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Etoposide VP a semisynthetic podophyllotoxin
2022-05-04
Etoposide (VP-16), a semisynthetic podophyllotoxin derivative agent, is widely used as a chemotherapic treatment for many cancers (Hande, 1998). VP-16 has been known that its activity is mediated by the interaction with topoisomerase II (an ATP-dependent nuclear enzyme) which regulates DNA topology
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The stress of accelerated lactate
2022-05-04
The stress of accelerated lactate production in cancer 1400W dihydrochloride is moderated by the overexpression of lactate transporters – symporters for lactate anions and protons called monocarboxylate transporters (MCTs) – that are capable of bidirectional transport depending on the environmental
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br Potential endogenous agonists of
2022-05-04
Potential endogenous agonists of GPR35 The first endogenously produced chemical that was shown to be able to activate GPR35 was the tryptophan metabolite kynurenic Cy5 Firefly [8]. When human GPR35 was expressed along with a mixture of promiscuous and chimeric G proteins 9, 10 (Box 1) in CHO cell
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GPR is present primarily in the pancreas
2022-05-04
GPR119 is present primarily in the pancreas and the intestine. Activation of GPR119 increases insulin, GLP-1, GIP and PYY secretion. GPR119 agonists stimulate insulin release in a glucose-dependent manner. The glucose dependent insulin secretion (GIDS) mechanism makes GPR119 an attractive target for
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It may seem counterintuitive that a lymphocyte which
2022-05-04
It may seem counterintuitive that a lymphocyte which is unable to proliferate could have neoplastic potential since the very definition of neoplasia is one of autonomous clonal expansion of a cell. The lack of co-stimulatory molecules CD27 and CD28 can potentially be overcome by activating NK cell r
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GT cells were treated in two ways specifically
2022-05-04
GT1-7 insulin receptor were treated in two ways; specifically, they were either dosed or transfected with VP, reflecting the extracellular and intracellular actions of VP, respectively. A dose of 200 pg/ml VP in culture supernatants was effective in stimulating GnRH in the supernatant and cell extr
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Based on work from our labs with mGlu NAMs
2022-05-04
Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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Our exploration of Domain focused on the
2022-05-04
Our exploration of Domain 1 focused on the role of the carbonyl linker in (). We found that replacement of this group by a methylene unit as in or direct attachment of the thiophene ring to the central aromatic core as in did not significantly impact potency. The thiophene ring in could be replaced
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Through a large scale phylogenetic
2022-05-04
Through a large-scale phylogenetic analysis of UDG superfamily in more than 1000 completely sequenced genomes, it is shown that family 3 Aprotinin receptor can be separated into two clades with the traditional family 3 SMUG1 as one of them (Fig. 1) [31]. UDG enzymes in another clade are present in
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thrombopoietin receptor agonist br Acknowledgment br Introdu
2022-05-04
Acknowledgment Introduction Positive and negative reinforcement are known as the two pivotal components in various models of drug dependence. Compulsive drug seeking behavior results from both the euphoric effects of drug use (positive reinforcement) and the unpleasant withdrawal signs followi
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While TUNEL staining is traditionally thought
2022-05-04
While TUNEL staining is traditionally thought to be an apoptosis marker, studies have shown that TUNEL can stain necrotic glycogen synthase kinase 3 [19], [20], [21]. Furthermore, DNA degradation has also been observed in necrotic cells [22]. TUNEL staining alone is therefore insufficient to distin
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br Material and methods br Results br Discussion Functional
2022-05-04
Material and methods Results Discussion Functional characterization of naturally occurring GCK mutations in patients with impaired glucose homeostasis has widened our knowledge of the catalytic and regulatory mechanisms of this enzyme [3]. In this work, we have biochemically characterized a
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br Conflict of interest br Acknowledgements br Introduction
2022-05-04
Conflict of interest Acknowledgements Introduction Second generation antipsychotic drugs (SGAs) such as olanzapine are widely used in treating individuals with schizophrenia and bi-polar disorder and are increasingly prescribed for other conditions such as anxiety (Pringsheim and Gardner, 2
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The MeO CFO phen yl
2022-05-04
The 1-MeO-4-CFO-phen-2-yl group was then selected for the C-3 position when we investigated the aryl substituents at the C-6 position of indazole. As shown in , C-6 position seems to be more tolerant than the C-3 position, as all the aryl groups examined exhibited potent hGCGR activity. Interestingl
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After initial optimization of the
2022-05-04
After initial optimization of the distances we obtained the structure iG shown schematically in Fig. 1. This is the telomeric fragment of chromosome with the noncanonical structures of i-motif and G-quadruplex placed symmetrically in the middle of the duplex. Obviously, we consider the situation whe
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