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MoAbs targeting the tumourigenic pathways such as
2021-06-07
MoAbs targeting the tumourigenic pathways, such as IGF-1R may theoretically have a dual working mechanism. On the one hand they block pathways having an anti-tumour working mechanism, and on the other hand they may also stimulate an immunological response inducing a reaction of the patients own immu
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In addition to providing substantial
2021-06-05
In addition to providing substantial insight into substrate recognition, structural studies have revealed important details about mechanisms of glycosylation and HCF-1 cleavage [28,30,33]. Activation of the nucleotide-sugar is accomplished through interactions of the β-phosphate with the N-terminus
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Apart from the ET system s role in regulating
2021-06-05
Apart from the ET system's role in regulating blood vessel tone, it is also involved in a variety of cellular processes that are relevant to DR. For example, the ET receptors influence the survival of retinal ganglion Danazol (McGrady et al., 2017; Tonari et al., 2012), development of the retinal va
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The significance of the difference
2021-06-05
The significance of the difference in the DDR2 binding specificity towards fibrillar and non-fibrillar collagens is not understood, but may imply differences in biological responses when chondrocytes bind to different collagens in the growth plate. Investigations by Labrador et al. (2001) have shown
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histone acetyltransferase br Acknowledgments We thank our co
2021-06-05
Acknowledgments We thank our colleagues who have contributed to our understanding of the histone acetyltransferase and the structure and function of APC/C, and apologize to those whose work we were unable to cite here. We thank J. Rajan Prabu for making the movies showing APC/C conformational ch
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FOX proteins constitute a large class of transcription facto
2021-06-05
FOX proteins constitute a large class of transcription factors with multiple functions, from development and organogenesis to regulation of metabolic and immune functions. The Fox transcription factor is characterized by a 100-amino-acid wing helix or forkhead DNA-binding domain. In addition, the FO
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The differences between ground and
2021-06-05
The differences between ground and transition state properties are exemplified by a comparison of our human–yeast results with those of a structural study of possible differences in ubiquitin-Uba-1 binding in yeast (known structure) with human (simulated in [12]). Their discussion focuses on Ubiquit
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Verapamil a calcium channel blocker used
2021-06-05
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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In studies directed toward the
2021-06-05
In studies directed toward the development of sequence-specific major-groove binding small Peramivir synthesis [11], we desired a non-intercalating molecular scaffold that could direct attached moieties into the major groove. As an initial step toward this goal, we wished to study the DNA binding m
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The possibility that a carboxyl group
2021-06-05
The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a
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The first example of a broadly acting antiviral drug
2021-06-05
The first example of a broadly-acting antiviral drug is ribavirin, a nucleoside analogue that was proposed to act directly at the level of the viral polymerase, although an indirect effect via inhibition of the host-cell IMP dehydrogenase and depletion of the GTP pool seems more plausible [9]. Anoth
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MTX and MTXPGs block the
2021-06-05
MTX and MTXPGs block the activity of the key enzyme DHFR (Fig. 1), which converts folates to their active forms – dihydrofolate (DHF) and tetrahydrofolate (THF). MTXPGs also potently inhibit thymidylate synthase (TS). Furthermore, during dTMP synthesis, TS utilizes the cofactor 5,10-methylene THF, w
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Studies on the external dehydrogenases of N crassa have
2021-06-05
Studies on the external dehydrogenases of N. crassa have shown that the NDE1 protein is a Ca2+-dependent external NADPH dehydrogenase, while NDE2 is characterized as a dehydrogenase oxidizing both cytosolic substrates (external NADH and/or NADPH) (Carneiro et al., 2004, Melo et al., 2001). All three
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Although PQQ has nutritional importance and pharmacological
2021-06-05
Although PQQ has nutritional importance and pharmacological effects in higher organisms, including humans [15], until recently, there was no clear evidence for the use of PQQ as a co-factor in a eukaryotic enzyme. This review presents a novel eukaryotic PQQ-dependent quinohemoprotein recently discov
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DNA promoter hypermethylation is an important mechanism in e
2021-06-05
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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