• The typical pharmacophore for GPR agonists contains four par

  2021-09-02

  

  The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors

• br Experimental br Acknowledgments This

  2021-09-02

  

  Experimental Acknowledgments This project was generously supported by Grünenthal GmbH and IECB. We also thank the staff members of the technical platform of IECB and Grünenthal GmbH for their availability and their skills. Introduction Glucocorticoids (GCs) are essential steroid hormones t

• It is increasingly argued that the immunosuppressive effects

  2021-09-02

  

  It is increasingly argued that the immunosuppressive effects of GCs are conferred indirectly by GR through the activation of genes encoding proteins that inhibit the black and white film of proinflammatory genes 86, 87, 88. Genomic studies offer another mechanism compatible with the idea that GC-m

• The structural modelling studies gave

  2021-09-02

  

  The structural modelling studies gave a view of arsenic mediated covalent modifications possible in Cx43. In order to look for the biochemical effects of Arsenic on Cx43 and Cx43 mediated GJIC formation, and in order to further decipher the mechanism involved in Arsenic induced decreases in expressi

• The PK profile and tissue distribution of which has

  2021-09-02

  

  The PK profile and tissue distribution of 30, which has biological properties almost equivalent to those of 12, were examined in comparison with 12. Analog 30 was evaluated in a 6 h rat PK study at an intravenous (iv) dosing of 1 mg/kg in 10% 2-hydroxypropyl--cyclodextrin (HP-β-CD) (Table 2) and an

• FFAs concentration response curves for increasing intracellu

  2021-09-02

  

  FFAs concentration–response curves for increasing intracellular calcium and receptor phosphorylation showed a difference of ≈1 order of magnitude indicating a relatively large receptor reserve, which is expected for a transfected model, and that high receptor occupancy is necessary to induce recepto

• 5 of 17000 australia FXa is a vitamin K

  2021-09-02

  

  FXa is a vitamin K-dependent serine protease consisting of two chains linked by a disulfide bridge. The heavy chain contains 303 5 of 17000 australia and the light chain has 139 amino acids. The catalytic triad comprised of Ser195, His57, and Asp102  exhibits the trypsin-like β-barrel structure [12

• Finally the optimized leads and were

  2021-09-02

  

  Finally, the optimized leads (−)- and (−)- were tested in rat model of CIPN (3 and 30 mg/kg, po, qd, administered for 7 days) and the results have been shown in . Under acute set up, after single oral administration at 30 mg/kg, both the compounds exerted significant improvement of the NP condition

• The question arises as to

  2021-09-02

  

  The question arises as to how the massive conformational changes determining whether APC/CCDC20–MCC is inhibited or able to catalyze MCC ubiquitylation are naturally controlled? This transition likely involves APC/C regions near the subunit APC15, because reducing cellular APC15 levels stabilizes MC

• Several reports have exploited the

  2021-09-01

  

  Several reports , , , , have exploited the application of HRM for detecting differentially methylated DNA. Even though DNA methylation analysis by HRM cannot determine the methylation status of individual CpGs, it does provide a robust and inexpensive method to differentiate DNA based on the overal

• In the past few years DNA templated fluorescent

  2021-09-01

  

  In the past few years, DNA-templated fluorescent metal nanoparticles have been developed as ideal alternatives to organic dyes due to their facile synthetic process, outstanding optical properties, ultrafine size, and fine biological compatibility. Since the first successful demonstration of DNA-tem

• br Author Contributions br Acknowledgments br Introduction M

  2021-09-01

  

  Author Contributions Acknowledgments Introduction Many anticancer agents bind covalently to DNA, introduce bulky adducts, and inhibit DNA metabolic processes including repair, replication and transcription.1., 2., 3. Frequently, the first enzymes to encounter DNA adducts are DNA helicases.

• The following is the supplementary data

  2021-09-01

  

  The following is the supplementary data related to this article. Introduction Diacylglycerol kinase (DGK) phosphorylates diacylglycerol (DG) to produce phosphatidic 6,7-dihydroxy Bergamottin (PA) (Baldanzi, 2014, Goto et al., 2006, Merida et al., 2008, Sakane et al., 2007, Topham and Epand, 200

• br Molecular modeling simulation study Molecular modeling

  2021-09-01

  

  Molecular modeling simulation study Molecular modeling study was performed through docking of the test compounds into the binding site of hDHFR enzyme using Discovery Studio 2.5 software. Computational docking is an algorithm designed to determine the suitable position and the orientation of the

• In agreement with the study on porcine microsomes

  2021-09-01

  

  In agreement with the study on porcine microsomes (Ekstrand et al., 2015), our results indicated a somewhat higher degree of inhibition of CYP2E1 activity in the male pools compared to females. Nevertheless, the degree of this hoechst 33258 receptor inhibition did not reach 50%, indicating that que

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