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Paclitaxel Similarly spectrophotometric titrations were carr
2021-09-02

Similarly, spectrophotometric titrations were carried out under conditions identical to those used for the fluorescence titrations. exhibited a predominant Paclitaxel band at around 493 nm. The titrations with all G-quadruplex DNAs resulted in a hypochromic effect along with a bathochromic shift o
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The overall very satisfactory potency profile of compounds a
2021-09-02

The overall very satisfactory potency profile of compounds 7a–l suggests that 1,3,4-thiadiazole-2-carboxamide moiety was a suitable periphery group to add to the 3-phenylpropanoic nmda receptor antagonist core in order to improve affinity to FFA1. The agonist activity in this series appears to be p
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Regarding IAV types of hemagglutinin and types
2021-09-02

Regarding IAV, 18 types of hemagglutinin and 11 types of neuraminidase were described and none of the commercialized antiviral drugs are susceptible to protect against all strains that will emerge from the animal reservoir (Webby and Webster, 2003). The strong dependencies of influenza viruses on we
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Most enzymes involved in the addition and removal of ubiquit
2021-09-02

Most VUF 11207 fumarate involved in the addition and removal of ubiquitin bind weakly to an overlapping surface on ubiquitin. Previously, Sidhu and colleagues diversified this surface and then used phage display to screen these libraries of ubiquitin variants (UbVs) for binding to DUBs and E3 ligas
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In addition to G coupling it is important to
2021-09-02

In addition to Gα coupling, it is important to consider that the transition from goal-directed to habitual drug taking also relies on striatal D2R-A2AR heterodimers. Following cocaine self-administration, D2R-A2AR density is increased in the NAc, leading to greater antagonism of the inhibitory (anti
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There are numerous theories of
2021-09-02

There are numerous theories of schizophrenia etiopathology and genetics is often taken into consideration [25]. The dopamine D2 receptor is important since it is blocked by typical antipsychotic drugs with high affinity which is correlated with the ability to control psychotic symptoms in schizophre
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The synthesis of tricyclic analogs is described
2021-09-01

The synthesis of tricyclic analogs 28–33 is described in Scheme 3. Oxidative C–C bond cleavage of the terminal olefin of 39i afforded a tricyclic product 52 without isolation of an aldehyde expected as an intermediate. Aminolysis of the chloride 52 with optionally substituted anilines afforded 28–30
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br The LSCP model and its properties
2021-09-01

The LSCP model and its properties In this section, we first introduce the LSCP model in Section 2.1. Some examples of the model are presented in Section 2.2 and basic properties of the model are presented in Section 2.3. Finally, Section 2.4 introduces finite dimensional approximations necessary
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In humans individual differences in prefrontal
2021-09-01

In humans, individual differences in prefrontal dopamine are partially caused by the Val158Met single-nucleotide polymorphism on the catechol-O-methyltransferase gene (COMT). This gene controls activity of the COMT enzyme, which degrades extracellular catecholamines including dopamine. The Val varia
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The substitution of serine by an
2021-09-01

The substitution of serine 185 by an alanine led to an increase of EGF-R stabilization along with a better binding of PRK1, a RhoB effector described to be involved in EGF-R intracellular traffic. Overall these data indicated that the phosphate group on serine 185 impaired its binding to the effecto
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In S cerevisiae Mek a paralog of the checkpoint
2021-09-01

In S. cerevisiae, Mek1, a paralog of the checkpoint kinase Chk2, mediates cell-cycle arrest in response to meiotic defects (Bailis and Roeder, 2000, Xu et al., 1997). Mek1 is associated with meiotic chromosome axes, where its activation requires interactions with two other axis proteins, Hop1 and Re
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At one time the biological effects
2021-09-01

At one time, the biological effects of cAMP were thought to be mediated exclusively by Protein Kinase A (PKA). Consistent with this, PKA inhibitors have been shown to reverse the effects of cAMP-elevating agents on VSMC proliferation [5]. However, we recently reported that cAMP-mediated inhibition o
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Whichever interactions are formed between the DS domains
2021-09-01

Whichever interactions are formed between the DS domains and the collagen ligand, they are expected to lead to structural changes within the DDR dimer that are propagated across the cell membrane to result in DDR autophosphorylation (Noordeen et al., 2006). Tight coupling of the extracellular confor
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The inhibition of mRFP Ub
2021-09-01

The inhibition of mRFP-Ub–E1 formation by ginsenosides Re was not in time-dependent in vitro (Fig. 4B). Fifty micrometres ginsenoside Rg1 decreased E1 activity to 0.24- to 0.36-fold over 30min. This finding suggests that ginsenoside Rg1 may irreversibly inhibit mRFP-Ub–E1 formation or a tight-bindin
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During germ cell development in
2021-09-01

During germ cell development in mouse, de novo Dnmts regulate the genomic imprinting and silence of repeat elements. Dnmt3A methylated H19, Dlk1/Gtl2, and Sine B1, whereas Dnmt3B methylated microsatellite repeat elements, the two Dnmts co-methylatedRasgrf1, IAP, and Line1 repeat elements (Lucifero e
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