• br Substrate Interactions Outside of the Catalytic Cleft As

  2022-07-13

  

  Substrate Interactions Outside of the Catalytic Cleft As for other types of protein–protein interactions, kinase–substrate docking interactions can occur through large binding interfaces or through recognition of short linear sequence motifs. For kinases with a large number of substrates, the use

• Etoposide VP a semisynthetic podophyllotoxin derivative agen

  2022-07-13

  

  Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology

• br Conflict of interest statement br Acknowledgements RF is

  2022-07-13

  

  Conflict of interest statement Acknowledgements RF is supported by Pancreatic Cancer Research Fund (grant to MF); MF is supported by Prostate Cancer UK (PG12-23 and PG13-029). Background Lysophosphatidylinositol Molecular species and the biosynthesis of phosphatidylinositol, the precu

• Excessive adiposity is also a key

  2022-07-13

  

  Excessive adiposity is also a key pathogenic factor in the development of CVD. Through reductions in bodyweight, GPR120 agonism is therefore also implicated as a potential therapy for obesity and heart and vessel disease. In addition to weight loss, when compared with their wild-type littermates, GP

• Strengths The primary feature of GPR agonists

  2022-07-13

  

  Strengths The primary feature of GPR119 agonists resides in their dual mechanism of action in regulating blood glucose 1, 2, 3, 15. GPR119 agonists stimulate GLP-1 release from intestinal L Exendin-3 (9-39) amide as well as glucose-dependent insulin secretion and insulin promoter activity enhancem

• Acknowledgments This research was supported by the

  2022-07-13

  

  Acknowledgments This research was supported by the Korea Research Institute of Chemical Technology (KRICT) funded by the Ministry of Science, ICT & Future Planning (KK1703-G00, KK1707-C05, SI1707-02, KK-1607-C09, and SKO1707C05) and a grant of the Korea Health Technology R&D Project through the Kor

• br Introduction In the treatment of patients

  2022-07-13

  

  Introduction In the treatment of patients with AIDS and human immunodeficiency virus type 1 (HIV-1), anti-retroviral therapy (ART), which uses anti-HIV drugs such as protease inhibitors, integrase inhibitors and reverse transferase inhibitors, has made a major contribution. There are still some s

• Based on work from our labs with mGlu NAMs and

  2022-07-13

  

  Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]

• Accumulating studies revealed a decline of

  2022-07-13

  

  Accumulating studies revealed a decline of TET1 expression in various cancers including breast, liver, colon, skin, prostate cancers [[36], [37], [38]]. Contrast to these studies, our previous research shows that TET1 is overexpressed in EC and improves the efficacy of chemotherapy in EC, coincide w

• Excessive extracellular glutamate may induce excitotoxic neu

  2022-07-13

  

  Excessive extracellular glutamate may induce excitotoxic neuronal damage in disorders of the CNS (Schwartz et al., 2003). EAATs are considered to contribute to prevention of excitotoxicity by glutamate uptake. Our data revealed that expression levels of membrane EAAT proteins in astrocytes are much

• br Vesicular glutamate transporters VGLUTs br Conclusions Du

  2022-07-13

  

  Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,

• Furthermore we argued that an inability to

  2022-07-13

  

  Furthermore, we argued that an inability to encode or monitor the temporal sequence of events or episodes in order to discriminate between other similar or related events (encoding what-happened-when) could result in an increased susceptibility to proactive interference and, thus, in principle expla

• br Materials and methods br Results br

  2022-07-13

  

  Materials and methods Results Discussion Our data show that the ghrelin receptor, Ghsr, links energy homeostasis with a form of adult hippocampal plasticity. The presence of Ghsr on mature DG neurons suggest that acyl-ghrelin may modulate NSPCs indirectly, possibly via soluble factors such

• In this study we demonstrate that the ETS transcription fact

  2022-07-13

  

  In this study, we demonstrate that the ETS transcription factor ETV5 is involved in the regulation of ghrelin system in response to the altered nutritional state. In the recent multiple GWAS studies, three single nucleotide polymorphisms (SNPs) of ETV5, rs7647305 (Thorleifsson et al., 2009; Willer e

• We are aware that the classical biochemical view is

  2022-07-13

  

  We are aware that the classical biochemical view is centered on the local concentrations of specific ion and molecules rather than on cell electric potentials. However, important downstream processes can be influenced by acting locally on these potentials because they regulate the conductance of the

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