• Several dehidropregnenolone derivatives functionalized at C

  2024-05-08

  

  Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic

• MLN another selective Aurora A inhibitor is

  2024-05-08

  

  MLN8237, another selective Aurora-A inhibitor is said to be more potent than MLN8054 and to cause less benzodiazepine-like side effects based on structure modulation by the addition of a methoxy group to either end of the MLN8054 molecule. It was studied [62] in a once daily (QD) schedule for 7 days

• Receptors containing an x y subunit interface where x and

  2024-05-07

  

  Receptors containing an αx/γy subunit interface, where x=1, 2, 3, 5 and y=1–3, form a high-affinity binding site for benzodiazepines (Figure 1A), for the later developed Z-drugs of different chemotypes, and for a large number of chemically distinct research compounds 17, 18 (Box 1 for examples). For

• From an historical perspective ligands for GPCRs adrenaline

  2024-05-07

  

  From an historical perspective, ligands for GPCRs (adrenaline, serotonin, natural product libraries or morphine, to name a few) have been identified before their receptor counterparts, at a time when the concept of receptor itself was controversial [15]. Although many cognate receptors for endogenou

• There is a delicate balance between ROS generation and scave

  2024-05-07

  

  There is a delicate balance between ROS generation and scavenging by the protective antioxidant defenses in the cell. Antioxidant systems present in the AZD3514 include enzymes like superoxide dismutase (SOD), catalases, glutathione peroxidases (GPxs) and peroxiredoxins (PRxs) (Fig. 3) [38]. SODs ar

• br Materials and methods br Results br Discussion In

  2024-05-07

  

  Materials and methods Results Discussion In this study, the orphan receptor GPR25 was cloned from several representative vertebrate species including zebrafish. Although the overall amino adefovir sequence identity among these species is not high (38–52%), our synteny analysis clearly indi

• br Acknowledgements We thank the National Natural

  2024-05-07

  

  Acknowledgements We thank the National Natural Science Foundation of China (41576156), Shandong Province Science and Technology Development Plan (2015GSF121045), Yantai Science and Technology Development Plan (2015ZH078), and the Public Science and Technology Research Funds Projects of Ocean (No.

• The initial demonstration of the potential of MALDI TOF MS

  2024-05-07

  

  The initial demonstration of the potential of MALDI-TOF MS for testing antifungal susceptibility of pathogenic fungi came from a proof-of-concept study by Marinach et al. [31] who monitored the changes of the proteome of C. albicans SB 203580 hydrochloride exposed to different concentrations of flu

• In conclusion our study has identified a

  2024-05-07

  

  In conclusion, our study has identified a splice site src inhibitor (c.1769-1G > C) in the AR gene from two patients with complete androgen insensitivity syndrome. The c.1769-1G > C mutation may provide us new insights into the molecular mechanism involved in splicing defects underlying CAIS. Our f

• AR Vs are truncated AR proteins lacking the

  2024-05-07

  

  AR-Vs are truncated AR proteins lacking the AR ligand-binding domain (AR-LBD) [6]. While AR-Vs have frequently been detected in CRPC, their expression and functional role in benign prostate tissues and primary prostate cancers is not readily apparent. Structural rearrangements in the AR gene and alt

• The molecular mechanisms that mediate the plasticity of the

  2024-05-07

  

  The molecular mechanisms that mediate the plasticity of the NMJ are not well understood. PGC-1α is a master regulator of the NMJ gene expression program 23, 24, and thus AMPK might indirectly regulate the NMJ via its broad influence on the coactivator. Cerveró et al.[6] recently provided more direct

• A rate limiting step in the generation of kynurenine

  2024-05-07

  

  A rate-limiting step in the generation of kynurenine and xanthurenic ahr inhibitor is the oxidation of N-formyl-kynurenine to l-kynurenine via indolamine 2,3-dioxygenase (IDO) or tryptophan dioxygenase (TDO). IDO and/or TDO knockdown decreases and ectopic over-expression increases production of end

• br Acknowledgments and Disclosures br Introduction In mammal

  2024-05-07

  

  Acknowledgments and Disclosures Introduction In mammals, ejaculated sperm requires a finite period of residence in the female reproductive tract to become competent for fertilization (Visconti et al., 1995a, Visconti et al., 1995b). Once oocytes are matured, it is important for these cells to

• Nilvadipine The specific binding domain between PGK in group

  2024-05-07

  

  The specific binding domain between PGK in group B strepotocci (GBS) and actin had been reported . PGK as the actin-binding protein identified in TMW 1.1434, which displayed highly significant adhesion was investigated for the binding sites and compared to bacteria with less strong adhesion to acti

• The fact that the BPloopAsn

  2024-05-07

  

  The fact that the α1-BPloopAsn141 regains its α-Btx binding with a Kd similar to that of the wild type α1 ECD [18], suggests that the AChBP Cys-loop does not interfere with the correct conformation of the mutant ECD. Data from analogous mutants of the human neuronal α7 subunit ECD showed improved li

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