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The physiological role of the UCNs in
2019-11-04

The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown to
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br Results br Discussion Cell responds to fluctuating enviro
2019-11-04

Results Discussion Cell responds to fluctuating environmental factors by activating a set of compensatory mechanisms including changes in the lipid profile. Compensatory reactions occurring in membranes in response to phosphate deprivation include replacement of phospholipids by phosphorus-fre
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The in vitro cytotoxicity of the prodrugs was assessed in
2019-11-04

The in vitro cytotoxicity of the prodrugs was assessed in the LS174T human colon cell line (). The results were found to reflect the stability of the prodrugs, with the unstable urea compounds ( and ) giving relatively poor cytotoxicity differentials between prodrugs and parents (i.e., approximately
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The enzymatic activity of recombinant
2019-11-04

The enzymatic activity of recombinant sponge P4H was assayed in vitro both at 37°C, the standard enzymatic kinetics temperature, and at 15°C, the typical sea temperature of C. reniformis marine environment (Fig. 2C). Surprisingly the data obtained indicate that the sponge enzyme has a lower activity
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br Diverse functions of ERK pathway Same as
2019-11-04

Diverse functions of ERK pathway Same as the other MAPK cascades, the ERK pathway is activated by several extracellular stimuli and different internal routes. ERK vitally tunes the function of various substrates in all cellular components; the nucleus, cytoplasm, membranes and the cytoskeleton. E
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Based upon these findings on portions A and B novel
2019-11-04

Based upon these findings on portions A and B, novel scaffolds of EP4 antagonist, and (R & R=()-Me; =Cl; R=H), shown in , were identified. We next focused on optimizing portion C of these scaffolds. We utilized for an alternative synthesis of nicotinamide scaffold , which is quite effective for
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Previously we have described increased expression of both cy
2019-11-04

Previously, we have described increased expression of both cytokine and chemokine mRNA (e.g. MCP-5 and fractalkine) in the left ventricle of male EP4-KO mice with dilated cardiomyopathy [2]. Takayama et al. [31] have shown that PGE2 potently inhibits cytokine/chemokine secretion (MCP-1, interleukin
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ci-1033 In the present study we first examined the
2019-11-04

In the present study, we first examined the in vivo and ex vivo effects of androgens on ep1 ci-1033 in the olfactory rosette of male B. sinensis. Thereafter, we cloned two different B.sinensis ar cDNAs and investigated their roles in the effects of 11-KT on ep1 expression. Material and methods
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Y27632 synthesis br Acknowledgments br Introduction Inflamma
2019-11-04

Acknowledgments Introduction Inflammation is the protective reaction of the body to infection, injury, or irritation with the aim to remove harmful stimuli such as pathogens, damaged cells, or allergic irritants and to initiate the healing process. Inflammatory abnormalities play a crucial rol
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In addition to G coupling
2019-11-04

In addition to Gα coupling, it is important to consider that the transition from goal-directed to habitual drug taking also relies on striatal D2R-A2AR heterodimers. Following cocaine self-administration, D2R-A2AR density is increased in the NAc, leading to greater antagonism of the inhibitory (anti
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The repair pathway of DNA DSBs
2019-11-04

The repair pathway of DNA-DSBs through HR and the role of BRCA1 in repair kinetics by HR is also an important factor to unravel the radiation sensitization of novel small molecule inhibitors. The involvement of the breast cancer susceptibility gene 1 (BRCA1) in tumorigenesis and its role in facilita
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Till date several predictive models
2019-11-04

Till date, several predictive models have been developed by different research groups to speed up the process of library selection and drug optimization (Walters et al., 1999, Caldwell, 2000, Plewczynski et al., 2006, Wang and Ramnarayan, 1999, Pogorelcnik et al., 2015, Greenbaum et al., 2002, Sadow
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Estrogen receptor related receptor ERR like other
2019-11-04

Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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NMS-E973 Besides having a remarkable progestogenic
2019-11-04

Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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Raloxifene is a second generation SERM that has
2019-11-04

Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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