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GPR co localizes with ghrelin in the duodenum
2021-09-11
GPR120 co-localizes with ghrelin in the duodenum [17], α-gustducin in the small intestine and type II taste bud cells 18, 19, neuropeptide Y centrally in the arcuate nucleus [20] and glucagon-like peptide 1 (GLP-1) in the colon and circumvallate papillae taste bud cells 6, 21, 22. Interestingly GPR1
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In conclusion the present study demonstrated that peripheral
2021-09-11
In conclusion, the present study demonstrated that peripheral nerve exposure to HIV gp120 increased the expression levels of the P2Y12 receptor in DRG SGCs and enhanced mechanical and thermal hyperalgesia in rat models. Up-regulation of the P2Y12 receptor in DRG SGCs further promoted the release of
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Fatty acids have been repeatedly shown to increase
2021-09-11
Fatty acids have been repeatedly shown to increase the responsiveness of pancreatic islets to glucose both in vitro and in vivo[6]. The recent identification of GPR40 as a receptor for free fatty acids that is localized to the pancreatic islet cells has therefore stimulated interest in obtaining sma
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In respect of clinical development Takeda
2021-09-11
In respect of clinical development Takeda has pioneered the field with the GPR40 agonist TAK-875 or fasiglifam (Figure 2A), which in phase-II studies decreased HbA1c as efficiently as sulfonylurea without signs of hypoglycemia [24]. This was obtained with surprisingly little effect on systemic insul
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br Results and discussion br Conclusions TZDs represent a
2021-09-11
Results and discussion Conclusions TZDs represent a well-studied group of antidiabetic agents. Based on previous observations of the ability of some TZDs to activate FFAR1, we designed five scaffolds consisting of the TZD head, a linker, and a carefully selected privileged structure. For the p
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br Introduction Glucose is the major carbon
2021-09-11
Introduction Glucose is the major carbon source in most organisms. Cancer monensin in particular require a steady source of energy to maintain growth and proliferation, and preferentially use glycolysis for their energy supply even under aerobic conditions. Glucose uptake in mammals is mainly me
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While TUNEL staining is traditionally thought to be an
2021-09-11
While TUNEL staining is traditionally thought to be an apoptosis marker, studies have shown that TUNEL can stain necrotic Pimasertib [19], [20], [21]. Furthermore, DNA degradation has also been observed in necrotic cells [22]. TUNEL staining alone is therefore insufficient to distinguish apoptosis
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br Summary br Acknowledgement br GR A Nuclear Receptor with
2021-09-11
Summary Acknowledgement GR: A Nuclear Receptor with Widespread Physiological Impact GR, or NR3C1 (see Glossary), is a transcription factor (TF) that regulates gene expression in nearly every cell of the body. A member of the nuclear receptor (NR) superfamily, its ligand-binding domain confe
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(+)- Corydaline Encouraged by the observation obtained from
2021-09-10
Encouraged by the observation obtained from region A, we selected the structure of 1 as the next template to successively pursue the SAR on regions B-D of 1 (lower side of Fig. 2). Next, we turned attention to the external aromatic ring of 1 to verify the impact on the antagonistic activity and prep
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The release of FBPase and aldolase
2021-09-10
The release of FBPase and aldolase from subcellular structures of muscle was dependent on the presence of the crowding agent imitating the physiological conditions – PEG 8000 (Table 1). The amount of both enzymes associated with structures of muscle gap 27 was about 6–7 times higher in the presence
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Fatty acid amide hydrolase FAAH
2021-09-10
Fatty Doripenem amide hydrolase (FAAH) is a membrane-bound enzyme which releases arachidonic acid and ethanolamine by breaking amide bond of AEA. It also controls the cellular uptake of AEA, by creating and maintaining an inward concentration gradient leading to AEA-facilitated diffusion via a spec
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The effect of combined A and PD
2021-09-10
The effect of combined A-192621 and PD 155080 treatment on the Mevastatin during endotoxin infusion is quite different compared to either drug used alone (Wanecek et al., 1999). After administration of both antagonists in combination, cardiac index increased to baseline values within 30 min, and wa
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MK cyclobutylpiperidin yl oxyphenyl methyl trifluoromethyl q
2021-09-10
MK-3134 (3-[4-(1-cyclobutylpiperidin-4-yl)oxyphenyl]-2-methyl-5-(trifluoromethyl)quinazolin-4-one) was synthesized by Merck, as the structurally constrained analogue of MK-0249 (Nagase et al., 2008). This H3R inverse agonist has MW 457.49, seven HBA, and MLogP 4.58, with one violation in terms of dr
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In the adult normal spinal
2021-09-10
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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ARM1 sale In conclusion studies of the regulation of the HO
2021-09-10
In conclusion, studies of the regulation of the HO-1/BVR/CO pathway by selective pharmacological approaches may lead to the discovery of novel compounds for the treatment of diverse diseases. Recent results validate the use of advances in targeting HO-1 in various vascular diseases. However, there a
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