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Formyl peptide receptors FPRs are a family of
2021-09-06
Formyl peptide receptors (FPRs) are a family of surface-expressed, G protein-coupled receptors [7]. The three members, FPR1, FPR2 and FPR3, share significant sequence homology, but have different functional properties [7]. While FPRs are mainly expressed by innate leukocytes, they are also found on
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CC is a widespread disorder affecting up
2021-09-06
CC is a widespread disorder affecting up to 20% of people worldwide, which also deteriorates the quality of life of patients and causes a substantial economic burden to society. There are 3 categories of CC: normal-transit constipation, slow-transit constipation and defecatory or rectal evacuation d
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br Introduction The fibroblast growth
2021-09-06
Introduction The fibroblast growth factor receptor (FGFR) pathway is an important oncogenic driver in malignant cancer. It controls cellular processes such as cell proliferation, differentiation, migration, cytidine australia progression, metabolism, and survival. In non–small-cell lung cancer,
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bcl-2 Potential roles for S P in angiogenesis cancer and aut
2021-09-06
Potential roles for S1P in angiogenesis, cancer, and autoimmune diseases such as RA have been reported [73]. In RA synoviocytes, S1P has been shown to enhance expression of prostaglandin E2 (PGE2) and cyclooxygenase-2 (COX-2) in response to the pro-inflammatory cytokines, TNF-α and interleukin (IL)-
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Introduction Vesicular exocytosis an intracellular membrane
2021-09-06
Introduction Vesicular exocytosis, an intracellular membrane trafficking pathway, is a ubiquitous process for intercellular communication. It occurs when an intracellular vesicle fuses with the cell membrane and subsequently releases an infinitely minute number of chemical or biochemical messengers
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Here we report the kinetics of inhibition of the
2021-09-06
Here, we report the kinetics of inhibition of the MYST HAT family member KAT8 by MG149, and a calculation of the inhibitory constant Ki of MG149 for KAT8. The inhibition of HATs by MG149 could be correlated to inhibition of histone acetylation in murine PCLS upon MG149 treatment, as determined by a
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In the adult normal spinal cord the resident cells mainly
2021-09-06
In the adult normal spinal cord, the resident cells mainly include neurons, astrocytes, oligodendroglia and microglia (Lecca et al., 2012, Miyagi et al., 2012). After SCI, the lesion microenvironment is complex, which includes the functional changes of CNS resident cells and the infiltration of leuk
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exendin 4 receptor A series of P P ureas were explored first
2021-09-06
A series of P3-P4 ureas were explored first and their anti-NS3 protease activity, antiviral properties in a HCV replicon cell-based assay and PK profiles examined. Installation of a methyl group on the P4 side nitrogen exendin 4 receptor of the urea yielded , a molecule which retained intrinsic pot
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We also evaluated the effect of varying ionic str http
2021-09-06
We also evaluated the effect of varying ionic strength. These experiments included previously characterized H3 (residues 1–21) and SNAIL (residues 1–9) peptides [8], [34] to allow a comparative analysis with different ligands (Fig. 1A). As shown in Fig. 2 and listed in Table 2, it is evident that a
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br Transparency declaration br Acknowledgements br Hepatitis
2021-09-06
Transparency declaration Acknowledgements Hepatitis C Virus (HCV) infection represents a disease of significant global impact that afflicts around 170 million people worldwide., A small proportion of infected people clear the virus naturally, whilst the majority develop chronic hepatitis C (
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Direct Mouse Genotyping Kit Introduction In the s nitric oxi
2021-09-06
Introduction In the 1980s, nitric oxide (NO) was first characterized as critical to both innate immunity and endogenous signaling in animals [[1], [2], [3], [4], [5]]. NO was the first gaseous signaling molecule synthesized by animals to have its biochemical signaling pathway fully described [2]. P
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Several studies have found that GPR
2021-09-06
Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected CRT0044876 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (R
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br Conclusion br Acknowledgements This work was supported by
2021-09-06
Conclusion Acknowledgements This work was supported by a Grant-in-Aid for challenging Exploratory Research (15K12715) and was a partly supported by Suzuken Memorial Foundation (2014). The authors would like to thank Enago (www.enago.jp) for the English language review. G protein-coupled rec
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In addition to their functional activation
2021-09-06
In addition to their functional activation of GPR109A, compounds of the pyrazolopyrimidine class also enhanced the binding of nicotinic Sennoside A to the receptor. For instance, increased the binding of H-nicotinic acid to the receptor (black curve) in a concentration-dependent manner, whereas unla
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As part of their ongoing effort in the field Kalypsis
2021-09-06
As part of their ongoing effort in the field, Kalypsis recently disclosed that quinazolinones 5 [49], imidazo[1,2-a] [1,2]diazepin 6 [50] and quinolines 7 [51] all had activity as small molecule modulators of TGR5 (Figure 4). Intercept, however, disclosed different bile Fmoc-Gly-OPfp sale derivativ
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