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Recently AFF was used to convert an
2023-08-25

Recently, AFF was used to convert an FN3-based binder specific to the Src homology 2 (SH2) domain of cAbl kinase into an allosterically regulated, intermolecular fluorescent switch (Figure 2D). Binding to cAbl kinase co-operatively stabilized the assembly of the FN3-based binder from two partial fra
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Immunohistochemistry Hearts from young and aged mice were co
2023-08-25

Immunohistochemistry: Hearts from young and aged mice were collected at the indicated times, fixed overnight in 10% formalin, and embedded in paraffin. Serial 5-μm heart sections from each group were analyzed. Samples were stained with H&E for routine histologic examination. Immunohistochemical stai
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Until now five muscarinic receptor M genes
2023-08-24

Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l
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The next level of possible correlation
2023-08-24

The next level of possible correlation and comparison between the α7 and 5HT3 receptors is at the subunit arrangement and protein folding. Crystal structures of the nicotinic and serotoninergic 900 80 receptors [45], [46] reinforced the concept of similarities between these families of receptors. N
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Brain damage diseases such as cerebral ischemia
2023-08-23

Brain damage diseases, such as cerebral ischemia, brain trauma and infection are characterized by the increase in oxygen free radicals. Therefore, deeper understanding of the character and mechanism of free radical damage in the brain is important to ultimately relieve diseases and promote recovery
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IGF signaling has been shown
2023-08-23

IGF-1 signaling has been shown to induce Torcetrapib receptor changes via interacting with MKK-p38 signaling (Serra et al., 2007) and by perturbing Foxo3a signaling (Stitt et al., 2004), among other mechanisms. The current study demonstrates that the acetyl group itself may be limiting, since IGF-1
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From an historical perspective ligands for GPCRs adrenaline
2023-08-23

From an historical perspective, ligands for GPCRs (adrenaline, serotonin, Z-DEVD-AFC or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenous ligands were
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Another hypothesis is angiogenesis inhibition Angiogenesis i
2023-08-23

Another hypothesis is angiogenesis inhibition. Angiogenesis is a process that involves the growth, migration and differentiation of endothelial KN-93 hydrochloride to form new blood vessels. Angiogenesis favorably influences tumor growth and also influences tumor invasion of vessels, resulting in t
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We designed SSOs that block APP exon
2023-08-23

We designed SSOs that block APP exon 17 splicing and induce the production of an alternatively spliced APP mRNA lacking exon 17 (APPΔex17). APPΔex17 mRNA encodes an APP protein isoform that lacks 49 biotin 100 mg including the γ-secretase cleavage sites that give rise to the toxic, AD-associated Aβ
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Aldose reductase AR is an NADPH dependent aldo keto
2023-08-22

Aldose reductase (AR), is an NADPH-dependent aldo-keto reductase very well studied as a catalyst of glucose conversion to sorbitol in the polyol pathway [11], [12]. In the diabetic lens characterized by chronically high levels of glucose, AR is responsible for production of high levels of sorbitol a
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Mechanisms implicated in antinociception by A R agonists
2023-08-22

Mechanisms implicated in antinociception by A3R agonists in neuropathic pain are summarized in Box 3. Cellular transduction mechanisms for A3Rs include inhibition of cyclic AMP, PKA via Gαi, interactions with PLC/IP3/DAG and signaling via Gαi and Gαq, and interactions with PI3K/MEK/ERK via βγ subuni
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Synthesis pharmacological evaluation for the binding at hA
2023-08-22

Synthesis, pharmacological evaluation for the binding at hA, hA and hA ARs, and efficacy at hA subtype of the synthesized compounds, together with the assessment of their theoretical ADME properties were the guidelines in this preliminary drug discovery investigation. The synthetic pathways which y
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NSAIDs induce gastrointestinal toxicity and evoke
2023-08-22

NSAIDs induce gastrointestinal toxicity and evoke Amphotericin B by decreasing the production of gastroprotective prostanoids and by redirecting the COX substrate AA into LT biosynthesis, thereby causing vasoconstriction in gastric mucosa and airways (Celotti and Laufer, 2001; Koeberle and Werz, 201
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Inactivation of the proton pump comes with luminal
2023-08-22

Inactivation of the proton pump comes with luminal alkalinization of the targeted vesicles such as lysosomes (Fig. 2b). Lysosome pH can also be raised stoichiometrically by addition of a membrane-permeable weak c75 such as methylamine or chloroquine which accumulates in its protonated, non-membrane
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A positive correlation between nasopharyngeal CCL and CCL co
2023-08-22

A positive correlation between nasopharyngeal CCL3 and CCL5 [16] concentrations and illness severity was shown in evaluating patients with RSV bronchiolitis [17]. CCL5 and CCL3 are important for monocyte and lymphocyte recruitment to the lung during RSV infection [7], [16], [18]. Despite the signifi
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