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br AKT signaling is essential
2023-08-28
AKT signaling is essential during early dorsal patterning, neural crest induction and maturation AKT signaling modulates EMT and migration of the neural crest cells The defining feature of NC cells is their delamination from the dorsal neural epithelium. At the end of neurulation, mature premi
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An important observation in our
2023-08-28
An important observation in our study is the lack of effect of paroxetine pretreatment alone on β2AR membrane expression, which suggests that paroxetine, and pharmacologic inhibition of GRK2 in general, does not directly induce changes in receptor dynamics. Rather, the decreased ligand-induced β-arr
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Since pyrrolopyrimidine dithiolanes and both displayed parti
2023-08-26
Since pyrrolopyrimidine dithiolanes and both displayed particularly excellent levels of ACK1 inhibition, these analogs were viewed as potential candidates for further investigation in tumor xenograft experiments. While in vitro metabolic studies indicated that pyrrolidine was predicted to be sign
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The small fishers with little or no quota who
2023-08-26
The small fishers with little or no quota who remained relied on quota leasing arrangements to continue their fishing operations. Such arrangements had relatively high transaction costs and by early 2000 it appeared that the demise of the small fisher was imminent [2]. The introduction in 2001 of t
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LAQ824 Vortioxetine is a multimodal antidepressant that acts
2023-08-26
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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At present drugs that specifically inhibit YAP activity are
2023-08-26
At present, drugs that specifically inhibit YAP activity are not available. In fact, verteporfin, which was originally described as a specific inhibitor of YAP-TEAD interaction, has been recently shown to exert its activity through selective induction of proteotoxicity rather than through YAP inhibi
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The synthetic route for the aminobenzoxazole scaffold with a
2023-08-26
The synthetic route for the aminobenzoxazole scaffold with a solvent accessible moiety is described in . Nitration of methoxyphenol and subsequent hydrogenation of the resulting nitro hydrocort afforded compound . Aminobenzoxazole was formed by the reaction of compound with BrCN in EtOH. The solvent
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Consistent with a damaging role for increased LOX activity
2023-08-26
Consistent with a damaging role for increased 12/15-LOX activity in stroke, systemic administration of the 12/15-LOX inhibitor, LB1, 2 h after permanent focal cerebral ischemia significantly reduced infarct size 24 h after the ischemia, and the treatment group demonstrated improved behavioral and he
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Receptors containing an x y subunit interface where
2023-08-26
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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Dopaminergic neurons are vulnerable to oxidative products an
2023-08-26
Dopaminergic neurons are vulnerable to oxidative products and inflammatory responses; these processes may play important roles in the etiology of PD. Because glial Mitomycin C are the main generators of inflammatory responses in the CNS, the possibility that PD results from glial cell dysfunction m
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We report here the case of
2023-08-26
We report here the case of a patient with probable genetic prion disease with a Creutzfeldt-Jakob disease-like phenotype associated with a rare PRNP E196K mutation who initially exhibited atypical clinical manifestations principally characterized by behavioral abnormalities. Case report An 80-ye
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Several strategies have been employed to design
2023-08-26
Several strategies have been employed to design and engineer peptide biosensors of kinase activity, which are quite different from the strategies developed to generate genetically encoded KARs. In all cases, Bcl Family Set I australia induces changes in the spectral properties of the fluorophore(s)
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br MHCI peptide editing N terminal
2023-08-26
MHCI peptide editing, N-terminal extensions and the peptide loading complex Conventionally, peptide-MHCI binding is thought to require both amino- and carboxyl-termini for stable interaction (Madden, 1995; Bouvier and Wiley, 1994). Peptides with longer than optimal length (10–13 residues) have be
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Recently two distinct small molecule inhibitors of PHGDH
2023-08-26
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Fmoc-Arg(Pbf)-OH with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces th
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Introduction Aldose reductase ALR is the first
2023-08-26
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occur
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