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Docking studies were performed on the
2025-01-09
Docking studies were performed on the selected compounds to explore their binding patterns and to examine SAR in more detail. The co-crystal structure of ATX in complex with PF-8380 (PDB code: ) was selected for the docking studies due to structural similarity of the most potent compound with PF-83
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However there are studies revealing the dark side of autopha
2025-01-09
However, there are studies revealing the “dark side” of autophagy at later stages in cancers, when oncogenes (mainly K-ras and B-raf) are activated and/or tumour suppressors such as PTEN and p53 are inactivated. These studies are based on the use of GEMM and deletions of essential autophagy genes (A
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estrone vs estradiol Treatment of all of the GYN cancer cel
2025-01-09
Treatment of all of the GYN cancer estrone vs estradiol in this study with ATRi not only reduced phosphorylation of Chk1 at Ser345 following genotoxic stress, but also phosphorylation of ATM. Loss of phospho-ATM following ATRi treatment is not likely due to non-specific targeting of ATM by ETP-464
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Despite these conflicting data about COX ER
2025-01-09
Despite these conflicting data about COX-2/ER correlations, a large body of evidence supports that elevated COX-2 expression in breast cancer is a constant feature of high stage disease and a predictor of worse outcome. Upregulation of COX-2 protein has been identified in approximately 40% of cases
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Circular dichroism CD provides useful information about prot
2025-01-09
Circular dichroism (CD) provides useful information about protein structure, the extent and rate of structural changes and ligand binding. CD is a form of light ICI 118,551 hydrochloride spectroscopy that measures differences in the absorbance of right- and left-circularly polarized light (rather t
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br Discussion Missense mutations transversions of the
2025-01-09
Discussion Missense mutations (transversions) of the first nucleotide of the phenylalanine 71 5 at position 1174 (F1174) of the anaplastic lymphoma kinase gene can result in substitutions to leucine or valine (F1174L/V) while missense mutation (transversion) of the second nucleotide of the pheny
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Our findings establish a critical link
2025-01-08
Our findings establish a critical link between HemAC-Lm dimeric structure and cAMP synthesis that helps in explaining how globin-A domain influences AC domain. The following possible homodimeric structure of wild type full length HemAC-Lm has been proposed to explain the role of this globin-A domain
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Introduction Adenosine monophosphate cAMP is
2025-01-08
Introduction Adenosine 3′,5′-monophosphate (cAMP) is a general-purpose signaling molecule present in most branches of life. Intracellular cAMP levels control diverse cellular functions. In bacteria, cAMP regulates metabolism by activation of the catabolite activator protein (CAP), also known as cAM
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Based on our previous work and the
2025-01-08
Based on our previous work [13] and the observation that SNX9 is a partner for ACK, we have investigated interactions involving the SH3 domain of SNX9, and identified for the first time synaptojanin-1 as an alternate partner. This SH3 domain can bind a single site in ACK1, but multiple sites in the
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The adoptive transfer experiments additionally demonstrated
2025-01-08
The adoptive transfer experiments additionally demonstrated the role of cholinergic regulation in the antibody immune response. Injection of LPI-stimulated B lymphocytes significantly up-regulated both the IgM and IgG responses to cytochrome c in the host. Obviously, this effect was due to activatio
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In an effort to determine if
2025-01-08
In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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Herein we disclose novel dihydropyrano c pyrazoles
2025-01-08
Herein, we disclose novel 2,4-dihydropyrano[2,3-c]pyrazoles that inhibit human ATX (hATX). Our results demonstrate and further support previous findings showing that a desired biological action can be achieved without targeting the catalytic site of the enzyme. Moreover, this study validated hen egg
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br Conclusions br Acknowledgments br Introduction To die or
2025-01-08
Conclusions Acknowledgments Introduction To die or not to die – that is the question. Christian de Duve created the word “autophagy” in 1960’s for the first time (Klionsky et al., 2016). The word “autophagy” was derived from the Greek roots “auto” (self) and “phagy” (eating) and referred to
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br Synthetic lethal approaches In addition to the
2025-01-08
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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br Antioxidant polymers conjugates Natural antioxidants are
2025-01-08
Antioxidant-polymers conjugates Natural antioxidants are usually used as a substitute for synthetics but some degradation phenomena could influence their applications. For example, ascorbic Tetraethylammonium chloride as a natural antioxidant undergoes yellowish coloration as a result of oxidati
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