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From an industrial perspective the low turnover numbers and
2019-07-12
From an industrial perspective, the low turnover numbers and limited substrate scope of α-KG halogenases still represents a significant challenge. However, in light of the fact that currently no chemical processes are available for the selective halogenation of aliphatic carbon centers in complex mo
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br Introduction Natural killer NK cells have an unique abili
2019-07-12
Introduction Natural killer (NK) cells have an unique ability to directly lyse transformed, virus-infected or stressed cells without prior sensitization or major histocompatibility complex (MHC) class I restriction [1], [2]. They were initially defined and shown to be important effectors of the i
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CysLTs trigger contractile and inflammatory processes
2019-07-12
CysLTs trigger contractile and inflammatory processes through the specific interaction with cell surface receptors belonging to the rhodopsin family of the G protein-coupled receptor (GPCR) genes. Until now, two receptor subtypes have been cloned, namely CysLT1 and CysLT2[8]. In particular, when the
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The oxidation of the lipid
2019-07-11
The oxidation of the lipid fraction of meat is an extremely complex process because of the high sensitivity of oxidation products to decomposition, their reactions with other components, the complex effect of catalysts and the presence of antioxidants. These changes are the main cause of limited she
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EP is the major receptor to mediate PGE
2019-07-11
EP4 is the major receptor to mediate PGE2-induced inflammatory pain. EP4 is upregulated by AI-10-49 in DRG neurons [16]. Intrathecal injection of the EP4 agonist produced pain responses [25]. Either systemic or local injection of EP4 antagonists relieves inflammatory pain [3], [16], [26]. However,
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br Discussion Before comparing our results with
2019-07-11
Discussion Before comparing our results with structural studies, we can turn to the Wiki on transition state theory (1935), which explains the reaction rates of elementary chemical reactions in terms of two parameters in one dimension. Structural studies contain information on the ground state, a
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After activation AKT phosphorylates target
2019-07-11
After activation, AKT phosphorylates target proteins involved in cell growth, metabolism and survival (Manning and Cantley, 2007). For example, AKT phosphorylates the pro-apoptotic protein BAD, preventing it from binding to and inactivating Bcl-xL in mitochondria (Datta et al., 1997). In turn, Bcl-x
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br Inhibition of DHODH The final products
2019-07-11
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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Targeting both PARP and DHODH
2019-07-11
Targeting both PARP-1 and DHODH for anti-cancer therapy would certainly be beneficial as these enzymes share a common role in the DNA replication and repair mechanisms which are involved in the hyper-proliferation of cancer cells. Since benzimidazole-containing compounds have been reported to show g
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The serotonin transporter gene encodes an integral membrane
2019-07-11
The serotonin transporter gene () encodes an integral membrane protein that transports serotonin from the synaptic spaces into the presynaptic neurons. The encoded protein terminates the action of serotonin and recycles it in a sodium-dependent way. This protein is a target of psychomotor stimulants
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The binding pattern of was analysed by flexible molecular
2019-07-11
The binding pattern of 1 was analysed by flexible molecular docking. The Betamethasone Dipropionate inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains resi
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Besides having a remarkable progestogenic effect an addition
2019-07-11
Besides having a remarkable progestogenic effect, an additional characteristic of DRSP is its strong antimineralocorticoid effect and antiandrogenic action [11]. DRSP is characterized by an antimineralocorticoid effect that is stronger when compared to progesterone. The decreasing synthesis of proge
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br Introduction Oral contraceptives OCs are
2019-07-11
Introduction Oral contraceptives (OCs) are the most commonly used medication for contraception all over the world and are also used in the treatment of menstrual disturbances and hyperandrogenism in women with polycystic ovary syndrome [1]. The impact of OC steroids on cardiovascular pathophysiol
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Minocycline HCl Molecular docking study of compound was perf
2019-07-11
Molecular docking study of Minocycline HCl was performed using the Schrödinger Small-Molecule Drug Discovery Suite taking advantage of known X-ray crystal structures of activated EPAC2 protein. The model shows that compound occupies the CBD of EPAC2 and forms hydrogen bonds with Arg448 and the cy
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Nitric oxide synthase NOS is a
2019-07-11
Nitric oxide synthase (NOS) is a predominant enzyme of immune system, which elaborates nitric oxide (NO) from the amino Amphotericin B arginine (Arg). NO mediates vasodilatation, blood pressure regulation, neurotransmission, host defense, and macrophage-mediated immunity, among an array of other fu
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