• Determination of relative potency EC by dose response

  2021-07-14

  

  Determination of relative potency (EC50) by dose response assays in vitro is subject to the same sources of variability as determination of affinity, since the EC50 and Hill slope of the dose response curve are highly dependent on the binding of ligand to a competing receptor that may be present, an

• The glycolytic pathway is a catabolic route

  2021-07-14

  

  The glycolytic pathway is a catabolic route that ends with the synthesis of pyruvate (Pyr). In Arabidopsis embryos, the conversion of phosphoenolpyruvate (PEP) to Pyr, catalyzed by pyruvate kinase (PK), is mainly located in the plastids [10], [11]. The preceding reaction is catalyzed by enolase (ENO

• Therefore HNE is an attractive therapeutic

  2021-07-14

  

  Therefore, HNE is an attractive therapeutic target and the design of new HNE inhibitors is a demanding field that has been extensively investigated in order to provide inhibitors with new molecular architectures, including the potent oxo-β-lactam class [14]. In the present work, a coumarin-based oxo

• MGCD0103 br Conclusions br Introduction The terms endocrine

  2021-07-14

  

  Conclusions Introduction The terms endocrine active and endocrine disruptive have been used to describe an ever-expanding list of naturally-occurring and synthetic compounds that interact with mammalian hormonal systems, and in particular, the reproductive system. These compounds have been ass

• naphthalimide a well known DNA

  2021-07-13

  

  1,8-naphthalimide, a well-known DNA intercalator, has been extensively investigated in the development of antitumor agents [10]. Some of the naphthalimide derivatives, such as amonafide, elinafide and bisnafide (Fig. 1), have entered into phase II clinical trials stage [10]b), [11]. Among them, elin

• br Discussion Although DNA has a limited

  2021-07-13

  

  Discussion Although DNA has a limited chemical stability it has long been known that DNA in blood stains may remain relative stable for weeks, months, or even years at ambient temperature,1, 2, 3, 4, 5, 6 and samples (e.g., reference samples) that have been transferred to a matrix, e.g., FTA® pap

• br Materials and methods br

  2021-07-13

  

  Materials and methods Results Discussion Tuberculosis is caused by the mycobacterium M. tuberculosis, a pathogen able to survive in the hostile conditions through sophisticated defence mechanisms. In an attempt to clarify some aspects of the M. tuberculosis defence mechanisms, we have inves

• We had earlier reported that

  2021-07-13

  

  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

• Three DDR binding sites have been

  2021-07-13

  

  Three DDR2 binding sites have been mapped on the collagen triple helix by us for collagen type 1 and by others using the collagen toolkit for collagen type 2. All of the three reported binding sequences are conserved in the α1 chain of collagen types 1, 2 and 3. The central motif sequence GARGQAGVMG

• br Application of the screening system

  2021-07-13

  

  Application of the screening system for ITP-binding proteins Inosine is a nucleoside with hypoxanthine as a base. Inosine nucleotides are relatively abundant in human AT-101 because inosine monophosphate (IMP) is a general precursor molecule for the de novo synthesis of AMP and GMP or a product o

• In summary our data show

  2021-07-13

  

  In summary, our data show a novel mechanism: CPD-mediated autoprocessing of C difficile toxins regulates their proinflammatory activities. Thus, our study provides a new understanding of the molecular mechanisms of the pathogenesis of C difficile toxins and insights into designing new therapeutics a

• With a favorable spectrum of

  2021-07-13

  

  With a favorable spectrum of CRTh2 dependent in vitro and in vivo efficacy demonstrated, the off-target activity of compound 18 was investigated, first against a panel of prostanoid receptors and related eicosanoid targets (Table 8), where no significant activities at 10μM concentration were found i

• The inhibition of FAS by C produces

  2021-07-13

  

  The inhibition of FAS by C75 produces an accumulation of malonyl-CoA which is difficult to reconcile with the activation of CPT1 reported by others [2], [16], [17], [18]. To unravel this paradox the mechanism of action of C75 needs to be examined. We recently demonstrated that C75 is converted in vi

• Many authors have described the existence

  2021-07-13

  

  Many authors have described the existence of correlation between viability and moisture content and therefore, water availability. Sabuquillo et al. (2010) demonstrated that only Penicillium oxalicum conidial formulations whose initial moisture contents ranged between 5 and 14% retained their viabil

• br Multi hierarchical structure of collagen Protein structur

  2021-07-13

  

  Multi-hierarchical structure of collagen Protein structure is the foundation of protein functions and properties. It is generally accepted that the protein has biological function only when it has tertiary structure or above. Among the identified 28 types of collagen, most is known about type I c

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