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Dvorsky, R.

Publications and source records attributed to Dvorsky, R..

2 recordsLinked to original sources

Identification of SIRT4 as a novel paralog-specific interactor and candidate suppressor of C-RAF kinase in MAPK signaling

Cellular responses leading to development, proliferation, and differentiation rely on RAF/MEK/ERK signaling that integrates and amplifies signals from various stimuli to cellular downstream responses. The clinical significance of C-RAF activation has been reported in many types of tumor cell proliferation and developmental disorders, which requires the discovery of potential C-RAF protein regulators. Here, we identify a novel and specific protein interaction between C-RAF, among the RAF kinase paralogs, and SIRT4 among the mitochondrial sirtuin family members SIRT3, SIRT4, and SIRT5. Structurally, C-RAF binds to SIRT4 through the N-terminal cysteine-rich domain (CRD; a.a. 136-187), and on the other side, SIRT4 requires predominantly the C-terminus (a.a. 255-314) for full interaction with C-RAF. Interestingly, SIRT4 interacts specifically with C-RAF in a pre-signaling inactive (serine 259 phosphorylated) state. Consistent with this finding, ectopic expression of SIRT4 in HEK293 cells results in upregulation of pS259-C-RAF levels and concomitant reduction of MAPK signaling as evidenced by strongly decreased phospho-ERK signals. Thus, our findings propose another extra-mitochondrial role of SIRT4 and suggest that SIRT4 functions as a cytosolic tumor suppressor of C-RAF-MAPK signaling, besides its known metabolic tumor suppressor role towards glutamate dehydrogenase and glutamine levels in mitochondria.

biochemistry↗

ω-imidazolyl-alkyl derivatives as new preclinical drug candidates for NASH therapy

Cytochrome P450 2E1 (CYP2E1) and its production of ROS play an essential role in the development and progression of inflammatory liver diseases such as alcoholic steatohepatitis. For this isoenzyme we have developed two new inhibitors - 12-imidazolyl-1-dodecanol (I-ol) and 1-imidazolyldodecane (I-an) - and wanted to test their effect on the related disease of non-alcoholic steatohepatitis (NASH). The fat-rich Lieber-DeCarli diet, which was administered over the entire experimental period of 16 weeks, was used for disease induction in the rat model, while the experimental substances were administered in parallel over the last four weeks. This high-calorie diet pathologically altered the ROS balance, the amount of adipocytokines, TNF- and lipids as well as the activities of liver enzymes. Together with the histological examinations, the conclusion could be drawn that the diet led to the formation of NASH. I-ol and to a lesser extent I-an were able to shift the pathological values towards the normal range - despite continued administration of the noxious agent. I-ol, in particular, showed an extremely good tolerability in the acute toxicity study in rats. Thus, CYP2E1 appears to be a suitable drug target as well as I-ol and I-an promising drug candidates for the treatment of NASH.

pharmacology and toxicology↗