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A high throughput small molecule ACK biochemical inhibition
2024-12-23
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 raf inhibitors to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work w
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br Conflict of interest statement br Benign prostatic
2024-12-23
Conflict of interest statement Benign prostatic hyperplasia (BPH) is a highly complex process characterized by an increased number of epithelial and stromal Capsaicin in the transition zone. , , Autopsy studies by McNeal detail the evolution of histological changes within these 2 cellular com
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The extent to which GPCR oligomerization is a regulated proc
2024-12-23
The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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Axl which belongs to the Tyro Axl
2024-12-23
Axl, which belongs to the Tyro-Axl-Mer (TAM) family of RTKs, has been reported to regulate a variety of physiological processes including cell survival, proliferation, migration and adhesion, through the activation of the phosphoinositide 3-kinase (PI3K)/V-akt murine thymoma viral oncogene homolog (
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Small kinase inhibitors have been developed to
2024-12-23
Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical ph
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The present study indicates elevated ATX
2024-12-23
The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In wnt signaling pathway to the current gold standard for diagnosis, total fasting serum bile salt levels, ATX appe
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Our current knowledge on autophagy
2024-12-23
Our current knowledge on autophagy broadly differentiates it into three types: macroautophagy, microautophagy, and chaperone-mediated autophagy. Macroautophagy mainly involves the sequestration of cytoplasmic contents in a double-walled membrane followed by the fusion with the lysosomes. The lysosom
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We conducted the largest drug screen to date in HPV
2024-12-23
We conducted the largest drug screen to date in HPV-positive cancers and identified Aurora kinase inhibitors as effective and understudied drugs in HNSCC and CESC. These drugs cause apoptosis and cell cycle arrest in vitro and decrease tumor size in vivo. This is the first published study to demonst
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Recent studies have demonstrated significant
2024-12-23
Recent studies have demonstrated significant cross-talk between XRCC1 (a key player in ethidium bromide poisoning excision repair (BER) and single strand break repair) and DDR [30], [31], [32]. ATM and DNA-PKcs are known to be involved in the phosphorylation of XRCC1 to promote BER [30], [31]. We ha
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Many naphthoquinone derivatives have been previously obtaine
2024-12-23
Many naphthoquinone derivatives have been previously obtained from fungi in the genus Fusarium isolated from various sources, F. oxysporum from the root of citrus (Nagia and El-Mohamedy, 2007), Fusarium sp. (No. b77) from the mangrove plant (Shao et al., 2010), F. solani and F. oxysporum from fibrou
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br Experimental section br Acknowledgements This work was fu
2024-12-23
Experimental section Acknowledgements This work was funded by the Italian Association for Cancer Research (AIRC IG18590 to A.A.), by “Fondi di Ateneo-University of Pisa” years 2009 and 2010 (E. N., S. N., E. O., and A. R.) and partially by the Unipi project P.R.A.2016_27 (E. N., E.O. and A. R.
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br Eprosartan The AT R
2024-12-23
Eprosartan The AT1R antagonist eprosartan is approved for the treatment of essential PAI-1 modulator and may be administered using a convenient once-daily regimen. The drug is a well-tolerated and effective antihypertensive agent with benefit in the secondary prevention of cerebrovascular events
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br Acknowledgements This work was supported by National Natu
2024-12-23
Acknowledgements This work was supported by National Natural Science Foundation of China (Nos. 21376172, 21528601 and 21621004) and the Natural Science Foundation of Tianjin from Tianjin Municipal Science and Technology Commission (Contract No. 16JCZDJC32300). Introduction Alzheimer’s disease
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br Acknowledgments and Disclosures br Introduction Over the
2024-12-23
Acknowledgments and Disclosures Introduction Over the last decade, the most visible strategy for the treatment of Alzheimer's disease (AD) has been amyloid β peptide (Aβ) immunotherapy (reviewed in [1]). Although the first efforts with Aβ immunotherapy failed to complete clinical trials [1], A
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br Applications of ATN in clinical trials In pivotal trials
2024-12-21
Applications of ATN in clinical trials In pivotal trials, the use of biomarkers will also have to be considered in the context of regulatory risk and scrutiny. Although an important intended application of the framework is in research studies, its use will undoubtedly impact clinical development
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