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SM-164 australia The overall decrease in consummatory drive
2022-07-25

The overall decrease in consummatory drive seen in rodents treated with naltrexone in previous studies is in accordance with the effects seen with mice treated with SNAP 37889 in this study. While it may seem inappropriate to use a broad-acting drug like SNAP 37889 that suppresses overall consummat
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Due to the presence of all FGFRs in
2022-07-22

Due to the presence of all FGFRs in the epithelium, there are several FGFs ligands that could be binding to these FGF receptors, namely FGFs 1–4, 8–10, 16 and 18–20. By evaluating the known roles of FGFs in epithelial-mesenchymal interactions and in bone development, this list can be reduced. For ex
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Main Text FFAR GPR is a long
2022-07-22

Main Text FFAR1 (GPR40) is a long-chain fatty 90 (LCFA) receptor highly expressed and enriched in enteroendocrine cells, where it senses LCFAs generated from dietary triglycerides, and in pancreatic islet cells, where it acts as a powerful stimulator of insulin secretion. However, the physiologica
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Introduction Thrombotic disorders including ischemic heart d
2022-07-22

Introduction Thrombotic disorders including ischemic heart disease, deep venous thrombosis, and ischemic stroke represent one of the most common causes of death in the world [1]. All these conditions relate to states accompanied by a shift of hemostasis balance into a coagulation side because of va
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br Materials and methods br Results
2022-07-22

Materials and methods Results Discussion Numerous studies have identified important roles for HIF-1α in cellular function and dysfunction through its transcriptional activity [4]. A few studies have reported that HIF-1α is translocated to the mitochondria in human and mouse cancer cell line
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The inhibitory activities against HDAC and HDAC of title com
2022-07-22

The inhibitory activities against HDAC1 and HDAC6 of title compounds were evaluated in a fluorescent assay using SAHA and ACY-1215 as positive control. The results were displayed in A. Compounds – with linker containing 5–7 carbons showed good inhibitory activities against HDAC6. They also displayed
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br Trifluoromethylketones This group of compounds was demons
2022-07-22

Trifluoromethylketones This group of compounds was demonstrated to bind the zinc CID 755673 synthesis in the active site due to its easy hydration, forming the required chelating intermediate. Ontaria et al. [92] have proposed variations around the cap group of trifluoromethylthiophene as the co
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Analysis of the thermosensory responses conferred by chimeri
2022-07-22

Analysis of the thermosensory responses conferred by chimeric proteins suggests that both the ECD and ICD of AFD-rGCs contribute to their thermoresponsive properties. The presence of the GCY-18 or GCY-23 ICD and TMD in chimeric protein combinations generally corresponds to a higher or lower , respec
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br Acknowledgments This research was partially supported
2022-07-22

Acknowledgments This research was partially supported by the National Key Research and Development Program of China (2018YFD1000800); the National Natural Science Foundation of China (No. 31872943; No. 31501779 and No. 31372059>); 12th Five-Year State Science and Technology Support Program (2014B
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Introduction Glycogen synthase kinase GSK is an enzyme playi
2022-07-22

Introduction Glycogen synthase kinase-3 (GSK-3) is an enzyme playing multiple roles in animal tissues and organs, and 6063 is not an exception. Apart from involvement in regulation of apoptosis and survival GSK-3 influences neuronal morphology, synapse formation, memory reconsolidation in adult bra
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As disclosed in our preceding paper medicinal chemistry SAR
2022-07-21

As disclosed in our preceding paper, medicinal chemistry SAR optimization of an HTS hit led to the discovery of , a potent and selective GPR119 agonist. This scaffold differs significantly from the ‘classical’ GPR119 pharmacophore, exemplified by the examples and (). Notably, Chk1 and MK2 Inhibit
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GPR agonistic activity was evaluated for the human GPR recep
2022-07-21

GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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The mD gene obtained from Dr Dimiter S Dimitrov was
2022-07-21

The mD1.2 gene obtained from Dr. Dimiter S. Dimitrov was inserted into a pComb3X vector. The transcription and translation of pComb3X plasmid in cells is inhibited by rifampicin, which binds to bacterial DNA-dependent RNA polymerase. However, in the strain BL21 (DE3) expression system, there is ov
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The dramatic increase in the development of
2022-07-21

The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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Hippo signaling is an emerging
2022-07-21

Hippo signaling is an emerging tumor suppressor pathway that plays key roles in normal physiology and tumorigenesis through the regulation of cellular proliferation and survival [4]. In humans, YAP is over-expressed as a result of genomic amplification of the 11q22 locus in a wide spectrum of human
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