New Building Blocks for March 2023_ChemScene - 코아사이언스

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Building Blocks & Bioactive Molecules 전문제조사 ChemScene 수입/공급 업체 코아사이언스 입니다.

 

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The NLR family pyrin domain containing protein 3 (NLRP3) inflammasome is a multimeric protein complex[1]. Structurally, NLRP3 inflammasome contains three domains: the leucine-rich repeat-containing receptors (LRR) domain, the nucleotide-binding and oligomerization (NACHT) domain and pyrin domain (PYD). NLRP3 is a unique pattern recognition receptor (PRR) that can be widely stimulated by bacterial, viral and fungal pathogens, the environment and the host. Anomalous NLRP3 inflammasome activation has been implicated in the pathogenesis of a wide variety of human diseases and contributes to acute and chronic inflammation-associated complex diseases, including arthritis, atherosclerosis, diabetes, multiple sclerosis, Alzheimer’s disease and Parkinson’s disease. Accordingly, inhibitors of the NLRP3 inflammasome may be useful in the treatment of these diseases. To date, more than ten NLRP3 inhibitors have entered into clinical trials[2-10].

A series of building blocks will be used as molecular fragments in the design of NLRP3 inhibitors.

 

[1] Journal of Medicinal Chemistry (2021), 64, 1, 101-122.
[2] Journal of Medicinal Chemistry (2022), 65, 21, 14721-14739.
[3] Journal of Medicinal Chemistry (2022), 65, 18, 11985-12001.
[4] European Journal of Medicinal Chemistry (2023), 245, 114919.
[5] European Journal of Medicinal Chemistry (2022), 236, 114357.
[6] European Journal of Medicinal Chemistry (2020), 185, 111822.
[7] Bioorganic & Medicinal Chemistry Letters (2021), 46, 128160.
[8] WO2021239885A1.
[9] WO2023004257A1.
[10] WO2023275366A1.

 

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