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In addition researchers studying GPR agonists favor
2022-09-08
In addition, researchers studying GPR119 agonists favor the developing of candidate drugs that are more potent than DPP-4 inhibitors given that the latter are moderate agents in the treatment of DM. Although it TASIN-1 is unclear why Sanofi-Aventis chose to terminate collaboration with Metabolex (n
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One difficulty in studying gp is that
2022-09-08
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how biotin 100 mg respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AMD3100
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Oxidative stress results from the disequilibrium between lev
2022-09-08
Oxidative stress results from the disequilibrium between levels of prooxidant molecules produced and the ability of a biological system to detoxify and neutralize the reactive molecules [14]. OS is a chronic, self-perpetuating state of damage to cells and increased inflammation resulting from the co
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Acknowledgments br Introduction The gut derived hormone oxyn
2022-09-07
Acknowledgments Introduction The gut-derived hormone oxyntomodulin (OXM) is a naturally occurring dual agonist of both the glucagon receptor (GCGr) and glucagons-like peptide 1 receptor (GLP-1r). Structurally OXM is the 29 Deazaneplanocin receptor of glucagon with a C-terminal octapeptide tail.
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More polar substituents introduced on the position of the
2022-09-07
More polar substituents introduced on the 5-position of the aniline ring (e.g., dimethyl amine in ) decreased the lipophilicity of the compounds (4.3 for vs 5.1 for ), but did not affect their potency. For instance, was highly potent in vitro and demonstrated a surprising 51% lowering of Aβ42 in m
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br Materials and methods Unless
2022-09-07
Materials and methods Unless stated otherwise, all chemicals were from Sigma-Aldrich and were of the cell culture grade. HL-1 cardiomyocytes were presented by Dr. W.C. Claycomb (Louisiana State University Health Science Center, New Orleans, LA, USA) [8]. Results and discussion Acknowledgeme
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br Experimental br Results and
2022-09-07
Experimental Results and discussion One of the major challenges of oral drug delivery via nanocarriers is the fairly low efficiency of crossing the intestinal barrier. While there is the possibility of a paracellular transport for polar substances below 1000 Dalton [26], the key mechanism of o
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Here we show that Hippo signaling
2022-09-07
Here, we show that Hippo signaling components are expressed during epicardium formation. To determine the significance of Yap and Taz in the developing epicardium, we generated epicardium-specific Yap/Taz double-knockout mice. Genetic deletion of Yap and Taz using Sema3d mice leads to embryonic leth
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br Author Contributions br Acknowledgments
2022-09-06
Author Contributions Acknowledgments We thank Hiroyuki Miyoshi, Makoto Nakanishi, Yoshikazu Johmura, Yuki Okada, Yoshinori Makino, Takashi Sutani, and Katsuhiko Shirahige for kindly providing materials and technical information, Shiho Takahashi-Kariyazono for technical advice, and all members
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br Mechanism of action of herbs
2022-09-06
Mechanism of action of herbs and their active constituents used in hair loss treatment The hair growth cycle consists of 4 stages known as the anagen (active growth phase; takes 2–7years), catagen (involuting or regressing phase; takes approx. 2weeks), telogen (short resting phase; takes approx.
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Mapping and separation of the anti
2022-09-05
Mapping and separation of the anti-GlyT1C epitopes allowed us to verify the existence of calpain cleavage sites in isolated mouse synaptosomes. In order to allow calcium to enter the intrasynaptosomal compartment and activate endogenous calpain, we incubated synaptosomes in hypoosmotic high (200μM)
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The two competitive bivalent GlxI inhibitors polyBHG
2022-09-05
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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The two competitive bivalent GlxI inhibitors polyBHG
2022-09-05
The two competitive bivalent GlxI inhibitors polyBHG2-62 (=1nM) and polyBHG2-54 (=0.3nM) () were designed based on the transition-state analog -(-bromophenyl--hydroxycarbamoyl) glutathione (BHG) by an examination of the X-ray crystal structure of human GlxI in complex with one CHG at each active sit
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Ebastine br Materials and Methods br Results All
2022-09-03
Materials and Methods Results All of the studied transporter genes were expressed at detectable levels in all the analyzed samples at mRNA level by means of applied rt-PCR method (CTEbastine was observed for ABCC4, ABCC1, ABCG2, SLC22A3, and SLC22A18 (less than 10% of mean expression for the h
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The third generation cephalosporin antibiotics can
2022-09-03
The third-generation cephalosporin daprodustat can cross the blood brain barrier (BBB) [94]. In addition, several studies have shown that CEF can also cross the BBB [95,96] through a facilitated transport process [95]. However, due to the fact that CEF has poor bioavailability when taken orally, CE
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