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Despite the importance of intratumor phenotypic
2022-01-03

Despite the importance of intratumor phenotypic heterogeneity for tumor progression and therapy resistance (Marusyk et al., 2012, Marusyk and Polyak, 2010), our understanding of regulators of this process and our ability to modulate them are very limited. Recent advances in genomic sequencing and si
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Originally identified as a GPCR upregulated on Burkitt lymph
2021-12-31

Originally identified as a GPCR upregulated on Burkitt lymphoma cells upon Epstein-Barr virus infection (Birkenbach et al., 1993), Ebi2 was later found to play critical roles in immunity by regulating the migration of activated Glyoxalase I inhibitor to extrafollicular sites for early plasmablast r
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Restless running behavior was first described in mice after
2021-12-31

‘Restless running behavior’ was first described in mice after administration of 30mg/kg i.p. ALX-5407 and was thought to be due to an augmentation of NMDA-induced dopamine activity [27]. The motor impairments caused by ALX-5407 were confirmed by Perry et al. [10] and extended to another sarcosine-de
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Pyridostatin To maintain low Glu concentrations in the synap
2021-12-31

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino Pyridostatin is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and
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Bestatin hydrochloride Xenobiotic metabolizing enzymes are c
2021-12-31

Xenobiotic metabolizing enzymes are classified as being phase I, phase II and transporter enzymes, with phase I enzymes metabolizing lipophyllic xenobiotics to make them more polar so that the phase II enzymes can perform the necessary conjugation reactions that afford elimination. Although the phas
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In mammals a major physiological role of the GHSR gene
2021-12-31

In mammals, a major physiological role of the GHSR gene appears to be in regulating food intake and energy homeostasis by partaking in the neuronal mechanisms involving neuropeptide Y and agouti-related protein (Nakazato et al., 2001, Chen et al., 2017). In our study, determination of the abundance
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Emerging evidence has shown that pharmacological FXR agonism
2021-12-30

Emerging evidence has shown that pharmacological FXR agonism attenuates chronic alcohol treatment-induced liver injury and steatosis [18], [19], while whole-body FXR knockout worsens alcohol-induced liver injury [19]. This suggests that FXR plays an important role in ALD development. However, defici
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br Conclusions Symptoms from bilateral thalamic edema caused
2021-12-30

Conclusions Symptoms from bilateral thalamic edema caused by increased venous hypertension can be reversed with appropriate management of the inciting vascular lesion. This case demonstrates a rare patient with decreased CBF in the thalamus in SPECT and completely recovered after factor Xa inhibi
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Several named antagonist ligands have
2021-12-30

Several named antagonist ligands have figured noticeably in preclinical studies, with proved clear ability to release neurotransmitters and having efficacy in preclinical animal models. Consequently, this has encouraged ongoing research on improved agents with potency, selectivity, and better drug-l
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G P also plays a
2021-12-30

G6P also plays a critical role in regulating HK2 binding to mitochondria. Elevated levels of intracellular G6P weaken HK2 binding to mitochondria, causing the enzyme to translocate to the cytoplasm and facilitate anabolic glucose metabolism. Acidosis similarly induces HK2 translocation from mitochon
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Accompanied with apoptosis other ways of neuronal death also
2021-12-30

Accompanied with apoptosis, other ways of neuronal death also occur in ischemic foretinib due to the impairment of mitochondrial homeostasis [16]. Oxidative DNA damage activates poly (ADP-ribose) polymerase 1 (PARP-1) to induce regulated necrosis, referred to as parthanatos, in the brain [17]. Over-
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Nevertheless the frequency of CTCs was higher in patients wi
2021-12-30

Nevertheless, the frequency of CTCs was higher in patients with metastatic breast cancer, which is to be expected because cancer RPC1063 from the original clone that caused the metastasis probably had features favoring their spread throughout the body. When we take HER2+ CTC counts ≥ 3 as a “strong
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Hh signaling pathway plays an essential role in the regulati
2021-12-30

Hh signaling pathway plays an essential role in the regulation of invertebrate and vertebrate tissue development and metabolic homeostasis. Components of Hh signaling pathway have been identified in succession, including Hh ligands, membrane protein receptors, cytoplasmic components and transcriptio
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In our previous studies examining
2021-12-30

In our previous studies examining erectile responses in sGCα1−/− mice, we found that the sGCα1 subunit was required to obtain proper erectile responses to substances generally known to exert their actions by sGC.17, 18 Based on our previous observation of residual relaxing responsiveness to exogenou
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In parallel we were also preparing and evaluating other pipe
2021-12-30

In parallel, we were also preparing and evaluating other piperidine bioisosteres and modifications to – to further access additional novel intellectual property (IP) space. Modeling work suggested that 4-position homologated piperidines, as well as 3-position homologated azetidines overlapped favora
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