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It is an aspiring task to apply
2021-10-11
It is an aspiring task to apply the glutamate biosensor for in vivo measurements in Doxorubicin australia tissue. Due to a relatively large size of the electrode used in this work, the biosensor fits only ex vivo applications. However, it is possible to apply platinum microelectrodes 50–100 μm in d
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ppar agonist br Vesicular glutamate transporters VGLUTs br C
2021-10-11
Vesicular glutamate transporters (VGLUTs) Conclusions Due to the molecular cloning of EAAT and VGLUT subtypes, a better understanding of the functional properties of these carriers has been elucidated over the last few years. In the case of the EAATs, specific blockers, such as trans-2,4-PDC,
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We tested this hypothesis with
2021-10-11
We tested this hypothesis with two experiments. In the first experiment OVX monkeys implanted with an E2 fiin (this results in LH levels similar to the level during the follicular phase) were treated with daily injections of letrozole for 1 week and then EB was injected systemically mimicking the pr
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br Secretase modulators a loss of pharmacology
2021-10-11
γ-Secretase modulators: a loss of pharmacology? A lack of translation from in vitro to in vivo pharmacology is an unresolved issue among most GSMs. R-flurbiprofen was tested in clinical trials, however, it did not achieve statistical significance on either of its primary endpoints – cognition or
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Homeobox genes can promote oncogenesis through multiple mech
2021-10-09
Homeobox genes can promote oncogenesis through multiple mechanisms, including gene translocation, loss of heterozygosity, gene amplification, DNA methylation, ASP015K sale remodeling, etc. For instance, translocation-mediated fusion of HOXA9 or HOXA13 on chromosome 7p15 with the nucleoporin gene NU
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4-iodo-SAHA receptor In our cohort each patient had a median
2021-10-09
In our cohort, each patient had a median of 2 Anti-FXa measurements performed daily and a median of 1 infusion rate change daily to maintain therapeutic unfractionated heparin levels. Previously, several studies have documented that APTT-based protocols lead to more fluctuations in comparison with A
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One PKC target that controls cortical actin structure is
2021-10-09
One PKC target that controls cortical FAUC-365 receptor structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC release
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br Materials and methods br Results br Discussion mmLDL
2021-10-09
Materials and methods Results Discussion mmLDL is an important risk factor for cardiovascular disease, but its mechanism is still unclear. Previously, we co-cultured mmLDL with the coronary artery and basilar artery and found that mmLDL could upregulate ETB receptor expression in both [16],
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The H autoreceptors distributed mainly in the CNS act as
2021-10-09
The H3 autoreceptors distributed mainly in the CNS act as a negative feedback on histamine synthesis and release from histaminergic neurons. Histamine is involved in many physiological functions such as sleep-wake regulation, circadian and feeding rhythm, thermal regulation, locomotion, learning, co
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taselisib As evidenced by SARs and crystallographic data HO
2021-10-09
As evidenced by SARs and crystallographic data, HO-1 has at least three main crucial regions for inhibitor binding. The most crucial area, the so-called eastern region, is able to allocate the azole ring that represents the first anchoring point by establishing a coordination binding to the heme fer
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cetrimonium bromide Epigenetic drugs such as HDAC inhibitors
2021-10-09
Epigenetic drugs, such as HDAC inhibitors, regulate gene expression by affecting the activity of histone or DNA modifying enzymes and their associated transcriptional response [141]. BET bromodomain protein inhibition is another epigenetic approach for blocking the Hedgehog pathway at the downstream
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Other N substituted carboxamide oxy pyridine
2021-10-09
Other N-substituted-6-carboxamide-3-oxy-pyridine derivatives 52a, 52h, 52i, and 53h were synthesized using an alternative route. The Pd-catalyzed Heck aminocarbonylation of 44 or 45 with (PPh3)2PdCl2 catalyst in the presence of Et3N under CO atmosphere successfully provided various N-substituted-6-c
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Roughly million people who are currently infected
2021-10-09
Roughly 15 million people who are currently infected with HBV are co-infected with the hepatitis D virus (HDV) (WHO, 2017b). The superinfection not only leads to more severe liver damage and early onset of cirrhosis, but also to a higher mortality than HBV mono-infection (Rizzetto, 1983; WHO, 2017b)
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The PAS and CC domains of sGC have
2021-10-09
The PAS and CC domains of sGC have been studied less by comparison, though their function in sGC signal transduction is likely important. PAS domains are versatile as they can play varied roles in different proteins, such as quaternary structure organization, cofactor binding, and signal transductio
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After establishing improved GSNOR potency some
2021-10-09
After establishing improved GSNOR potency, some of the potent inhibitors were further evaluated for microsomal stability and CYP inhibition studies (). Majority of the tested analogs revealed high metabolic stability in human and rat liver microsomes, and moderate to low stability in mouse liver mic
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