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While the direct effects of
2023-11-02

While the direct effects of 5-ARI lead to a dramatic Bay 11-7085 in serum DHT levels, other laboratory values are also affected by 5-ARI use. Serum testosterone elevations are known to occur with both finasteride and dutasteride use, but values will typically remain within the normal laboratory ran
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Although the role of apelin and APJ receptor
2023-11-02

Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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cx 5461 TLRs play a key role
2023-11-02

TLRs play a key role in pathogen recognition and early response. In our study, we showed an increase of TLR2 mRNA and protein expression after BMECs were stimulated by S. aureus, as seen for BMECs in a previous study [25]. Although most studies describe TLR4 as a primary receptor for Gram-negative b
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Several strategies have been employed
2023-11-02

Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, Omecamtiv mecarbil induces changes in the spectral properties of the fluorophore(s) incorpo
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The AT hook motif is highly conserved
2023-11-02

The AT-hook motif is highly conserved in evolution from bacteria to humans and is found in one or more copies in a large number of other, non-HMGA, proteins, many of which are transcription factors or are involved in chromatin remodeling [8]. For example, AT-hook peptide motifs are essential compone
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Finally impaired endothelial integrity culminates in an incr
2023-11-02

Finally, impaired endothelial integrity culminates in an increased plasma protein concentration in the interstitial space, and thus accumulation of fluid in the ECM, favoring the swelling of the face and limbs [2] mainly. Concurrently with this systemic change, there is intense activation of coagula
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To the best of our knowledge this
2023-11-02

To the best of our knowledge, this is the first study documenting the SCC modulatory effect at central and kidney level on the shift in the vasoconstrictor-vasodilator ratio of mRNA expression of angiotensin receptors toward vasoconstriction in XY-SCC and/or vasodilation in XX-SCC mice. From these r
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The Irbesartan Diabetic Nephropathy Trial enrolled patients
2023-11-02

The Irbesartan Diabetic Nephropathy Trial enrolled patients with type 2 diabetes, proteinuria of at least 0.9 g/24 h, BP >135/85 mmHg and moderate kidney impairment (creatinine 88 to 265 µmol/L in women or 106 to 265 µmol/L in men). Patients were randomized to receive irbesartan (titrated from 75 to
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Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases A
2023-11-01

Gliomas and Aldehyde Dehydrogenase Aldehyde dehydrogenases (ALDHs) are key metabolic enzymes involved in regulation of glycolysis/gluconeogenesis pathways as well as in the detoxification of endogenous and exogenous aldehydes, regulating cell function and homeostasis. ALDHs play important roles in
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br Perspectives and challenges Previously the main focus
2023-11-01

Perspectives and challenges Previously, the main focus of development of adenosine targets for pain was on A1Rs, due to prominent antinociception in multiple preclinical models and preliminary observations in human trials. However, delivery of agonists can be limited by other (e.g. cardiovascular
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We have previously reported alterations of the thymus
2023-11-01

We have previously reported alterations of the thymus in AChR-MG patients, especially in their germinal center LY364947 (defined as CD19+CD38+ cells by flow cytometric analysis). First, we found that, in MG thymi, this subset failed to show the normal down-regulation of Bcl-2, suggesting that autor
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Tumor suppressor ARF regulates the activity of
2023-11-01

Tumor suppressor ARF regulates the activity of p53 by inhibiting the functions of Mdm2. ARF is induced by hyperproliferative signals emanating from oncogenic Ras, overexpressed c-myc, and from deregulated E2F . ARF prevents p53 degradation and leads to increased p53 function by sequestering Mdm2 to
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In the nineties we knew that baclofen was the stereo
2023-11-01

In the nineties we knew that (-)baclofen was the stereo-selective ligand for the GABAB receptor which had been recognised by Norman Bowery as a receptor for GABA, which was different from the GABAA receptor (Hill and Bowery, 1981). GABAB receptor antagonists were also synthesised and made available
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Crystal structures were obtained of sulfonamide and amide as
2023-11-01

Crystal structures were obtained of sulfonamide 18 and amide 19 as a derivative of amide 36 (Fig. 7A and B). The precise rotameric orientation of amide 36 was of significant interest to understand the compound's interaction with the protein. As it would be difficult to assign the rotomer of 36, the
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Non steroidal anti inflammatory drugs
2023-11-01

Non-steroidal anti-inflammatory drugs, which include aspirin and ibuprofen, target COX-2 activity to inhibit inflammation. It has been shown that daily use of a nonsteroidal anti-inflammatory drugs is associated with reduced ER-positive breast cancer recurrence in obese and overweight women. More pr
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