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The same applies also to intermediate formally obtained by e
2023-01-09
The same applies also to intermediate , formally obtained by elimination of the R substituent from compound . If compared to the thienopyrimidine derivatives (series , C), the thieno[3,2-]pyridazin-5(4H)-ones – explored herein seem to maintain similar size and shape and also analogue structural char
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leukotriene receptor antagonists ATM is generally regarded t
2023-01-09
ATM is generally regarded to be the principal mediator of the G1 leukotriene receptor antagonists checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular con
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Molecular simulation has proven useful
2023-01-09
Molecular simulation has proven useful in describing the dynamics and energetics of NMDA receptor LBD cleft closure and the potentiating role of glycans (Yao et al., 2013, Dai and Zhou, 2013, Dai and Zhou, 2015, Dai and Zhou, 2016, Dutta et al., 2015, Omotuyi and Ueda, 2015, Sinitskiy and Pande, 201
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In addition to peroxyl radicals the most found
2023-01-09
In addition to peroxyl radicals, the most found radical forms in biological systems, some of assays took into account other free radicals such as superoxide anion, hydroxyl, hydrogen peroxide, singlet oxygen and peroxynitrite. ORAC procedure was also modified using different radical sources such as
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At the top of the S subsite cylinder are two
2023-01-09
At the top of the S1 subsite cylinder are two “cap” residues: E572 and M1034 [13]. Atomic structures of PfA-M1 have revealed important clues into potential roles for the cap residues in substrate selection. In the PfA-M1:bestatin co-crystal structure ([13]; Fig. 1), the P1 phenyl ring occupies the S
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br Acknowledgements br Introduction Diabetic
2023-01-09
Acknowledgements Introduction Diabetic complications are responsible for increased morbidity and mortality of diabetic patients. Increased flow of DPQ mg through the polyol pathway under conditions of hyperglycemia contributes to the development of diabetic complications. Aldose reductase (AL
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In summary the role of HT and differe
2023-01-09
In summary, the role of 5-HT and different types of 5-HTRs in gating plasticity induction in neocortical circuits remains unclear, with variable and seemingly contradictory effects reported for LTP induction in cortical sensory fields (e.g., V1, enhanced LTP: Inaba et al., 2009, Kojic et al., 1997,
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The first result of this paper is parallel to the
2023-01-05
The first result of this paper is parallel to the positivity result given in [16]: Here the definition of approximate ACHE metric is the same as in [18]. See Definition 1 for details. The second result of this paper is parallel to the 49 9 mg extension formulae given in [2]. In particular, while i
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Inhibitors of mPGES are considered as safe alternative
2023-01-05
Inhibitors of mPGES-1 are considered as safe alternative to NSAIDs in the treatment of chronic inflammatory diseases that are characterized by excessive PGE2 production (Bahia et al., 2014; Khurana and Jachak, 2016; Koeberle et al., 2016; Korotkova and Jakobsson, 2014; Norberg et al., 2013; Psarra e
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Cancer cells manifest characteristic abnormal
2023-01-05
Cancer Trigonelline receptor manifest characteristic abnormal growth properties accompanying clonal evolution of cells displaying progressively increasing genomic instability capable of invasion and metastasis to distant organ sites. With the emerging knowledge about the role of known oncogene and
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The LO has so far only
2023-01-05
The 15-LO-1 has so far only been found in humans and rabbit reticulocytes [3], [20] and the rabbit 15-LO-1 protein demonstrate 81% identity to the human 15-LO-1. However, rabbit monocytes express an enzyme with mainly 12-LO activity [20], [21]. The high degree of sequence conservation between these
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The known crystal structures of class C
2023-01-05
The known crystal structures of class C GPCR VFTs do not include attached TM domains, therefore current conformational data may not accurately reflect the dynamics of extracellular domains in full-length receptors. Nevertheless, compelling mechanisms of signal transduction can still be postulated. S
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Receptors containing an x y subunit interface where x and
2023-01-05
Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For
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Non steroidal anti inflammatory drugs which include aspirin
2023-01-05
Non-steroidal anti-inflammatory drugs, which include aspirin and ibuprofen, target COX-2 activity to inhibit inflammation. It has been shown that daily use of a nonsteroidal anti-inflammatory drugs is associated with reduced ER-positive breast cancer recurrence in obese and overweight women. More pr
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Introduction The burden of cardiovascular disease CVD
2023-01-05
Introduction The burden of cardiovascular disease (CVD) is undisputed, accounting for approximately a third of global deaths (17.5 million people in 2012) (WHO, 2012). Atherosclerosis leads to the development of coronary heart disease (CHD) which accounts for more than 40% of these deaths (WHO, 201
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