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Previously we described that cadmium induces a more pronounc
2023-03-16
Previously, we described that cadmium induces a more pronounced, but not selective, cell death on primary cholinergic neurons from basal forebrain (Del Pino et al., 2014). Degeneration of septal cholinergic neurons from basal forebrain, as happens in AD, results in memory deficits (Scheiderer et al.
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Having established the structural requirements for potency
2023-03-16
Having established the structural requirements for potency in both the biochemical and biomarker (CRA) assays, we evaluated key compounds in the metabolic stability assay. Disappointingly, we found that all compounds had high intrinsic clearances in mouse microsomes. To ascertain whether the in vitr
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Here we report discovery of highly selective pan
2023-03-16
Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of dpp-4 inhibitors bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interactio
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In liver the essential organ of lipoprotein synthesis
2023-03-16
In liver, the essential organ of lipoprotein synthesis, ACL plays a fundamental role in lipogenesis and steroidogenesis by supplying cytosolic Finasteride to both pathways. By using a tricarboxylic acid cycle intermediate (citrate) to produce acetyl CoA, ACL can be seen as an important bridge betwee
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Aromatization of the pyrrole ring after anion
2023-03-16
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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Thalidomide is now a well known antiangiogenic
2023-03-16
Thalidomide is now a well known antiangiogenic agent. This property of thalidomide is being extensively researched upon, for its significant utility in the treatment of various malignant tumors. Studies show that thalidomide efficaciously inhibits various pro-angiogenic factors such as tumor necrosi
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br AMPK as a druggable target AMPK signaling
2023-03-15
AMPK as a druggable target AMPK signaling has attracted considerable attention within the past decades, owing to the capacity of pharmacological compounds (e.g., 5-aminoimidazole-4-carboxamide-1-β-D-ribofuranoside [AICAR] and metformin) or natural compounds (e.g., resveratrol) to activate AMPK in
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Dose Response Studies Against Puromycin Sensitive
2023-03-15
Dose–Response Studies Against Puromycin–Sensitive Aminopeptidase (PSA). PSA is a ubiquitous metallopeptidase encoded by the NPEPPS gene with subcellular distribution in the cytosol and nucleus [49]. Comprising of a 919 amino SJ 172550 sequence, it has a broad substrate specificity, and is responsib
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At the organismal level skeletal muscle
2023-03-15
At the organismal level, skeletal muscle, lung and adipose tissues mediate net de novo synthesis and release of glutamine, whereas net glutamine catabolism occurs in the kidney [7]. The liver exhibits net glutamine consumption coupled to urea production in the post-absorptive state, and net glutamin
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br Neurological development and BCAAs Glutamate is an import
2023-03-15
Neurological development and BCAAs Glutamate is an important excitatory neurotransmitter in the brain, and BCAAs (especially leucine) function to synthesize glutamate in astrocytes around neurons, since leucine enters the brain from the blood more rapidly than other jw products and provides ∼25%
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The G R mutation is located at the
2023-03-15
The G1202R mutation is located at the solvent front of the ALK kinase domain adjacent to the inhibitor's binding pocket. Although barely reported in the setting of crizotinib resistance, it has emerged as the most refractory mutation to both the first- and second-generation ALK inhibitors. The large
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The specific binding domain between PGK in group B strepotoc
2023-03-15
The specific binding domain between PGK in group B strepotocci (GBS) and actin had been reported . PGK as the actin-binding protein identified in TMW 1.1434, which displayed highly significant adhesion was investigated for the binding sites and compared to bacteria with less strong adhesion to actin
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During years research efforts at Los Alamos National Laborat
2023-03-15
During 2002–2004years research efforts at Los Alamos National Laboratory (LANL) focused on constructing a quantum computer based on regular arrays build from neutral radical molecules possessing one single unpaired PD 169316 spin. The idea was built on the ability to manipulate individual electron
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Osteoblasts have been thought to be the major cell type
2023-03-15
Osteoblasts have been thought to be the major cell type that expresses RANKL (Suda et al., 1999) which is a ligand for osteoprotegerin (OPG) and which functions as a key factor for osteoclast differentiation and activation. Recently, Nakashima and his colleagues (Nakashima et al., 2011) demonstrated
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Derivatives of M that possess either an alkyne or
2023-03-15
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these ceritinib to maintain 5-HTR antagonist properties as (+)-M100907 was demonstrat
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