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Analysis of Table shows that compound b in
2020-10-17

Analysis of Table 1 shows that compound 7b, in which the biphenyl scaffold does not bear any substituent, displays its inhibitory potency in the micromolar range (IC50 = 11 μM). If the amide bridge is moved from position 1 to 3 of the biphenyl system, product 7c is yielded, whose potency is about 4
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Extracellular uridine can be transported across
2020-10-17

Extracellular uridine can be transported across the cell membrane to enter the nucleotide salvage pathway. A colon cancer cell line supplemented with uridine was capable of growing normally in the presence of 1 μM brequinar (Peters et al., 1992). The supplemented uridine may be transported into the
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br Conclusion New series of
2020-10-17

Conclusion New series of thiazolo[4,5-d]pyridazine and imidazo[2′,1′:2,3]thiazolo[4,5-d]pyridazine were designed and synthesized using thiazole as scaffold based on its previously observed activity as DHFR inhibitor. Compounds 13 and 43 (Fig. 9) proved to be the most active DHFR inhibitors with I
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Introduction DHFR is an important enzyme in both mammals and
2020-10-17

Introduction DHFR is an important enzyme in both mammals and microorganism including Mycobacterium tuberculosis (Mtb). It catalyzes folic glatiramer acetate conversion to dihydro and tetrahydro folic acid which is a crucial step in folate pathway [1]. Inhibition of folate pathway leads to interrupt
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We had earlier reported that collagen
2020-10-17

We had earlier reported that collagen fibers with intact native banded structure were occasionally observed in the kinase-deficient, membrane-anchored DDR2 ECD (DDR2/-KD) samples; however, in our DDR1/ECD and DDR2/ECD samples, observation of native banded structure of collagen was far more infrequen
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dabigatran etexilate synthesis Several of the keloid like le
2020-10-17

Several of the keloid-like lesions seen in these individuals were pigmented. It is of potential relevance that genetic variants in DDR1 [MIM: 600408] have been associated with vitiligo, and DDR1 activation is involved when dabigatran etexilate synthesis are attached to collagen-IV fibers. Because D
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DNA promoter hypermethylation is an important mechanism in e
2020-10-17

DNA promoter hypermethylation is an important mechanism in epigenetic modulation of gene expression.[16], [17], [18] When the promoter CpG island of a gene is hypermethylated, the transcription and its associated function of the gene will be subsequently altered.[19], [20], [21] In human cancers, we
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The isolation of a proteinaceous putative inhibitor of cyste
2020-10-17

The isolation of a proteinaceous putative inhibitor of cysteine proteases from the extracts of Y. enterocolitica and E. coli was performed by affinity chromatography on immobilized and inactivated papain (Fig. 7A). Instead of the column variant of this technique (Tsushima et al., 1992), we used a ba
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br Conclusion br Acknowledgements This work
2020-10-17

Conclusion Acknowledgements This work is supported by the National Natural Science Foundation of China (41806151, 41706144), the National Natural Science Foundation of China (31330082). We would like to thanks the support of young science and technology talents training fund of South China Agr
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A neurotoxic syndrome called Intermediate syndrome has
2020-10-16

A neurotoxic syndrome called “Intermediate syndrome” has been described after acute cholinergic crisis, which has been interpreted as the result of pre- and postsynaptic disruptions of neuromuscular transmission (Senanayake and Karalliedde, 1987). Other toxic effects with unknown molecular targets h
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br The estrogen receptors History
2020-10-16

The estrogen receptors: History and discovery In 1958, Elwood Jensen discovered the estrogen receptor, the first receptor ever encountered for any hormone, by showing that reproductive female tissues were able to uptake estrogen from the circulation by binding to proteins. He later demonstrated t
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Damage of PE HD due to both mechanisms is
2020-10-16

Damage of PE-HD due to both mechanisms is usually considered to emerge from a local stress concentration in the material, leading to the initiation of a crack, which subsequently propagates further through the material, and finally leads to macroscopic failure. In this process, crack growth occurs o
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Angiomatoid fibrous histiocytoma originally described as ang
2020-10-16

Angiomatoid fibrous histiocytoma (originally described as angiomatoid malignant fibrous histiocytoma) is a soft tissue tumor of intermediate biologic potential. AFH typically arises within extremity deep dermis and subcutis in children and young adults,157, 158, 159 but can arise in older adults and
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Given the potency enhancing effect of the butyl group this
2020-10-16

Given the potency enhancing effect of the 4--butyl group, this substitution was incorporated into the Eastern portion of the molecule for further SAR investigations (). Removal of the phenol group (SR19822) or moving it from the -position to the -position (SR19552) or led to significant loss of acti
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br Results br Discussion We first tested for
2020-10-16

Results Discussion We first tested for any adverse effect of ATR on learning and memory with a MWM test, which is used to assess hippocampal spatial learning and memory abilities in rodents (Vorhees and Williams, 2006). In the place navigation test, the escape latency – or time spent locating
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