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cannabinoid receptor agonist We also found downregulation of
2019-08-13
We also found downregulation of TRIM32 in the hearts of dilated and hypertrophic cardiomyopathy patients in addition to TAC and phenylephrine treated mice [51]. TRIM32 and Dysbindin are known to interact in skeletal muscle, and we could confirm this interaction in cardiomyocytes as well. In cardiomy
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During the past decade it became
2019-08-13
During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo
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On the opposite side sPLA X has also been
2019-08-13
On the opposite side, sPLA2-X has also been implicated in the pathology of cancer [167,168]. Human sPLA2-X induces lipid droplet formation in Ras-driven MDA-MB-231 triple-negative breast cancer vx 765 and promotes their survival during nutrient stress. It acts through the products of its enzymatic
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Of note BRQ and LFM are two well known
2019-08-13
Of note, BRQ and LFM are two well-known immunosuppressive agents (Batt, 1999). As for LFM, it was reported as immunosuppressive therapy for bone marrow (Avery et al., 2004) and renal (Chon and Josephson, 2011) transplantation. Accumulating evidence indicated that organ transplant patients irrelevant
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There was a good alignment profile between
2019-08-13
There was a good alignment profile between compound 26 (IC50 0.06μM) and MTX (IC50 0.08μM) explaining its activity pattern (Fig. 5a). Fig. 5b clearly indicates a different alignment profiles where carbonyl groups are not on the same side between 25 (IC50>100.0μM) and MTX which is in consistency with
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The focus of this review is on the diacylglycerol acyltransf
2019-08-13
The focus of this review is on the diacylglycerol acyltransferase (DGAT, EC 2.3.1.20) enzymes, DGAT1 and DGAT2, that catalyze the esterification of a fatty acyl moiety to a DAG molecule to produce TAG. These enzymes commit DAG to being stored as TAG rather than being diverted for the synthesis of ph
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This work was supported by grants from the Institute of
2019-08-13
This work was supported by grants from the Institute of Cancer Research (ICR) and Biotechnology and Biological Sciences Research Council (BB/I014276/1 and BB/M013782/1). Main Text In 2006, Warburg et al. described an apparently distinct connective-tissue disorder characterized by blepharophimosi
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We aim to apply the same technology to target other
2019-08-13
We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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Substituents at the C position An oxygen containing substitu
2019-08-12
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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Altogether the results of this study
2019-08-12
Altogether, the results of this study demonstrate that peripheral blockade of both ETA and ETB receptors reduces tumor-induced facial heat hyperalgesia and increased spontaneous grooming, without modifying ongoing nociception. It is possible to suggest that bosentan is acting upon both receptors pr
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It is interesting to note that our
2019-08-12
It is interesting to note that agomelatine our results show a very similar behavior in binding of DDR2 ECD to immobilized a-telo (bovine-dermal) versus telo- (rat-tail) collagen I as a function of its oligomeric state. Thus, the telopeptide region of tropocollagen exerts little influence on DDR2-co
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Preliminary studies evidenced the presence of CRFr in gamma
2019-08-12
Preliminary studies evidenced the presence of CRFr in gamma-aminobutyric acid-ergic (GABAergic) neurons of the hippocampus (Yan et al., 1998). In fact, in this CX5461 area, CRF inhibits glutamate release through CRF1r (Bagosi et al., 2015), leading to a decrease in the GABA concentration in the hypo
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br These component origins have been chosen as they
2019-08-12
These component origins have been chosen as they CAY10433 are well-defined options related to developing with components (see for example Morisio and Torchiano (2002); Carney and Long (2000) and Gacek and Arief (2004)). The individual component origins (COTS, OSS, in-house developed components a
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Hepatic steatosis is strongly associated with insulin resist
2019-08-09
Hepatic steatosis is strongly associated with insulin resistance. Numerous studies in humans and animals have shown that insulin-resistant states are often accompanied by hepatic steatosis (Angulo and Lindor, 2001, Marchesini et al., 1999, Marchesini et al., 2005, Petersen and Shulman, 2006, Seppala
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oxytocin receptor A putative SHBG receptor SHBG
2019-08-09
A putative SHBG oxytocin receptor (SHBG-R) has been postulated for about thirty years [66], [69], [70]. The characterization of this receptor has been researched by several groups. There are different ideas on how this receptor works. On the one hand Fortunati et al. provide evidence that SHBG is al
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