• Here we report discovery of highly selective pan Aurora

  2024-10-08

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of nutlin 3 bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the interaction. To ide

• There are however concerns of potential side effects

  2024-10-08

  

  There are however, concerns of potential side-effects that should also be taken into account. Even though some studies pointed towards a potentially greater radiosensitising effect in p53-deficient tumours, ATM inhibition radiosensitises trpv4 in general, which raises the concern of normal tissue t

• Apelin is a bioactive peptide and endogenous ligand for

  2024-10-08

  

  Apelin is a bioactive peptide and endogenous ligand for the APJ receptor (APLNR), a member of the G protein coupled receptor family that shares a similar sequence as the angiotensin type-1 receptor (AT1) [5]. Early studies demonstrated that the apelin/APLNR receptor axis plays a significant role in

• Introduction Enzymatic browning degrades quality

  2024-10-08

  

  Introduction Enzymatic browning degrades quality, safety, and nutritional values of various fruits or vegetable products. For example, the color of apple or potato is generally yellowish, representing freshness. However, they are extremely susceptible to enzymatic browning because of abundant polyp

• Experimentally the ECD spectrum of showed three ECD bands po

  2024-10-08

  

  Experimentally, the ECD spectrum of 1 showed three ECD bands: positive ones at 260 and 200nm, and a negative one at 230nm (Fig. 4). Meanwhile, there is only one broad positive ECD band starting from 300nm in the ECD spectrum of 2. ECD spectra of 1 and its derivatives attracted great interest because

• The aldehyde reductase AKR A and aldose

  2024-10-03

  

  The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.

• AKT activity is also self limiting through its substrate GSK

  2024-10-03

  

  AKT activity is also self-limiting through its substrate GSK3β; the kinase activity of which is negatively regulated by AKT phosphorylation (Fig. 3; Li, Liu, & Gao, 2009). GSK3β activation results in phosphorylation and subsequent ubiquitin mediated degradation of PHLPP (Li et al., 2009). AKT activa

• AhR was proven to participate in

  2024-10-03

  

  AhR was proven to participate in carcinogenesis. Its high expression was demonstrated in a variety of tumors, i.e. pancreatic, prostate, urinary tract, lung and papillary thyroid carcinoma (Safe et al., 2013, Mian et al., 2014). However, cell line studies showed variable AhR levels/responses. AhR kn

• Introduction Diabetic nephropathy is a rapidly growing cause

  2024-10-03

  

  Introduction Diabetic nephropathy is a rapidly growing cause of end-stage renal disease [1]. Glomerular, tubular and vascular toxicity resulting from hyperglycemia (glucotoxicity) have been evaluated extensively at the molecular level as contributing factors for diabetic nephropathy [[1], [2], [3]]

• Regarding A Rs and A ARs basal

  2024-10-03

  

  Regarding A1Rs and A2ARs, basal conditions generate a low tone of endogenous adenosine and cause A1R activation, in contrast to situations of increased adenosine where A2AR activation becomes dominant. When adenosine concentrations rise, e.g. during hypoxia, also time appears likely important in reg

• Tacrine an aminoacridine derivative Fig

  2024-10-03

  

  Tacrine, an aminoacridine derivative (Fig. 1, A), was the first AChE inhibitor approved for treatment of AD [12], [13]. This compound was withdrawn from the market due to its hepatotoxicity [14]. In spite of tacrine's side effects, it is still an attractive lead compound for medicinal chemists due t

• Even within the context of

  2024-10-03

  

  Even within the context of evidence-based interventions for tobacco screening, the science is imperfect. For example, patients who screen positive for current smoking should receive cessation counseling and prescribed known effective nicotine replacement therapy based on the Public Health Services G

• Loss of virulence in ACL mutants may be

  2024-10-01

  

  Loss of virulence in ACL mutants may be caused by defect in vegetative growth and conidial germination, and reduced trichothecene production. However, supplement of potassium acetate restored the defects in germination rate and vegetative growth, but not virulence in wheat heads (Table 2, Fig. 2B),

• The uterine muscle also changes to meet

  2024-10-01

  

  The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind

• Animal fat appears to increase C perfringens counts

  2024-10-01

  

  Animal fat appears to increase C. perfringens counts compared with vegetable oil, so there may indeed be some advantage to vegetable diets at least in terms of fat sources (Knarreborg et al., 2002). Small grains such as wheat, rye, oats, and barley, with high levels of non-starch polysaccharides are

15645 records 80/1043 page Previous Next First page 上5页 7677787980 下5页 Last page