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A number of GCK activators for
2021-12-30

A number of GCK activators for treating T2D have been developed and tested but not progressed successfully from clinical trials into therapy [45]. Our observations suggest that increased risk of hypoglycemia might be possible, particularly if drugs penetrate into brain. A further possibility is that
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Vandetanib br Acknowledgements Supported by the grant from
2021-12-30

Acknowledgements Supported by the grant from National Natural Science Funds of China (81371262). I would like to express my heartfelt gratitude to Professor Yonghua Zhu, who help language editing. Introduction Glucocorticoids are steroid hormones secreted from the adrenal glands in response t
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Introduction The Hedgehog Hh signaling pathway
2021-12-30

Introduction The Hedgehog (Hh) signaling pathway regulates embryonic organogenesis, tissue patterning, and cell differentiation (Armas-Lopez et al., 2017, Ingham and McMahon, 2013). Aberrant activation of Hh signaling pathway contributes to tumor formation and development of various cancers includi
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br Introduction The nature of chemotherapies is to
2021-12-29

Introduction The nature of chemotherapies is to relieve the tumor burden of the patients by eliminating cancer Eltrombopag sale via inducing cell death, mostly regulated cell death represented by apoptosis [1,2]. Dozens of anticancer agents including clinically used ones kill cancer cells by pro
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br General aspects of HDACs br General aspects of
2021-12-29

General aspects of HDACs General aspects of HDAC inhibitors Based on the previous elements, inhibitors designed for HDAC have in common a well-admitted pharmacophore model (Fig. 7A). This model is composed of a zinc binding group (ZBG), attached to a linker chain mimicking the lysine side chai
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To further investigate the relationship between the pro neur
2021-12-29

To further investigate the relationship between the pro-neurogenic and therapeutic actions, we analyzed the effect of VP2.51 in the presence of the antimitotic agent TMZ. No overt side effects were found at the time of testing as assessed by direct observation of the behavior of the animals in their
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br STAR Methods br Acknowledgments This work was
2021-12-29

STAR★Methods Acknowledgments This work was supported by the American Diabetes Association (grant 1-12-BS-161 to J.D.P.), an NIH predoctoral T32 in Autoimmunity and Immunopathology grant (AI089443-05 to D.M.P.), the NIH (grant DK099550 to H.M.T.), the American Association for Cancer Research (S
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br Acknowledgements This work was supported by
2021-12-29

Acknowledgements This work was supported by the National Key Research and Development Program of China [2017YFD0400106]; Innovation of modern Project[F18R02-03]. Introduction The Vesiculovirus genus is one of the six genera of the rhabdovirus family. The prototype vesiculovirus is vesicular s
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To maintain low Glu concentrations in the synaptic cleft
2021-12-29

To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino PI3K Akt mTOR Compound Library is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynapt
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br Acknowledgments br Introduction Postmenopausal osteoporos
2021-12-29

Acknowledgments Introduction Postmenopausal osteoporosis, which is primarily caused by TMP269 deficiency, has been a worldwide health problem and threatens postmenopausal women of all races. An estimated 80% of osteoporosis patients in the United States are women, and approximately 30% of pos
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Murine models of sickle disease
2021-12-28

Murine models of sickle disease have been valuable tools in the study of human SCD pathogenesis [15], [16], and will continue to be central to development of novel approaches to disease treatment. The SAD mouse model of sickle disease is particularly remarkable for its erythrocyte dehydration phenot
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Clinical data showed TAK was rapidly absorbed with
2021-12-28

Clinical data showed TAK-875 was rapidly absorbed with a half-life of 28-30h and clearance primarily through glucouronidation in the liver with minimal urinary clearance [30]. TAK-875 made the glycosylated hemoglobin (HbA1c) levels fall significantly from baseline after 24-week administration in onc
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The FAAH inhibitor activity of the ethoxycarbonyl phenyl
2021-12-28

The FAAH inhibitor activity of the 3-(5-(ethoxycarbonyl)-1-phenyl-1H-pyrazol-3-yl)phenyl cyclohexylcarbamates was investigated by preparation of compounds (43–52, Table 3). These new compounds displayed an important loss of activity in comparison with the corresponding regioisomers 5-phenyl compound
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The molecular mechanisms underlying VSMC ETB receptor upregu
2021-12-28

The molecular mechanisms underlying VSMC ETB receptor upregulation have been studied after 24–48h organ culture in both coronary and cerebral arteries. The increased expression of contractile ETB receptor at these time points has been shown to depend on transcriptional mechanisms and PKC and the ext
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BMP signals play pivotal roles in the
2021-12-28

BMP signals play pivotal roles in the various processes of chondrogenesis [12], [13]. At early stages of chondrogenesis, BMP signaling regulates the differentiation of mesenchymal PF-4708671 into chondrocytes via the induction of Sox9[29]. The loss of Noggin, a BMP antagonist, results in the overgro
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