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muscarinic receptor antagonists In the FARM motifs of
2022-06-15

In the FARM motifs of GGPPSs, hydrophobic muscarinic receptor antagonists are replaced by aliphatic amino acids, which are more flexible residues and allow the entrance of longer substrates into the pocket (Wang and Ohnuma, 2000). It has been reported that the lepidopteran Manduca sexta CA possesse
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Integrase inhibitors have been licensed for use
2022-06-15

Integrase inhibitors have been licensed for use in the UK since 2008. BHIVA now recommend starting all treatment naïve patients on a regimen containing two NRTIs, plus one of the following: a ritonavir boosted PI, an NNRTI, or an integrase inhibitor. They make further recommendations for patients wi
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In order to find better LODs LOQs and peak shape
2022-06-15

In order to find better LODs, LOQs and peak shape researchers used different derivatization agents along with dansyl chloride. However, these procedures required longtime for sample preparation, low recovery, the chance of contamination; products instability and some reagents were unable to derivati
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Apoptosis is one of critical toxic mechanisms of benzene met
2022-06-15

Apoptosis is one of critical toxic mechanisms of benzene metabolites. In this work, overexpression of HIF-1a could significantly reduce the increase in cell apoptosis caused by 40 μM BQ. At the meanwhile, anti-apoptotic protein Bcl-2 level was significantly elevated in HIF-1a overexpression cells th
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Importantly recent in vivo results demonstrated
2022-06-15

Importantly, recent in vivo results demonstrated that combining an HDACi and a IKK inhibitor significantly reduced ovarian tumor growth compared with either inhibitor alone [26]. The slowest tumor growth in the HDACi/IKK inhibition combination group was associated with the lowest CXCL8 tumor and pla
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br Methods br Results br Discussion Peptide therapeutics rep
2022-06-15

Methods Results Discussion Peptide therapeutics represents a unique class of biopharmaceuticals that continues to evolve in drug discovery and development. We and others have been particularly interested in bioengineering innovative pGC-A and/or pGC-B peptide activators. This has been succe
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An interesting question is why RhoF has
2022-06-15

An interesting question is why RhoF has such the slow rate of GDP dissociation. The amino 2 deoxyglucose sale mutations in a presumable GDP-binding site of RhoF had only moderate effects on the GDP dissociation (Fig. 3C), which suggests a mechanism involving the global amino acid sequence of RhoF,
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PRT 4165 GSTP catalyzed reduction of Prdx enhances its perox
2022-06-15

GSTP1-1 catalyzed reduction of Prdx6 enhances its peroxidase activity. Using standard NADPH/GR/GSH-coupled assays we used cell lysates from the transiently transfected PRT 4165 to measure the influence of GSTP1 allelic variation on peroxidase activity. Specificity for detection of Prdx6 activity wa
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Several studies have found that GPR possesses a distinct pha
2022-06-14

Several studies have found that GPR55 possesses a distinct pharmacology from that of CB1 and CB2, and that only certain cannabinoids act at this receptor. In transfected GSK2801 expressing hGPR55, out of more than 20 synthetic and endogenous cannabinoids evaluated, only 2 compounds, SR141716A (Rimon
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As part of our discovery efforts searching for
2022-06-14

As part of our discovery efforts searching for small molecule GPR119 agonists, we analyzed active pharmacophores of known agonists from the literature, and found that -methylsulfonylphenyl and substituted 4-hydroxyl piperidine are common fragments. In our initial efforts, we linked these two fragmen
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br Conflicts of interest br Introduction Antiretroviral
2022-06-14

Conflicts of interest Introduction Antiretroviral therapy (ART) is effective in reducing mortality (Detels et al., 1998), and preventing mother-to-child transmission (MTCT) (CDC, 1994, Connor et al., 1994) and sexual transmission of HIV (Cohen et al., 2011). However, the optimal time to start
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Extending the issue of the species differences the
2022-06-14

Extending the issue of the species differences, the role of neuroestradiol in the preovulatory GnRH/LH surge might be specific to primates or species with a luteal phase. For example, animals with a true luteal phase, such as monkeys and sheep, exhibit a long preovulatory GnRH surge, lasting well af
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The DNA cleavage activity assay in the present
2022-06-14

The DNA cleavage activity assay in the present study also demonstrated the DNA glycosylase activities of SMUG1, NEIL1, TDG, and NTHL1 for 5OHU paired with A. While our findings on the activities of SMUG1 and NEIL1 were consistent with the results reported from previous studies [25], [50], the activi
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honokiol In contrast to UDG SMUG exhibits
2022-06-14

In contrast to UDG, SMUG1 exhibits dramatically lower product yield in its excision of U, and this is not dependent on sequence context. Though we cannot rule out that a small amount of the product is derived from a duplex contaminant, our extensive purification techniques limit the amount of contam
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First class II fusion proteins
2022-06-14

First, class II fusion proteins are known to transition from a (homo- or hetero-) pre-fusion dimer to a post-fusion trimer [57], [58], [59], [60], [61], [62] through a monomeric intermediate [63], [64], and a crystalline structure of a monomer of Rift Valley fever virus (a phlebovirus, member of the
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