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Activation of sGC induces the generation of
2021-10-21
Activation of sGC induces the generation of cyclic guanosine monophosphate (cGMP), phosphorylation of protein kinase G (PKG) and changes in activity of effector proteins such as phosphodiesterases (PDE), ion channels and ion pumps [43]. This pathway eventually leads to dilation of Ac-DEVD-pNA (bron
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Strengths The primary feature of
2021-10-20
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 ganciclovir australia as well as glucose-dependent insulin secretion and insulin promoter activity enhanceme
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br Disclosure statement br Acknowledgements We
2021-10-20
Disclosure statement Acknowledgements We thank Dr. Rona Carroll for her contribution to the preparation of the manuscript and Dr. Iosif Pediaditakis for his contribution to the preparation of the figures. This work was supported by NIHR01 HD019938 to U.B.K. Introduction The mammalian hypot
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Fourthly the distribution sites after
2021-10-20
Fourthly, the distribution sites after i.c.v. injection of FAM-ghrelin(1–7)-NH2 were explored in mice using the technologies of fluorescence labeling. The green fluorescence of FAM-ghrelin(1–7)-NH2 was strongly distributed in these structures of lateral ventricle, lateral septal nucleus, dorsal part
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br Voltage dependent anion channel VDAC is a ubiquitous prot
2021-10-20
Voltage-dependent anion channel VDAC is a ubiquitous protein showing well conserved structural and functional properties in spite of major variations in its sequence (for review see [50]). Most of what we know about VDAC electrophysiological properties (for reviews, see [51], [52]) was initially
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Many extracellular matrix ECM proteins are ligands and regul
2021-10-20
Many extracellular matrix (ECM) proteins are ligands and regulators of integrin/FAK signaling and are involved in various aspects of cancer progression, including growth, survival, invasion, and metastasis (Lu et al., 2012). Tubulointerstitial nephritis antigen-like 1 (Tinagl1), a secreted extracell
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In addition to the regulation of SV
2021-10-20
In addition to the regulation of SV exo- and Lauric Acid by Ca2+ influx retrieval of SV membranes depends on the exocytic insertion of SV components into the presynaptic membrane: If exocytic SV fusion in neurons is abrogated by genetic inactivation of the core release machinery (e.g. knockout of M
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Multi targeting agents are of major interest in modern drug
2021-10-20
Multi-targeting agents are of major interest in modern drug design and discovery. Design of such compounds can be applied to H3R antagonists for the purpose of achieving optimum efficiency as performed for some preclinical candidates such as recently for contilisant (Bautista-Aguilera et al., 2017;
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Several studies have indicated that PLD
2021-10-20
Several studies have indicated that PLD-regulated PA signaling intersects with Rho-mediated cytoskeletal remodeling to drive mesenchymal-like cellular features, and it is known that Rho signaling has the potential to induce YAP/TAZ nuclear activity. Accordingly, Han et al. (2018) provide evidence th
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br Funding This study was supported by
2021-10-20
Funding This study was supported by grants-in-aid for scientific research from the Japan Society for Promotion of Science (grant 16K186462 to Dr. Tomizawa, grant 16K19989 to Dr. Kobayashi, and grant 16H05433 to Dr. Mitsudomi) and a research grant from Boehringer-Ingelheim (to T. Mitsudomi). Co
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br Substrate Interactions Outside of the Catalytic Cleft As
2021-10-20
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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Cysteine Cys residues are frequently found
2021-10-20
Cysteine (Cys) residues are frequently found to be highly conserved within functional, regulatory, catalytic, or binding sites of proteins. Thiol or thiolate chemistry imparts active sites with unique properties like nucleophilicity, high affinity metal binding, and disulfide bond assisted multimeri
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This study is intriguing for several reasons
2021-10-20
This study is intriguing for several reasons. For acute pancreatitis and acute hepatitis, the early impact of inflammatory cell activation has recently been highlighted and macrophages seem to play a critical role in the disease initiation and severity., , To activate the NLRP3 inflammasome, a 2-ch
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Overall our results indicated the involvement of
2021-10-20
Overall, our results indicated the involvement of GABAAR in controlling GnRH/LH release through mechanism which included GABA action on molecular processes leading to GnRH biosynthesis. This is consistent with previous in vivo [14,54] and in vitro [55] studies in ewes suggesting that GABA inhibits G
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Recent data from an investigation conducted with beta cell
2021-10-20
Recent data from an investigation conducted with beta-cell cultures and animals suggest that FFAR1 gene Oxaliplatin is modulated by stimulation of peroxisome proliferator-activated receptor gamma (PPARG) [10]. Intriguingly, in 2001 we had demonstrated effects of the PPARG Pro12Ala single nucleotide
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