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Because AM had limited efficacy on rodent
2022-06-07

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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br RESULTS br DISCUSSION In this study we found impaired
2022-06-07

RESULTS DISCUSSION In this study, we found impaired apoptosis in the peripheral blood of RA patients when compared with peripheral blood from normal controls. Our previous studies have shown that the number of CD4 + T XAP044 increased while regulatory T (Treg) cells diminished in the peripher
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Considering their good FAAH inhibitory activity compounds an
2022-06-07

Considering their good FAAH inhibitory activity, compounds and have been selected for an in vivo study in a DSS-induced colitis model. Specific Pathogen Free male 7weeks old C57/Bl6 mice received 2.5% DSS in drinking water during 8days. Concomitantly, they were administrated daily intraperitoneally
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GDC-0349 br Sources of funding This work was supported
2022-06-07

Sources of funding This work was supported by grants from the Canadian Institutes of Health Research (CIHR) (No. MOP-111096) and from the Heart and Stroke Foundation of Canada awarded to Dr. Danielle Jacques. Disclosures Acknowledgments Introduction A large number of epidemiological, hu
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Following the discovery of diketo compounds S and L
2022-06-07

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent Milnacipran HCl based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase
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br Conclusion The histamine H receptor has been
2022-06-07

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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br Conflict of interest br Acknowledgements br
2022-06-07

Conflict of interest Acknowledgements A Class of Unconventional, Dimerization-Activated GTPases GTP-binding proteins, or GTPases, are a superfamily of proteins that regulate numerous cellular pathways 1, 2, 3, 4. Pioneering work on the extended Ras subfamily of GTPases, exemplified by Ras,
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Introduction Epigenetic alterations play an important role i
2022-06-07

Introduction Epigenetic alterations play an important role in carcinogenesis. Aberrant promoter CpG island hypermethylation causes transcriptional gene silencing [1], and has been documented for a number of genes in prostate cancer (PCA) [2]. Histone modifications are also important regulators of t
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br Introduction Excitatory pyramidal neurons
2022-06-07

Introduction Excitatory pyramidal neurons are generated in the cortical ventricular zone and migrate into the cortical plate alongside the radial glial processes (Chanas-Sacre et al., 2000, Hartfuss et al., 2001, Noctor et al., 2001, Rakic, 1972, Tan et al., 1998). Neuronal migration determines t
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Recently several groups reported that four
2022-06-07

Recently, several groups reported that four orphan receptors, GPR40, GPR41, GPR43, and GPR120, can be activated by free fatty acids. Short-chain fatty acids are specific agonists for GPR41 and GPR43 . Medium and long-chain fatty acids can activate GPR40 and GPR120 . Our previous report showed that
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For some agonists these stable GPR
2022-06-07

For some agonists, these stable GPR119 responses were resistant to washing. Thus, sustained activation could continue, for at least a number of hours, even after removal of free agonist. These data are consistent with reports for other GPCR systems that do not desensitize (Calebiro et al., 2009, Fer
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In three independent groups identified GPR A
2022-06-07

In 2003, three independent groups identified GPR109A (HM74A) and GPR109B (HM74), two GPCRs, as the receptors for niacin., , GPR109A, which is present in all species, is a high affinity receptor for niacin., GPR109B, which is only present in human and chimpanzee, is a low affinity receptor for niac
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Of the patients that presented a CD dip with
2022-06-07

Of the 11 patients that presented a CD4 dip with no cause identified other than HIV-infection, 9 had CD4 counts >200 cells/μL in the next measurement and all experienced the event during the first 24 months of follow-up. Intra-laboratory measurements and individual patient physiologic factors also i
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br Introduction Prostate cancer is the
2022-06-06

Introduction Prostate cancer is the most commonly diagnosed cancer and the second leading cause of cancer deaths in men in the United States, accounting for about 30,000 cancer deaths annually [1]. Epidemiological studies that show geographical variations in prostate cancer incidence and mortalit
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br Materials and methods br Results
2022-06-06

Materials and methods Results Discussion The glucose transporter GLUT1 can be acutely activated or inhibited in L929 fibroblast read full article by a wide variety of reagents or nutrient conditions [[9], [10], [11], [12],36,50]. This abrupt change in the activity of GLUT1 occurs within min
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