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br Conflicts of interest br
2021-05-06
Conflicts of interest Acknowledgements This study was funded by Kuwait University Research Administration (Project MI03/10). Introduction Epidemiological, experimental and biologic plausibility support a cardioprotective effect of estrogens in women [1]. Indeed, women are protected until t
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Three kinase inhibitors dasatinib type I imatinib type II an
2021-05-06
Three kinase inhibitors dasatinib (type I), imatinib (type II) and nilotinib (type II), identified initially as inhibitors of tyrosine kinase BCR-ABL, were found to target DDRs in a chemical proteomic profiling study (Bantscheff et al., 2007, Hantschel et al., 2008). These tyrosine kinase inhibitors
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br Discussion Several DPP inhibitors
2021-05-06
Discussion Several DPP-4 inhibitors are currently available for use in the treatment of type 2 diabetes mellitus. Due to the different chemical structures there are marked differences both in the binding kinetics on the target enzyme [10] and also different pathways of elimination [13] exist. In
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Dihydrofolate reductase DHFR is an excellent molecular targe
2021-05-06
Dihydrofolate reductase (DHFR) is an excellent molecular target for this study because it has been and is currently studied by using different molecular modeling techniques [6], [7], [8], [9]. Kerrigan et al. have reported an interesting review about recent progress in molecular dynamics simulations
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The data from drug screening in P berghei Fig
2021-05-06
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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Herein we explored by docking studies the effectiveness of
2021-05-06
Herein, we explored by docking studies the effectiveness of replacing the dimethyl substitution at C (6) of dihydrotriazine with a folded azaspiro-containing substituent, along with the introduction of differently substituted phenyl- and benzyl-rings or alkyl chains, linked at the position 1 of the
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Acanthopanax senticosus Rupr Maxim Harms a nontoxic herb bel
2021-05-06
Acanthopanax senticosus (Rupr. & Maxim.) Harms, a nontoxic herb belongs to the family of Araliaceae, which found in Northeast Asia. A. senticosus traditionally used as a tonic to treat rheumatism, diabetes, and hepatitis [7]. Previous phytochemical and biological investigations found its roots and s
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br Materials and methods br Results br Discussion Although
2021-05-05
Materials and methods Results Discussion Although no increase in DAPK activity was detected at early time points associated with neuronal apoptosis, it is possible that the spread of apoptosis through the Dexlansoprazole following HI is not synchronized enough to yield a large, consistent
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The X ray crystal structure
2021-05-05
The X-ray crystal structure of palbociclib bound to CDK6 without a Norethindrone mg (PDB ID: 5L2I) is very similar to that of the CDK6-cyclin V structure (Fig. 7B). However, the drug binds to the αCout conformation of monomeric CDK6 while it binds to the αCin conformation of the CDK6-cyclin V compl
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In contrast exposure of CRF a receptors to
2021-05-05
In contrast, exposure of CRF2(a) receptors to h/rCRF in living cells produced a strikingly weak translocation of βarrestin2 to the membrane. Specifically, we found a markedly lower magnitude and slower rate of βarrestin2 recruitment to CRF2(a) receptors in response to h/rCRF concentrations as high a
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It has long been known that native BChE is a
2021-05-05
It has long been known that native BChE is a major factor in the inactivation of cocaine, an ester-type drug of abuse [190]. But recently some researchers conceived the idea that BChE mutations could improve that function to a point that would favorably impact cocaine overdose. Rapid progress was ma
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HA activates its receptor channels to cause
2021-05-05
HA activates its receptor channels to cause an inward chloride flux in the insect nervous system (Hardie, 1989). Two genes encoding the subunits of these channels were first identified in D. melanogaster: one previously known as ort (also differently named as hclA, DM-HisCl-α1, hisCl2 and Dm HA-Cl I
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br TRIM TIF A RNF TRIM contains a RING
2021-05-05
TRIM24 (TIF1A, RNF82) TRIM24 contains a RING-both B-boxes-coiled coil conserved structure at the N-terminus with bromo and PHD domains prior to C-terminal end (Fig. 3). This transcriptional intermediary factor is well studied in the context of transcriptional activation of nuclear receptor via ac
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In conclusion our data demonstrated that montelukast and
2021-05-05
In conclusion, our data demonstrated that montelukast and pranlukast non-competitively blocked P2Y signaling in several cell systems, but in a relatively nonsubtype-specific manner. The functional antagonism was especially evident at heterologously expressed P2Y1 and P2Y6 receptors, at which IC50 va
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br Experimental section br Results br Discussion In our
2021-05-05
Experimental section Results Discussion In our previous work (Rashidi et al., 2018) we isolated a novel glucarpidase whose raised Canagliflozin did not cross-react with the one in clinical use. In principle, therefore, it would be possible to delay the production of antibodies in a patient
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