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78 4 br Angiotensin receptor neprilysin inhibitors Sacubitri
2025-01-07
Angiotensin receptor-neprilysin inhibitors Sacubitril/valsartan is the first-in-class ARNI, comprising of molecular moieties of valsartan (ARB) and a neprilysin inhibitor prodrug, sacubitril (AHU377) [51]. Upon ingestion, sacubitril is rapidly metabolised into an active neprilysin inhibitor, sacu
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Earlier studies with SERMs identified that distinct chemical
2025-01-07
Earlier studies with SERMs identified that distinct chemical scaffolds have the ability to induce unique conformational changes in the ER, resulting in interaction with different cofactor subsets. The same has been demonstrated with SARMs, which induce distinct conformational changes compared to tes
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To guide our attempts at achieving
2025-01-07
To guide our attempts at achieving AKT potency and selectivity against p70S6K and other kinases from (p70 S6K IC: 0.004 μM) and , we took advantage of exploiting the subtle sequence differences in the active sites of the AGC family kinases, we utilized the information around crystal structure of AK
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Derivatives of M that possess
2025-01-07
Derivatives of (+)-M100907 that possess either an alkyne or an azide have been synthesized. The most active enantiomer was obtained by resolution of a relatively early intermediate in the synthesis. The ability of these N6-Methyl-dATP to maintain 5-HTR antagonist properties as (+)-M100907 was demon
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Taken together our results indicated that LOX can be
2025-01-07
Taken together, our results indicated that 5-LOX can be induced in mice by MPTP injection, and the 5-LOX inhibitor MK-886 reduced the death of dopaminergic neurons. MK-886 also reduced the LTB4 ddhGTP induced by MPTP. The development of the novel 5-LOX or FLAP inhibitors may provide a new therapeut
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Biotin-11-dCTP PCR Acknowledgements The work was supported b
2025-01-07
Acknowledgements The work was supported by grants from Swedish Research Council (J.Z.H.) (A.R.M.). We thank Protein Science Facility (PSF), Department of Medical Biochemistry and Biophysics, Karolinska Institute, Stockholm, Sweden. We thank Prof. Ralf Morgenstern (Department for Environmental Medic
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br Results br Discussion Autophagy is
2025-01-06
Results Discussion Autophagy is considered as an important process in physiological and pathological ovarian function. It is related mainly to follicular atresia and CL regression (for review see [20]). However, an involvement in luteal cell survival is also proposed [21], [22]. The present st
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Aurora kinases were initially identified as protein kinases
2025-01-06
Aurora kinases were initially identified as protein kinases essential for error-free chromosome segregation during mitosis and meiosis. Aurora A appears to control premetaphase events, such as bipolar spindle assembly 3, 4, with Aurora B and C directing metaphase and postmetaphase events, including
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To the best of our knowledge only cases of
2025-01-06
To the best of our knowledge, only 3 cases of an E196K mutation have been described since it was first identified in 2000 [15], [16], [17], although 5 cases, accounting for 1.1% of all genetic TSE cases, were reported with no precise data on the clinical phenotypes in the EUROCJD collaborative surve
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br Introduction The principal pathways of adrenal and
2025-01-04
Introduction The principal pathways of adrenal and gonadal steroidogenesis have been known for over 50 years (reviewed by Miller and Auchus, 2011). Cholesterol is first converted to pregnenolone via three reactions, 20-hydroxylation, 22-hydroxylation and scission of the 20,22 carbon–carbon bond,
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br Autophagy in the central nervous system The autophagic pr
2025-01-04
Autophagy in the central nervous system The autophagic process appears to be very important for the cells of the central nervous system, as it allows to maintain the functional integrity of the nervous tissue. Indeed macroautophagy is involved in the regulation of homeostasis of the CNS, playing
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Recent studies have indicated that
2025-01-04
Recent studies have indicated that V-ATPase activity negatively regulates vacuolar fusion in vivo[17]. Since we have demonstrated that the pah1Δ Kaempferol derivative have a more acidic vacuolar pH than the WT cells, and the genes involved in the pump activity are upregulated compared to WT, the pa
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The main function of ATR CHK signaling is activating cell
2025-01-04
The main function of ATR/CHK1 signaling is activating conotoxin synthesis checkpoint arrest for S and G2 phases in mammalian cells. There are three checkpoints in response to DNA damage: G1/S, G2/M, and S-phase. The G2/M checkpoint can prevent cells that incur DNA damage in G2 phase or progress int
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The distribution and subcellular localization differs betwee
2025-01-04
The distribution and subcellular localization differs between the subtypes of mGlu receptors. Most mGlu receptors are broadly expressed in the brain, except for mGlu6, which is restricted to the retina. Some mGlu receptors are additionally found in glial cells, such as mGlu3 and mGlu5 (Aronica et al
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Several alterations have been or can be associated to
2025-01-04
Several alterations have been or can be associated to the decreased tolerance of steatotic liver to I/R injury. Previous studies demonstrated that upregulation of the mitochondrial uncoupling protein-2 (UP2) is strictly related to the increase of I/R injury in steatotic liver [4]. UPR induction is c
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