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In our studies of leucine and BCH in
2025-01-23
In our studies of leucine and BCH in pancreatic islets and clonal insulin cell lines, we noticed that leucine was a slightly stronger stimulant of insulin release. Previous studies showed that leucine can be metabolized to CO2[11], [12], [13], [14] and can increase acetoacetate in pancreatic islets
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BRD-9424 Available data thus indicate that there are at leas
2025-01-23
Available data thus indicate that there are at least two ways that HMGA proteins can induce localized changes in the chromatin structure of inducible gene promoters, both of which involve positioned nucleosomes that must be “remodeled” before gene transcription can occur. The first mechanism is exem
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We conclude that Tetrapleura tetraptera fruits extract posse
2025-01-23
We conclude that Tetrapleura tetraptera fruits extract possess antiplasmodial activity and the results of this study justifies and confirms the traditional usage of this plant as malarial remedy. Acknowledgement Introduction The phylum apicomplexa comprises of nearly 5000 species, most of whi
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br Nanoparticle Conjugated Topoisomerase Inhibitors The safe
2025-01-23
Nanoparticle-Conjugated Topoisomerase Inhibitors The safety and efficacy of topotecan administered as LDM or MTD have been evaluated in several preclinical studies and a few clinical trials whose results showed that there can be significant adverse effects likely precluding its use in patients [5
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The Nagoya Heart Study enrolled
2025-01-23
The Nagoya Heart Study enrolled patients with hypertension and type 2 diabetes or impaired Lenalidomide hydrochloride tolerance (12). Patients were randomized to valsartan- or amlodipine-based regimens with a BP target of ≤130/80 mmHg. The primary outcome was a composite of sudden cardiac death, my
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This unsuspected antagonistic interaction of androgen with
2025-01-23
This unsuspected antagonistic interaction of androgen with OXER1 could therefore explain the effect of plant derived compounds with this ligand-receptor system. For example, wedelolactone, a coumestan found in Eclipta alba (false daisy) and in Wedelia calendulacea that is the major component of ecli
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Calcium entry through postsynaptic NMDARs activates intracel
2025-01-23
Calcium entry through postsynaptic NMDARs activates intracellular signaling cascades including Ca2+/calmodulin (CaM)-dependent protein kinase II (CaMKII) and calcineurin. The spatiotemporal abundance of this Ca2+/CaM complex determines the direction of synaptic plasticity, resulting in LTP (Malinow
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AAT enzyme activity was readily
2025-01-23
AAT enzyme activity was readily detected in crude cell-free extracts obtained from berry tissues of all accessions but displayed different substrate selectivities (Fig. 2). Cell-free extracts derived from ‘Muscat Hamburg’ berries showed the highest AAT activity with all alcoholic substrates tested,
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To guide our attempts at achieving
2025-01-23
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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However although in vitro studies in heterologous systems ha
2025-01-22
However, although in vitro studies in heterologous systems have provided very important indications of potential novel pharmacology, the studies with endogenous receptors in native tissues are essential to provide evidence for GPCR heteromerization in vivo and to confirm its physiological relevance.
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We found that several anticancer drugs inhibit HT
2025-01-22
We found that several anticancer drugs inhibit 5-HT3 Thioguanine current in vitro. Several studies have suggested that 5-HT3 receptor antagonists have anti-mitogenic and apoptotic effects on colorectal and breast cancer cell lines (Ataee et al., 2010, Hejazi et al., 2015). Irinotecan is used freque
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We observed PACAP immunoreactivity in the
2025-01-22
We observed PACAP2 immunoreactivity in the molecular layer of the cerebellar cortex in zebrafish. This result is consistent with the reporting of PACAP immunoreactivity in the soma and fibers of Purkinje cells and the presence of PACAP mRNA in the Purkinje-cell and granular-cell layers in rats [43]
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Toxicity is the main reason for the failure at all
2025-01-22
Toxicity is the main reason for the failure at all stages of the new drug development process. The major part of safety-related attrition occurs at preclinical phases while predicting preclinical safety liabilities earlier in the drug development process. This strategy enables the design and/or sele
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Although effects of low concentrations of agonist were not
2025-01-22
Although effects of low concentrations of agonist were not as thoroughly documented for heteromeric receptors such as the major Cefepime Dihydrochloride Monohydrate α4β2 nAChR, a similar mechanism of action was described to explain the potentiation of these receptors with low concentrations of acet
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br Funding br Introduction l Dihydroxyphenylalanine l DOPA i
2025-01-22
Funding Introduction l-3,4-Dihydroxyphenylalanine (l-DOPA) is the gold-standard treatment for the motor symptoms of Parkinson's disease (PD); however, its chronic use induces severe motor complications that eventually limit its long-term efficacy (Bastide et al., 2015). The most disabling side
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