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 …

[HTML][HTML] Therapeutic potential of PANoptosis: innate sensors, inflammasomes, and RIPKs in PANoptosomes

A Pandeya, TD Kanneganti - Trends in Molecular Medicine, 2024 - cell.com
The innate immune system initiates cell death pathways in response to pathogens and
cellular stress. Cell death can be either non-lytic (apoptosis) or lytic (PANoptosis, pyroptosis …

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 …

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 …

Discovery of NP3-253, a Potent Brain Penetrant Inhibitor of the NLRP3 Inflammasome

A Mackay, J Velcicky, N Gommermann… - Journal of Medicinal …, 2024 - ACS Publications
Activation of the NLRP3 inflammasome in response to danger signals is a key innate
immune mechanism and results in the production of the pro-inflammatory cytokines …

Recent advances in the treatment of gout with NLRP3 inflammasome inhibitors

Y Tian, X He, R Li, Y Wu, Q Ren, Y Hou - Bioorganic & Medicinal Chemistry, 2024 - Elsevier
Gout is an autoinflammatory disorder characterized by the accumulation of monosodium
urate crystals in joints and other tissues, representing the predominant type of inflammatory …

First‐in‐human safety, tolerability, and pharmacokinetic results of DFV890, an oral low‐molecular‐weight NLRP3 inhibitor

E Gatlik, B Mehes, E Voltz, U Sommer… - Clinical and …, 2024 - Wiley Online Library
This first‐in‐human study evaluated the safety, tolerability, single‐and multiple‐dose
pharmacokinetic profiles with dietary influence, and pharmacodynamics (PD) of DFV890, an …

Deep-Learning-Driven Discovery of SN3–1, a Potent NLRP3 Inhibitor with Therapeutic Potential for Inflammatory Diseases

C Shi, T Gao, W Lyu, B Qiang, Y Chen… - Journal of Medicinal …, 2024 - ACS Publications
The NLRP3 inflammasome plays a central role in the pathogenesis of various intractable
human diseases, making it an urgent target for therapeutic intervention. Here, we report the …

The role of NLRP3 and NLRP12 inflammasomes in glioblastoma

S Rajkhowa, S Jha - Genes & Immunity, 2024 - nature.com
Glioblastoma (GBM) is the deadliest malignant brain tumor, with a survival of less than 14
months after diagnosis. The highly invasive nature of GBM makes total surgical resection …

Novel Macrocyclic NLRP3 Inhibitors

S Mesch, J Shannon, D Miller, A MacLeod… - Journal of Medicinal …, 2024 - ACS Publications
Aberrant activation of NLRP3 due to persistent tissue damage, misfolded proteins or crystal
deposits has been linked to multiple chronic inflammatory disorders such as cryopyrin …