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Extensive pharmacological and structural analysis shows GCGR
2021-12-09
Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in 5-fu 14, 17, 20. Functionally identical to REMD-477, REMD2.59 is a
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Contradictory results have been described
2021-12-09
Contradictory results have been described regarding the role of the Shh pathway during vertebrate skeletal myogenesis. Different studies have shown that Shh can increase or inhibit myoblasts proliferation and terminal muscle differentiation, depending on the experimental model [[1], [2], [3], [4], [
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The effect of exercise on plasma ghrelin has previously been
2021-12-09
The effect of exercise on plasma ghrelin has previously been investigated mostly in humans using exercise regimens such as treadmill running, cycling, and rowing, and also in a few rodent studies and in some other animal models. While many of these clinical studies and some preclinical studies demon
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nicotinic receptor agonist Emergent studies have recently sh
2021-12-09
Emergent studies have recently shown that Sherpas living at high altitude have adaptations that make life at high altitude more compatible. Sherpas are known to have blood Hb concentrations about the same as lowlanders and Han populations [30]. This is different from what happens to lowlanders, Han
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A model substance often used in the
2021-12-09
A model substance often used in the studies of oxidative processes in erythrocytes is tert-butyl hydroperoxide (t-BHP), which, being lipophilic, passes easily across the erythrocyte membrane [9]. In erythrocytes treated with t-BHP (0.1–3mM) for less than 1h, a dramatic decline in the reduced glutath
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br Conflict of interest statement br Introduction br
2021-12-09
Conflict of interest statement Introduction Gap junction assembly Induced disassembly of gap junctions The regulation of connexin and gap junction turnover are still not well understood. This is, in part, due to the fact that while the overall turnover of connexin molecules is fairly con
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In the upper part of the intestine a
2021-12-09
In the upper part of the intestine a small amount of conjugated BAs are reabsorbed via passive diffusion, whereas the part of BAs that escape enterohepatic circulation passes into the colon where they undergo bacterial conversions such as deconjugation, dehydroxylation or dehydrogenation, into secon
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br Materials and methods br Results
2021-12-09
Materials and methods Results Discussion It is known that MAPKs and Akt signaling can regulate cell migration [[24], [25], [26]]. In this study we found that dTAT-WKYMVm stimulates ERK, p38 and Akt phosphorylation in naïve CD4 T cell (Fig. 3A). However their activation did not affect naïve
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Because FPR is expressed in VSMCs and its
2021-12-09
Because FPR-1 is expressed in VSMCs and its role in non-hematopoietic cells is still unclear, we questioned whether FPR-1 would have physiological relevance for vascular behavior, in the same way as it does in neutrophils (Ca2+ homeostasis and CGP 53353 polymerization). First, we tested if FPR-1 is
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In conclusion a novel series of GPR agonists containing nitr
2021-12-09
In conclusion, a novel series of GPR40 agonists containing nitrogen heterocyclic rings derived from TAK-875 were designed and synthesized. The structural activity relationship studies indicated that the substituents on the nitrogen 5416 had a remarkable effect on the GPR40 agonistic activity. Compo
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br Acknowledgments br Introduction Prenyltransferase catalyz
2021-12-09
Acknowledgments Introduction Prenyltransferase catalyzes the head-to-tail condensation between isopentenyl diphosphate (IPP, 1) and an allylic prenyl diphosphate to produce several prenyl diphosphates, which are then converted into steroids, carotenoids, prenyl side-chains of quinones, and pre
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Famprofazone DZNep is a PRC inhibitor that inhibits S adenos
2021-12-09
DZNep is a PRC2 inhibitor that inhibits S-adenosylhomocysteine hydrolase, resulting in cellular accumulation of S-adenosylhomocysteine. S-adenosylhomocysteine is a competitive inhibitor of methyl donor for methyltransferases [38]. DZNep targets EZH2 by reduction in the level of the enzyme H3K27me3 a
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On the other hand imidazolylcyclopropane derivatives and
2021-12-09
On the other hand, imidazolylcyclopropane derivatives and having a 2-substituted benzimidazolyl group showed moderate binding affinities for both the HR and HR. Replacement of 4-chlororbenzylamino group of with a benzimidazolyl group () led to increase the affinity for the HR more than 5-fold ( = 18
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The central region of Azalanstat can be substituted
2021-12-08
The central region of Azalanstat can be substituted with connecting alkyl chains of different nature and length. Interesting results were given by compounds with a four or five DHEA receptor chain, incorporating heteroatoms, such as oxygen (Fig. 2, compound 4) or sulfur, and different functional gro
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br Funding This work was partially supported by the National
2021-12-08
Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Werth
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