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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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The original Bee Synch methodology now
2021-09-11
The original Bee Synch methodology (now termed Bee Synch I) utilizes a 5-day CIDR, GnRH (GnRH-1) and PGF on day 0, double dose of PGF on day 5, and FTAI with GnRH (GnRH-2) at 66 h after CIDR removal. Cruppe et al. (2014) reported that the inclusion of GnRH on day 0 does not contribute appreciably to
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br GnRH receptor expression is altered
2021-09-11
GnRH receptor expression is altered within GnRH neuronal cells Kisspeptin failed to stimulate GnRH expression in our line of GT1-7 cells. Instead, we have found that kisspeptin increased the expression of the GnRH receptor in these CP 31398 dihydrochloride synthesis (Sukhbaatar et al., 2013). Ba
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The role for noggin in telencephalic development
2021-09-11
The role for noggin in telencephalic development and also adult neural stem cell expansion and differentiation has been debated, and noggin has been suggested to exert diverse effects in these events (Bachiller et al., 2000, Bonaguidi et al., 2008, Colak et al., 2008; de Chevigny et al., 2008, Li et
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