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Imatinib STI is a first line tyrosine
2019-10-15
Imatinib (STI-571) is a first-line tyrosine kinase inhibitor (TKI) targeted at breakpoint cluster region-Abelson kinase (ABL) for the treatment of chronic myeloid leukemia (CML) [26]. As a type II inhibitor, imatinib achieves significant selectivity by binding to an inactive DFG-out conformation (DF
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Introduction Collagen fibrillogenesis the assembly of collag
2019-10-15
Introduction Collagen fibrillogenesis, the assembly of collagen fibers, is a critical process in the development, maturation, and repair of mammalian tissue. Alterations in the structure and amount of deposited collagen fibers can greatly alter the integrity of the whole tissue. Even a single point
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rhein clinical CYP A and CYP D are
2019-10-15
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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The mRNA expression of asEP studied by RT PCR shows
2019-10-14
The mRNA expression of asEP4 studied by RT-PCR shows that EP4 is expressed in many different tissues in Atlantic salmon which is comparable to other species (Sugimoto and Narumiya, 2007) although some distinct differences are present. For example, in mice the expression of EP4 receptor was found to
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Eggs have been recognized as an important contributor of fun
2019-10-14
Eggs have been recognized as an important contributor of functional ingredients for humans [3]. Egg yolk is composed of various biologically active proteins. The water-soluble proteins of egg yolk have been examined for their functional effects on longitudinal bone growth during the growth period in
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The aniline R group was extensively
2019-10-14
The aniline R2 group was extensively explored and a large variety of substitution was tolerated at several positions on the aryl ring (). Notably, substitution at the 3-position often gave increased potency. Increasing lipophilic bulk at this position gave increasing potency within an ether series (
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In order to assess quantitatively
2019-10-14
In order to assess quantitatively the contribution of the ung, dug and dut (+)-Apogossypol to uracil-DNA accumulation in E. coli, we have developed a novel method for measuring uracil residues in DNA that is based on the approach of Kow and co-workers [33] for measuring AP-sites in DNA. The method,
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br CDK Inhibitors for the Treatment of inflammatory Diseases
2019-10-14
CDK Inhibitors for the Treatment of inflammatory Diseases Several CDKs have been implicated as regulators of inflammatory gene expression. It will thus be very important to determine the relative contributions of the various CDKs and their kinase function on a systematic basis. This work will be
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The binding pattern of was analysed by
2019-10-14
The binding pattern of 1 was analysed by flexible molecular docking. The SCH772984 inserted into the narrow ATP binding site of CK2 (Fig. 2). As shown the aliphatic chain of 1 was located at the edge of the pocket and established van der Waals interactions with the side chains residues of Ile95, Me
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The crystal structure of full length CHK is still
2019-10-14
The crystal structure of full-length CHK is still unsolved. However, the close homology between CHK and Csk suggests that these kinases share a similar structure. Therefore, the engagement of the CHK SH2–kinase linker with the αC-helix could control the activity of the CHK kinase domain. Sequence al
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This investigation est http www apexbt
2019-10-14
This investigation establishes that there is a genetic difference in the enolase loci that correlates with both vegetative growth and virulence phenotypes. DNA sequence analysis of enolase loci from seven P. larvae strains reveals a single SNP that alters the protein sequence at position 331 (Table
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br Abbreviations br Introduction br Collagen induced DDR act
2019-10-14
Abbreviations Introduction Collagen-induced DDR activation A key feature of DDRs is their ability to bind both fibrillar and non-fibrillar collagens (Shrivastava et al., 1997, Vogel et al., 1997). DDR1 and DDR2 recognize the GVMGVO (O, hydroxyproline) motif within fibrillar collagens I–III
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br Discussion The biochemical separation of exonuclease
2019-10-14
Discussion The biochemical separation of exonuclease activity from DNA-PK dependent endonuclease activity reported in this manuscript is consistent with genetic separation of Artemis enzymatic activity. Mutations in the protein which result in disruption of endonuclease activity have no effect on
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br Materials and methods br Results br Discussion ParI the
2019-10-14
Materials and methods Results Discussion ParI, the first C5-DNA-MTase from a psychrophilic bacterium to be characterized, displays DNA methylation activity in vivo and in vitro. Its biophysical characteristics are consistent with large regions of disorder including thermal unfolding transit
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Classical DHFR inhibitors such as methotrexate MTX bind tigh
2019-10-14
Classical DHFR inhibitors such as methotrexate (MTX) bind tightly to the enzyme and possess adequate clinical pharmacokinetics. MTX bind to the DHFR binding site through the formation of hydrogen bonds with Asn64, Lys68, Arg28, Arg70, Val115 and Ile7 amino Palosuran residues as well as hydrophobic
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