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Synthesis of these hydrazide inhibitors
2022-06-16

Synthesis of these hydrazide inhibitors is outlined in , . Condensation of Boc-carbazate with desired aldehyde resulted in hydrazone of type which were reduced to alkylated hydrazides using NaBH and toluenesulfonic acid. The resulting alkylated hydrazides were acylated with Forskolin chlorides or i
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In order to better manage HBV infection and related
2022-06-16

In order to better manage HBV infection and related liver diseases, it is critical to develop new antiviral strategies to increase the rate of functional or complete cure of HBV infection (HBsAg loss and cccDNA elimination), achieving more than viral suppression (Zeisel et al., 2015). As a result, m
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The following are the supplementary data related
2022-06-16

The following are the supplementary data related to this article. Transparency Document Acknowledgements Introduction Nitric oxide (NO) is an important signaling molecule mediating several physiological functions including vasodilation, platelet anti-aggregation, inhibition of interstitial
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Recently it was found that hypoxia results in the
2022-06-16

Recently, it was found that hypoxia results in the phosphorylation of β-catenin at Y654 in a Src-dependent manner (Xi et al., 2013). All β-catenin phosphorylated at this residue was found complexed with Hif1α and it was demonstrated that this β-catenin phosphorylation was required for Src to promote
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Continuing studies of endocannabinoid ligands
2022-06-16

Continuing studies of endocannabinoid ligands at GPR55 reveal that virodhamine (O-arachidonylethanolamine) and AEA can act as a partial agonists at GPR55; at high micromolar concentrations can inhibit β-arrestin recruitment (Sharir et al., 2012). It is likely that there are allosteric as well as ort
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br Pharmacology br Background to GPR function br
2022-06-16

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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We first investigated the influence of the acyl group of
2022-06-16

We first investigated the influence of the -acyl group of the glycine amide side chain and found that shorter linkers lead to better activities (–); simple -benzoyl substituents were always superior to the 3-arylpropanoyl group present in the high-throughput hit (). Electron withdrawing substituent
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An alternative approach to improving pharmacokinetic profile
2022-06-16

An alternative approach to improving pharmacokinetic profile while retaining high GlyT1 potency was also pursued. Libraries were prepared in which potency enhancing piperidine C4 substituents were combined with clearance lowering truncated alkyl sulfonamides. The result was the discovery of (). Unl
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p16 Tamoxifen is still the most frequently used selective es
2022-06-16

Tamoxifen is still the most frequently used selective estrogen receptor mediator (SERM) in premenopausal women suffering from estrogen receptor positive (ER+) breast carcinomas [15]. Although this therapy has been proven very successful, about 20–30% of ER+ breast tumors will not respond, or acquire
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We were able to obtain several crystalline
2022-06-16

We were able to obtain several crystalline forms of CHAV Gth. The first one corresponded to the post-fusion conformation [14]. The comparison of this structure with that of VSV-Gth post-fusion conformation revealed that the PHD is the most divergent domain, with the largest differences confined to t
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Although side effects as paresthesia
2022-06-16

Although side effects as paresthesia due to the application of β-alanine are known, a study in 2006 pointed out that there are no clinical (biochemical or hematological) changes after a long-term supplementation with β-alanine. In 2015, the International Society of Sports Nutrition rejected any argu
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Mast cells isolated from mice and
2022-06-16

Mast AZ 10606120 dihydrochloride mg isolated from mice and rats are able to take up histamine from the microenvironment (Day and Green, 1962, Cabut and Haegermark, 1966). It has been considered that the uptake of extracellular histamine into bone marrow-derived mast cell granules is mediated by two
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br SMO antagonists pitfalls and limitations The first Hh
2022-06-15

SMO antagonists: pitfalls and limitations The first Hh inhibitor discovered was cyclopamine, a naturally occurring alkaloid isolated from Veratrum californicum[21], which inactivates SMO by directly binding to its hepathelical bundle. Nevertheless, cyclopamine has shown several limitations as a d
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br Acknowledgements br Introduction Ghrelin is a potent orex
2022-06-15

Acknowledgements Introduction Ghrelin is a potent orexigenic hormone and growth hormone secretagogue mainly derived from the stomach [1], [2], [3], [4], [5]. Other pleiotropic actions of the hormone include those that are glucoregulatory, food reward-enhancing, gastric motility-enhancing, and
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(-)-Bicuculline methobromide br Contributions br Acknowledge
2022-06-15

Contributions Acknowledgements This research was supported by Natural Sciences and Engineering Research Council (NSERC) Discovery grant No. 341538 and Ontario Graduate Scholarships to HM and VS. Introduction Sexual size dimorphism describes size difference between male and female individua
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