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A high throughput screening campaign led to the
2024-08-03
A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity
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br Declaration of interest br Funding
2024-08-03
Declaration of interest Funding Introduction The endocrine disruptor bisphenol A (BPA) is a high-production chemical used in several consumer products, including polycarbonate bottles, epoxy resins, dental sealants, and thermal paper receipts (Geens et al., 2012). Importantly, BPA monomers
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Use of RASB is associated with
2024-08-03
Use of RASB is associated with potential concerns about side effects such as acute kidney injury or hyperkalemia, and clinicians are reluctant to prescribe RASB in patients with severe renal dysfunction (estimated GFR Conclusions Conflict of interest Acknowledgement Introduction Renin-an
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This development notwithstanding the chemotherapeutic treatm
2024-08-02
This development notwithstanding, the chemotherapeutic treatment for leukemia has stagnated over the last 40 years [35]. Main treatment options necessitate aggressive chemotherapy to target leukemic cells [36], [37], [38], [39]. Several limitations of current treatment options include the use of ant
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Initially DPP DPP and prolyl tripeptidyl
2024-08-02
Initially, DPP4, DPP7, and prolyl tripeptidyl peptidase A (PtpA) were the only exopeptidases identified in P. gingivalis. These share substrates according to their altered specificities, as DPP4 is highly specific for Pro at the penultimate position from the N-terminus (P1 position), though it accep
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Imaging QTL studies may have several potential advantages
2024-08-02
Imaging QTL studies may have several potential advantages over case-control studies, including increased power . Imaging endophenotypes of disease in QTL studies can separate patients and normal subjects more accurately and therefore limit the confound of including asymptomatic subjects in the contr
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Young et al described the role of adenine
2024-08-02
Young et al. [40] described the role of adenine monophosphate-activated protein kinase (AMPK) in the translocation of GLUT4 in the heart. The AMPK is activated during muscle contraction [74] by converting AMP to ATP. The adenosine analog, 5-aminoimidazole-4-carboxamide ribonucleotide (AICAR), is a c
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Besides its multiple peripheral effects adiponectin may
2024-08-02
Besides its multiple peripheral effects adiponectin may ameliorate insulin resistance by acting in the brain, and intracerebroventricular administration of adiponectin in rodents decreases body weight by stimulating energy expenditure [13]. Adiponectin most likely crosses the blood-CSF-barrier (BCB)
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Our results using RT PCR confirm earlier findings Wilisch et
2024-08-02
Our results using RT-PCR confirm earlier findings (Wilisch et al., 1999, Bruno et al., 2004) including the presence of both the P3A+ and P3A− isoforms of the α-subunit (Beeson et al., 1990). The lack of detection of the ε-subunit mRNAs in some thymomas, and lack of α-, β-, δ- and γ-subunit mRNAs by
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br Conclusion Biotransformation of trachyloban oic acid
2024-08-02
Conclusion Biotransformation of trachyloban-19-oic Quinidine by S. racemosum provided three products. Oxidation of compound 1 at C-17 (2–3), as well as rearrangement of 1 into a kaurane diterpene hydroxylated in C-16 and C-17 (4) were crucial for increasing AChE inhibitory activity. Compound 3 w
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There are several reports about the expression of AChRs and
2024-08-02
There are several reports about the expression of AChRs and their modulation to osteogenic factors in osteoblasts (Rothem et al., 2011, Sato et al., 2010, Walker et al., 2001). The normal osteocytic MLO-Y4 AG-14361 australia expressed multiple subtypes, which was demonstrated by the detection of M1
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br Acknowledgements We thank Dr Stefan Schulte Merker and hi
2024-08-02
Acknowledgements We thank Dr. Stefan Schulte-Merker and his group members at the Hubrecht Institute (Utrecht, the Netherlands) for their invaluable support of the zebrafish studies. Our work is supported by grants from the Dutch Cancer Society (KWF) and the Netherlands Organisation for Scientific
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Skeletal pain associated with bone fracture is
2024-08-02
Skeletal pain associated with bone fracture is another area of critical need for a novel pain medication. NSAIDs and opiates are the two major therapies currently used to manage bone fracture pain. However, both of these therapies lead to significant unwanted side effects. Using the osteotomy model
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br Experimental procedures br Results br Discussion Major
2024-08-01
Experimental procedures Results Discussion Major depressive disorder is among the leading causes of disability worldwide (Vos et al., 2015). One of the major causal or exacerbating factors of depression is long term stress or psychological trauma (Liu and Alloy, 2010). Dysregulation of the
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Weak and transient interactions of HMGB proteins in such hit
2024-08-01
Weak and transient interactions of HMGB proteins in such hit-and-run mechanisms are understandable given that “fluorescence loss in photobleaching” (FLIP) experiments employing GFP-labeled HMGBs have shown that in living cells they are the most mobile of all nuclear proteins [144]. The entire pool o
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