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For the NSCLC patients with EGFR activating mutations EGFR T
2022-10-14

For the NSCLC patients with EGFR-activating mutations, EGFR-TKIs (gefitinib and erlotinib) are effective clinical therapies [21], [22]. However, approximately 10% of patients harboring EGFR-sensitizing mutations exhibit intrinsic resistance, and up to 40% do not attain a major response to treatment
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br Results br Discussion Context
2022-10-14

Results Discussion Context-specific and dynamic post-translational protein modifications are well-established regulators of the signaling pathways that protect eukaryotic DNA integrity during the tremendous task of replication. Advancements in speed, resolution, and sensitivity of MS-based tec
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br Material and methods br Results
2022-10-13

Material and methods Results Discussion Nimodipine administration inhibited the level of AMP-activated protein kinase (AMPK) phosphorylation, a sensor of cellular energy status that directs metabolic Cy7.5 NHS ester (non-sulfonated) to support cellular growth and survival. CCH influences t
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Selumetinib We also measured macrophage infiltration and CLS
2022-10-13

We also measured macrophage infiltration and CLS presence in peri-gonadal AT from db/db mice and controls. CLS are morphological features within AT that are accurate indicators of adipocyte death and macrophage infiltration [56]. An earlier study showed that CLS macrophages account for >90% of the t
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br Hypothesis The hypothesis is that AhR in
2022-10-13

Hypothesis The hypothesis is that AhR in skin diseases could be an objective of study for future dermatological therapies. Both stimulation and inhibition of the receptor might have significant influences on neoplastic or inflammatory skin diseases. However, at present the functions of AhR are un
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Following the discovery of diketo compounds
2022-10-13

Following the discovery of β-diketo compounds S-1360 [31] and L-731988 [32] as anti-HIV integrase inhibitors, a group of researchers discovered a potent StemRegenin 1 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase.
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br Discussion Considering cardiovascular risk factors
2022-10-13

Discussion Considering cardiovascular risk factors, there was a significant difference in prevalence of dyslipidemia in both groups, 57.5% in HIV-infected stroke patients compared to 8.9% in the HIV-uninfected patients. These results are similar to that of Chow et al. who found a dyslipidemia pre
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As comparators compounds and were made using the pyrazolopyr
2022-10-12

As comparators, compounds and were made using the pyrazolopyridine core with the CF triazole attached. The 2-fluorophenyl group was replaced with the methylpyrimidine in compound . The potency of these compounds were very good and compound looks attractive from a physicochemical perspective as it
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Beside its role in NF B
2022-10-12

Beside its role in NF-κB and IL-1β activation, the NRLP3 pathway is closely involved in another essential pathophysiologic mechanism such as the cellular calcium homeostasis. Full activation of the NRLP3 inflammasome requires decreased extracellular K concentrations resulting in decreased osmotic pr
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br Funding This work was partially supported
2022-10-12

Funding This work was partially supported by the National Institute on Alcohol Abuse and Alcoholism, award R00AA021264, startup funds from the Department of Immunology, Herbert Wertheim College of Medicine, and the Office of Research and Economic Development at FIU, and pilot funds from Dr. Wert
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With an ever increasing incidence rate of type diabetes and
2022-10-12

With an ever-increasing incidence rate of type 2 diabetes and obesity, it is imperative to develop new therapeutic regimes that may provide a benefit both in terms of efficacy and tolerability. The existing portfolio of drugs for the treatment of metabolic disorders, primarily type 2 diabetes and ob
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JNJ26481585 receptor As preclinical toxicity and efficacy bo
2022-10-12

As preclinical toxicity and efficacy both appear to be associated with GlyT1 inhibition, it remains to be determined whether on-target toxicity can be separated from efficacy. The present study evaluated a series of GlyT1 inhibitors for target potency, mode of inhibition, residence time, activity in
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The kinetic data obtained from incubation
2022-10-12

The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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These differences have led to the recognition
2022-10-12

These differences have led to the recognition that the extent to which transport contributes to shaping postsynaptic signals likely reflects a balance between the density of transporters and the amount of l-glutamate in the synaptic cleft. Consequently, those synapses exhibiting the characteristics
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Free fatty acid receptor FFAR
2022-10-12

Free fatty Nicotine Difartrate receptor 1 (FFAR1, also known as GPR40) belongs to the family of G protein-coupled receptors (GPCRs) and was de-orphanized in 2003 as a receptor for medium-to long-chain free fatty acids (FFAs) [9,10]. Mainly expressed in beta cells of pancreatic islets, GPR40 can be
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