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br In some but not all human vessels
2020-11-09

In some, but not all, human vessels, a small population of ETB (usually RG7112 synthesis with atherosclerotic lesions did not show any increase. In agreement, in experimental medicine studies in both heart failure patients and volunteer controls, selective ETA antagonism (BQ123) caused the expect
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In conclusion we have identified Ednra as a
2020-11-09

In conclusion, we have identified Ednra as a downstream direct target of Hoxa9 and Meis1. Upregulation of Ednra has a role in the progression of Hoxa9+Meis1-induced leukemia and targeting Ednra together with other chemotherapies may have therapeutic benefits for leukemia [30]. Ednra inhibitors in th
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br Roles of DDR in epithelial
2020-11-09

Roles of DDR1 in epithelial cell differentiation Roles of DDR1 in cell migration, and invasion Dichotomous functions of DDR1 in disease progression Conclusions and perspectives The switch in gsk3 inhibitor from DDR1 to DDR2 during EMT is another important issue. The DDRs may exert distin
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br Mechanisms of acquired resistance to
2020-11-09

Mechanisms of acquired resistance to 1st and 2nd generation EGFR inhibitors After treatment with first or second generation EGFR TKIs, virtually all patients after approximately 12 months develop acquired resistance (AR). Different mechanisms of AR to EGFR TKIs have been reported to date and may
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br RING dimerization RING type
2020-11-09

RING dimerization RING-type domains are found in many different structural contexts. While many exist as single-chain MG-262 (Fig. 3A), a notable feature of RING-type E3s is their tendency to form homodimers and heterodimers (Fig. 3C–F). Homodimeric RING-type E3s include cIAP, RNF4, BIRC7 (shown
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Together the protein engineering approaches
2020-11-09

Together, the protein engineering approaches employed by Teyra et al., (2019) demonstrate the effectiveness of affinity maturation for improving the affinity of UbVs, but this comes at a cost in terms of specificity. Indeed, the most effective UbV was the dimeric construct generated from UbVs isolat
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br Results br Discussion Many assays in
2020-11-06

Results Discussion Many assays in the literature for DBH require the use of catalase to protect the active site from hydrogen peroxide, which is a by-product in the initial step of the reaction. For the non-immobilized enzyme there was a visible increase in the rate with increasing amounts of
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An important question is to
2020-11-06

An important question is to what extent any differences in radioligand characteristics may have contributed to discrepancies between studies. Two studies on schizophrenia addressed this question directly by using [11C]SCH 23390 and [11C]NCC 112 in the same individuals, not finding any differences be
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DGK deficiency caused a significant increase in the
2020-11-06

DGKδ deficiency caused a significant increase in the SERT protein level, but its mRNA level was not affected (Fig. 1). These results suggest that SERT protein stability is directly reduced by interaction with the DGKδ protein. In contrast, DGKδ deficiency regulated both TPH-2 and MAO-A protein and m
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Keeping the cofactor content oligomeric state subcellular lo
2020-11-06

Keeping the cofactor content, oligomeric state, subcellular localization, and membrane association in view, DHODH has been broadly divided into two classes, class 1 and class 2 [26], [27]. In many species it is present to either cytoplasm (Class 1) or to the inner mitochondrial membrane (or plasma m
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br Acknowledgements br Introduction Chemokines are a
2020-11-06

Acknowledgements Introduction Chemokines are a superfamily of chemotactic cytokines that play important roles in regulating cell migration and activation under inflammatory conditions (Nomiyama et al., 2008; Peatman and Liu, 2007; Zlotnik and Yoshie, 2000), such as angiogenesis (Arenberg et al
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Compound was generated using a literature procedure and requ
2020-11-06

Compound was generated using a literature procedure and required two-step Dess–Martin-periodinane/Pinnick oxidation prior to the methylation of the sulfonamide. Compound () was obtained from the Suzuki coupling of the methyl ester intermediate (en route to Pyridostatin ). Hydrolysis of all methy
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Acidic substituents showed moderate biochemical activity but
2020-11-06

Acidic substituents () showed moderate biochemical activity, but these compounds showed reduced cellular potency. Additional compounds bearing a carboxylic cotransport were also prepared and tested (data not shown). All of acidic compounds showed low cellular potency regardless of their biochemical
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PGE exerts its functions by binding to different
2020-11-06

PGE2 exerts its functions by binding to different receptors. Four different subtypes of PGE2 receptors are found in mammals and are designated as EP1-4. These are G-protein coupled receptors that belong to a family of seven rhodopsin-like transmembrane spanning receptors. They are structurally diffe
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Introduction PGE is a major mediator present at sites
2020-11-06

Introduction PGE2 is a major mediator present at sites of inflammation [1]. It is well established that PGE2 contributes to the localized and systemic symptoms of inflammation. A key study by Portanova et al. [2] demonstrated that anti-PGE2 Probenecid were able to reverse the swelling and pain in
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