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So what makes a FFAR agonist different and interesting
2021-11-12

So what makes a FFAR1 agonist different and interesting? As shown in the , the cellular mechanism is different from those of present insulin-releasing pharmacotherapies—namely the secretion initiators (sulphonylureas and meglitinides) and the incretin-based secretion potentiators (glucagon-like pept
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PS-341 We have presented evidence that only muscle FBPase
2021-11-12

We have presented evidence that only muscle FBPase is detectable within HL-1 cells. This is consistent with past findings of the Eschrich's group, which showed that in rat heart PS-341 expression of FBPase is almost exclusively limited to the muscle isozyme [3]. Results of our preliminary experime
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We found the FAAH CC genotype only confers risk
2021-11-12

We found the FAAH CC genotype only confers risk for anxiety if the CRFR1 minor allele combination is also present. Additionally, the FAAH AA/AC genotype was riskier than the CC if the three CRFR1 minor ppar pathway were not present. This result is somewhat contrary to our prediction as we hypothesiz
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We found the FAAH CC genotype only confers risk
2021-11-12

We found the FAAH CC genotype only confers risk for anxiety if the CRFR1 minor allele combination is also present. Additionally, the FAAH AA/AC genotype was riskier than the CC if the three CRFR1 minor UCB 35625 were not present. This result is somewhat contrary to our prediction as we hypothesized
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One PKC target that controls cortical actin
2021-11-12

One PKC target that controls cortical ro3 sale structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC releases MARCKS
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br Conclusion The histamine H receptor has been
2021-11-12

Conclusion The histamine H3 receptor has been the focus of a great deal of research over the past four decades and in this context, substantial progress has been made in developing H3R-related ligands. The involvement of H3Rs in many neurological disorders has been documented by several lines of
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In an RNAi screen to interrogate the function
2021-11-12

In an RNAi screen to interrogate the function of transmembrane proteins in ISCs/EBs, we identified the SJ protein tetraspanin 2A (Tsp2A) as a tumor suppressor. Further characterization reveals that Tsp2A expression initiates in ISCs and Tsp2A protein assembles at the SJs in the progenitor ciprofloxa
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We acknowledge some important limitations to the study Given
2021-11-12

We acknowledge some important limitations to the study. Given that SEER is a national database of abstracted clinical information, there is selection bias as to which patients underwent RS testing. As clinicians are selecting which patients to test, the RS distributions may not reflect the true dist
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Since we found miR b
2021-11-12

Since we found miR-15b-5p to be differentially expressed along the porcine intestine in 31 day old piglets in a former study [10], the entire miRNA family was analyzed in terms of interaction with potential target-genes. In silico analysis predicted miR-15 family members to target the hedgehog signa
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br Heme oxygenase inhibitors Historically the first class of
2021-11-12

Heme oxygenase-1 inhibitors Historically, the first class of competitive HO-1 inhibitors was represented by MPs, heme analogs in which the central iron NSC228155 of heme is exchanged by another element, such as zinc, cobalt, tin, or chromium. These molecules compete with heme for binding to the e
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GW was also the starting point for a study by
2021-11-11

GW4064 was also the starting point for a study by an independent research group. The co-crystal structure of GW4064 with FXR suggested the potential for favorable hydrogen bond interactions between the isoxazole 3-aryl group and several receptor residues such as Tyr373 and Ser336. Replacing the 2,6-
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A localization of GK to
2021-11-11

A localization of GK to both a cytoplasmic and perinuclear area of normal rat pancreatic beta-cells was reported in 1996 (Noma et al., 1996), which changed on acute hyperglycemia to a more diffuse staining throughout the cytoplasm. The localization of GK within the nucleus was first reported by Mura
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Rare mutations can impair the molecular function of GR
2021-11-11

Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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br Acknowledgments We would like to acknowledge Jenna Hall
2021-11-11

Acknowledgments We would like to acknowledge Jenna Hall, Marita Rivir, Kathleen Smith, Joyce Sorrell, and Emily Yates for assistance with in vivo pharmacology studies. We would like to acknowledge Joe Chabenne and Steph Mowery for assistance with in vitro cell-based assays, and Patrick J. Knerr f
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The focused set of cyclopentapyrazoles produced
2021-11-11

The focused set of cyclopentapyrazoles produced six compounds with sufficient activity to warrant the evaluation of kinetic solubility. Despite the improved activity of the series, these compounds remain stalwartly insoluble (), indicating the need for additional chemical modifications which address
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