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In the late s Solvay Pharmaceuticals discontinued
2024-10-16
In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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br Results and discussion The classical radiochemical adenos
2024-10-16
Results and discussion The classical radiochemical adenosine kinase assays developed to monitor AdK activity utilize [3H]adenosine or [14C]adenosine, respectively. The assays are terminated by spotting the incubation mixture onto diethylaminoethyl (DEAE) anion exchange filter disks or onto a poly
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br Thymic expression of AChR
2024-10-16
Thymic expression of AChR Both linear unfolded epitopes of AChR subunits and the intact AChR are avidly expressed in thymus, particularly by thymic epithelial cells and myoid cells [17], [18], [19]. AChR-antibody positive MG patients often show thymic hyperplasia, characterized by lymphoid follic
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Osteoblasts have been thought to be the major cell
2024-10-16
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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br Methods br Results and discussion br Conclusions
2024-10-16
Methods Results and discussion Conclusions Acknowledgements The authors thank Dr. Francois Alhenc-Gelas (then INSERM U367, Paris, France), who kindly provided the plasmid for truncated soluble recombinant human ACE – WTΔ, Dr. Elena Arablinskaya (Institute of Phtiziopulmonology, Moscow, R
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Arginases from several species and tissues have been found t
2024-10-16
Arginases from several species and tissues have been found to be inhibited by amino acids [51]. In the present study, monocarboxyilic amino acids with five or more carbon atoms such as ornithine, lysine, valine, leucine and isoleucine inhibited CL-ARG. The results revealed that as the amino Nalidixi
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Introduction Hepatocellular carcinoma HCC is one of the most
2024-10-16
Introduction Hepatocellular carcinoma (HCC) is one of the most difficult cancers to treat, and it threatens human health severely [1]. Although various interventions, including surgical operation, radiofrequency ablation, and chemotherapy, have been endorsed, the prognosis of HCC patients remains p
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Previous studies to investigate the functions of
2024-10-15
Previous studies to investigate the functions of AHR in Treg cytochalasin d have employed a loss-of-function approach, using AHR complete-null mice, or a gain-of-function approach by ligand administration. However, these approaches may confound the interpretation of the results. For example, the bro
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Nystatin The inhibition of the exacerbated inflammatory resp
2024-10-15
The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors
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br LOX in colorectal cancer
2024-10-15
5-LOX in colorectal cancer Colorectal cancer (CRC) like other malignancies exhibits an overexpression of 5-LOX. Ohd et al. (Ohd et al., 2003) revealed in a study that malignant colon tissues overexpress 5-LOX activity and retain elevated levels of inflammatory mediators, leukotrienes. Additionall
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Acknowledgments br P c is expressed in several
2024-10-15
Acknowledgments P450c17 is expressed in several steroidogenic tissues, including the adrenal cortex, the ovary, and the testes (). Thus, 17α-hydroxylase/17,20-lyase is a key enzyme required for the production of both cortisol and sex steroids. This enzyme defect blocks the synthesis of cortisol,
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Recent findings imply that proper
2024-10-14
Recent findings imply, that proper Na+/K+-ATPase function is crucial for unimpaired development of the vertebrate heart. Targeted knockout of Na+/K+-ATPase α1 in mice led to early embryonic lethality whereas heterozygous knockout mice displayed severe hypocontractile hearts [52]. Pharmacological inh
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Several studies have explored the relationship
2024-10-14
Several studies have explored the relationship between dental implants and MRONJ development. López-Cedrún JL et al. [13] reported that BRONJ developed after implant treatment in nine patients who were taking bisphosphonates orally. The mean interval between the initiation of treatment and the onset
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Androgen receptor translocates from the cytoplasm
2024-10-14
Androgen receptor translocates from the cytoplasm to the nucleus after binding to its ligands (Quigley et al., 1995). In the current study, although propofol did not significantly affect total androgen receptor protein levels, it significantly decreased nuclear androgen receptor levels. These findin
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In our previous work diffuse
2024-10-14
In our previous work, diffuse deposition patterns of neocortical Aβ and a hierarchical upward spreading pattern of tau were determined with in vivo 18F-florbetaben and 18F-flortaucipir positron emission tomography (PET) studies, based on the regional frequency of involvement by tau and Aβ (Cho et al
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