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In the late s Solvay Pharmaceuticals
2024-05-18
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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Encouraged by this observation a systematic SAR study
2024-05-18
Encouraged by this observation, a systematic SAR study on the A ring -alkoxy was conducted as summarized in . The A ring methoxy-containing KRCA-0008 was proven an optimal substituent in terms of potency after all and its bigger size derivatives were detrimental in both biochemical and H3122 cellula
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ACh induced changes in respiratory frequency could
2024-05-18
ACh-induced changes in respiratory frequency could be of interest. They may reveal an important mechanism of respiratory modulation at the caudal NTS level. ACh-induced increases in respiratory frequency within this region have been also reported by Furuya et al. (2014). Changes in respiratory timin
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Apocynin synthesis Specifically equity injections in a multi
2024-05-18
Specifically, equity injections in a multinational affiliate X located in an ACE country can be passed on as lending to another group member Y located in a different country with a high corporate income tax rate. For the group member Y, the interest on the loans is tax deductible, and at the same ti
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AMG-458 receptor In the last decade the zebrafish has emerge
2024-05-18
In the last decade, the zebrafish has emerged as a valuable vertebrate model to systematically dissect the genetic underpinnings of both vertebrate heart development and function [8,9], as well as distinct cardiac diseases such as congenital heart disease [10], cardiomyopathies [11,12] and cardiac a
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br Acknowledgments This work was supported by the Swiss Nati
2024-05-18
Acknowledgments This work was supported by the Swiss National Science Foundation. 15-Lipoxygenase 1 (15-LOX-1) is a nonheme, iron-containing enzyme predominantly expressed in reticulocytes, eosinophils, macrophages, mast cells, and bronchial epithelial cells . 15-LOX-1 is a key enzyme involved
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Although the exact mechanisms are not
2024-05-18
Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in climbazole expressin
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The approach of enzymatically converting
2024-05-18
The approach of enzymatically converting an analyte and detecting it by the resulting small pH changes near the reduced graphene oxide (rGO) surface has successfully been pursued in case of urea (Piccinini et al., 2017). Furthermore, this work reported that electrostatic layer-by-layer (LbL) assembl
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br Materials and methods br
2024-05-18
Materials and methods Results RT-PCR showed that both arginase 1 and 2 were expressed in the OB of Korean roe deer (Fig. 1). Immunoblotting detected arginase 1 in the OB of roe deer (Fig. 2A, left lane) at a molecular weight of approximately 37kDa, which is the size of the enzyme in the rat O
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Autophagy is a self protecting cellular catabolic
2024-05-18
Autophagy is a self-protecting cellular catabolic pathway that degrades and recycles cytoplasmic contents for the maintenance of cellular homeostasis (Shao et al., 2016b). Macrophage autophagy plays an essential role in atherosclerosis by safeguarding DMAT sale against oxidative stress, reducing ap
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In a missense mutation at codon
2024-05-17
In 1989, a missense mutation at codon 102 of the PRNP gene was first reported to be associated with GSS and, in 1991, the same mutation was also found in affected members of the “H” family (Hsiao et al., 1989; Kretzschmar et al., 1991). By 1995, the pedigree of the “H” family included 221 family mem
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2024-05-17
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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AR Vs are truncated AR proteins lacking
2024-05-17
AR-Vs are truncated AR proteins lacking the AR ligand-binding domain (AR-LBD) [6]. While AR-Vs have frequently been detected in CRPC, their expression and functional role in benign prostate tissues and primary prostate cancers is not readily apparent. Structural rearrangements in the AR gene and alt
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br LO synaptic integrity and memory Interestingly
2024-05-17
12/15LO, synaptic integrity, and memory Interestingly, several groups have found that 12/15LO directly modulates synaptic function. Normandin and colleagues reported that pharmacological inhibition of 12/15LO modulates rat hippocampal long-term depression (LTD), a process by which neuronal synapt
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In summary our data have
2024-05-17
In summary, our data have shown that one mechanism by which glucose may mediate monocyte–endothelial cell interaction in the retinal endothelial cells is via the 12/15-LO pathway Furthermore, our current and previously published data [20,22] indicate a differential role of endothelial 12/15-LO versu
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