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Following the discovery of diketo compounds
2022-09-01
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 AS-1404 based derivative (1) as the inhibitor of HIV integrase functioning at the 3′-processing and strand transfer steps of HIV integrase. Bioass
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Parkinson s disease is another neurodegenerative disorder af
2022-08-31
Parkinson's disease is another neurodegenerative disorder affecting H3Rs. The most common clinical symptoms of this disease are rigidity, bradykinesia, rest tremor, loss of postural reflexes, and gain impairment owing to progressive degeneration of the dopaminergic neurons in the nigro-striatal neur
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br References and recommended reading Papers of
2022-08-31
References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Introduction Male sexual maturation includes gonadal maturation, secondary sexual characteristics, and the attainment of reproductive capacity [1]. Male sexual di
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Following nerve injury Shh expression is upregulated in neur
2022-08-31
Following nerve injury, Shh expression is upregulated in neuronal cell bodies of the facial and sciatic nerves. Additionally, Shh appears to be required for normal regeneration in vivo, and promotes motor neuron survival in vitro (Martinez et al., 2015; Akazawa and Kohsaka, 2007). Based on these obs
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To characterize the basic functions
2022-08-31
To characterize the basic functions of GPR84 in phagocytes, we have utilized the receptor selective antagonist GLPG1205 (a small selective antagonist of GPR84 developed by Galapagos NV [14]) together with ZQ16 (2-(hexylthio) pyrimidine-4,6-diol), a potent GPR84 selective agonist identified in a high
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Thermal analysis of the NQ peptide was
2022-08-30
Thermal analysis of the NQ21 peptide was performed with the Solar CM2203 spectrofluorometer. We prepared three 1 μg/mL peptide solutions with different Piperine mg levels (5.0, 7.4, 8.5) in 0.01 M phosphate buffers. Each solution was slowly heated up from 28 °C to 54 °C with a step of 1 °C. Spectra
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As a part of our continuing
2022-08-29
As a part of our continuing efforts towards discovery of new class of compounds against different therapeutic areas and based on the literature reports, we designed a dual pharmacophore which possess a long aliphatic chain of free fatty acids and a phenyl propanoid part of known GPR40 agonists. Here
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Ru II complexes have been
2022-08-29
Ru(II) complexes have been reported to be both duplex and G-quadruplex structure stabilizers, and potent anticancer agents [[11], [12], [13], [14]]. Barton, Norden, as well as Ji groups have provided detailed information about recognition and reactions of classical duplex DNA by Ru complexes [[47],
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br Results br Discussion Immune mediated
2022-08-29
Results Discussion Immune-mediated chronic inflammatory diseases (e.g. rheumatoid arthritis, psoriasis, multiple sclerosis, and inflammatory bowel disease) are characterized by a dysregulated migration of leukocytes from blood vessels into inflamed tissues. To date, several new targets and in
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TNKS 22 Some malignant human tumors cells also express FPRs
2022-08-29
Some malignant human tumors TNKS 22 also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and resistance to apoptosis [
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In an effort to more fully explore
2022-08-26
In an effort to more fully explore the structure–activity relationships of the ALLINIs and potentially attenuate resistance to known mutants, the central scaffold of these compounds was identified as a potential site for structural manipulation. Specifically, we wished to examine whether a scaffold
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br Introduction The role of histamine
2022-08-26
Introduction The role of histamine in allergic responses, anaphylaxis, and gastric DIG-11-dUTP sale secretion has been well described in both human and veterinary medicine. New roles for histamine and its receptors, however, have been elucidated over the last two decades (Smuda and Bryce, 2011),
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Camptothecin is a type of
2022-08-26
Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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It is extremely difficult to predict a
2022-08-26
It is extremely difficult to predict a plausible conformer of hsGCαβ heterodimer with right orientation of multiple domains. Even though the template identities in case of dimeric domains were not high enough but still we modelled the entire heterodimeric structure of hsGCαβ with a reasonable and ju
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gamma secretase inhibitor Interestingly systemic circulating
2022-08-26
Interestingly, systemic circulating levels of NOx were not dramatically increased by treatment with isosorbide mononitrate or sodium nitrite at a dose which exerted beneficial effects on the progression of PH. In line with our results, Mathew et al. [13] demonstrated that the long-acting NO donor mo
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