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br P Y receptor structure br Pharmacology
2019-11-30
P2Y receptor structure Pharmacology Several subtype selective compounds have been developed in recent years (Jacobson and Müller, 2016; Rafehi and Müller, 2018). These compounds are helpful tools for analyzing the roles of P2Y receptor subtypes in physiology and pathophysiology. The present ar
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Some of the psychoactive actions of nicotine are
2019-11-30
Some of the psychoactive actions of nicotine are mediated by the nigrostriatal and mesolimbic pathways (Di Chiara, 2000, Di Chiara et al., 2004). The nigrostriatal pathway originates in the dopaminergic neurons located in the substantia nigra and terminates in the putamen and nucleus caudatus which
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The anticholinesterase activities of all subfractions derive
2019-11-30
The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active
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br Conclusions and future perspectives It is now
2019-11-30
Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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Curcumin is a polyphenol extracted from turmeric which
2019-11-29
Curcumin is a polyphenol extracted from turmeric, which is commonly used as a spice and food-coloring agent in many cultures [9]. Curcumin possesses anti-inflammatory, antioxidant, and cancer-preventive properties [10], [11], [12]. In addition to these well-known effects, consuming curcumin may bene
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Selective inhibitor of phosphodiesterase type PDE I
2019-11-29
Selective inhibitor of phosphodiesterase type 5 (PDE5I) is commonly used for ED treatment. PDE5I exhibits its vasodilatory effect by inhibiting the degradation of cyclic guanosine monophosphate (cGMP), which relaxes the smooth muscle and allows increased blood flow for penile tumescence. Udenafil (D
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Iberiotoxin synthesis The role of Epac in the regulation of
2019-11-29
The role of Epac in the regulation of intracellular Ca homeostasis and contractility is still matter of debate. In rat adult cardiomyocytes, acute Epac stimulation decreased the amplitude of Ca transients [6], [9], [10] with either no changes [6] or increments [9] in cell shortening, suggesting an e
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br Activatable optical imaging probes Optical
2019-11-29
Activatable optical imaging probes Optical fluorescence imaging, which directly detects photons emitted from fluorescent probes, has become as a powerful analytical method to study biological processes both in vitro and in vivo. It is characterized by high sensitivity, is free of radioactive irra
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mth1 pathway br Target enzyme attributes and substrate
2019-11-29
Target enzyme attributes and substrate peptide selection Protein kinases catalyze the phosphorylation of serine, threonine, and tyrosine residues in both proteins and peptides using ATP as the phosphoryl donor. The human kinome is comprised of 518 protein kinases and 40 lipid kinases. The vast ma
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PP 3 Breast cancer is the most common neoplasm in women
2019-11-29
Breast cancer is the most common neoplasm in women, with approximately 231,840 new cases of invasive breast cancer, 60,290 additional cases of in situ breast cancer and 40,290 deaths occurring in 2015 in the United States. Meanwhile, about 2350 men will be diagnosed with breast cancer, and 440 men w
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Based on the similar activities of Rad p and
2019-11-29
Based on the similar activities of Rad6p and Cdc34p (i.e., both are E2 ub-conjugating enzymes) on ubiquitinylation of p33 replication protein, we propose that Rad6p and the plant Ubc2p mono- and bi-ubiquitinate the viral replication proteins in order to facilitate the recruitment of the cellular ESC
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br Materials and methods br Results br
2019-11-29
Materials and methods Results Discussion Ubiquitination is an important eukaryotic process that defines the fate of proteins and their functionality. It has multiple roles in cell survival, differentiation and development (Glickman and Ciechanover, 2002). Ubiquitination is usually known as
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Functional studies suggested the presence of a cysLT recepto
2019-11-29
Functional studies suggested the presence of a cysLT1 receptor. We observed an LTD4-induced cytosolic calcium response, albeit one that was very weak by most standards. The magnitude of the average response was partially explained by the low percentage of TC-I 2000 showing a very transient response
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ABT-888 Alzheimer s disease AD is a chronic progressive
2019-11-29
Alzheimer’s disease (AD) is a chronic, progressive neurodegenerative disorder of the ABT-888 which is considered a leading cause of dementia and affects 20–30 million people worldwide. Presently, a suitable treatment and prevention strategy against AD is hardly available. Various studies have been
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Compound was prepared from chloroindole
2019-11-29
Compound was prepared from 6-chloroindole () () by acylation, to give , and subsequent reduction to give . The thiazole was then installed using conditions developed by Buchwald and co-workers to give . Hydrolysis of the ester yielded the thiazole EX 527 derivative (). Derivatives and were prep
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