus on TLR agonists and antagonists. IUBMB Life 73:1, pages 10-25.
Crossref
Snigdha Samarpita, Joo Young Kim, Mahaboob Khan Rasool & Kyoung Soo Kim. (2020) Investigation of toll-like receptor (TLR) 4 inhibitor TAK-242 as a new potential anti-rheumatoid arthritis drug. Arthritis Research & Therapy 22:1.
Crossref
Ingrid Aneman, Dillan Pienaar, Sonja Suvakov, Tatjana P. Simic, Vesna D. Garovic & Lana McClements. (2020) Mechanisms of Key Innate Immune Cells in Early- and Late-Onset Preeclampsia. Frontiers in Immunology 11.
Crossref
Yajing Chen, Zhisen Zeng, Haoran Ying, Chuang Wu & Shuzhen Chen. (2020) Superparamagnetic iron oxide nanoparticles attenuate lipopolysaccharide‐induced inflammatory responses through modulation of toll‐like receptor 4 expression. Journal of Applied Toxicology 40:8, pages 1067-1075.
Crossref
Mahesh Chandra Patra, Asma Achek, Gi-Young Kim, Suresh Panneerselvam, Hyeon-Jun Shin, Wook-Yong Baek, Wang Hee Lee, June Sung, Uisuk Jeong, Eun-Young Cho, Wook Kim, Eunha Kim, Chang-Hee Suh & Sangdun Choi. (2020) A Novel Small-Molecule Inhibitor of Endosomal TLRs Reduces Inflammation and Alleviates Autoimmune Disease Symptoms in Murine Models. Cells 9:7, pages 1648.
Crossref
Robert Root-Bernstein. (2020) Synergistic Activation of Toll-Like and NOD Receptors by Complementary Antigens as Facilitators of Autoimmune Disease: Review, Model and Novel Predictions. International Journal of Molecular Sciences 21:13, pages 4645.
Crossref
Cindy Patinote, Nour Bou Karroum, Georges Moarbess, Natalina Cirnat, Issam Kassab, Pierre-Antoine Bonnet & Carine Deleuze-Masquéfa. (2020) Agonist and antagonist ligands of toll-like receptors 7 and 8: Ingenious tools for therapeutic purposes. European Journal of Medicinal Chemistry 193, pages 112238.
Crossref
Mahesh Chandra Patra, Maria Batool, Muhammad Haseeb & Sangdun Choi. (2020) A Computational Probe into the Structure and Dynamics of the Full-Length Toll-Like Receptor 3 in a Phospholipid Bilayer. International Journal of Molecular Sciences 21:8, pages 2857.
Crossref
Holly Richendrfer & Gregory D. Jay. (2020) Lubricin as a Therapeutic and Potential Biomarker in Sepsis. Critical Care Clinics 36:1, pages 55-67.
Crossref
Alluri Siddhartha Varma, Girish Suragimath, Apurva Pisal, Pooja R Disale & Sameer Zope. (2019) Toll-like Receptors: Molecular Microbe Sensors in Periodontium. World Journal of Dentistry 10:5, pages 396-401.
Crossref
Xuejiao Cui, Yongping Liu, Shuo Wang, Na Zhao, Jing Qin, Yushu Li, Chenling Fan, Zhongyan Shan & Weiping Teng. (2019) Circulating Exosomes Activate Dendritic Cells and Induce Unbalanced CD4+ T Cell Differentiation in Hashimoto Thyroiditis. The Journal of Clinical Endocrinology & Metabolism 104:10, pages 4607-4618.
Crossref
Alberta Serwah Anning, Godwin Kwakye-Nuako, Elvis Ofori Ameyaw, Mba-Tihssommah Mosore & Kwame Kumi Asare. (2019) In vitro activity of Erythrophleum ivorense extract against the promastigote stage of cutaneous Leishmania parasite, a member of Leishmania (Mundinia) enriettii complex isolates from Ghana. Access Microbiology 1:7.
Crossref
Asma Achek, Masaud Shah, Ji Young Seo, Hyuk-Kwon Kwon, Xiangai Gui, Hyeon-Jun Shin, Eun-Young Cho, Byeong Sung Lee, Dong-Jin Kim, Sang Ho Lee, Tae Hyeon Yoo, Moon Suk Kim & Sangdun Choi. (2019) Linear and Rationally Designed Stapled Peptides Abrogate TLR4 Pathway and Relieve Inflammatory Symptoms in Rheumatoid Arthritis Rat Model. Journal of Medicinal Chemistry 62:14, pages 6495-6511.
Crossref
Annette K. Brenner & Øystein Bruserud. (2019) Functional Toll-Like Receptors (TLRs) Are Expressed by a Majority of Primary Human Acute Myeloid Leukemia Cells and Inducibility of the TLR Signaling Pathway Is Associated with a More Favorable Phenotype. Cancers 11:7, pages 973.
Crossref
You Dong Liu, Liang Yu, Le Ying, Jesse Balic, Hugh Gao, Nian Tao Deng, Alison West, Feng Yan, Cheng Bo Ji, Daniel Gough, Patrick Tan, Brendan J. Jenkins & Ji Kun Li. (2019) Toll‐like receptor 2 regulates metabolic reprogramming in gastric cancer via superoxide dismutase 2 . International Journal of Cancer 144:12, pages 3056-3069.
Crossref
Yu Toyoda, Tappei Takada, Masakazu Umezawa, Fumiya Tomura, Yoshihide Yamanashi, Ken Takeda & Hiroshi Suzuki. (2019) Identification of hepatic NPC1L1 as an NAFLD risk factor evidenced by ezetimibe‐mediated steatosis prevention and recovery. FASEB BioAdvances 1:5, pages 283-295.
Crossref
Hyuk-Kwon Kwon, Mahesh Chandra Patra, Hyeon-Jun Shin, Xiangai Gui, Asma Achek, Suresh Panneerselvam, Dong-Jin Kim, Suk-Jong Song, Riwon Hong, Kyoung Soo Kim, Yang Gyun Kim, Francis Y. Lee, Dae-Hyun Hahm, Sang Ho Lee & Sangdun Choi. (2019) A cell-penetrating peptide blocks Toll-like receptor-mediated downstream signaling and ameliorates autoimmune and inflammatory diseases in mice. Experimental & Molecular Medicine 51:4, pages 1-19.
Crossref
Vijayakumar Gosu, Seungwoo Son, Donghyun Shin & Ki-Duk Song. (2019) Insights into the dynamic nature of the dsRNA-bound TLR3 complex. Scientific Reports 9:1.
Crossref
Vinita Mishra & Chandramani Pathak. (2019) Human Toll-Like Receptor 4 (hTLR4): Structural and functional dynamics in cancer. International Journal of Biological Macromolecules 122, pages 425-451.
Crossref
Eman L. Dadashian, Erin M. McAuley, Delong Liu, Arthur L. ShafferIIIIII, Ryan M. Young, Jessica R. Iyer, Michael J. Kruhlak, Louis M. Staudt, Adrian Wiestner & Sarah E. M. Herman. (2019) TLR Signaling Is Activated in Lymph Node–Resident CLL Cells and Is Only Partially Inhibited by Ibrutinib. Cancer Research 79:2, pages 360-371.
Crossref
Kritika Gupta, Marianne Saldanha, Mruganka Parasnis, Padma V. Devarajan, Ratnesh Jain & Prajakta Dandekar. 2019. Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis. Targeted Intracellular Drug Delivery by Receptor Mediated Endocytosis 323 349 .
Mensiena B. G. Kiewiet, Renske Dekkers, Martine P. Gool, Laurien H. Ulfman, Andre Groeneveld, Marijke M. Faas & Paul Vos. (2018) Identification of a TLR2 Inhibiting Wheat Hydrolysate. Molecular Nutrition & Food Research 62:23, pages 1800716.
Crossref
Koji Naruishi & Toshihiko Nagata. (2018) Biological effects of interleukin‐6 on Gingival Fibroblasts: Cytokine regulation in periodontitis. Journal of Cellular Physiology 233:9, pages 6393-6400.
Crossref
Sonya VanPatten & Yousef Al-Abed. (2017) High Mobility Group Box-1 (HMGb1): Current Wisdom and Advancement as a Potential Drug Target. Journal of Medicinal Chemistry 61:12, pages 5093-5107.
Crossref
Yasufumi Nishikawa, Yukari Kajiura, Jung Hwan Lew, Jun-ichi Kido, Toshihiko Nagata & Koji Naruishi. (2017) Calprotectin Induces IL-6 and MCP-1 Production via Toll-Like Receptor 4 Signaling in Human Gingival Fibroblasts. Journal of Cellular Physiology 232:7, pages 1862-1871.
Crossref
Tong Shi, Liqin Li, Guochao Zhou, Chen Wang, Xuejun Chen, Ruihua Zhang, Jianfu Xu, Xiaojing Lu, Hui Jiang & Jisheng Chen. (2017) Toll-like receptor 5 agonist CBLB502 induces radioprotective effects <italic>in vitro</italic>. Acta Biochimica et Biophysica Sinica 49:6, pages 487-495.
Crossref
Seolhee Park, Hyeon-Jun Shin, Masaud Shah, Hey-Young Cho, Muhammad Ayaz Anwar, Asma Achek, Hyuk-Kwon Kwon, Byugsung Lee, Tae Hyeon Yoo & Sangdun Choi. (2017) TLR4/MD2 specific peptides stalled in vivo LPS-induced immune exacerbation. Biomaterials 126, pages 49-60.
Crossref
B Kornblit & K Müller. (2016) Sensing danger: toll-like receptors and outcome in allogeneic hematopoietic stem cell transplantation. Bone Marrow Transplantation 52:4, pages 499-505.
Crossref

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.