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The rationale for developing HDACi as anticancer agents was
2022-06-16

The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and Benidipine HCl arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hemat
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br Conclusion br Funding br Availability of data and materia
2022-06-16

Conclusion Funding Availability of data and materials Authors' contributions Ethics approval and consent to participate Consent for publication Competing interests Introduction Hepatitis C virus (HCV) infection is a global public health problem. An estimated 71.1 million peop
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Substrate affinity and specificity can
2022-06-16

Substrate affinity and specificity can be enhanced by docking interactions, in which regions distal to the site of squalene epoxidase bind to grooves, pockets, or surfaces outside of the kinase catalytic cleft 1, 2, 5, 6. Like catalytic site interactions, docking interactions can involve recognitio
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br Experimental br Acknowledgements This work
2022-06-16

Experimental Acknowledgements This work was financially supported by Ministry of Knowledge and Economy (10032113) and Ministry of Education, Science and Technology (20100000297). Introduction To ensure accurate chromosome segregation, cohesion between sister chromatids must be maintained u
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br Acknowledgments This review is based in part on
2022-06-16

Acknowledgments This review is based in part on research conducted with financial support from the General Research Fund (17112914) of the Hong Kong Research Grant Council and from the Seed Funding Programme for Basic Research by University Research Committee of the University of Hong Kong (20151
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PG 01037 dihydrochloride synthesis br Family A Receptors as
2022-06-16

Family A Receptors as Promiscuous Sensors for Peptone and Free Fatty Acids (FFAs) In addition to the family C 7TM receptors, several family A 7TM receptors are promiscuous in their ligand preferences, and several respond to organic nutrients from food, notably protein degradation products and FFA
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Interestingly zaprinast administration not only
2022-06-16

Interestingly, zaprinast administration not only prevents the development of hypersensitivity but also enhances opioid effectiveness. Opioids have long been considered among the most effective drugs used to treat pain (Watkins et al., 2005; Mika et al., 2013; Szczudlik et al., 2014a, Szczudlik et al
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As natural ligands of GPR several long chain
2022-06-16

As natural ligands of GPR120, several long chain polyunsaturated fatty acids (Lc-PUFAs) have been demonstrated to modulate the 3T3-L1 adipogenic differentiation. However, the effects of the Lc-PUFAs are inconclusive. DHA is shown to inhibit, promote or even not affect the differentiation of preadipo
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GnRH ant have been designed to obtain pharmacological
2022-06-16

GnRH-ant have been designed to obtain pharmacological compounds to block the pituitary–gonadal axis without the undesirable flare effect exerted by GnRH itself or by the GnRH-a (see Section 2.2). GnRH-ant competitively block the binding of GnRH to GnRHRs (Schally, 1999; Tan & Bukulmez, 2011); they p
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Neurotransmitter transporters are rapidly recycled from and
2022-06-16

Neurotransmitter transporters are rapidly recycled from and to the membrane. For instance, the GABA transporter GAT1 is recycled in a calcium and depolarization dependent manner. GAT1 located in the plasma membrane is internalized to a subpopulation of small vesicles different from the classical neu
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We observed the reduced expression of the GluN a
2022-06-16

We observed the reduced expression of the GluN2a subunit in the temporal and entorhinal cortexes and ventral hippocampus, which may result in the predominance of GluN2b-containing NMDA receptors during the latent period. Previously, using the same model, we revealed the reduction of the GluN2a/GluN2
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br Methods br Acknowledgements The authors thank the ZLS gro
2022-06-16

Methods Acknowledgements The authors thank the ZLS group members, particularly Li Li and Elijah Roberts, for many helpful discussions. They also wish to thank Nathan Baker for APBS assistance, Jan Jensen for help with PROPKA 2.0, Susan Martinis for experimental interpretations, and John Stone
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br Results and discussion br Conclusion In conclusion
2022-06-16

Results and discussion Conclusion In conclusion, we designed and synthesized a novel series of thiosemicarbazide-1,2,3-triazole hybrids 10a-o. Further, α-glucosidase inhibitory activity of the synthesized compounds 10a-o was evaluated. The obtained results showed that all the synthesized thios
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The translation of our rat findings to bovine and human
2022-06-16

The translation of our rat findings to bovine and human lenses revealed that the expression of glucose transporters was more straightforward in bovine and human than in the rat lens, since only GLUT1 was detected in these lenses. Using the C-terminal GLUT1 antibody, we observed bands for GLUT1 in al
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In order to facilitate the preparation of
2022-06-15

In order to facilitate the preparation of 2-aminothiazoles containing novel D-ring substitutions, a convergent synthetic route was selected which requires the synthesis of common precursor . Straightforward aromatic substitution of 3,4-difluoroacetophenone using 4-methylimidazole provided access to
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