Recent progress and prospects of small molecules for NLRP3 inflammasome inhibition

N Li, R Zhang, M Tang, M Zhao, X Jiang… - Journal of Medicinal …, 2023 - ACS Publications
NLRP3 inflammasome is a multiprotein complex involved in host immune response─ which
exerts various biological effects by mediating the maturation and secretion of IL-1β and IL …

Medicinal chemistry strategies targeting NLRP3 inflammasome pathway: A recent update from 2019 to mid-2023

M Duan, L Sun, X He, Z Wang, Y Hou, Y Zhao - European Journal of …, 2023 - Elsevier
Nod-like receptor protein 3 (NLRP3), a therapeutic target that has a close relationship with
inflammatory diseases, has drawn significant attention from researchers in the field. An …

Discovery of clinical candidate NT-0796, a brain-penetrant and highly potent NLRP3 inflammasome inhibitor for neuroinflammatory disorders

D Harrison, A Billinton, MG Bock… - Journal of Medicinal …, 2023 - ACS Publications
The NLRP3 inflammasome is a component of the innate immune system involved in the
production of proinflammatory cytokines. Neurodegenerative disorders, including …

Novel aryl sulfonamide derivatives as NLRP3 inflammasome inhibitors for the potential treatment of cancer

V Albanese, S Missiroli, M Perrone… - Journal of Medicinal …, 2023 - ACS Publications
The NLRP3 inflammasome is a critical component of innate immunity that senses diverse
pathogen-and host-derived molecules. However, its aberrant activation has been associated …

Discovery of triazinone derivatives as novel, specific, and direct NLRP3 inflammasome inhibitors for the treatment of DSS-induced ulcerative colitis

N Li, X Jiang, R Zhang, N Ye, M Tang… - Journal of Medicinal …, 2023 - ACS Publications
NLRP3 is an intracellular sensor protein that causes inflammasome formation and
pyroptosis in response to a wide range of stimuli. Aberrant activation of NLRP3 …

Discovery of potent, orally bioavailable, tricyclic nlrp3 inhibitors

J Velcicky, P Janser, N Gommermann… - Journal of medicinal …, 2024 - ACS Publications
NLRP3 is a molecular sensor recognizing a wide range of danger signals. Its activation
leads to the assembly of an inflammasome that allows for activation of caspase-1 and …

[HTML][HTML] Interrogating direct NLRP3 engagement and functional inflammasome inhibition using cellular assays

KA Teske, C Corona, J Wilkinson, D Mamott… - Cell Chemical …, 2024 - cell.com
As a key regulator of the innate immune system, the NLRP3 inflammasome responds to a
variety of environmental insults through activation of caspase-1 and release of the …

First‐in‐human phase 1 trial evaluating safety, pharmacokinetics, and pharmacodynamics of NLRP3 inflammasome inhibitor, GDC‐2394, in healthy volunteers

F Tang, R Kunder, T Chu, A Hains… - Clinical and …, 2023 - Wiley Online Library
Inappropriate and chronic activation of the cytosolic NOD‐, LRR‐, and pyrin domain‐
containing 3 (NLRP3) inflammasome, a key component of innate immunity, likely underlies …

[HTML][HTML] Inflammasomes in Atherosclerosis—From Pathophysiology to Treatment

P Theofilis, E Oikonomou, C Chasikidis, K Tsioufis… - Pharmaceuticals, 2023 - mdpi.com
Atherosclerosis, a chronic inflammatory disease characterized by arterial plaque
accumulation, remains a significant global health challenge. In recent years …

[HTML][HTML] JT002, a small molecule inhibitor of the NLRP3 inflammasome for the treatment of autoinflammatory disorders

G Ambrus-Aikelin, K Takeda, A Joetham, M Lazic… - Scientific Reports, 2023 - nature.com
The NLRP3 inflammasome is an intracellular, multiprotein complex that promotes the auto-
catalytic activation of caspase-1 and the subsequent maturation and secretion of the pro …