Oltipraz - CAS 64224-21-1
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Not Intended for Therapeutic Use. For research use only.
HIF/HIF Prolyl-Hydroxylase
Oltipraz, a promising cancer chemopreventive agent, is a bifunctional inducer, modulating both phase I and II drug-metabolizing enzymes to enhance carcinogen detoxification.
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1.Mitochondrial succinate dehydrogenase is involved in stimulus-secretion coupling and endogenous ROS formation in murine beta cells.
Edalat A1, Schulte-Mecklenbeck P, Bauer C, Undank S, Krippeit-Drews P, Drews G, Düfer M. Diabetologia. 2015 Jul;58(7):1532-41. doi: 10.1007/s00125-015-3577-9. Epub 2015 Apr 15.
AIMS/HYPOTHESIS: Generation of reduction equivalents is a prerequisite for nutrient-stimulated insulin secretion. Mitochondrial succinate dehydrogenase (SDH) fulfils a dual function with respect to mitochondrial energy supply: (1) the enzyme is part of mitochondrial respiratory chains; and (2) it catalyses oxidation of succinate to fumarate in the Krebs cycle. The aim of our study was to elucidate the significance of SDH for beta cell stimulus-secretion coupling (SSC).
2.Nuclear factor E2-related factor-2 (Nrf2) expression and regulation in male reproductive tract.
Wajda A1, Łapczuk J1, Grabowska M2, Słojewski M3, Laszczyńska M2, Urasińska E4, Droździk M5. Pharmacol Rep. 2016 Feb;68(1):101-8. doi: 10.1016/j.pharep.2015.07.005. Epub 2015 Jul 31.
BACKGROUND: Nuclear factor E2-related factor-2 (Nrf2, Nfe2l2) plays an important, protective role in many tissues. However, information on molecular mechanisms of detoxification and drug metabolism regulated by Nrf2/NRF2 in testis and epididymis is scarce, but it may help to better characterize the function of blood-testis and epididymis barriers.
3.The role of Nrf2 in pathology of pleomorphic adenoma in parotid gland.
Droździk A1, Kowalczyk R2, Jaworowska E3, Urasińska E4, Kurzawski M5. Med Sci Monit. 2015 Apr 30;21:1243-8. doi: 10.12659/MSM.892674.
BACKGROUND: Pleomorphic adenoma (benign mixed tumor) is one of the most common salivary gland tumors. However, the processes involved in its carcinogenesis are not well defined. This study aimed to define the contribution of Nfr2 (nuclear factor (erythroid-derived 2)-like 2) to pleomorphic adenoma pathology. The Nrf2-controlled gene system is one of the most critical cytoprotective mechanisms, providing antioxidant responses.
4.ATF3-mediated NRF2/HO-1 signaling regulates TLR4 innate immune responses in mouse liver ischemia/reperfusion injury.
Rao J1, Qian X, Li G, Pan X, Zhang C, Zhang F, Zhai Y, Wang X, Lu L. Am J Transplant. 2015 Jan;15(1):76-87. doi: 10.1111/ajt.12954. Epub 2014 Oct 30.
Activating transcription factor 3 (ATF3) is a stress-induced transcription factor that has been shown to repress inflammatory gene expression in multiple cell types and diseases. However, little is known about the roles and mechanisms of ATF3 in liver ischemia/reperfusion injury (IRI). In warm and cold liver IRI models, we showed that ATF3 deficiency significantly increased ischemia/reperfusion (IR)-stressed liver injury, as evidenced by increased serum alanine aminotransferase levels, histological liver damage, and hepatocellular apoptosis. These may correlate with inhibition of the intrahepatic nuclear factor erythroid-derived 2-related factor 2/heme oxygenase-1 (NRF2/HO-1) signaling pathway leading to enhancing Toll-like receptor 4/nuclear factor kappa beta (TLR4/NF-κB) activation, pro-inflammatory programs and macrophage/neutrophil trafficking, while simultaneously repressing anti-apoptotic molecules in ischemic liver. Interestingly, activation of NRF2/HO-1 signaling using an NRF2 activator, oltipraz (M2), during hepatic IRI-rescued ATF3 anti-inflammatory functions in ATF3-deficient mice.
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