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Finally considering the encouraging inhibitory and selectivi
2020-04-27
Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of e
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The ADME profile of AAT
2020-04-27
The ADME profile of AAT-008 () was very promising, with high stability in HLM. The pre-clinical pharmacokinetic properties of AAT-008 were also assessed in rats (Sprague-Dawley, male), dogs (beagle, male), and monkeys (cynomolgus, male). The experimentally determined parameters are summarized in .
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Covalent inhibitors are well suited for
2020-04-26
Covalent inhibitors are well suited for targeting the E1 amyloid definition of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable
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The identification of a gatekeeper mutation also suggests th
2020-04-26
The identification of a gatekeeper brilliant blue also suggests that alternative DDR2 inhibitors may be required to overcome acquired resistance. Additional DDR2 inhibitors that have been isolated include the recently identified alkaloid natural products discoipyrroles A-D and the chemotherapeutic
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This study has several limitations First despite
2020-04-26
This study has several limitations. First, despite the relatively large number of participants for a pharmacological neuroimaging study, sample sizes for examining the modulation of THC effects by COMT BAY 57-1293 were small. Therefore, these particular findings should be interpreted with caution a
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Multiple protein species are known to naturally exist for th
2020-04-26
Multiple protein species are known to naturally exist for the transmembrane receptors DDR1 and DDR2. Five splice variants have been characterized for DDR1 (“a” through “e”). The d and e isoforms lack the intracellular kinase domain of DDR1. The splicing of DDR1 to various extents has been reported i
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Sulfaphenazole sale Supported by the Austrian Science Fund F
2020-04-26
Supported by the Austrian Science Fund FWF (grant P22521-B18 to A.H.) and the Austrian National Bank (grant 14263 to A.H.). K.J. was funded by the PhD Program DK-MOLIN (FWF-W1241). Acknowledgements Introduction Acute lung injury (ALI) and acute respiratory distress syndrome (ARDS), a more sev
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In this study we observed alterations in
2020-04-26
In this study, we observed alterations in mRNA levels of CRF receptors in the PFCx and Hip during the development of sensitization. In particular, in the Hip both CRF receptors showed significantly increased Glycyrrhizic acid when the sensitization condition was established. Similarly, CRF2 recepto
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br Stem cell based therapies In the previous years
2020-04-26
Stem cell–based therapies In the previous years, excessive efforts have been conducted to induce the least aggression and more efficient sources of human cardiomyocytes for different application, particularly for myocardial regeneration. The pluripotent stem cell seems to be an appropriate candid
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Many studies have found that
2020-04-26
Many studies have found that there is an aberrant DNA methylation in the imprinting control region of development-related genes in the spermatozoa of oligozoospermic men (Kobayashi et al, 2007, Marques et al, 2004, Marques et al, 2008), which most likely results from expressional changes in the DNMT
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While the mechanism of DHODH inhibition induced differentiat
2020-04-26
While the mechanism of DHODH inhibition-induced differentiation is not fully understood, this phenomenon may be caused by pyrimidine depletion. Pyrazofurin, an inhibitor of OMP decarboxylase, was able to induce differentiation and suggests pyrimidine depletion as a potential mechanism (Sykes et al.,
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br In order to determine the physiological roles of
2020-04-26
In order to determine the physiological roles of WT (wild type) EWSR1, Dr. Lee\'s group established a conventional Ewsr1 KO mouse [38]. Since then, the Ewsr1 KO (−/−) mouse model has successfully been utilized to decipher many important in vivo roles of EWSR1 (Fig. 1). EWSR1 deficiency alters m
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In ER group Histopathological examination followed
2020-04-26
In ER + group, Histopathological examination followed by Fluorescence in situ hybridization (FISH) had revealed the absence of HER2 receptors. Co-targeting of ER and HER2 appears to provide benefit without a significant increase in toxicity although formal trials have not been carried out [18]. Adop
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The AURA trial was a phase
2020-04-26
The AURA trial was a phase I/II study evaluating the safety, tolerability and activity of Osimertinib in patients with EGFR-mutated NSCLC progressing after a previous EGFR TKI. The phase I component of the study included a dose escalation part (Osimertinib 20mg to 240mg), using a rolling six design,
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Compound was synthesized by the directed
2020-04-26
Compound () was synthesized by the directed -metallation procedure (DOM) at the stage of the amide using butyl lithium and dry ice as CO source for the introduction of the carboxylic group. Thiophene amides were prepared from commercial 3-thiophenecarboxylic MOG (35-55) by conversion into the aci
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