• More than thirty enzymes with

  2020-09-30

  

  More than thirty enzymes with PLA2 activity have been described and, based on sequence similarities, they are currently classified in 16 groups, each containing several sub-groups [16]. However, based on biochemical features these enzymes are frequently grouped into six major families: secreted phos

• The glycolytic pathway is a catabolic route that ends with

  2020-09-30

  

  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

• CYP A and CYP D are among the main drug

  2020-09-30

  

  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

• Our approach including the characterization of histone modif

  2020-09-30

  

  Our approach, including the characterization of histone modifications in scarce NK subsets, allowed us to identify super-enhancers, which associate with genes endowing a given cell type with its unique identity (Hnisz et al., 2013). Especially intriguing were SEs with distinct activities in NK subse

• Several eukaryotic E enzymes including BRE RNF and RAD

  2020-09-30

  

  Several eukaryotic E3 enzymes, including BRE1 [49], RNF8 [50], and RAD18 [24], [51], have been reported to partner with UBE2B in the ubiquitination of various targets. We examined the expression levels of these E3 enzymes in HONE1 and TW01 cells; RAD18 was highly expressed in these Oxaliplatin mg (

• Several functions of FAT have been suggested It has been

  2020-09-30

  

  Several functions of FAT10 have been suggested. It has been shown that FAT10 binds noncovalently to the mitotic spindle checkpoint protein MAD2 and that this binding might cause chromosome instability in the cancer Stiripentol receptor overexpressing FAT10 (Liu et al., 1999, Ren et al., 2006). In o

• Advances in the total chemical synthesis of ubiquitin have

  2020-09-30

  

  Advances in the total chemical synthesis of ubiquitin have enabled the efficient synthesis of new and improved ubiquitin-based reagents. Using an optimized linear synthesis, ubiquitin can now be easily obtained in high yield and purity [35]. Using this synthetic methodology, ubiquitin can be functio

• Cy5 NHS ester(Et) receptor Similarly synthetic analogs of Al

  2020-09-30

  

  Similarly synthetic analogs of Alogliptin by replacing the cyanobenzyl group with the butynyl group have been synthesized and tested as selective DPP-4 inhibitors [7], [8]. Additionally, quinazolines [9], [10], pyridopyrimidinediones [11], pyrazolopyrimidinones [12] and pyrimidines [13] as DPP-IV in

• br Material and methods br Results and discussion br

  2020-09-29

  

  Material and methods Results and discussion Conclusions Acknowledgements S. De thanks DST, New Delhi for generous grant of the SERC Fast Track Scheme No. SR/FT/CS-057/2008. R. Kundu thanks the University of Kalyani for financial assistance. We are grateful to Prof. K. Bhattacharyya of IA

• Recent studies from the literature

  2020-09-29

  

  Recent studies from the literature have identified new terbinafine hydrochloride of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-

• Our recent discovery M P H R A S of

  2020-09-29

  

  Our recent discovery (M.P., H.R., A.S.) of a highly selective and in vivo active DDR1 small-molecule inhibitor provides evidence that DDR1 is a druggable pharmaceutical target, and some details of our efforts are provided below. To avoid the repurposing of known kinase inhibitor structural motifs, w

• Introduction Cytochrome P CYP A is the most

  2020-09-29

  

  Introduction Cytochrome P450 (CYP)3A is the most important enzyme involved in the metabolism of 30–40% of currently prescribed drugs [1]. The g protein coupled receptors level and activity of CYP3A show large intra- and inter-individual variability, which contributes to unpredictable drug response

• Alvocidib flavopiridol is a piperidine chromenone http

  2020-09-29

  

  Alvocidib (flavopiridol) is a piperidine-chromenone derivative (Fig. 6D) that is not FDA approved, but is in clinical trials for breast, endometrial, and several other cancers and hematological malignancies (Table 4) [[100], [101], [102], [103], [104]]. This drug targets CDK9 (IC50 = 3.2 nM) and CDK

• Physiological changes induced by CRF are mediated

  2020-09-29

  

  Physiological changes induced by CRF are mediated through CRF1 and CRF2 receptors (Chang et al., 1993, Lovenberg et al., 1995). Previous findings with CRF1 receptor antagonists showed that activation of CRF1 receptor is involved in maternal separation-induced ultrasonic vocalizations (Kehne et al.,

• To determine the time course of

  2020-09-29

  

  To determine the time course of ZD2767P+CPG2 DNA–DNA interstrand cross-link formation, HT29 and LS174T colorectal tumour Vidofludimus synthesis were exposed to the drug for 10, 30 or 60 min. The levels of DNA interstrand cross-links in HT29 or LS174T cells did not increase with exposure time, sugge

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