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High throughput screening HTS of
2021-04-01
High throughput screening (HTS) of the AstraZeneca 597 sale collection was conducted and identified oxadiazole amide () originating from a kinase directed screening library (although inactive against a panel of kinases). This compound had moderate potency as a DGAT-1 inhibitor (IC=0.52μM) and was
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Our results indicate that C CoA is
2021-03-31
Our results indicate that C75-CoA is formed in the hypothalamus following stereotaxic injection of C75. Inhibition of hypothalamic CPT1 by C75-CoA in vivo, as seen in our experiments, is independent of the putative inhibition by malonyl-CoA, which may be formed after the action of C75 either on FAS
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dpn This work started from the standard version of the CPA
2021-03-31
This work started from the standard version of the CPA model [17] and investigated its known weaknesses: 1) not meeting the defined critical temperature, 2) missing the temperature dependence of pure component saturated liquid densities, 3) using an α function in the cubic term that can provide unre
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In rodent models the loss
2021-03-31
In rodent models, the loss of estrogens through ovariectomy has been shown to promote the development of intracranial aneurysms. Conversely, the administration of an RN 1734 australia receptor beta agonist restores its protective effect, but is abolished with the introduction of a nitric oxide synt
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Williamson et al interrogated the
2021-03-31
Williamson et al. [30] interrogated the fusion gene status of 210 appropriately reviewed and annotated RMS specimens divided into three groups: ERMS (n=77); fusion gene-positive ARMS (n=94); and fusion gene-negative ARMS (n=39), the latter comprising a group of tumor samples that appeared histologic
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Prostaglandin E receptor subtype EP is a transmembrane
2021-03-31
Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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We continued to investigate the contribution of
2021-03-31
We continued to investigate the contribution of the EP1 IPI-504 synthesis to nociceptive sensitization by utilizing its natural ligand PGE and tested the effect of local subcutaneous injection of PGE (5nmol in 5μl) into one hindpaw on mechanical and heat pain thresholds. Wild-type mice displayed ma
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Neonatal hydronephrosis induced by TCDD exposure via lactati
2021-03-31
Neonatal hydronephrosis induced by TCDD exposure via lactation has a critical window for onset: the incidence of this disease peaks around PNDs 1–4, followed by a rapid decrease to a substantially null level in adulthood (Couture-Haws et al., 1991; Yoshioka et al., 2016). The EP1 protein was localiz
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br Experimental Procedures br Acknowledgments br Introductio
2021-03-31
Experimental Procedures Acknowledgments Introduction The ability of the affiliative and nurture hormone oxytocin (OT) to attenuate stress has been observed across psychological, neurological, and physiological levels [1], [2]. We and others have demonstrated that, in the gut, OT can lessen
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br Introduction The protein Epidermal Growth Factor Receptor
2021-03-31
Introduction The protein Epidermal Growth Factor Receptor Tyrosine Kinase (EGFR-TK) play important role in non small-cell lung carcinoma (NSCLC) and vital therapeutic progress withinin the treatment of this ailment has revamped the past ten years through the exploitation of this insight (Mok et a
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N-acetyl D-galactosamine Despite the weak and transient natu
2021-03-31
Despite the weak and transient nature of E2–E3 interactions, this binding is required for the transfer of ubiquitin to the substrate. The low affinity characteristics of this interaction may be due to the fact that E2s use the same surface to interact with E1s and E3s, and hence while binding to an
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Some family I DNA ligases
2021-03-30
Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human leukotriene receptor antagonist I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained activ
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N methyl d aspartate NMDA receptor antagonists
2021-03-30
N-methyl-d-aspartate (NMDA) receptor antagonists, such as MK-801 and phencyclidine, induce cognitive dysfunction in both mice and humans [18]. In addition, antipsychotic drugs ameliorate MK-801-induced cognitive dysfunction; therefore, the acute application of MK-801 can be used as an animal model o
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On the basis of the findings described
2021-03-30
On the basis of the findings described above, a series of heterotricyclic analogs were designed and synthesized. The human CRF1 receptor binding and antagonist activity data for newly designed heterotricyclic core antagonists 28–33 are described in Table 3. Most of the tricyclic core analogs listed
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TR provides requirements for qualification of commercial PLC
2021-03-30
TR-107330 (1996) provides requirements for qualification of commercial PLC. It uses the criteria of NUREG/CR-6421. EPRI TR-104159 (1995) includes experience about dedicating COTS SW for PLC-based digital systems such as DAFAS (Diverse Auxiliary Feedwater Actuation System) and Emergency Diesel Bus Lo
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