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3965 Most human diseases e g cancer diabetes and neurodegene
2023-09-21
Most human diseases (e.g., cancer, diabetes, and neurodegenerative diseases) are complex and multifactorial. Several investigations in the literature focused on new multi-target drug development, which implies active pharmacophores incorporation in one scaffold (Meunier, 2008, Lazar et al., 2004, Te
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In Pham et al employed the microsphere based technology to
2023-09-21
In 2014, Pham et al. [22] employed the microsphere-based technology to create a Luminex probe-based assay for the rapid identification of single nucleotide polymorphisms that are known to confer resistance to one or more echinocandins in C. glabrata. The targets for the FKS probes were generated usi
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In addition unconventional mechanisms of internalization can
2023-09-21
In addition, unconventional mechanisms of internalization cannot be ignored. It is generally believed that the conventional homologous internalization of a GPCR depends on the activation of G proteins, since GRK activation requires the pre-activation of G proteins (Fig. 2). Feng et al. demonstrated
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br Introduction Sustained over activation of
2023-09-21
Introduction Sustained over-activation of neurohormonal systems is a hallmark in the pathophysiology of cardiac dysfunction following myocardial infarction (MI) and heart failure (HF). Inhibitors of the renin-angiotensin Creatinine synthesis system (RAAS) constitute cornerstones of pharmacotherap
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Gratifyingly compound also demonstrated improved physicochem
2023-09-20
Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and
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Sphingolipids such as ceramides and glucosylceramides are an
2023-09-20
Sphingolipids, such as ceramides and glucosylceramides, are an important class of bioactive lipids. The levels of these lipids change as a function of adipose tissue mass and functionality, and are partially driven by cellular availability of palmitoyl-CoA. Aberrant accumulation of ceramide, glucosy
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Through activation of the CD GOPC pathway attenuated vaccina
2023-09-20
Through activation of the CD46–GOPC pathway, attenuated/vaccinal MeVs rapidly induce a transient phase of autophagy which then diminishes with no signs of negative regulation and precedes a second autophagy phase related to viral protein synthesis [115]. In sharp contrast, virulent MeVs do not inter
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Based on currently available knowledge autophagy supports ad
2023-09-20
Based on currently available knowledge, autophagy supports adipocytes development and differentiation. In animals with specific skeletal muscle WZ811 of Atg7, reduced adipogenesis was shown. In rodents, autophagy was decreased in adipose tissue of animals fed with high-fat diet (HFD). In contrast,
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Ryoichi et al modified potent clinical candidate VX
2023-09-20
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 Material and methods br Results br Discussion
2023-09-20
Material and methods Results Discussion Although we were not able to detect 12/15-LOX mRNA in the lungs of 12/15-LOX knockout mice substantial amounts of 15-HETE could be detected in BALF. In fact, significant synthesis of 15-HETE in 12/15-LOX mice have been already reported [17]. The redun
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Cetrorelix In conclusion our data highlight that variable an
2023-09-20
In conclusion, our data highlight that variable anti-oxidative Cetrorelix could be released through peptic hydrolysis of CMP fractions. Although casein hydrolysates produced a larger number of peptides (Table 1) with variable antioxidant capacities, all the peptides from whey hydrolysate exhibited
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In an effort to increase antioxidant properties of
2023-09-20
In an effort to increase antioxidant properties of peptides from WP, Le Maux et al. (2016) altered the hydrolysis conditions (pH, enzyme type, reaction time, and temperature). Hydrolysis of WP (81% protein) test samples with papain (EC 3.4.22.2) at a constant pH of 7.0 gave significantly higher ORAC
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Second the choice of the PAABD is critical for
2023-09-20
Second, the choice of the PAABD is critical for an efficient and sensitive biosensor. The sequence of the PAABD should present high affinity and efficient recognition of the phosphorylated substrate, as opposed to poor affinity for the unphosphorylated substrate, and should display a fully reversibl
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br Small molecule homoisoflavonoid in
2023-09-20
Small molecule homoisoflavonoid in combination with anti-VEGF therapy Basavarajappa et al. [11] reported a new synthetic homoisoflavonoid compound, SH-11037 by modifying the structure of naturally occurring homoisoflavonoid cremastranone. SH-11037 exhibited promising inhibition of human retinal m
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Long term blood pressure regulation is linked to
2023-09-19
Long term blood pressure regulation is linked to renal function through the mechanisms of pressure natriuresis (Evans et al., 2005), which has been shown to be modulated by the RAS (Hall et al., 1999). Key components of the RAS are expressed throughout the kidney, and are implicated in renal excreto
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