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A general synthetic pathway to these tricyclic
2022-04-16

A general synthetic pathway to these tricyclic structures is described in (detailed procedures can be accessed in the patent application WO 2011/014520 A2). Benzylation of the appropriate ketoester using KHMDS, followed by treatment with DMF-dimethyl acetal yielded the racemic (dimethylamino)-methy
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It has been found that WHI P a JAK inhibitor
2022-04-16

It has been found that WHI-P131, a JAK3 inhibitor, induced apoptosis of CD4+ T Ponesimod (Cetkovic-Cvrlje et al., 2012). Also, other JAK3 inhibitors (AG490 and WHI-P154) caused apoptosis in anaplastic large cell lymphoma (Amin et al., 2003). Taking into account the proapoptotic action of JAK inhibi
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Rapid action of E on GnRH
2022-04-16

Rapid action of E2 on GnRH neurons has been known for some time. E2 hyperpolarizes guinea pig GnRH neurons, alters cAMP production in GT1-cells and stimulates or inhibits [Ca2+]i oscillations within 15 min (Lagrange et al., 1995; Navarro et al., 2003; Temple et al., 2004; Romanò et al., 2008). Impor
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To test this concept we took advantage
2022-04-16

To test this concept, we took advantage of our large supply of various 2-pyridyl containing [3.1.0] cores (inactive with alkyl or aryl sulfonamides) and prepared the -methylimidazole sulfonamide analogs and (), as work form Merck demonstrated that the 2-pyridyl moiety was superior to the original
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The unique ability of R PabI to specifically excise
2022-04-16

The unique ability of R.PabI to specifically excise WY-14643 sale from a palindromic sequence is based on a novel structural architecture that is distinct not only from other DNA glycosylases but also from other proteins [88]. In the absence of DNA, R.PabI forms a dimer with a central, highly twiste
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br Materials and methods br Results
2022-04-15

Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the Methods of neurons and glial cel
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br Experimental br Results br Discussion The use of
2022-04-15

Experimental Results Discussion The use of Dex-BSA asa membrane-limited glucocorticoid has been met with some skepticism, mainly for its assumed instability. Here we provide conclusive evidence that Dex-BSA is stable in solution over an extended period of time and at high temperature (i.e.,
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Rare mutations can impair the molecular function of
2022-04-15

Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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Interruption of glucagon signaling pathway targeting glucago
2022-04-15

Interruption of glucagon signaling pathway targeting glucagon receptor (GCGR) by gene knockout, antisense oligonucleotides or specific antagonists induces α-cell hyperplasia and alleviates hyperglycemia and other metabolic symptoms in diabetic animals and patients [[7], [8], [9]]. Here we used a ful
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To date three GAL subtype receptors have been cloned and
2022-04-15

To date, three GAL subtype receptors have been cloned and characterized, GALR1, GALR2 and GALR3. However, it is unknown which one(s) of the three subtype receptors in Amsacrine hydrochloride is most effective to regulate insulin resistance in diabetic rats as yet. Recent studies fromanimalmodels of
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After initial optimization of the
2022-04-15

After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe
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To further investigate if GPR was
2022-04-15

To further investigate if GPR40 was the functional target of these phenylpropiolic arn 509 analogs, GW-1100, a selective antagonist of GPR40-mediated Ca2+ elevations in HEK293 cells with an IC50 value equal to 1 μM, was used to inhibit agonist-induced intracellular calcium flux [15]. HEK293-GPR40 ce
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br Results br Discussion Our
2022-04-15

Results Discussion Our studies highlight MUFAs as key lipid modulators of both non-apoptotic and apoptotic cell death. Recent studies show that a more mesenchymal phenotype, de-differentiation, and acquired resistance to targeted inhibitors, can all promote a ferroptosis-sensitive cell state (
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br Materials methods br Results FAS c AA
2022-04-15

Materials & methods Results FAS c.-671AA, AG and GG genotypes and A and G LY335979 frequencies were similar in both patients with FMF and healthy control groups, and no significant difference was found (P>0.05, Table 1). The frequency of TC genotype in FASLG in the healthy controls was signif
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br Introduction It is well known that
2022-04-15

Introduction It is well known that conventional cancer treatment strategies, such as surgery, radiotherapy, and chemotherapy all have their own limitations, which lead to an unsatisfactory therapeutic effect. Under this situation, the combination of two or more therapeutic strategies has recently
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