Goparaju, G. Franzoso, M.T. Lotze, T. Krausz, H.I. Pass, M.E. Bianchi, M. Carbone Programmed necrosis induced by asbestos in human mesothelial cells causes high-mobility group box 1 protein release and resultant inflammation Proc Natl Acad Sci U S A, 107 (2010), pp. 12611-12616 ...
This work received financial support from PT national funds (FCT/MCTES, Fundação para a Ciência e Tecnologia and Ministério da Ciência, Tecnologia e Ensino Superior) through the project units UIDB/50006/2020 and UIDP/50006/2020 (LAQV-Requimte), and the Institute of Biomedicine (iBiMED...
Fig. 2 PARP1 PARylates NAT10 at K1016, K1017, and K1020 both in vitro and in vivo. A Four GST-NAT10 deletion mutants (∆1–201, ∆202–488, ∆489–753, and ∆754–1025) and GST control were bacterially purified, and subjected to in vitro PARation assay in the presence of...
After incubation for 20 h in the absence or presence of LPS (in the absence or presence of other compounds), the cells were fixed in 2% paraformalde- hyde in PBS for 1 h. The cells were washed three times in PBS and then three times (5 min each) with PBS supple- mented with ...
Additionally, terminal small steric aroyl, para-substituted phenyl, and unsubstituted heteroaryl substituents substantially improved the potency. Cellular inhibition assays with a matched pair of V79 (wild- type) and V-C8 (BRCA2-deficient) cells further confirmed that four analogs (17, 43, 47, ...
When the structure of bisamide was introduced on the para-position of the benzene ring, and the fluorine atom was introduced at 2-position simultaneously, the inhibition rates of compound 15a were increased against PARP1 and BRD4, respectively. Similar trends were observed in the inhibition rates...
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The group identified [124/131I]I2-PARPi (para-iodinated) as the lead candidate, which showed high PARP1 affinity (IC50 = 9 nM) and specificity, shown by blocking. In vivo, [124/131I]I2-PARPi was able to delineate orthotopic glioblastoma xenografts using PET as well as SPECT imaging ...
To monitor the PARylation of DNA-conjugated SA, recombinant SA (rSA) was used since it can be readily captured via commercialized MB-NTA-Ni through the NTA–Ni–oligohistidine interaction [60]. In the first trial, PARP1 was activated by binding to biotin–dsDNA and then PARated to form bi...