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In view of the ubiquitous distribution of the
2025-02-18
In view of the ubiquitous distribution of the arachidonate 12S-lipoxygenase isoforms and the variety of cellular reactions influenced by the resulting arachidonate metabolites, these products widely play important roles in many biological systems. The development of new type-specific inhibitors of t
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br Hypothesis The hypothesis is that AhR in skin diseases
2025-02-17
Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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br AhR Modulators It is now well recognized
2025-02-17
AhR Modulators It is now well recognized that ligand-activated AhR induces an immune tolerance response by acting directly on the antigen-presenting DCs and indirectly by increasing the population of immunosuppressive Tregs 24, 95, 96. In addition to inhibiting the formation or depleting the AhR
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Steroidal CYP inhibitors can further be
2025-02-17
Steroidal CYP17 inhibitors can further be classified based on their mode of action, namely as mechanism-based inhibitors and type I and type II competitive inhibitors [129]. Recent studies investigated other biological targets than CYP17, and some new compounds have shown interesting dual activity a
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The syntheses of a and b are
2025-02-17
The syntheses of 27a and 27b are shown in Scheme 5. Substituted naphthalene 21c was brominated using N-bromosuccinimide (NBS) and 2,2′-azobis(2-methylpropionitrile) (AIBN) to yield 25, which was subjected to lactam cyclization to form 26a and 26b, respectively. Deprotections of each UNC669 yielded
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Introduction Cancer which is responsible for a million death
2025-02-17
Introduction Cancer, which is responsible for a million deaths each year, is universally feared, and approximately 50% of newly diagnosed cases can be cured [1]. The existing cancer treatments, including surgery, chemotherapy, radiotherapy or a combination of them, are quickly losing efficacy. The
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Purification of Rv c In order
2025-02-17
Purification of Rv2477c. In order to investigate the catalytic capabilities of Rv2477c, we expressed the protein as an N-terminal histidine-tagged fusion protein in E. coli BL21 cells and purified the protein by cobalt-affinity chromatography. As shown in Fig. 2A, the 65 kDa fusion protein was expre
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Hepatoid adenocarcinoma closely resembles HCC and in some
2025-02-15
Hepatoid adenocarcinoma closely resembles HCC and in some cases can be indistinguishable morphologically. Hepatoid adenocarcinoma is an aggressive neoplasm, and metastasis to the liver is common [12]. Gastric metastasis from HCC has also been reported [27]. Distinguishing hepatoid adenocarcinoma fro
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Another interesting aspect of neutralizing
2025-02-15
Another interesting aspect of neutralizing AP-1 is the inhibition of interactions between AP-1 and Smad proteins, which synergize to activate the TGF-β1-responsive genes involved in hypertrophic growth of the heart muscle and in the development of cardiac fibrosis. Through preventing AP-1 activation
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Sorafenib was the first small RTK
2025-02-15
Sorafenib was the first small RTK inhibitor drug to be developed and was initially approved against renal cell carcinoma, then against hepatocellular carcinoma (HCC) and more recently for differentiated thyroid treatment [111]. Sunitinib soon followed, being approved for gastrointestinal stromal tum
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jnk inhibitor Luo Dehm Raj Luo Attard Balk Bevan Burnstein
2025-02-15
Luo, Dehm, Raj. Luo, Attard, Balk, Bevan, Burnstein, Cato, Cherkasov, De Bono, Dong, Gao, Gleave, Heemers, Kanayama, Kittler, Lang, Lee, Logothetis, Matusik, Plymate, Sawyers, Selth, Soule, Tilley, Weigel, Zoubeidi, Dehm, Raj. Luo, Attard, Balk, Bevan, Burnstein, Cato, Cherkasov, De Bono, Dong,
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br Conclusions br Material and methods br
2025-02-15
Conclusions Material and methods Conflicts of interest Acknowledgements Introduction Currently more than 30 human proteins are implicated in a range of degenerative disorders owing to their misfolding and misassembly into various aggregate structures and leading to at least 20 serious
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Aldicarb br The lipoxygenase pathway and microvascular compl
2025-02-15
The 12/15-lipoxygenase pathway and microvascular complications of diabetes The 12/15-lipoxygenase pathway in adipose tissue Only recently has adipose tissue been recognized as a highly metabolically active endocrine organ imparting profound local and systemic inflammatory effects. Adipose tiss
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br Experimental br Acknowledgment br Introduction The NADPH
2025-02-15
Experimental Acknowledgment Introduction The NADPH-dependent reduction of d-glucose catalyzed by aldose reductase (E.C.1.1.1.21) (AR) is considered as one of the phenomena leading to the onset of long term diabetic complications [as review see: [1], [2]. In fact, the reduction of the sugar
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Secondly as pointed out by
2025-02-15
Secondly, as pointed out by Sulentic and Kaminski in their recent paper [90], most of the AhR literature to date has focused on mouse AhR. Although both mouse and human AhR are interchangeable in many in vitro systems, the in vivo ligand binding affinity is drastically different between the two AhRs
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