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br Improvement of endothelial function The vascular endothel
2023-12-15
Improvement of endothelial function The vascular endothelium is a single layer of muscarinic receptor antagonists that lines the inner surface of all blood vessels and the heart. In addition to function as a selective barrier to prevent the diffusion of macromolecules from the blood lumen to the
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Imatinib is a well known anticancer
2023-12-15
Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing topotecan (K562 cell
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Ryoichi et al modified potent
2023-12-15
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br ACL A Metabolic Checkpoint for Sensing Excess
2023-12-15
ACL: A Metabolic Checkpoint for Sensing Excess Nutrients? During normal transitions between fasting and feeding, cells maintain energy homeostasis by integrating energy and nutrient status signals at key metabolic nodes, coordinating multiple processes. For example, the AMP-activated protein kina
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br Introduction Throughout early prophase
2023-12-15
Introduction Throughout early prophase I, meiotic cells intentionally generate DSBs as part of a stringently controlled process to initiate homologous recombination (HR). HR is a critical DSB repair pathway that ultimately permits the exchange of genetic information between homologous chromosomes
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br Experimental section br Acknowledgements The authors than
2023-12-14
Experimental section Acknowledgements The authors thank Prof. Yongbing Cao from School of Pharmacy, the Second Military Medical University, for providing the fluconazole-resistant strains of Candida albicans(strain 100 and strain 103). This work was supported by Program for Innovative Research
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br Identification of the croaker mAR
2023-12-14
Identification of the croaker mAR cDNA Testosterone (T) was observed to alter steroidogenesis through a nongenomic mechanism (not blocked by the transcription inhibitor, actinomycin D) in Atlantic croaker ovarian tissues (Braun and Thomas, 2003). This action of T was mimicked by T conjugated to B
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Recently two distinct small molecule inhibitors of PHGDH wer
2023-12-14
Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer Kif15-IN-2 with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces the growt
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These mutations induce the gene auto
2023-12-14
These mutations induce the gene auto-activation in 10–40% of adenocarcinomas, triggering the EGFR-signaling pathway in the absence of ligand. That leads to an uncontrolled acceleration of cell proliferation, survival and anti-apoptotic signals (Couraud et al., 2012). The frequency of these mutations
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br There are three types of HT receptors HT
2023-12-14
There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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br Experiment br Results and discussion br
2023-12-14
Experiment Results and discussion Conclusion Introduction Tuberculosis (TB) is a chronic specific bacterial infection caused by bacteria of the Mycobacterium tuberculosis [1]. TB remains one of the deadliest diseases in the world. It is the second leading infectious cause of death after
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At the last follow up nine patients had
2023-12-14
At the last follow-up, nine patients had discontinued pyridostigmine within the first year postoperatively. Only one patient required pyridostigmine at a higher dose, but this was accompanied by successful weaning of prednisolone. None of the 5 patients who were on pyridostigmine treatment alone pri
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Nowadays more than kinases have
2023-12-13
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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While it is known that circulating LDL C
2023-12-13
While it is known that circulating LDL-C levels are largely regulated by either controlling the rate of hepatic production of its triglyceride-rich precursor VLDL particle or the rate of LDLR-mediated LDL particle clearance [58], it should be noted that important differences exist between rodents an
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Macitentan In this study we have generated new FRET reporter
2023-12-13
In this study, we have generated new FRET reporters to screen all submembrane domains of AT1R for interactions with CaM. We identified a new CaM-binding domain on the receptor’s SMD2 (a.a. 125 – 141), confirmed interactions at SMD4JM (a.a. 309 – 327) and characterized the full interacting domain in
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