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Estrogen receptor related receptor ERR like other
2019-11-04
Estrogen receptor-related receptor γ (ERRγ), like other members of the ERR subfamily, is a constitutively active orphan nuclear receptor, though unlike ERRα and β, it is more selectively expressed in metabolically active and highly vascularized tissues such as heart, kidney, brain, and skeletal musc
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NMS-E973 Besides having a remarkable progestogenic
2019-11-04
Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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Raloxifene is a second generation SERM that has
2019-11-04
Raloxifene is a second generation SERM that has tissue-specific effects that differ from those of tamoxifen. Raloxifene was marketed for prevention and treatment of osteoporosis in postmenopausal women in the US and Europe. In a phase II randomized double-blind study, tamoxifen and raloxifene were e
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Purvalanol B The prospects of the use of this novel
2019-11-04
The prospects of the use of this novel approach for the selective local thermo-activation of enzymes include biomedical and biotechnological applications. As NPs could be engineered to gain access to Purvalanol B through the endosomal compartment [47] or through non-endocytotic pathways [48], [49],
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For most enolases fluoride acts as an
2019-11-04
For most enolases, fluoride acts as an inhibitor, while Mg2+ is the most important metal activator. In yeast systems, metal cations and fluoride bind to enolase at the active center of the enzyme, forming a complex. The complex blocks the binding of substrates to the enzyme in yeast systems, thereby
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Though the physiological roles of microglia derived elastase
2019-11-04
Though the physiological roles of microglia-derived elastases in the CNS are not well understood, their involvement in the metabolism of cholecystokinin [41] and in the processing of plasminogen to produce a low molecular weight plasminogen that enhances neurite outgrowth has been reported [38]. Ex
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br Materials and methods br Results br Discussion In
2019-11-02
Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor nos abbreviation sale recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoids c
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The structure of the HOIP RBR LDD module bound to
2019-11-02
The structure of the HOIP RBR–LDD module bound to UbcH5~Ub reveals insights into an activated HOIP component [47]. Contacts between the E2~Ub and the non-cognate RBR module in the crystal suggest how a structure in which the active sites of the E2 and the E3 are in close proximity might look. In thi
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Raloxifene HCl br Introduction Addiction to opioids such as
2019-11-02
Introduction Addiction to opioids such as morphine is a chronic disorder that affects the mesocorticolimbic dopaminergic pathway in the brain. Activation of the pathway ultimately leads to dopamine release in the nucleus accumbens (NAc) (Di Chiara et al., 1998) and stimulation of dopamine recepto
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Support for Cloninger s personality
2019-11-02
Support for Cloninger\'s personality theory comes also from molecular genetic studies. Given the high heritability of personality it is plausible that gene variants explain variance in RD. In A 77-01 to endocrine studies, which relate hormone levels mostly in the periphery (blood, saliva, urine) to
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br Conclusions This report describes the discovery of a new
2019-11-02
Conclusions This report describes the discovery of a new class of host-directed antiviral agents characterized by a 1-aryl-4,6-diamino-1,2-dihydrotriazine scaffold, responsible for a host (human) DHFR inhibition mechanism. Host-targeting antivirals represent an alternative and emerging strategy t
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We also determined the uracil content of CJ DNA by
2019-11-02
We also determined the uracil content of CJ236 DNA by thin-layer chromatography of in vivo32P- or [6-3H]uracil-labeled CJ236 2′-deoxyribose 5′-monophosphates as well as by LC/MS of deoxyuridine and thymidine 2′-deoxynucleosides (Table 1, Table 2, Table 3). Examination of the 32P data showed that, ba
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From the general synthetic route we
2019-11-02
From the general synthetic route, we first synthesized a directed set of analogues of general formula , keeping the synthesis simple by using a symmetrical pyrazole (R=R=Me). The SAR of a set of 30 compounds in the GTPγS binding assay turned out to be quite tight: only 4 (13%) compounds showed moder
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br Conclusion The preclinical data reported
2019-11-02
Conclusion The preclinical data reported in this study shows that LAS191859 is a potent and safe CRTh2 antagonist, with a long receptor residence time that provides a sustained in vivo efficacy. This property is reflected in the prolonged duration of action of LAS191859 in in vitro and in vivo fu
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Thus based on our prior results
2019-11-02
Thus, based on our prior results above, we hypothesized that B cells derived from ESCs are also B-1 cells and HSC independent. To test this hypothesis, we induced mouse ESCs on OP9 stromal cells into B-progenitors and transplanted them into sublethally irradiated NOD/SCID/Il2rγcnull (NSG) neonates.
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