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SIN-1 chloride receptor The suboptimal trypsin selectivity p
2021-10-12
The suboptimal trypsin selectivity profile of DPC423 prompted us to investigate additional P moieties for potency and selectivity. Glycinamide P () showed low nanomolar binding affinity against fXa which suggested that this P moiety sits deeper into the S pocket of fXa. To further elaborate on this
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br Introduction The fibroblast growth factor receptor FGFR p
2021-10-12
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, ZD 9379 progression, metabolism, and survival. In non–small-cell lung cancer, the most fr
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br Problem of cellular retention not
2021-10-12
Problem of cellular retention not only affects the cellular activity of the nanoparticles and nanocomplexes but can also have ramifications in their in vivo applications. While inorganic nanoparticles are being developed extensively for detection as well as treatment of different human diseases, i
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The ETA receptor has a higher
2021-10-12
The ETA receptor has a higher affinity for endothelin-1 than the two other agonists, with an affinity order of endothelin-1>endothelin-2>endothelin-3, while the ETB receptor exhibits similar affinities for all three isopeptides (Arai et al., 1990b, Sakurai et al., 1990). Earlier studies of the selec
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DIS used standard methods for locating and contacting
2021-10-12
DIS used standard methods for locating and contacting persons for interview, including the use of phone calls, letters, in person contact, and contact through social media. During this time period, contacts of persons with diagnosed HIV (first-generation contacts) were tested for HIV and, regardless
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br H R agonists In search for potent and
2021-10-12
H2R agonists In search for potent and selective H2R agonists, comprehensive structure–activity relationship studies have been conducted and led to the first H2R agonists, e.g. 4(5)-methylhistamine (16) which is actually now used as selective H4R agonist (Fig. 4) (Durant et al., 1975, Lim et al.,
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The identity of organelles is defined by
2021-10-12
The identity of organelles is defined by a particular set of molecules present on their surface. Most organelles in the endomembrane system (i.e., endoplasmic reticulum, Golgi apparatus, endosomes, and lysosomes) carry Rab GTPases (hereafter referred to as Rabs), which serve as binding platforms for
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Our study has strengths and
2021-10-12
Our study has strengths and limitations. We believe we are the 1st to report a novel model of secondary hypogonadism. Several animal models for hypogonadotropic hypogonadism (kisspeptin and the kisspeptin receptor knockout) exist but we are unaware of animal models of secondary hypogonadism with dif
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A general synthetic pathway to these
2021-10-12
A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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In the present study we found that the expression of
2021-10-12
In the present study, we found that the expression of GPR120 in decidua from women of spontaneous abortion was significantly downregulated compared to the decidua from that of normal pregnancy. Moreover, GPR120 deletion (GPR120−/−) or inhibition predisposed mice to LPS or RU486 induced abortion, ind
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TGR is a class A GPCR transducing signal through
2021-10-12
TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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br Background In resource limited countries many HIV
2021-10-12
Background In resource-limited countries, many HIV patients currently do not have reliable access to essential diagnostic laboratory tests, including CD4, clinical chemistry, hematology, viral load, and diagnosis of common co-infections. CD4 T cell count monitoring remains an important surrogate
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Peripheral injury or disease induced alterations in synaptic
2021-10-12
Peripheral injury- or disease-induced alterations in synaptic efficacy occur not only at the first synapse made by the primary nociceptive afferents in the spinal dorsal horn but are also operational in several regions processing the sensorimotor as well as emotional-affective components of pain, su
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Both preclinical and clinical studies have identified a
2021-10-11
Both preclinical and clinical studies have identified a distributed set of CNS nuclei that participate in cognitive control of feeding behavior. Preclinical studies that utilize restricted access feeding schedules (RFS) indicate that rodents learn to anticipate delivery of scheduled meals as indicat
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A mutation in stearoyl coenzyme A desaturase gene was report
2021-10-11
A mutation in stearoyl coenzyme A desaturase 1 gene was reported to reduce sebum production and monounsaturated fatty acids (MUFA) synthesis in mice, which was accompanied with impaired clearance of gram-positive bacteria-induced skin infection (Georgel et al., 2005). Interestingly, gram-positive ba
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