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GPR agonistic activity was evaluated
2021-10-11
GPR119 agonistic activity was evaluated for the human GPR119 receptor in a cell-based cAMP assay. The results expressed the potency as EC values and the inherent activity (IA) as percentages which were compared to the test compound with oleoylethanolamide (OEA), an endogenous ligand of GPR119 (defin
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Molecular properties as well as metabolic stability in rat
2021-10-11
Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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LbGlcK and the HsHxKIV d glucose complex PDB entry
2021-10-11
LbGlcK and the HsHxKIV-d-glucose complex (PDB entry 3IDH) [17] were superimposed from individual subunits. The active site regions revealed the key Pazopanib Hydrochloride binding residues to be present for LbGlcK; also, the superposition showed that HsHxKIV had residues that were absent in LbGlcK,
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The sexual dimorphism in dlGALR a
2021-10-11
The sexual dimorphism in dlGALR1a and dlGALR1b receptors found in the gonads of adult fish led us to hypothesize that the gene expression difference between female and males might be attributed to the differences in steroid production between female and male gonads. Interestingly we have found that
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br Conflict of interest br Introduction Endometriosis is
2021-10-09
Conflict of interest Introduction Endometriosis is defined as the presence of endometrial glands and stroma outside the uterus, most often in the pelvic peritoneum and ovaries. This disorder affects an estimated 10% of women in the reproductive age group and is basically an estrogen-dependent
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Following nerve injury Shh expression is upregulated
2021-10-09
Following nerve injury, Shh expression is upregulated in neuronal cell bodies of the facial and sciatic nerves. Additionally, Shh appears to be required for normal regeneration in vivo, and promotes motor neuron survival in vitro (Martinez et al., 2015; Akazawa and Kohsaka, 2007). Based on these obs
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The dramatically reduced expression of CFTR in human colorec
2021-10-09
The dramatically reduced expression of CFTR in human colorectal cancer tissues identified herein is consistent with our previous findings using human breast cancer tissues, prostate cancer tissues, and colon cancer tissues, and suggests that the loss of CFTR is likely a general phenomenon in epithel
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Apo E is defined as a polym http www apexbt
2021-10-09
Apo E is defined as a polymorphic protein arising from three alleles. The human Apo E gene was widely studied and described to be located on chromosome 19, closely linked to the Apo C-I/C-II gene complex [9]. The three major alleles, termed Epsilon-2, Epsilon-3 and Epsilon-4 have been reported [10].
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Although we showed that RBL H Sc cells took
2021-10-09
Although we showed that RBL-2H3 Sc98 Voreloxin Hydrochloride synthesis took up histamine from the microenvironment, it was unclear which transporter mediated its passage across the plasma membrane. Other biogenic amines have selective transporters that belong to the neurotransmitter sodium symporte
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To further investigate the molecular mechanisms that
2021-10-09
To further investigate the molecular mechanisms that underlie glycine's β-cell protective effects through its antioxidative activity in diabetes, we used a H2O2/high glucose-induced apoptosis cell model. Similar effects on ROS generation of high glucose and H2O2 support the in vivo results, suggesti
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Human GS is a multi subunit complex
2021-10-08
Human GS is a multi-subunit complex consisting of four components: presenilin 1 (PS1), presenilin enhancer 2 (PEN-2), anterior pharynx-defective 1A (APH-1A) and nicastrin (NCT) (Fig. 1a) [5,6]. PS1 comprise nine transmembrane helices (TM 1–9) and contains the catalytic aspartate residues in its TM6
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In the course of our ongoing attempts to photolabel alloster
2021-10-08
In the course of our ongoing attempts to photolabel allosteric binding sites of γ-aminobutyric KJ Pyr 9 type A (GABAA) receptors, we were met with the need for relatively large (near mg) quantities of recombinant protein. Rather than establishing a stable cell line we sought to optimise the process
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Next we conducted subgroup analyses with stratification
2021-10-08
Next, we conducted subgroup analyses with stratification along interaction variables, namely the PPARG SNP and fasting NEFA. The study population was thus stratified into high and low NEFA (along the median NEFA, 561 μmol/L), and PPARG minor allele (Ala) carriers. This stratification resulted in 4 s
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The investigation in vitro revealed that aldolase as well
2021-10-08
The investigation in vitro revealed that aldolase, as well as FBPase, has affinity to α-actinin, one of the structural protein of the Z-line (Rakus et al., 2003a, Mamczur et al., 2005). Therefore, the existence of in vivo heterologous complex, consisting of aldolase, FBPase and α-actinin has been po
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Sperm exocytosis or acrosome reaction AR is a
2021-10-08
Sperm exocytosis or acrosome reaction (AR) is a regulated secretion with special characteristics essential for fertilization. The AR relies on the same highly conserved molecules that drive intracellular membrane fusion and exocytosis in all other Heme Colorimetric Assay Kit (see [59] for a recent
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