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Ryoichi et al modified potent clinical candidate VX with
2024-09-27
Ryoichi et al. modified potent clinical candidate VX-680 (6) with 3-cyano-6-(5-methyl-3-pyrazolamino)pyridine as Aurora kinase inhibitor. Substituted cyano pyridine derivative (7) inhibited proliferation of HCT-116 cells with an IC50 value of 115 nM. It showed tumor inhibition in mice model at a dos
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br Structure of V ATPase V ATPase is a
2024-09-27
Structure of V-ATPase V-ATPase is a highly conserved multi-subunit enzyme that uses energy from ATP hydrolysis to transport protons across membranes [2], [3], [4]. It consists of two major functional domains, V1 and V0 (Fig. 1). The former has eight different subunits (A, B, C, D, E, F, G, and H)
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In our approach using BRET and FRET there is a
2024-09-27
In our approach using BRET and FRET, there is a substantial increase in BRET and FRET signals between Giα2 or Giα3-YFP and CFP- Gγ2/Rluc-Gγ2 upon apelin-13 activation, indicating that Gαi2, Gαi3 and N-terminus of Gβ1γ2 subunits become closer without subunit dissociation. In contrast, both the FRET a
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Applications for protein switches are
2024-09-27
Applications for protein switches are numerous. In diagnostics, protein switches can detect analytes as components of inexpensive homogeneous assays that do not require specialized equipment or time-consuming incubation and washing steps characteristic of immunoassays [8]. Protein switches have also
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In our study we provide evidence for the existence of
2024-09-26
In our study we provide evidence for the existence of an endosome-lysosomal pathway for the proteolytic degradation of AR triggered by its interaction with the ESCRT-I component TSG101. The following findings of this study support this notion: (1) We showed that TS101 interacts with endogenous or ec
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In a recent series of
2024-09-26
In a recent series of studies from our laboratory, to characterize the contractile systems within the rat PreScission protease for GST tag removal wall, three conditions were identified that led to detrusor activity: spontaneous micro-contractions, electrical field stimulated (EFS) contractions and
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AdipoR and AdipoR have been reported to
2024-09-26
AdipoR1 and AdipoR2 have been reported to be present in almost all type of tissues and low NE 100 hydrochloride levels have been observed in white adipose tissue (Inukai et al., 2005). These receptors have been observed to become deregulated with the onset of obesity, resulting in a reduced level of
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br Conflicts of interest br Acknowledgments br Significance
2024-09-26
Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A
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Although our data show that agrin accelerates the innervatio
2024-09-26
Although our data show that agrin accelerates the innervation of engineered muscle tissue following implantation, there are still several issues that need to be considered. First, the use of primary muscle stem or progenitor STF 31 (satellite cells) instead of an immortalized muscle cell line (C2C12
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Several in vivo and in vitro studies have demonstrated chang
2024-09-25
Several in vivo and in vitro studies have demonstrated changes in bioactive lipid profiles under hyperglycemic conditions and have linked these changes with increased leukocyte adhesion and vascular dysfunction during diabetes. This input has originated partly from lipidomic studies that showed elev
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Aromatization of the pyrrole ring after anion capturing usin
2024-09-25
Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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br Introduction Hepatocellular carcinoma HCC is an aggressiv
2024-09-25
Introduction Hepatocellular carcinoma (HCC) is an aggressive and malignant cancer detected in clinical practice, as it is the third key reason of tumor-related deaths worldwide, with > 800, 000 mortalities every year (Torre et al., 2015). Current treatments for HCC are surgical therapy, liver tra
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br Materials and methods br
2024-09-25
Materials and methods Results Discussion Fluoride can readily penetrate cellular membranes and seriously damage the structure and physiological function of cells (Zhou et al., 2015). Several studies have shown that excessive fluoride can decrease the viability of cells and that the growth o
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Although the role of apelin and APJ receptor in cardiovascul
2024-09-25
Although the role of apelin and APJ receptor in cardiovascular functions has been well-elucidated, little is known for the effect of the central apelinergic system on gastrointestinal (GI) functions. In mice, it has been found previously that central exogenous apelin-13 decreased gastric emptying (G
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Coincident with APJ receptor several
2024-09-25
Coincident with APJ receptor, several cell types in the body can synthesize apelin protein. For example, the highest apelin concentrations in the body have been found in the rat central nervous system, pituitary gland, lungs, cardiac muscle, gastrointestinal tract and mammary glands, with lower valu
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