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SJB2-043 is a ubiquitin-specific protease USP1 inhibitor (IC50 = 544 nM using USP1/UAF1 complex) that exhibits anti-proliferation efficacy against chronic and acute myeloid leukemia lines (IC50 <2 µM; K562, OCI-AML3, SK-NO1, U937) and primary acute myelogenous leukemia (AML) patient-derived leukemic cells by promoting the degradation of transcription factor DNA binding 1 (ID1). SJB2-043 is also reported to be an allosteric site-targeting inhibitor against PLPro (IC50 = 0.56 μM), the papain-like cysteine protease with deubiquitination and deISGylation activities that suppress host innate immune responses toward SARS-CoV-2 infection.
储存分类代码
11 - Combustible Solids
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WGK 3
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Chia-Chuan Cho et al.
ChemMedChem, 17(1), e202100455-e202100455 (2021-08-24)
As the pathogen of COVID-19, SARS-CoV-2 encodes two essential cysteine proteases that process the pathogen's two large polypeptide products pp1a and pp1ab in the human cell host to form 15 functionally important, mature nonstructural proteins. One of the two enzymes
Minyoung Noh et al.
Frontiers in pharmacology, 12, 695009-695009 (2021-06-22)
Endothelial barrier integrity is important for vascular homeostasis, and hyperpermeability participates in the progression of many pathological states, such as diabetic retinopathy, ischemic stroke, chronic bowel disease, and inflammatory disease. Here, using drug repositioning, we discovered that primaquine diphosphate (PD)
Helena Mistry et al.
Molecular cancer therapeutics, 12(12), 2651-2662 (2013-10-17)
Inhibitor of DNA binding 1 (ID1) transcription factor is essential for the proliferation and progression of many cancer types, including leukemia. However, the ID1 protein has not yet been therapeutically targeted in leukemia. ID1 is normally polyubiquitinated and degraded by
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