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Camptothecin is a type of topo I inhibitor and
2022-10-04
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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We have previously reported on
2022-10-04
We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t
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br Molecular mechanisms underpinning GSNOR function in
2022-10-04
Molecular mechanisms underpinning GSNOR1 function in the defence response Recently, Arabidopsis GSNOR1 has been shown to govern the extent of S-nitrosylation of two key regulatory proteins, Non-Expresser of Pathogenesis-Related Genes 1 (NPR1) and SA binding protein 3 (SABP3), which are integral t
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Hair loss in women is polygenic and multifactorial
2022-10-04
Hair loss in women is polygenic and multifactorial with the additional influence of environmental factors. Several studies focused on the importance of several genes related to alopecia (Carey et al., 1993, Hillmer et al., 2008, Randall, 2008). FPHL involves progressive hair follicle miniaturization
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To this end we evaluated
2022-10-04
To this end, we evaluated novel D22 analogs for selectivity to inhibit substrate transport in OCT2, OCT3, and PMAT heterologous cell WP1066 systems, and in mouse hippocampal and striatal preparations. Chosen analogs were based upon availability of essential chemical precursors (e.g. 6-substituted-2
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br Acknowledgments This work was financially
2022-10-04
Acknowledgments This work was financially supported by the National Natural Science Foundation of China (No. 81703451) and the China Postdoctoral Science Foundation Grant (No. 2017M611269). Introduction According to the International League Against Epilepsy (ILAE), epilepsy is generally defin
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br Introduction Major depressive disorder
2022-10-04
Introduction Major depressive disorder (MDD) is a disease with poorly recognized etiology. Currently used antidepressant drugs, which mainly affect synaptic neurotransmitter levels, show full clinical efficacy in only one third of patients (Rush, 2007). Thus it is now generally accepted that the
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AD is an irreversible and progressive neurodegenerative dise
2022-10-02
AD is an irreversible and progressive neurodegenerative disease affecting the Golgicide A which insidiously destroys memory, thinking skills and cognition. Originally described in 1906 by German physician Alois Alzheimer, AD is characterized by the presence of intraneuronal neurofibrillary tangles
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As illustrated in among all synthesized compounds biphenyl d
2022-10-02
As illustrated in , among all synthesized compounds, biphenyl derivatives , , , , and with substitutions at the 3-position possessed the best FAAH inhibitory capacity. These 5 compounds demonstrated a good activity against FAAH with IC values in a submicromolar range. Nevertheless, when replacing th
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In an RNAi screen to interrogate the
2022-10-02
In an RNAi screen to interrogate the function of transmembrane proteins in ISCs/EBs, we identified the SJ protein tetraspanin 2A (Tsp2A) as a tumor suppressor. Further characterization reveals that Tsp2A expression initiates in ISCs and Tsp2A protein assembles at the SJs in the progenitor Adenosine
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Introduction As a compound class histone deacetylase inhibit
2022-10-02
Introduction As a compound class, histone deacetylase inhibitors (HDIs) have been remarkably successful in the treatment of T-cell lymphoma [1]. Vorinostat (suberanilohydroxamic PD128907 HCl mg or SAHA) was approved by the FDA in 2006 for the treatment of cutaneous T-cell lymphoma [2], [3]; romidep
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PLP has been found to be effective inhibitor of many
2022-10-01
PLP has been found to be effective inhibitor of many enzymes that have NECA for phosphate-containing substrates or effectors, including RNA polymerase [14], [15], reverse transcriptase [16], and DNA polymerase [17], [18]. Oka et al. [19], [20] reported that vitamin B6 deficiency generally enhances
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lcz696 Interestingly interactions between Smad and
2022-10-01
Interestingly, interactions between Smad3 and RhoA, the other small GTPase which is highly homologous to RhoB [9], could not be observed suggesting that the Smad3/RhoB interactions require amino lcz696 residues that are unique to RhoB. Combined with our previous observation that the RhoA gene, whic
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br Conclusion In this report we describe the synthesis
2022-10-01
Conclusion In this report, we describe the synthesis and evaluation of oxadiazole-based GSK3 inhibitors. Occupation of the ATP-binding pocket in its entirety led to the identification of several potent and selective compounds. These compounds are characterized by IC50 values in the low nanomolar
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Taken together specific antibodies and SR SIM
2022-10-01
Taken together, specific g 36 receptor and SR-SIM used in the study helped uniquely visualize the distribution of lymphocytes and macrophages with their molecular expression in human cochleae. Using SR-SIM, we verified that resident IBA1-positive macrophages are widely distributed in human cochlea (
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