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We first set out to identify the
2022-10-12

We first set out to identify the minimum pharmacophore. Early structure activity relationships (SAR) indicated that the chloro substituents were not required and that the benzisoxazole moiety could be replaced by a number of other groups. A broad survey of “left-hand” hydrophobic moieties was conduc
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TGR is a class A GPCR transducing
2022-10-12

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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The mD plasmid containing CD
2022-10-12

The mD1.2 plasmid containing CD4 domain 1 gene under the control of a promoter was obtained as a gift from Dr. Dimiter S. Dimitrov. The mD1.2 plasmid was digested using restriction endonuclease I (New England BioLabs, USA) to release the mD1.2 gene. The gene encoding the mD1.2 protein was elongated
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Based on the role of NMDA receptors
2022-10-12

Based on the role of NMDA receptors in initiation and propagation of epileptic seizures and on potentiation of NMDA function by glycine, it has been hypothesized that glycine will have proconvulsant activity (Foster and Kemp, 1989). Indeed, there is some evidence that human epileptogenic foci, remov
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br Introduction Verticillium dahliae Kleb is a soil borne
2022-10-12

Introduction Verticillium dahliae (Kleb.) is a soil-borne fungal pathogen that is able to infect hundreds of plant species, and causes vascular wilt disease [1], [2]. In nature, the infection of V. dahliae initiates from the germination of resting structures called microsclerotia [3]. The germina
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br Introduction Edible bird s nest EBN known as the
2022-10-12

Introduction Edible bird's nest (EBN), known as the health and precious food, is produced from the saliva secretion of several different swiftlet species. Researches have shown the nutritional value of the EBN with the containing of glycoproteins, carbohydrates, essential amino acids, minerals an
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It is becoming increasingly apparent that membrane lipids
2022-10-12

It is becoming increasingly apparent that membrane lipids play a critical role in modulating and regulating protein function. For example, embedding the homologous SLC1 transporter GltPh in a POPE bilayer allowed a third Na+ binding site to be identified from MD simulations [42], and the binding ene
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After brain injury adenosine levels rapidly increase in the
2022-10-12

After brain injury, adenosine levels rapidly increase in the brain [9,10]. As shown in our previous studies, the increased adenosine concentration acts on adenosine A2A receptors (A2ARs), increasing post-traumatic glutamate levels in the brain and exacerbating the severity of injuries [11,12]. Accor
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The dramatic increase in the development of
2022-10-12

The dramatic increase in the development of EAAT inhibitors and substrates over the last several years can likely be attributed to a number of experimental advances. Firstly, the isolation of the individual EAAT clones allowed each subtype to be selectively examined in well-characterized expression
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Extensive pharmacological and structural analysis shows GCGR
2022-10-12

Extensive pharmacological and structural analysis shows GCGR antibody REMD-477 competitively blocks GLC binding to the GCGR with 30-pM binding affinity, and can fully inhibit the receptor activity at low nanomolar concentrations in (S)-10-Hydroxycamptothecin mg 14, 17, 20. Functionally identical to
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Two excellent GSMs with clear pharmacological effect across
2022-10-11

Two excellent GSMs with clear pharmacological effect across rats, dogs, monkeys, and human subjects are BMS-932481 and BMS-986133 with IC50 at 6.6 and 3.5 nM to reduce Aβ42, respectively. Both GSMs exhibit dose- and time-dependent activity in vivo by decreasing Aβ1-42 and Aβ1-40 levels while increas
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Single cell reverse transcriptase PCR on A mellifera
2022-10-11

Single-cell reverse transcriptase-PCR on A. mellifera antennal lobe (AL) cells showed the expression of RDL as well as another GABA receptor like subunit, LCCH3 (Dupuis et al., 2010). Based on whole cell patch-clamp electrophysiology it was concluded that the predominant GABA receptors in AL cells a
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uPAR another newly discovered ligand
2022-10-11

uPAR, another newly discovered ligand, has implicated FPRL1 as a potential link between the fibrinolytic cascade and inflammation. uPA is a serine protease best known for its ability to regulate fibrinolysis and for its importance in tissue remodeling and tumor invasion [49]. However, uPA also induc
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Autophagy plays a multifaceted role in
2022-10-11

Autophagy plays a multifaceted role in regulating both the quality and quantity of protein (e.g., protein half-life and activity) and organelles (e.g., mitochondrial number and function), thus determining cell fate [15]. The induction of autophagy has been generally considered a programmed cell surv
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br References and recommended reading
2022-10-10

References and recommended reading Papers of particular interest, published within the period of review, have been highlighted as: Introduction Male sexual maturation includes gonadal maturation, secondary sexual characteristics, and the attainment of reproductive capacity [1]. Male sexual di
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