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Prenylation may turn a flavonoid from an agonist to
2021-05-22
Prenylation may turn a flavonoid from an agonist to an antagonist and improve the selectivity to both ERs depending on the position of the substitution. C-8 prenylation appears to promote antagonism to a larger extent than C-6 in ERα due to steric hindrance against generation of agonistic conformati
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Enalapril Maleate It is well known that acrolein
2021-05-22
It is well known that acrolein, a metabolite of cyclophosphamide, is responsible for the cyclophosphamide-induced cystitis, and that acrolein is capable of activating TRPA1 channels expressed in the capsaicin-sensitive primary afferents [2], [11]. In this context, it is likely that the early phase o
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The most significant finding was the inhibition of
2021-05-22
The most significant finding was the inhibition of EROD and BFCOD activity by CLO. Inhibition of EROD and BFCOD were reversible, as pre-incubation did not enhance CLO inhibitory potency, and no reductions in IC50 values were observed. We further characterized the kinetic pattern of inhibition using
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Further indirect evidence supporting an
2021-05-22
Further indirect evidence supporting an important role of DPP-4 in the modulating the actions of both incretins comes from the observations that analogues of GLP-1 and GIP, modified to be resistant to DPP-4 cleavage, were subsequently shown to have greater metabolic stability in vivo which was assoc
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br Conclusion The role of DNA PK target
2021-05-22
Conclusion The role of DNA-PK target in DNA DSB repair renders this Thymidine kinase of great medicinal interest in cancer chemotherapy especially the cancer types of linked to DNA defects. Due to the absence of 3D DNA-PK target structure, different ligand-based methods were applied for design o
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br Introduction Identification and correct storage
2021-05-22
Introduction Identification and correct storage of seminal stains are crucial for the investigation of sexual assault cases. Actually, undetected ‘cold’ cases involving sexual assault can be solved decades after investigations analysing DNA from stored evidences [1]. Recently, STR analysis and th
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Experiments on the rat model of E coli pyelonephritis perfor
2021-05-22
Experiments on the rat model of E. coli pyelonephritis, performed to investigate the relationship between the acute inflammatory processes and the permanent kidney damage (Brooks et al., 1974), have demonstrated a positive correlation between the degree of free radical-mediated renal injury and the
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br Conclusion In vivo pharmacokinetic studies showed that da
2021-05-22
Conclusion In vivo pharmacokinetic studies showed that dasatinib monohydrate pretreatment significantly decreased the blood level of CsA in rats, which was most probably due to the induction of CYP3A2 isoenzymes. The nilotinib pre-treatment had no significant effects on cyclosporine pharmacokinet
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br Materials and methods br Results br Discussion CDK has
2021-05-22
Materials and methods Results Discussion CDK4 has been identified recently as a potential therapeutic target in human breast cancer, liposarcoma, melanoma, and glioblastoma [[37], [38], [39]]. Due to the importance of CDK4 activity in cancer cells, CDK4 inhibitors have emerged as promising
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One strategy which is different from
2021-05-22
One strategy which is different from the above is to isolate a similar enzyme to the one under study which will not be recognized by the antibody of the original protein. This approach will lead to prolonging an enzyme’s activity. For example, a novel variant of Carboxypeptidase G2 (CPG2), which has
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Further studies are needed as continuation
2021-05-22
Further studies are needed as continuation of this work to explore the effects of type and position of substituents of pyridazinone ring on anti-inflammatory activity profile. Taking into consideration that the phenyl moiety at position 2 wasn't a favorable substituent, even certain studies may be r
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br Criteria for ER targeted fluorescent probes br
2021-05-21
Criteria for ER-targeted fluorescent probes Survey of fluorescent probes Proposed approach to high affinity fluorescent steroidal ER probes Our proposed approach to the development of a new generation of fluorescent estrogen receptor imaging agents employs many of the elements present in th
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Just as Dorin et al
2021-05-21
Just as Dorin et al. [2] and Nguyen et al. [3] write in regard to their models, our static model can be used to estimate the affinities of Oleandrin to albumin and CBG. Dorin et al. [2] estimates the K, but not K, since they find that their model is not particular sensitive towards changes in K. Our
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br Material and methods br Results br Discussion The
2021-05-21
Material and methods Results Discussion The results show for the first time that DDRs may be involved in the pathogenic mechanisms of neurodegenerative diseases. We found that DDR1 and DDR2 levels are up-regulated in post-mortem AD and PD brains, suggesting that these receptors play a role
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Breast cancer is the most common
2021-05-21
Breast cancer is the most common neoplasm in women, with approximately 231,840 new cases of invasive breast cancer, 60,290 additional cases of in situ breast cancer and 40,290 deaths occurring in 2015 in the United States. Meanwhile, about 2350 men will be diagnosed with breast cancer, and 440 men w
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