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In conclusion re evaluation of HER status
2021-10-11
In conclusion, re-evaluation of HER2 status is necessary to determine the appropriate use of anti-HER2–targeted therapy beyond disease progression. EGFR and c-met amplification, as well as PIK3CA mutation, are rarely associated with acquired resistance. Our results highlight the importance of formal
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Toc and Toc are GTPases that regulate
2021-10-11
Toc34 and Toc159 are GTPases that regulate initial steps of preprotein import [3,4,26]. It was shown that GTP hydrolysis of at least one receptor is necessary to initiate the translocation process [23,27]. As reported for other small G-proteins, Toc34 and Toc159 bind their cargo in a nucleotide-depe
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GPR GPR GPR GPR and GPR all shared
2021-10-11
GPR80, GPR81, GPR82, GPR93 and ψGPR79 all shared identities to P2Y GPCRs or P2Y-like oGPCRs. Previously, at least three different nucleotide receptor phenotypes have been observed in mammalian tissue, including GPCRs activated by D-erythro-Sphingosine (synthetic) nucleotides (e.g. P2Y1 and P2Y11), u
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br Significant efforts are currently
2021-10-11
Significant efforts are currently focused on non-dopaminergic strategies to address the unmet medical needs in schizophrenia, and targeting -methyl--aspartate (NMDA) MK 886 hypofunction has garnered a great deal of attention., , Elevation of synaptic glycine levels near NMDA-containing synapses, b
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Due to the high structural similarity between GlxI
2021-10-11
Due to the high structural similarity between GlxI and FosA, it is possible that GlxI directed evolution experiments could produce FosA enzymatic activity in a GlxI enzyme. Although the current investigation was unable to detect FosA activity by mutation of a key metal liganding residue in the activ
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br Materials and methods br Results
2021-10-11
Materials and methods Results Discussion l-glutamate is the major excitatory neurotransmitter in the brain, and is functionally involved in many processes of the nervous system which have been connected with several neurological diseases [4]. These conditions are characterized by the time-d
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br Acknowledgements br Introduction Aminoacyl tRNA
2021-10-11
Acknowledgements Introduction Aminoacyl-tRNA synthetases catalyze the formation of an ester bond between an amino aldehyde dehydrogenase inhibitor and the 3′ end of a tRNA in a two-step reaction. First, the amino acid is activated and an enzyme-bound adenylate intermediate is formed. Then, the
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The post translational modification O
2021-10-11
The post-translational modification O-GlcNAcylation is also dependent upon glucose fluctuations. O-GlcNAcylation has been linked to insulin resistance and glucose toxicity in diabetes and its comorbidities [11]. O-GlcNAcylation is a dynamic modification tightly regulated by the nutritional sensor UD
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The manner in which various
2021-10-11
The manner in which various residue side chains are oriented in the active site of HsHxKIV was a driving factor for why glucosamine analogues could not bind, as we previously proposed [16]. These compounds would have difficulty managing access into the active site based on residue P153 in addition t
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br Role of BKCa in Cardiovascular System br Perspective for
2021-10-11
Role of BKCa in Cardiovascular System Perspective for BKCa Channels as Potential Target for Cardiovascular Diseases The intermediate conductance Ca-activated K+ channels (IKCa; KCa3.1, also known as SK4, IK, IKCa1, SMIK) were first discovered in erythrocytes by Gardos (1958) and then also fo
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When tested in dog at mg kg showed a reduction
2021-10-11
When tested in dog at 20mg/kg, showed a reduction of 56% of Aβ42 in the cerebrospinal fluid (CSF) 8h post doing, comparable to that of (see ). Upon evaluation of RGFP966 sale in a one week repeated dose study in dog, at 10 and 20mg/kg/day, no increase in liver enzyme levels (ALT or AST) was obse
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Compounds were tested for GPR activity in a functional
2021-10-09
Compounds , were tested for GPR40 activity in a functional assay monitoring calcium flux in CHO Fomepizole transiently transfected with human GPR40 gene. As shown in , compound was found to be a nanomolar GPR40 agonist, while compound was much less potent than . To explore the structure activity
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The normal function of the FBPase enzyme is
2021-10-09
The normal function of the FBPase enzyme is to catalyze the hydrolysis of F1,6BP to F6P. This activity is induced by diabetes and starvation and is increased in diabetic rats. The level of FBPase can be normalized by insulin, however, similar information is not available from diabetic patients. FBPa
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br Conclusion Discovery of an
2021-10-09
Conclusion Discovery of an ideal orally active antithrombotic drug has remained elusive till date. Research efforts in this direction led to the discovery of numerous coagulation enzyme inhibitors including various thrombin and FXa inhibitors. Several preclinical studies have highlighted the impo
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BTL-105 Based on the inhibitory potency of
2021-10-09
Based on the inhibitory potency of C646 for HDAC6, we monitored α-tubulin acetylation; an HDAC6 substrate. C646 treatment provided pronounced inhibition of α-tubulin acetylation after both 6 and 20h of incubation, which argues against HDAC6 inhibition by C646 in RAW264.7 cells. The observed effect o
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