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In the late s Solvay Pharmaceuticals
2025-02-27
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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The cytoplasmic domain of muscle AChR is not accessible to
2025-02-27
The cytoplasmic domain of muscle AChR is not accessible to Terbinafine in vivo. Theoretically, therapy with the cytoplasmic domains should be safe. Safety is demonstrated by the facts that: (1) rats repeatedly immunized with the cytoplasmic domains in TiterMax adjuvant do not develop EAMG, although
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Several studies have recently used optogenetics
2025-02-27
Several studies have recently used optogenetics to selectively activate various cholinergic neurons (Jiang et al., 2014). However, most do not explicitly report direct release of GABA from cholinergic fibers, with the exception of our two studies described above (Saunders et al., 2015a, Saunders et
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Acknowledgments br Introduction Prostate cancer is the first
2025-02-27
Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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Introduction the DNA damage response important implications
2025-02-27
Introduction: the DNA damage response — important implications for tumour development and treatment Cells are invariably challenged by tens of thousands of lesions inflicted on their DNA everyday (Lindhal, 1993). This DNA damage can be caused exogenously by exposure to different types of radiation
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Crystal structures were obtained of sulfonamide
2025-02-27
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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A phase I trial has recently evaluated enzalutamide an
2025-02-27
A phase I trial has recently evaluated enzalutamide, an anti-androgen agent, in patients with ER- and AR-positive advanced BC to estimate safety and tolerability of enzalutamide therapy alone or in association to anastrozole, exemestane or fulvestrant [65]. The results of major clinical trials with
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br Conclusions In sum enhanced incentive motivation in
2025-02-26
Conclusions In sum, enhanced incentive motivation in obesity-prone rats is mediated by NAc CP-AMPARs. These neurobehavioral differences may render obesity-susceptible populations more sensitive to the motivational influence of food cues, producing more intense, focused, “wanting” that may limit t
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fructose 1 6 bisphosphatase The same applies also to interme
2025-02-26
The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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Acetylcholinesterase AChE activity and expression level
2025-02-26
Acetylcholinesterase (AChE) activity and expression level can be down regulated by TCDD in neuronal cells [3], [6]. Thus AChE could be considered as a target of the neuronal toxicity of dioxin. AChE has several types of transcripts by alternative splicing in the 3′ region of primary transcripts [7],
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Specifically equity injections in a multinational
2025-02-26
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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br Contemporary understanding for alcoholic
2025-02-26
Contemporary understanding for alcoholic cardiomyopathy Up-to-date, a number of theories are postulated for alcoholic cardiomyopathy including generation of mitochondrial reactive oxygen species (ROS), oxidative stress, neurohormonal overactivation (catecholamines and angiotensin II), apoptosis a
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Ryoichi et al modified potent clinical candidate VX with
2025-02-26
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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In the present study we
2025-02-26
In the present study we sought to decipher the role of ATP-citrate lyase and of the mitochondrial NADH-dependent Mae in the oleaginous yeast Y. lipolytica. Indeed, although this yeast is one of the major models for lipid metabolism, the function of these enzymes is still not clear. As the study of t
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Acknowledgments br Introduction Prostate cancer
2025-02-26
Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi