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br Synthetic lethal approaches In addition to
2024-09-30
Synthetic lethal approaches In addition to the potential utility of ATM and ATR as chemo- or radiosensitisers, recent studies suggest that such compounds may have single agent activity in certain subsets of patients through induction of synthetic lethality. Two genes are considered synthetically
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Optical coherence tomography angiography is another promisin
2024-09-29
Optical coherence tomography angiography is another promising method for the assessment of corneal neovascularization. This relatively new modality is not yet widely used in part because of current limitations in the definition of images produced, lack of functional information, and inability to det
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Immunohistochemistry in tissue samples showed the
2024-09-29
Immunohistochemistry in tissue samples showed the expression of several nuclear receptor co-activators, including NCOA1, NCOA2, NCOA3, CREBBP, and EP300, in 85–100% of 9-Phenanthrol tumors even some of which lacked AR expression (Boorjian et al., 2009). Knockdown of each co-activator also resulted
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Caspase-8, human recombinant protein Unlike in humans hepati
2024-09-29
Unlike in humans, hepatic expression of FGF21 increases in mice consuming KD and is a necessary mediator of the physiologic adaptations to the diet. FGF21 knockout (KO) mice gain, rather than lose weight on the diet [6]. FGF21 also activates BAT in part by increasing SNS drive [3,7]. In addition, th
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During the course of our ACK inhibitor program
2024-09-29
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of identif
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Aurora A or B selective and pan aurora
2024-09-28
Aurora -A or -B selective and pan-aurora inhibitors have demonstrated different preclinical and clinical therapeutic efficacies [2,[19], [20], [21], [22], [23]]. For example, clinical trials for a pan-Aurora inhibitor VX-680 (developed by Vertex) were halted at phase II for toxicity reasons (one cas
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In the present study we showed that LOX metabolites
2024-09-28
In the present study, we showed that 15-LOX metabolites, which are the precursors of anti-inflammatory and pro-resolving lipid mediators, were decreased in the unaffected skin area of the OS model rats by comprehensive lipidomics analyses. Furthermore, subsequent microarray analyses demonstrated tha
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ATM is required for the proper
2024-09-28
ATM is required for the proper function of the DNA-repair pathway in response to bleomycin-induced DNA damage in mammalian cells [55], [56]. Recent reports suggest that ATM activation by double-strand breaks leads to the subsequent ATR activation [57], [58], [59]. The recruitment of ATR to double-st
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We initially established using fMRI that auditory processing
2024-09-28
We initially established using fMRI that auditory processing by the caudomedial nidopallium (NCM) of male European starlings (Sturnus vulgaris) of species-specific aspects of songs (whistles and warblings i.e. high-pitched trills coming from the end of the warbling that are found in the repertoire o
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Introduction Cytochrome P CYP aromatase
2024-09-28
Introduction Cytochrome P450 19 (CYP19; aromatase) catalyzes the conversion of androgens to estrogens in a three-reaction sequence, where each step depends on NADPH and O2 [[1], [2], [3]]. The first two steps are accepted to be hydroxylations of the steroid C19 methyl group, whereas the final step
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Although apelin g kg shows negative early
2024-09-28
Although apelin 60μg/kg shows negative (early) and positive (late) inotropic effects, since ERK1/2 phosphorylation starts at the min 5 of administration [6], ERK1/2 phosphorylation mediate positive inotropic effects of apelin 60μg/kg. After the simultaneous inhibition of KOR and APJ the phosphoryla
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Despite the absence of disulfide bonds in its
2024-09-28
Despite the absence of disulfide bonds in its linear structure, KT43C displays antifungal and antibacterial activity. Disulfide bonds are determinants of defensins' integrity and have been reported to increase the antimicrobial activity (Jenssen et al., 2006). However, some linear derivatives of AMP
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br Under normal physiological conditions
2024-09-28
Under normal physiological conditions, the agonist binds to AT1R on the surface of the plasma membrane and activates the receptor, mediating downstream signaling. Then, activated AT1R is phosphorylated by protein kinase C (PKC) [13] or G protein coupled receptor kinases (GPKs, such as GRK2 [13], G
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br Study approval br Author contributions br Conflicts of in
2024-09-28
Study approval Author contributions Conflicts of interest Acknowledgements This work was supported by grants of the Youth Backbone Program (to Jianming Ying) of Cancer Hospital, CAMS, Beijing, Beijing Hope Run Special Fund of Cancer Foundation of China (LC2015A06) and the National Natura
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Synthesis of the pterin carboxamides was
2024-09-28
Synthesis of the pterin-7-carboxamides was achieved, as shown in , based on a previously reported method that utilizes DBU as a key additive to dissolve pterin in organic solvents and accelerate the reaction., With this method, the pterin-amino Saikosaponin A conjugates (–) were readily obtained by
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