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In addition to their functional
2022-10-10

In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic CCT241533 synthesis to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, wh
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TGR is a class A GPCR transducing signal through
2022-10-10

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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In vertebrates three cognate receptors or
2022-10-10

In vertebrates, three cognate receptors or receptor-like sequences have been identified with distinct distributions and functions (Millar, 2005, Neill et al., 2001). Only two types of GnRHR occur in mammals, though (Morgan and Millar, 2004). The mammalian type I GnRHR shares over 80% amino arginase
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Compared to previously reported atypical N glycosites that w
2022-10-10

Compared to previously reported atypical N-glycosites that were identified based on the deamidation of asparagine residues after PNGase F treatment [106], [107], these two studies further validated the identified atypical motif glycosites by directly identifying their intact glycopeptides. Since the
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During pain signal transmission glutamate is released
2022-10-10

During pain signal transmission, glutamate is released into the synaptic cleft, which, in turn, causes activation of N-methyl-d-aspartate (NMDA) receptors and hence neurotransmission across the synapse occurs. The synaptic concentration and resultant activity of glutamate are controlled by excitator
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AG 013736 MicroRNA or miRNA is group of RNA molecule of
2022-10-09

MicroRNA, or miRNA, is group of RNA molecule of about 22 nucleotides without protein-coding function. MicroRNAs are widely distributed in plants, animals and even some viruses and participant in both normal physiological and pathological processes by post-transcriptional regulation of gene expressio
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In this present study the availability of commercial GLUT an
2022-10-09

In this present study, the availability of commercial GLUT and SGLT Flurbiprofen directed against different epitopes, enabled us to screen for members of the SGLT family and compare the expression patterns of GLUTs and SGLTs in the different regions of the rat lens. Based on these regional and subc
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Phylogenetic trees of receptors for peptides
2022-10-09

Phylogenetic trees of receptors for peptides similar to glucagon from diverse vertebrate species typically are similar to the tree presented in Fig. 3 (Sivarajah et al., 2001, Chow et al., 2004, Irwin and Wong, 2005, Cardoso et al., 2005, Cardoso et al., 2006, Ng et al., 2010, Park et al., 2013, Hwa
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Introduction Glucose dependent insulinotropic polypeptide GI
2022-10-09

Introduction Glucose-dependent insulinotropic polypeptide (GIP) is a hormone secreted postprandially from enteroendocrine K cells in response to ingestion of either fat [1], protein [2], or carbohydrates [3]. GIP is primarily known for its glucose-dependent insulinotropic actions mediated via the G
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In conclusion a novel series of GPR agonists containing
2022-10-08

In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen motilin receptor agonist had a remarkable effect on the GPR40 agoni
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br STAR Methods br Acknowledgments
2022-10-08

STAR★Methods Acknowledgments We would like to thank V. Gladyshev (Harvard), H. Kornblum (UCLA), L. Greene (Columbia), and J. Baraban (Johns Hopkins) for constructive comments to the project and manuscript. We thank L. Gross and A. Kumar for assistance with editing. We thank L.M. Gerber and Z.
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The lack of biological activity http www
2022-10-08

The lack of biological activity of this family of compounds against T. cruzi is quite unexpected and cannot be attributable simply to the presence of a hydroxyl group at C-1. In fact, either compound 6 or risedronate (5), both bearing a hydroxyl group at C-1, are effective inhibitors of TcFPPS.21, 2
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Murine models of AML were used to
2022-10-08

Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia Busulfan receptor arrest through regulation of cyclin-dependent kinases and increased expressio
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In humans mutations in KDM A KDM
2022-10-08

In humans, mutations in KDM5A, KDM5B, and KDM5C are found in patients with ID, implicating KDM5-regulated transcription in the development or activity of neuronal tissues (Vallianatos and Iwase, 2015). KDM5D is Y-linked, and its role in cognition remains uncharacterized. Mutations in KDM5C are the m
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MAP Ks act at the level of MST to phosphorylate
2022-10-08

MAP4Ks act at the level of MST1/2 to phosphorylate LATS1/2 and regulate the Hippo pathway (Box 1). Of particular interest is the involvement of MAP4K4, a key metabolic regulator [88] and common polymorphisms in the MAP4K4 locus are associated with T2D and insulin resistance [89] in adipogenesis. In
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