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Verapamil a calcium channel blocker used clinically
2021-06-19

Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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br Author Contributions br Acknowledgments br Introduction M
2021-06-19

Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.
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Predictions of enzyme topology for
2021-06-19

Predictions of enzyme topology for DGAT2 are more difficult since the DGAT2 polypeptide sequences are more diverse across species than those of DGAT1. The length and function of the hydrophilic N-terminus preceding the first hydrophobic segment varies with species – for example, segments in fungi ar
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Effect of a C C double
2021-06-19

Effect of a C4-C5 double bond — The presence of a double bond at the substrate’s C4-C5 position affects the reactivity of Δ1-KSTDs to varying extent, depending on the enzyme. Most 3-ketosteroids that are converted by Δ1- KSTDs have this double bond. For some Δ1-KSTDs this double bond is even require
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CRF and urocortin produce marked effects
2021-06-18

CRF and urocortin 1 produce marked effects on the Primaquine Diphosphate when administered both i.v. or directly into the CNS (Parkes et al., 2001). Systemic i.v administration of CRF and urocortin 1 cause a marked and long-lasting reduction in mean arterial blood pressure in rats Briscoe et al., 2
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An intriguing feature of the pre and postsynaptic processes
2021-06-18

An intriguing feature of the pre and postsynaptic processes at the level of the VTA that have been shown to be mediated by CRF2 receptors [9], [34] is that they are exerted only by agonists with high affinity for both CRF2 receptors and CRF-BP. The four endogenous peptides of the CRF system have hig
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Rambabu et al reported A series of novel N substituted
2021-06-18

Rambabu et al. reported A series of novel N-substituted 2-(2-oxo-2H-chromen-4-yloxy)propanamide derivatives synthesized from readily available 4-hydroxy coumarin to the corresponding ethyl 2-(2-oxo-2H-chromen-4-yloxy)propanoate followed by hydrolysis and further reacted with different substituted am
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Quantum walks can be connected to extended CMV matrices as
2021-06-18

Quantum walks can be connected to extended CMV matrices as follows. If all Verblunsky coefficients with even index vanish, then the extended CMV matrix becomes which resembles the matrix representation U. One may notice, however, that in the extended CMV matrix , whereas in the quantum walk matri
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The absence of an observable time dependence of kobs on
2021-06-18

The absence of an observable time dependence of kobs on inhibitor concentration for jak kinase 3 with AChE and compounds 1, 3 and 4 with BuChE parallels a similar absence of time dependence for some related fluoro ketones with AChE. Nair et al. found that trifluoromethyl acetophenones with small met
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The modes of action of insecticides are classified by
2021-06-18

The modes of action of insecticides are classified by the Insecticide Resistance Action Committee (IRAC) [6]. In this classification, a large proportion of insecticides are categorized as nerve- and muscle-targeting insecticides, which encompass GABACl antagonists (Group 2) and GluCl allosteric modu
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In summary A is a potent orally available
2021-06-18

In summary, A-216546 is a potent, orally available endothelin receptor antagonist with a high selectivity for the endothelin ETA receptor. The potency and bioavailability of A-216546 suggest that it will have important utility for preclinical evaluation of the pathophysiology of the endothelin syste
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br Genomic actions in the breast br
2021-06-18

Genomic actions in the breast Conclusion Clinical studies suggest that progesterone and/or progestins may play a decisive role in the development of breast cancer in women using hormone therapy or oral contraceptives [3], [4]. However, this data are controversial to most experimental investiga
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In this work we fabricated a kind of multifunctional nanopar
2021-06-18

In this work, we fabricated a kind of multifunctional nanoparticles, based on HAuNS coated by chitosan-stearic sgk inhibitor copolymer (CSO-SA), which was employed frequently to form micelles for hydrophobic drug delivery in our previous work [21], [22]. The nanoparticles can encapsulate DiR effici
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br Activatable MRI probes MRI is
2021-06-18

Activatable MRI probes MRI is commonly used in clinics around the world and has the advantages of outstanding tissue-penetration depth and extremely high spatial resolution for in vivo imaging [33]. MRI has relatively poor sensitivity and usually requires mg115 mg agents to enhance the imaging c
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Recoverin is a kDa retinal
2021-06-18

Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the bms-690514 of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, character
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