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SC-10 br Introduction Nausea and vomiting are
2023-11-21
Introduction Nausea and vomiting are among the most distressing side effects associated with chemotherapy in cancer patients (Billio et al., 2010). Severe emesis can negatively affect a patient's nutritional state, ability to work and motivation, which can, in turn, interfere with the clinical co
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A high throughput small molecule
2023-11-21
A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found Posaconazole mg to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work
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Macitentan mg Taken together BRP represents a novel chemotyp
2023-11-21
Taken together, BRP-187 represents a novel chemotype of LT biosynthesis inhibitors with outstanding potency in human PMNL and monocytes activated under pathophysiological relevant conditions and with effectiveness in vivo. Using the PLA that visualizes the in situ interaction between 5-LO and FLAP i
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Matrix metalloprotease inhibitors are increasingly available
2023-11-21
Matrix metalloprotease inhibitors are increasingly available and tested for other indications in clinical trials. The present study suggests that either ADAM10 or TACE inhibition alone will not maximally restore leukocyte Axl function. We found that lower doses of ADAM10/TACE inhibitors exhibit simi
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br Results and discussion br Conclusion In
2023-11-21
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic 821 group extending from the C-3 position of the aniline and substituted groups at
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Nowadays more than kinases have
2023-11-21
Nowadays, more than 500 kinases have been identified of human genome [2]. Imatinib (Gleevec) was the first tyrosine kinase inhibitor approved by the US Food and Drug Administration (FDA) for the treatment of chronic myeloid leukemia [3], and kinases have become an attractive target for the developme
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Telomerase action at the telomere is highly
2023-11-21
Telomerase action at the telomere is highly regulated; it preferentially elongates the shortest telomeres, and recruitment of the enzyme complex to the telomere occurs in mid-S phase of the cell cycle (Bianchi and Shore, 2007, Britt-Compton et al., 2009, Teixeira et al., 2004, Hemann et al., 2001, T
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br Results br Discussion br Conclusions In summary this
2023-11-21
Results Discussion Conclusions In summary, this study provides novel report of pericardial adipose aromatase expression – in both human and rodent. We show that aromatase expression is remarkably upregulated with aging (Fig. 1C), and that total aromatase Astemizole conversion capacity is s
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The functions of HMGN protein are modulated by various post
2023-11-21
The functions of HMGN1 protein are modulated by various post-translational modifications, including phosphorylation , , , acetylation , and glycosylation . Phosphorylation in HMGN1 may influence its binding affinity to DNA or nucleosome-associated proteins and affect the sub-cellular localization an
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Since primitive societies plants herbs and seeds
2023-11-21
Since primitive societies, plants, herbs and seeds, rich in phytochemicals, were used due to their benefits in human health. These molecules were shown to present a diverse array of action mechanisms, including antioxidant activity, enzyme stimulation, hormones mimicking and by interfering with DNA
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abk Current treatment options for corneal neovascularization
2023-11-21
Current treatment options for corneal neovascularization include topical application of steroids220, 25, 35, 43 or surgical interventions: laser ablation,14, 203, 234, 48 photodynamic therapy (PDT),4, 93 and fine-needle diathermy.221, 238, 240, 261 Targeting proangiogenic molecules with topical or s
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GDC-0084 br Conclusions br Transparency document br Acknowle
2023-11-21
Conclusions Transparency document Acknowledgements This work was supported by a grant from the European Commission FP6 “Neuroprion” – Network of Excellence and Royal Veterinary College Bioveterinary science research project funding. We thank Professor Alun Williams (Cambridge University) fo
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TCEP br Role of AMPK in inflammation
2023-11-21
Role of AMPK in inflammation signaling Pro-inflammatory cytokines, such as interleukin (IL)-6 and tumor necrosis factor-α (TNF-α), activate Ikβ kinase (IKKβ), which phosphorylates IκBα, triggering the degradation of proteasomal IκB. This liberates active nuclear factor kB (NF-kB) to translocate i
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The mechanism of transformation into
2023-11-20
The mechanism of transformation into SCLC is unclear but the loss of retinoblastoma gene (RB) seems important and constitutes an initial event in the tumorigenic process. Some reports revealed the role of the RB gene loss in EGFR mutated NSCLC who transformed into SCLC [15]. In NGS we retrieved mut
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br KYN Acts on AhR To Induce Tolerogenic
2023-11-20
KYN Acts on AhR To Induce Tolerogenic Immunity IDO1 and TDO2 are intracellular heme-containing metalloproteins that catalyze the committing and rate-limiting step of the KYN pathway (KP) that converts the essential amino cdc42 inhibitor tryptophan to a series of biologically active second metabo
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