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c.194C > G (p.Ser65Trp). An arrow indicates the proband. Squares signify men, and circles women. The filled symbols represent affected individuals. A diagonal line across a symbol indicates a deceased person. CNSH, central nervous...
A–CThe protein expression of VHL in U373-shNC/shFBXO22, LN229-shNC/shFBXO22, and U87-Vector/FBXO22 cells was detected.D,EVHL mRNA expression in FBXO22 knockdown cells and FBXO22 overexpression cells was assessed by qRT-PCR assay.F,GAfter treatment with CHX, VHL protein expression was...
As a result, we identified 4,282 and 3,585 proteins, respectively, in the pooled cell lysates of RCC4 and 786-O cells (Supplementary Data 1,2). All quantification data were normalized and natural log transformed before further analysis. Differentially expressed proteins were determined by applyi...
in VHL patients are hemangioblastomas of the retina or optic nerve head. A hemangioblastoma is any case of angiomatosis, a proliferation of vascular endothelium, within the central nervous system. Retinal capillary hemangioblastomas are found in up to 70 % of VHL patients by 60 years of...
Targeting the estrogen receptor alpha (ERα) pathway is validated in the clinic as an effective means to treat ER+ breast cancers. Here we present the development of a VHL-targeting and orally bioavailable proteolysis-targeting chimera (PROTAC) degrader
J. Oxygen sensing by metazoans: the central role of the HIF hydroxylase pathway. Mol. Cell 30, 393–402 (2008). 7. Majmundar, A. J., Wong, W. J. & Simon, M. C. Hypoxia-inducible factors and the response to hypoxic stress. Mol. Cell 40, 294–309 (2010). 8. Kamura, T. et...
Hypoxia-inducible factor-1α (HIF-1α) plays central roles in the hypoxia response. It is highly expressed in multiple cancers, but not always correlated with hypoxia. Mutation of the von Hippel–Lindau (VHL) gene, which encodes an E3 ligase, contributes to the constructive activation of HIF...
significantly higher than that of VH032 (Table 1), in line with the increase in LogD7.4, suggesting that VH298 can move through cell membranes more efficiently, leading to an increase on available inhibitor in cells. We next examined potential cytotoxicity of VH298 and VH032 in a range of...