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Because serum ATX activity and plasma LPA are well
2024-06-26

Because serum ATX activity and pak 4 LPA are well correlated with liver fibrosis stage histologically, both of these parameters merit consideration as novel markers of fibrosis. However, serum ATX activity may be a more useful test from a clinical laboratory perspective. First, LPA can increase mar
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AGN 194310 receptor To maintain ATP levels postmortem muscle
2024-06-26

To maintain ATP levels, postmortem muscle mobilizes its glycogen reserves to yield AGN 194310 receptor 6-phsphate that proceeds through glycolysis. Glycogen degradation was affected by the interaction between treatment and time (Pinitiation of the experiment. We expected that if myosin ATPase is l
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Production of reactive oxygen species ROS during
2024-06-26

Production of reactive oxygen species (ROS) during RSV infection is one the important ways that neutrophils can injure the lungs [2], [24], [25]. Lipoxygenases are considered as an important source of producing ROS inside the Zotarolimus [26]. Several studies have indicated that the 12/15-LOX is a
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Previous studies have demonstrated ATR inhibition
2024-06-26

Previous studies have demonstrated ATR inhibition is effective for treating cancers combining with chemotherapies in lung adenocarcinoma, gastric cancer, HER2 positive breast cancer and chronic lymphocytic leukemia Sorafenib to enhance chemotherapy sensitivity [[16], [17], [18],[20], [21], [22]]. V
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Apelin is a peptide hormone and an endogenous
2024-06-26

Apelin is a peptide hormone and an endogenous ligand for a G protein-coupled receptor named APJ [7], [8], and apelin and APJ are widely expressed in human organs including hypothalamus, heart, lungs, kidneys, adipose tissue, muscles, and others [9]. Apelin is initially synthesized as a 77-amino-acid
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br Under normal physiological conditions
2024-06-26

Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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Introduction The burden of cardiovascular disease CVD
2024-06-26

Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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Thus far a tight coupling has been observed
2024-06-26

Thus far, a tight coupling has been observed between mAbs that target aggregated Aβ and the occurrence of ARIA. If ARIA-E is caused by increased trafficking to and clearance of fibrillar Aβ from cerebral vessels (20), mAbs could be designed with conformationally specific epitopes selective for solu
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Consideration of the rate of
2024-06-25

Consideration of the rate of product formation at different substrate concentrations and estimation of Michaelis-Menten parameters gives some insight into the possible mechanisms underlying the observed decreases in enzyme activity. Estimates based on two-substrate concentrations lack precision and
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Vortioxetine is a multimodal antidepressant that
2024-06-25

Vortioxetine is a multimodal antidepressant that acts as an inhibitor at the serotonin (5-HT) transporter (SERT), an agonist at 5-HT1A receptors, a partial agonist at 5-HT1B receptors, and an antagonist at 5-HT1D, 5-HT3 and 5-HT7 receptors (Bang-Andersen et al., 2011, Sanchez et al., 2015). Based on
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In the late s Solvay Pharmaceuticals discontinued the Phase
2024-06-25

In the late ‘90s, Solvay Pharmaceuticals discontinued the Phase 2 development of a promising potent and highly selective A1AR antagonist based on the pyrrolopyrimidine scaffold, SLV320 [43] (2, Chart 1, also named derenofylline; Ki hA1AR = 1 nM), for the treatment of acute heart failure [24]. In the
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The fact that the BPloopAsn regains its Btx binding with
2024-06-25

The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li
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br Discussion One binding site MB Fig is located in
2024-06-25

Discussion One binding site, MB327-1 (Fig. 4) is located in the extracellular domain between the γ and α subunits. MB327 adopts an extended conformation in the MB327-1 site and is oriented parallel to the channel. The second putative binding site, MB327-2 (Fig. 4) is situated deep inside the chan
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In fact serotonin is a major modulator
2024-06-25

In fact, serotonin is a major modulator of dopaminergic (DA) neuronal activity through the 5-HT2C receptor. Studies have shown that the selective 5-HT2C receptor agonist Ro60-0175 blocks the burst-firing of mesolimbic DA neurons, which project from the ventral tegmental area (VTA) to the nucleus acc
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Pyrimidine is the important pharmacology core in many
2024-06-25

Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the Bacitracin core as wel
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