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p38 pathway Estrogen related receptors ERRs are orphan nucle
2020-12-09
Estrogen-related receptors (ERRs) are orphan nuclear receptors and have three members including ERRα, ERRβ, and ERRγ (Yasumoto et al., 2007). Though they are termed as ERRs due to the sequence homology with estrogen receptors, they don’t need to bind estrogens to exert action. Generally, ERRs bind t
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human leukocyte elastase br Funding This work was supported
2020-12-09
Funding This work was supported by intramural funding of the Department of Internal Medicine I-Cardiology, University Hospital Aachen, RWTH Aachen. Acknowledgments Introduction Cyclic adenosine monophosphate (cAMP) is a central second messenger that controls a plethora of vital functions.
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Furan analogs and N methylpyrrole analogs had completely dif
2020-12-09
Furan analogs and N-methylpyrrole analogs had completely different SARs. For example, replacement of the furan-2-sulfonyl moiety of 6 with the furan-3-sulfonyl moiety resulted in 8 with a decreased EP1 PLX-4720 affinity and an increased antagonist activity, while the corresponding chemical modifica
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BMS 299897 Potential break through technology poised to over
2020-12-09
Potential break-through technology poised to overcome these above-mentioned limitations is that of the “substrate mediated enzyme prodrug therapy”, SMEPT (Fig. 1). Learning from the previously established enzyme prodrug therapies (EPT) and specifically the antibody-directed EPT (ADEPT) [12], develop
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The DDRs have also been
2020-12-09
The DDRs have also been shown to be regulators of certain immunological functions. DDR1 is expressed in stimulated peripheral blood mononuclear Folinic acid (Kamohara et al., 2001) and on activated T cells (Chetoui et al., 2011, Hachehouche et al., 2010, Kamohara et al., 2001). DDR1 can mediate cell
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A role for the E
2020-12-09
A role for the E2–E3 interface in governing mono- versus polyubiquitination is not mutually exclusive with that of the E2 backside, which has previously been shown to mediate polyubiquitination through its ability to bind to Ub [21], [25], [33]. Brzovic and colleagues first demonstrated the importan
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br UVC induced DNA damage a model
2020-12-08
UVC-induced DNA damage: a model to study DNA damage tolerance The UV components of sunlight that reaches the Earth surface are one of the most carcinogenic agents humans are exposed to, and the leading cause of skin cancer [4,12]. UV light causes different types of DNA damage through indirect and
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br Conclusions There is significant
2020-12-08
Conclusions There is significant interest in understanding the contribution of biological mechanisms to the non-linear/bilinear dose–response curves for DNA-reactive agents. Model monofunctional alkylating agents have datasets amenable to PoD determination for genotoxic effects in both in vitro a
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br Discussion The differences in the kinetic properties
2020-12-08
Discussion The differences in the kinetic properties of L-AmDH and LeuDH presented herein reflect a different kinetic mechanism. When compared to its parent enzyme, L-AmDH displayed a different substrate binding order, lower affinity for the keto substrate, and stronger product inhibition. The tw
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ApicomplexansApicomplexans are unicellular and spore forming
2020-12-08
ApicomplexansApicomplexans are unicellular and spore-forming obligate intracellular parasites that occupy diverse host niches (Mogi and Kita 2010). They have remodeled mitochondrial carbon and energy metabolism through reductive evolution. The development of novel drugs is now a very serious challen
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For a physiologically relevant interaction ligand and recept
2020-12-08
For a physiologically relevant interaction, ligand and receptor have to be expressed in the same place. Collagen II is found primarily in cartilage. DDR2 is expressed in proliferating chondrocytes in vivo, and its staining pattern in tibial growth plates is similar to that of collagen II. In additio
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CCG-1423 In conclusion DDR ECD was shown to be
2020-12-08
In conclusion, DDR1 ECD was shown to be sufficient for collagen mediated DDR1 oligomerization, and the oligomerized form binds to collagen with increased affinity. In full length receptors expressed on live cells, DDR1 oligomerization occurred on the cell surface in agreement with the role of DDR1 E
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br Cytokine profile in MPN Results
2020-12-08
Cytokine profile in MPN: Results from experimental investigation Cytokines are small molecules constituted by proteins or glycoproteins, which regulate the immune cell function and the immune system. They are secreted mainly by immune Liproxstatin-1 HCl but also by other cells such as epithelial
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Studies carried out with LTRAs before
2020-12-08
Studies carried out with LTRAs before the identification of the CysLT2R, showed a controversial picture, as results that suggest a role for cysteinyl-LTs in the expansion of ischemic damage and in cardiac dysfunction during reperfusion [5], [68], [69] were evenly balanced by others suggesting that t
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The following are the supplementary data related to this art
2020-12-08
The following are the supplementary data related to this article. Acknowledgments Introduction Drug-resistant epilepsy (DRE) occurs in approximate 30% of patients who suffer from epilepsy [1]. Temporal lobe epilepsy (TLE) is one of the most common partial seizures and the common cause of DRE
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