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The identification of novel kinase inhibitor scaffolds is hi
2023-05-25
The identification of novel kinase inhibitor scaffolds is highly desirable in order to develop selective kinase inhibitors. Small-molecule inhibitors of Interleukin-2-inducible T-cell kinase (Itk) that are based on the 3-aminopyridin-2-one fragment 1 have been reported. Despite derivatisation of 1 y
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Having demonstrated that Gq coupled mGluR a was necessary fo
2023-05-25
Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in
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The apoptosis promoting Bcl family includes BH only proteins
2023-05-25
The apoptosis-promoting Bcl-2 family includes BH3-only proteins (e.g., Bim, Bid and Bad) and multiple-domain proteins (e.g., Bax and Bak). At the time of apoptosis stimulation (e.g., DNA damage), only the BH3-only protein is activated, directly or indirectly promoting Bax/Bak oligomerization, changi
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br Introduction Quenchbody Q body
2023-05-24
Introduction Quenchbody (Q-body) immunoassay is a novel biosensing technology that uses the quenching of fluorescence by intrinsic tryptophan (Trp) residues in antibody variable regions when dye(s) are conjugated to an antibody or antibody fragments in appropriate position, and de-quenching while
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br Functional repercussions of each trimming pathway A main
2023-05-24
Functional repercussions of each trimming pathway A main difference between the two pathways presented in Fig. 1 lies in enzyme kinetics and selectivity. In pathway #1, the substrate for ERAP1 is free peptide, and so both kinetics and selectivity are determined by interactions between the peptide
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While A Rs communicate mainly with the D R subtype
2023-05-24
While A1Rs communicate mainly with the D1R subtype [36], A2AR and D2R interaction occurs mainly in basal ganglia. D2Rs colocalizes with A2ARs in this opioid receptor area where they are preferentially localized postsynaptically in the soma and dendrites of GABAergic striatopallidal neurons [69]. Th
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In earlier experiments on snails a behavioral model was
2023-05-24
In earlier experiments on snails, a behavioral model was employed of certain food rejection to study the mechanisms of the reconsolidation of long-term associative memory. It was found that conditioned food stimuli (reminder) presentation, combined with injections of NMDA glutamate receptor antagoni
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Normally the activity of the lyase increases
2023-05-24
Normally, the activity of the 17,20-lyase increases with the onset of adrenarche [7], [8], [15]. Adrenarche has previously been perceived as a relatively sudden event, occurring physiologically between 6 and 8years of age. However, results from our laboratory clearly indicated that adrenarche is a c
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br Disclosure br Acknowledgement br Introduction CYP A
2023-05-24
Disclosure Acknowledgement Introduction CYP17A1 is a multifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activities and is essential for the biosynthesis of steroidal jtc motors in male testes and adrenal glands. The 17α-hydroxylase activity of CYP17A1 is involved in the conve
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br Methods br Results br Discussion Autotaxin has been shown
2023-05-24
Methods Results Discussion Autotaxin has been shown to have effects on major cell types implicated in OA, notably chondrocytes, osteoblasts, osteoclasts, and synoviocytes, through its enzymatic product LPA [20]. However, a paucity of research exists on the involvement of autotaxin in OA. Fi
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Acknowledgments br Introduction Prostate cancer is the first
2023-05-24
Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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The Type A series contains of the
2023-05-24
The Type-A series contains 6 of the 11 confirmed hits, making it a highly attractive lead template. Seven (7) out of 8 Type-A series of 3-substituted-2-furoic acids are highly active (84–100% inhibition) at the high concentration of 100μM. We could deduce some interesting, albeit preliminary structu
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Fig summarizes the oxidative metabolism of arachidonic
2023-05-24
Fig. 1 summarizes the oxidative metabolism of arachidonic Cinchonidine by lipoxygenases cyclooxygenases and cytochrome P450. Lipoxygenases in humans are expressed in a tissue-specific fashion: 5-LOX is mainly expressed in leukocytes, 12-LOX in platelets, and 15-LOX-1 in reticulocytes, eosinophils,
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br Introduction Breast cancer is the
2023-05-18
Introduction Breast cancer is the most frequently occurring cancer in women, and despite the development of new therapies there has been little decline in the mortality rate over the past decade (Siegel et al., 2015). This is partly due to the genetic diversity of breast cancers, such that there
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These results from the present study are summarized
2023-05-17
These results from the present study are summarized in Table 1. Eight drugs (doxorubicin, epirubicin, daunorubicin, idarubicin, irinotecan, imatinib, sunitinib and gefitinib) inhibited 5-HT-induced 5-HT3A and 5-HT3AB currents; three (irinotecan, topotecan and mitoxantrone) showed different responses
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