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Several structural classes of ASK inhibitors mostly from
2024-11-09
Several structural Coumarin of ASK1 inhibitors, mostly from industry but also from academia, have been identified over the last decade. In 2012, Terao et al. (Takeda) reported imidazo[1,2-α]pyridine () as a potent ASK1 inhibitor derived from structure-based drug design. GSK, Merck and Gilead revea
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Limitations of this study include
2024-11-09
Limitations of this study include the use of HL-1 cardiomyocytes, which show different characteristics than primary cardiomyocytes [56]. Furthermore, sustained TAC in Ampkα1-deficient mice did not favorably influence cardiac function [33]. It must be kept in mind that global Ampkα1-deficiency may af
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Once apoptosis has been initiated the
2024-11-09
Once apoptosis has been initiated the HMGA proteins themselves undergo marked changes in both the types and extent of their post-translational modifications (PTMs; review in [149,175]), some of which are likely correlated with alterations in chromatin structure. For example, the early stages of apop
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Recently different kinds of A aggregation inhibitors have
2024-11-08
Recently, different kinds of Aβ aggregation inhibitors have been reported, including small molecules [8], peptides [9], and nanoparticles (NPs) [10]. The working mechanisms of the inhibitors are mostly to bind or adsorb Aβ molecules and to affect the conformational changes followed by blocking the a
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SAR405 br Introduction It is well known that when epithelial
2024-11-08
Introduction It is well known that when epithelial cells are deprived of anchorage, they undergo detachment-induced apoptosis, also known as anoikis. Cancer cells, by contrast, are able to suppress anoikis and survive under anchorage -independent conditions in the circulating system, which is tho
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Linagliptin is a recently approved dipeptidyl
2024-11-08
Linagliptin is a recently approved dipeptidyl peptidase-4 (DPP-4) inhibitor and widely considered as first-line treatment for patients with type 2 diabetes. DPP-4 is responsible for the inactivation of incretin hormones, such as glucagon-like peptide 1 (GLP-1). GLP-1 is released by the intestine aft
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A unique finding in this study
2024-11-08
A unique finding in this study is that 12/15-LO influences CREB phosphorylation in the murine brain. While previous reports have found that knockout of 5-lipoxygenase, a related enzyme that also uses arachidonic lasofoxifene for substrate, can regulate CREB phosphoryation in the context of Alzheime
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Initially DPP DPP and prolyl tripeptidyl peptidase A PtpA
2024-11-08
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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paf receptor The application of diuretics induce
2024-11-08
The application of diuretics induce an increased rate of water exiting brain cells encouraging the formation of increased intracellular polyphosphoric acid. In the absence of the diuretic water is retained in cells converting polyphosphoric paf receptor to monophosphoric acid. The latter change dec
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br We approached the definition of AD with
2024-11-08
We approached the definition of AD with the distinction between a syndrome and a disease in mind. Some will argue that a specific syndrome, that is, a multidomain amnestic dementia (after other potential etiologies have been excluded), should define AD in living people. Our position, however, is t
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Therefore to better understand the functional
2024-11-08
Therefore, to better understand the functional properties of Peruvian infusion tea plants and provide evidence for the development of functional food supplements containing the Peruvian infusion tea plant, the aldose reductase inhibition together with the antioxidant activities of 24 selected Peruvi
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br Introduction Alcohol i e ethanol is
2024-11-08
Introduction Alcohol, i.e., ethanol, is absorbed into the blood from the stomach to the small intestine, then distributed throughout the body. The metabolism of alcohol converting to acetic herpes simplex virus 1 basically involves two enzymes; alcohol dehydrogenase converting ethanol to acetald
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The cavity volume of the binding pocket may differ not
2024-11-08
The cavity volume of the binding pocket may differ not only between species but also among various AhR/ARNT isoforms within a single species. It is noteworthy that even a single amino BCTC substitution within a binding pocket may result in a change in the cavity volume. This, in turn, may affect th
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We observed PACAP immunoreactivity in the molecular layer
2024-11-08
We observed PACAP2 immunoreactivity in the molecular layer of the cerebellar cortex in zebrafish. This result is consistent with the reporting of PACAP immunoreactivity in the soma and fibers of Purkinje cells and the presence of PACAP mRNA in the Purkinje-cell and granular-cell layers in rats [43].
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Based on our previous work
2024-11-08
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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