ArticleJournal of the American Chemical Society2018
Diprovocims: A New and Exceptionally Potent Class of Toll-like Receptor Agonists.
Article in Journal of the American Chemical Society, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 20 papers.
What it found
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
20 citing papers in PubMed, 58 citations in OpenAlex.
- Discovery of Novel Small-Molecule Toll-like Receptor 2 Agonists via a Scaffold Hopping Strategy.ACS medicinal chemistry letters · 2026Article
- Can Phagocytosis, Neutrophil Extracellular Traps, and IFN-α Production in Systemic Lupus Erythematosus Be Simultaneously Modulated? A Pharmacological Perspective.International journal of molecular sciences · 2026Review
- Cyclovirobuxine D suppresses cancer stemness in osteosarcoma with implication of the noncanonical NF-kappaB pathway.Frontiers in pharmacology · 2026Article
- [Niranthin ameliorates Crohn's disease-like enteritis in mice by inhibiting intestinal epithelial cell apoptosis and protecting intestinal barrierNan fang yi ke da xue xue bao = Journal of Southern Medical University · 2025Article
- Ginsenoside Rh2 alleviates inflammatory response and enhances motor function recovery in spinal cord injury mice via the ROS/MAPK14 signaling pathway.Journal of ginseng research · 2025Article
- Self-assembling TLR2 agonists promote mucosal immune responses without pulmonary immunopathologic injuries in mice.NPJ vaccines · 2025Article
- Activation of NR2A-Wnt-TLR2 Signaling Axis in Satellite Glial Cells of the Dorsal Root Ganglion Contributes to Neuropathic Pain Induced by Nerve Injury in Diabetic Mice.Molecular neurobiology · 2025Article
- Microbiota mechanisms in cancer progression and therapy.Cell chemical biology · 2025Review
- Diprovocim protects against the radiation-induced damage via the TLR2 signaling pathway.Molecular medicine (Cambridge, Mass.) · 2025Article
- Small molecule modulators of immune pattern recognition receptors.RSC chemical biology · 2023Review
- Recent Advances in Studying Toll-like Receptors with the Use of Computational Methods.Journal of chemical information and modeling · 2023Review
- Immunotherapeutic Implications of Toll-like Receptors Activation in Tumor Microenvironment.Pharmaceutics · 2022Review
- Unraveling the Tomaralimab Epitope on the Toll-like Receptor 2 via Molecular Dynamics and Deep Learning.ACS omega · 2022Article
- Next-Generation Diprovocims with Potent Human and Murine TLR1/TLR2 Agonist Activity That Activate the Innate and Adaptive Immune Response.Journal of medicinal chemistry · 2022Article
- Knockdown of NDUFC1 inhibits cell proliferation, migration, and invasion of hepatocellular carcinoma.Frontiers in oncology · 2022Article
- Synthesis, structure-activity relationship studies and evaluation of a TLR 3/8/9 agonist and its analogues.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2021Article
- Nanomedicine-mediated alteration of the pharmacokinetic profile of small molecule cancer immunotherapeutics.Acta pharmacologica Sinica · 2020Review
- Emerging Adjuvants for Cancer Immunotherapy.Frontiers in chemistry · 2020Review
- Structural Basis of TLR2/TLR1 Activation by the Synthetic Agonist Diprovocim.Journal of medicinal chemistry · 2019Article
- Targeting Cellular and Tissue HIV Reservoirs With Toll-Like Receptor Agonists.Frontiers in immunology · 2019Review
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
Abstract
A screen conducted with nearly 100000 compounds and a surrogate functional assay for stimulation of an immune response that measured the release of TNF-α from treated human THP-1 myeloid cells differentiated along the macrophage line led to the discovery of the diprovocims. Unique to these efforts and of special interest, the screening leads for this new class of activators of an immune response came from a compound library designed to promote cell-surface receptor dimerization. Subsequent comprehensive structure-activity relationship studies improved the potency 800-fold over that of the screening leads, providing diprovocim-1 and diprovocim-2. The diprovocims act by inducing cell-surface toll-like receptor (TLR)-2 dimerization and activation with TLR1 (TLR1/TLR2 agonist), bear no structural similarity to any known natural or synthetic TLR agonist, and are easy to prepare and synthetically modify, and selected members are active in both human and murine systems. The most potent diprovocim (3, diprovocim-1) elicits full agonist activity at extraordinarily low concentrations (EC
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.