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Erythropoiesis involves the proliferation and differentiatio
2021-09-13

Erythropoiesis involves the proliferation and differentiation of hematopoietic stem BI6727 synthesis to mature RBCs. This process is a tightly-regulated to adjust rates of RBC production based on physiologic need. Fas-mediated apoptosis is one mechanism that controls erythropoiesis. The role of Fas
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br Materials and methods br Results br Conclusions
2021-09-13

Materials and methods Results Conclusions In general, the drug design process is very laborious, expensive and prone to errors. Various computational methods including docking and algorithms based on molecular dynamics and/or quantum chemistry can help considerably at the early stage of str
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br Although earlier studies had reported conflicting results
2021-09-13

Although earlier studies had reported conflicting results regarding the role of Ca2+ in regulating SV endocytosis, more recent data suggest that Ca2+ influx facilitates SV endocytosis in hippocampal neurons, the calyx of Held, and in inner hair 29 8 (Dittman and Ryan, 2009, Hosoi et al., 2009, Mos
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There are several limitations in our
2021-09-11

There are several limitations in our study. First, only the naturally occurring resistance-associated mutations in patients coinfected with HIV/HCV NCT-503 1b were analyzed. The result was only applicable to HCV genotype 1b, but not the HCV genotype 1a patients. We did not analyze the effect of gen
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According to literature RASs V M T S
2021-09-11

According to literature, RASs V36M, T54S, Q80K and R155K are considered primary resistance mutations to different PIs. RASs V36M and R155K can reduce susceptibility to recently approved PIs simeprevir, paritaprevir and grazoprevir [18], [31], [32]. T54S is associated to resistance for first-wave tel
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br Materials and methods br Results br Discussion br Conclus
2021-09-11

Materials and methods Results Discussion Conclusion Pharmacophore modeling was applied to explore new probable Glo-I inhibitors. Ninety two pharmacophoric models were generated representing diverse types of interaction between co-crystallized ligands and corresponding binding site. The g
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br Materials and methods br Results br
2021-09-11

Materials and methods Results Discussion The GO system is an important mechanism for maintaining the integrity of genetic material in many eukaryotic organisms. This is demonstrated by the high conservation, across different evolutionary lineages, of the sequences of the proteins that compo
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br Discussion The GlyR is responsible for mediating much
2021-09-11

Discussion The GlyR is responsible for mediating much of the neuronal inhibition in the brainstem and spinal cord, although these receptors are also found in a number of higher brain regions (Baer et al., 2009, Jonsson et al., 2012, Jonsson et al., 2009, Lynch, 2004). A variety of structurally-di
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Because AM had limited efficacy on rodent GPR we
2021-09-11

Because (AM-3189) had limited efficacy on rodent GPR40, we used two rodent models expressing human GPR40 to demonstrate efficacy of (AM-3189). First, we used human islet transplanted nude mice. In this model, endogenous pancreatic β-cells were ablated using streptozotocin, and mice were rescued to
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The central region of Azalanstat can
2021-09-11

The central region of Azalanstat can be substituted with connecting alkyl chains of different nature and length. Interesting results were given by compounds with a four or five Isoniazid synthesis chain, incorporating heteroatoms, such as oxygen (Fig. 2, compound 4) or sulfur, and different functio
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Mice with GSTP knock out show increased risk of
2021-09-11

Mice with GSTP1 knock out show increased risk of skin cancer when exposed to carcinogens like polycyclic aromatic hydrocarbons [23]. Most of the genetic association studies have focused on GSTP1 c.313G > A variant which results in isoleucine to valine substitution at amino Leupeptin residue number
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Further SAR was explored with
2021-09-11

Further SAR was explored with the imidazole series to achieve better enzyme inhibition activity (). In comparison to published earlier, replacing the amide with sulfonamide and reverse sulfonamide maintained the GSNOR inhibitory activity. It is clear that exchanging the phenyl ring (, and ) by t
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br Pharmacology br Background to GPR function br The emergin
2021-09-11

Pharmacology Background to GPR35 function The emerging function of GPR35 in the nervous system Conclusions The role of GPR35 in the modulation of synaptic transmission, neurogenic and inflammatory pain, and potential signalling pathways involved in these processes are beginning to emerge
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br Materials and methods br Results br Discussion br
2021-09-11

Materials and methods Results Discussion Disclosures Author contributions Acknowledgements Introduction Diabetes mellitus is one of the fastest growing chronic diseases worldwide, with an estimated prevalence of 382 million patients, of which about 90% have type 2 diabetes melli
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br FXR Agonists Azepinol b indole hEC nM efficacy eff
2021-09-11

FXR Agonists Azepinol[4,5-b]indole 1 (hEC50=600nM, efficacy (eff)=100%) was identified as a FXR agonist lead from a high-throughput screening effort. Structure–activity relationship (SAR) studies around the azepine ring demonstrated that dialkyl substitution at C-1 led to a 30-fold improvement in
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