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Materials and methods Standard curve for http www apexbt
2022-01-03
Materials and methods Standard curve for methylglyoxal. Different concentrations (10, 25, 50, and 100μM) of pure MG (Sigma) were derivatized with 1,2-diaminobenzene and the absorbance of the resulting derivative was read by Cary 50 Bio UV-Visible spectrophotometer (Varian). One milliliter of total
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Several studies have found decreased astroglial and neuronal
2022-01-03
Several studies have found decreased astroglial and neuronal cell numbers and Arecaidine but-2-ynyl ester tosylate damage after OP exposure. Neuronal loss and brain lesions increase proportionally to the severity and duration of OP-induced seizures (Albuquerque et al., 2006, Carpentier et al., 2000
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Gap junction channels exhibit different types of
2022-01-03
Gap junction channels exhibit different types of gating properties. One alternative mechanism that should be mentioned is loop gating in which the extracellular loop of connexin assumes a configuration to form a narrow pathway for closure of unopposed hemichannels [53] and docked junction channels [
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Our own search towards aryl imidazole
2022-01-03
Our own search towards aryl-imidazole derived GSMs led to the discovery of the benzimidazole derivative (). It is one of the most potent GSMs to date, suffering however from sub-optimal drug-like properties. More recently, we have described the design and synthesis of bicyclic triazolo-derivatives,
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In order to ensure that the decrease
2022-01-03
In order to ensure that the decrease in ethanol and morphine intake was not due to a sedative effect of SNAP 37889, locomotor activity and motor learning were assessed through behavioural paradigms. Using the locomotor test, SNAP 37889 did not alter any parameters of locomotion; this lack of sedatio
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Despite the two models for the HIV
2022-01-03
Despite the two models for the HIV-1 IN-aptamer complexes appeared to be comparable, disintegration assays revealed that 93-del inhibited C– or N-terminally truncated enzyme at the same extent, [18] whereas, T30695 required N-terminal domain (NTD) of the enzyme to exert its integrase inhibitory acti
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The finding of histamine action on ASICs also raises
2022-01-03
The finding of histamine action on ASICs also raises the question about possible action of other histamine receptor ligands. In the present work we selected several compounds and performed electrophysiological testing of their action on recombinant homomeric ASIC1a and ASIC2a. Nα-methylhistamine is
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br Acknowledgments This study was financially
2022-01-03
Acknowledgments This study was financially supported by National Science Center Poland grant No DEC-2011/02/A/NZ4/00031 (KKK), Jagiellonian University Medical College (Poland) grants: K/ZDS/007130 (SM) and K/ZDS/007131 (SM), COST Action CA15135 (DŁ, HS, KKK) and DFG INST 208/664-1 FUGG (HS). Than
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Kinases belonging to the Thousand and one
2022-01-03
Kinases belonging to the Thousand and one (Tao) family are conserved throughout evolution. Three Tao proteins are encoded in the human genome (TAO1, TAO2, and TAO3), while D. melanogaster possesses a single ancestral Tao kinase (Tao-1). Like Hpo and GckIII, Tao kinases belong to the Sterile 20-like
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br Materials and Methods A human
2022-01-03
Materials and Methods A431 (human skin SCC) and HT-297.T (human AK) cell lines were purchased from ATCC (Manassas, VA) and were maintained in DMEM supplemented with 10% fetal calf serum, 4 mM L-Gln, 1 mM sodium pyruvate, 100 U/mL penicillin, and 1 μg/mL streptomycin. Human HK1 and HK2 plasmids we
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In order to determine which
2021-12-31
In order to determine which complex of the electron transport chain is targeted by Authipyrin, a semi-intact assay was performed. The substrates of each complex were added separately in combination with Authipyrin or the respective control inhibitor. Seahorse XF plasma membrane permeabilizer (PMP) w
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br Introduction Soluble guanylyl cyclase GC maintains vascul
2021-12-31
Introduction Soluble guanylyl cyclase (GC-1) maintains vascular function through the NO/GC-1/cGMP pathway [1,2] by catalyzing the conversion of GTP into cGMP (Fig. 1). The GC-1 heme prosthetic group binds NO with picomolar affinity, resulting in a 100- to 200-fold increase in catalytic activity.
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Notably Cu labeled dimeric exendin subunit which
2021-12-31
Notably, 64Cu-labeled dimeric exendin-4 subunit, which was designated as 64Cu-Mal2Sar-(exendin-4)2, showed higher tumor uptake than that of the monomeric exendin-4 subunit [245]. Besides the most commonly-used GLP-1R agonists exendin-3 and -4 and their derivatives, exendin (9-39) exhibits strong bin
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Firstly the impact on activity
2021-12-31
Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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alkaline phosphatase inhibitor The mD gene obtained from Dr
2021-12-31
The mD1.2 gene obtained from Dr. Dimiter S. Dimitrov was inserted into a pComb3X vector. The transcription and translation of pComb3X plasmid in cells is inhibited by rifampicin, which binds to bacterial DNA-dependent RNA polymerase. However, in the strain BL21 (DE3) expression system, there is over
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