• In conclusion we designed novel E inhibitors based on

  2020-11-24

  

  In conclusion, we designed novel E1 inhibitors based on the three-dimensional structure of E1 in complex with ubiquitin. Following an enzymatic assay evaluating synthetic compounds , , and , we identified compound as a novel E1 inhibitor. Comparing the inhibitory activity of compound with and ,

• Furthermore elastase might not be the only

  2020-11-24

  

  Furthermore, elastase might not be the only regulator of CBG on cleaved and uncleaved form. In a study by Nenke et al. [85] α1-AT deficient subjects, who lack this native neutrophil elastase inhibitor, paradoxically have higher levels of uncleaved CBG and lower levels of CBG* [85]. Gender differenc

• Imatinib STI is a first line tyrosine

  2020-11-24

  

  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

• Cyclosporine NEORAL Oral Solution Novartis is an immunosuppr

  2020-11-24

  

  Cyclosporine (NEORAL® Oral Solution, Novartis) is an immunosuppressant widely used in organ transplantation and many other clinical conditions [12]. It undergoes extensive hepatic and intestinal biotransformation mainly via the metabolizing enzyme, CYP3A4 [[12], [13], [14], [15]]. Considering the na

• br Guidance of B cell localization by EBI br

  2020-11-24

  

  Guidance of B cell localization by EBI2 EBI2 expression and B cell disease Although chemoattractant receptors of the GPR family play essential roles in coordinating the migration of lymphocytes for efficient responses against pathogens, their dysregulation can result in the initiation or progr

• br Experimental Procedures br Author Contributions br Acknow

  2020-11-24

  

  Experimental Procedures Author Contributions Acknowledgments Introduction Oxysterols came to prominence in the late 1970's with the oxysterol hypothesis which proposed that the suppressive effect of cholesterol on its own synthesis is mediated through oxysterols not by cholesterol itself

• The strand domain swap in the UbV XR dimer

  2020-11-24

  

  The β strand domain swap in the UbV.XR dimer appears to be a unique arrangement for a Ub-based dimer. In solution, free Ub has a KD of ∼5 mM for the monomer-dimer equilibrium, and the two subunits in the dimer adopt a range of relative orientations involving residues from Ub’s β sheet (Liu et al., 2

• Phos-tag Acrylamide A novel series of DHODH inhibitors was

  2020-11-23

  

  A novel series of DHODH inhibitors was developed by us based on a lead that was discovered during a docking procedure and medicinal chemistry exploration. The activity of the initial lead was improved by a QSAR method and yielded low nanomolar inhibitors. Introduction The most common metabolic h

• br Experimental Procedures br Acknowledgments br Introductio

  2020-11-23

  

  Experimental Procedures Acknowledgments Introduction Incessant consumption of fossil fuels brings on global energy crisis and serious environmental concerns. Hence, the researchers have paid considerable attention to alternative renewable bioenergy. Microalgae has been considered as potenti

• br Results This study was carried out with

  2020-11-23

  

  Results This study was carried out with a series of engineered extracellular matrix films of collagen assembled at hydrophobic surfaces, which allow for independent control of supramolecular structure, mechanical stiffness, and receptor recognition sites [17], [21]. Vascular smooth muscle bryosta

• DAPK is a kD Ca calmodulin CaM regulated

  2020-11-23

  

  DAPK is a 160-kD Ca2+/calmodulin (CaM)-regulated Ser/Thr kinase that mediates cell death. The activated forms of DAPK and DRP-1 are capable of inducing two distinct cytoplasmic events characteristic of programmed cell death, including membrane blebbing and the formation of autophagic vesicles (Inbal

• AST 487 In addition to the blockade of airway smooth muscle

  2020-11-23

  

  In addition to the blockade of airway smooth muscle contractions, CysLT1 receptor antagonists also exerted a potent anti-inflammatory effect at this level. The oral administration of MEN91507, Pranlukast, Montelukast, and Zafirlukast also produced a long-lasting inhibition of leukotriene D4-induced

• Tunicamycin Cytochrome P CYP enzymes plays an essential role

  2020-11-23

  

  Cytochrome P450 (CYP-450) enzymes plays an essential role in pharmacology of drugs and toxicology of xenobiotics. Inhibition of these enzymes may lead to increase plasma levels of a concomitantly administered drug (Lee et al., 2013). It may prolong or reduce the pharmacological effects and increase

• br Acknowledgments br Introduction to the

  2020-11-23

  

  Acknowledgments Introduction to the somatic mitotic cell cycle Cell cycle dysregulation and cancer Structures of the cyclin-dependent protein kinases Structure of the CDK hydrophobic skeletons Classification of protein kinase-drug complexes Dar and Shokat defined three Azithromycin

• Under optimized assay conditions very low concentrations

  2020-11-23

  

  Under optimized assay conditions, very low concentrations (20pM) of [125I]YP20 bound to hCRF1-CHO sars-cov membranes with high specificity (>95% inhibited by 1μM astressin) and in a membrane protein-dependent manner. Specific binding was selective vs. the hCRF2α subtype because little specific bind

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