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br Acknowledgments We would like
2022-08-02

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
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FPR family Human FPR was
2022-08-02

FPR family Human FPR was first defined biochemically, in 1976, as a high affinity binding site on the surface of neutrophils for the prototypic N-formyl peptide formyl-methionine-leucyl-phenylalanine (fMLF). It was then cloned in 1990, by Boulay et al. from a differentiated HL-60 myeloid leukemia-c
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So what makes a FFAR agonist different and
2022-08-02

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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br Introduction More than structurally
2022-08-02

Introduction More than 30,000 structurally different isoprenoids, such as steroids, carotenoids, prenyl side-chain of quinones, prenyl proteins, and natural rubber, exist in nature. In a biosynthetic pathway, linear prenyl diphosphates are common structures as a precursor of isoprenoids, as shown
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b ng This SAR work led to the
2022-08-02

This SAR work led to the identification of compound 10r ((±)-2-[3-fluoro-4-[3-(hexylcarbamoyloxy)phenyl]phenyl]propanoic acid, ARN2508) [51] as a potent in vivo active inhibitor of intracellular FAAH and COX activities, which exerts profound anti-inflammatory effects in mouse models of IBD without c
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In the Joint United Nations Program on HIV
2022-08-02

In 2015, the Joint United Nations Program on HIV/AIDS (UNAIDS) proposed that by 2020, 90% of people living with HIV should be aware of their HIV status, as the first part of 90-90-90 strategy to end AIDS epidemic. Early detection of HIV allows initiating care for proper treatment, which impacts in m
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br Results br Discussion A key step
2022-08-02

Results Discussion A key step in the regulation of gene Pravastatin sodium is the methylation on H3K4, which is added by the multi-component MLL/COMPASS-like histone methyltransferases. Many studies have shown the requirement of shared core subunits for optimal methylation activity of catalyt
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In order to estimate the
2022-08-01

In order to estimate the influence of mitochondrial hypo-polarization on generated OMP, IMP was changed from the normal value of Δψi = −140 mV (Fig. 4A, D, G) to Δψi = −100 mV (Fig. 4B, E, H), resulting in lower magnitudes of calculated OMP for hypo-polarized 6063 (Fig. 4B). Similarly, a remarkable
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In the present study we focused on a
2022-07-30

In the present study, we focused on a role of the C-terminal segment in GCAP2 using two chimeric proteins, in which the C-terminal segment of GCAP2 was either replaced by the corresponding sequence of recoverin (chimera GR) or transferred into recoverin (chimera RG). We have monitored Ca-dependent c
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The difference in the expression of functional FFARs
2022-07-30

The difference in the expression of functional FFARs between neutrophils and monocytes/macrophages suggests that the role of FFA2R may be restricted to the very early phase of acute inflammation where neutrophils are dominating players called into action, whereas GPR84 may have a broader functional
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Despite the rapid development of synthetic ligands the endog
2022-07-30

Despite the rapid development of synthetic ligands, the endogenous ligands of GPR109A, GPR109B and GPR81 remained elusive until recently. This is probably the result of their relatively low potencies and their metabolite character (Table 1). Traditionally, agonists of GPCRs were believed to belong t
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GPR detection by reverse transcription polymerase chain reac
2022-07-29

GPR35 detection by reverse transcription-polymerase chain reaction (RT-PCR). Total RNA of cultured DRG neurons was extracted using the RNAqueous kit (Ambion). Complementary DNA (cDNA) was synthesized from 1μg of isolated total RNA with SuperScript III reverse transcriptase (Invitrogen). An aliquot o
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br Author contributions br Acknowledgements The
2022-07-29

Author contributions Acknowledgements The work was financially supported by a grant from the Investigator-Initiated Studies Program (Ref. #38124) from Merck Sharp & Dohme, and, in part, from Research Grants Council of the Hong Kong Special Administrative Region, China (Ref. No.: 14110314), awa
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In vertebrates three cognate receptors or receptor like sequ
2022-07-29

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 Amsacrine
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Flutamide synthesis The study of TcMYH protein is a step for
2022-07-29

The study of TcMYH protein is a step forward for the characterization of a GO system in T. cruzi. The complete system appears to be present and our findings demonstrate that is important to maintain DNA stability of the nuclear and mitochondrial genomes, particularly in the presence of oxidative str
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