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br Substrate Interactions Outside of the Catalytic
2021-09-27
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
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The eel and perhaps other euryhaline teleost fish
2021-09-27
The eel, and perhaps other euryhaline teleost fish, have the additional peptide, renoguanylin that exhibits high levels of expression within the kidney as well as the intestine. In terms of overall sequence, pre-prorenoguanylin is more homologous to pre-proguanylin than pre-prouroguanylin and a phen
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Unlike the bacterial SRP pathway for
2021-09-27
Unlike the bacterial SRP pathway for which the energetics, kinetics, and structure of almost every intermediate have been characterized, multiple questions remain for the GET pathway (Figure 3, marked with ‘?’). First, the targeting pathway demands distinct activities of Get3 before and after substr
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Several studies have proposed that high levels
2021-09-27
Several studies have proposed that high levels of KYNA in the Iloperidone contribute to cognitive dysfunctions presented by patients who suffer from schizophrenia [30], [31], [32], [33]. Considering that: (i) KYNA is a known GPR35 agonist [2], (ii) cognitive impairments in patients with schizophren
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In normal tissues the expression patterns of GPR
2021-09-27
In normal tissues, the expression patterns of GPR120 and GPR40 are not uniform. GPR120 is highly expressed in adipocytes, lung and intestinal tract, while GPR40 is shown to be expressed in pancreatic islet BS-181 HCl and intestinal tract [7], [20]. It is considered that the distribution of the GPR12
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GPR is a member of the G protein coupled receptor
2021-09-27
GPR119 is a member of the G protein-coupled receptor family, and is highly expressed in pancreatic β-cells and intestinal endocrine cells. It has been proposed that GPR119 agonists modulate glucose homeostasis by indirectly stimulating glucose-dependent insulin release through enhancing pancreatic c
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HOSu synthesis The kinetic data obtained from incubation of
2021-09-27
The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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Crystal structures from soluble E constructs Khan et al Kong
2021-09-27
Crystal structures from soluble E2 constructs (Khan et al., 2014; Kong et al., 2013) have revealed globular protein with no regular structure in spite of having eight disulphide bonds (Kong et al., 2013). Although 62% of the protein exists in loops or disordered structures, overall it was well-defin
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The role of the ER EK
2021-09-26
The role of the ER22/23EK variant which is associated with relative resistance to GC, as shown by a reduction of transactivating capacity in vitro and less suppression of sodium butyrate levels after 1mg DST in vivo. Relative GC resistance associated with the ER22/23EK polymorphism might protect fr
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CSL is endowed with an intrinsic
2021-09-26
CSL is endowed with an intrinsic transcription-repressive function, and CAF-effector genes are induced as a consequence of CSL downmodulation (Hu et al., 2012, Procopio et al., 2015), as it can occur upon exposure to pro-carcinogenic stimuli such as UVA or smoke-derived compounds (Menietti et al., 2
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Serotonin hydroxytryptamine HT is a
2021-09-26
Serotonin (5-hydroxytryptamine, 5-HT) is a monoamine with dual functions in the developing and matured brain. 5-HT regulates development of the read this article as a neurotrophic factor and is involved in emotion and cognition as a neurotransmitter in adulthood (Gaspar et al., 2003; Daubert and Co
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Albumin is the major carrier
2021-09-26
Albumin is the major carrier of free fatty acids (FFAs) in plasma [59], and harbours seven binding sites that are common to FFAs with a range of chain-lengths (C10-C18) across its three domains (Fig. 1a) [60,61]. In vitro, saturated, mono- and poly-unsaturated FFAs, with chain lengths ranging from C
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However the clinical development of was terminated in
2021-09-26
However, the clinical development of was terminated in 2013 due to the concerns over liver toxicity, raising important questions regarding the long-term safety and viability of targeting GPR40 and, more specifically, about our understanding of the pharmacobiology and signaling spectrum of this recep
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Tetrazole is one of the
2021-09-26
1-Tetrazole is one of the most commonly used bioisosteres for carboxylic acids arising from their similarity in pKa (ca. 4.5–4.9 vs 4.2–4.4, respectively)., Metabolically, tetrazoles may exhibit an advantage over carboxylic acids because they form -glucuronides which are not as chemically reactive a
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Interestingly the subcellular localization of FBPase in hepa
2021-09-26
Interestingly, the subcellular localization of FBPase in hepatocytes and proximal tubule Carboplatin reveals that FBPase is also able to translocate to the nucleus in these cell types. The nuclear localization of muscle-FBPase was recently reported [35]. This data corroborate our results on the abi
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