• The potential use of derivatives belonging

  2024-08-12

  

  The potential use of derivatives belonging to this series as therapeutic agents mostly depends on their pharmacokinetics and pharmacodynamics. The pharmacokinetic phase includes absorption, distribution, metabolism and excretion (ADME) of the studied compounds. Therefore, preliminary data for theore

• The fact that the BPloopAsn regains its

  2024-08-12

  

  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

• Application of the broad acting HTR antagonist

  2024-08-12

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

• However cancer and fibrotic diseases are the most extensivel

  2024-08-12

  

  However, cancer and fibrotic diseases are the most extensively studied disease states. ATX is connected to various cancers because it can stimulate chemokinesis and chemotaxis in melanoma cells. Upregulated ATX Cyanine 5-dCTP has been reported in breast cancer,, prostate cancer, thyroid cancer, non-

• br Autophagy inducers Macroautophagy is often seen as

  2024-08-12

  

  Autophagy inducers Macroautophagy is often seen as a cellular process capable of increasing the fitness of Zerumbone and overcome resistance to several forms of stress [9], [10]. As discussed above, it has been proposed by several authors that an effective strategy for enhancing sensitivity of c

• Here we report discovery of

  2024-08-09

  

  Here we report discovery of highly selective pan-Aurora kinase inhibitors through phenotypic screening. The co-crystal structure of patupilone synthesis bound in the ATP binding site of Aurora A is described, and provides insight into the possible structural basis for the selectivity of the intera

• Aprepitant receptor Among the most important Ca regulatory m

  2024-08-09

  

  Among the most important Ca regulatory mechanisms are the Plasma Membrane Calcium ATPase (PMCA) and Sarcoplasmic Reticulum Calcium ATPase (SERCA). These pumps belong to the family of P-ATPases, which share the formation of an acid-stable phosphorylated intermediate as part of their reaction cycle. P

• br Materials and methods br Results br Discussion Human

  2024-08-09

  

  Materials and methods Results Discussion Human MutL-family complexes (MutLα: MLH1-PMS2, MutLβ:MLH1-PMS1, MutLγ:MLH1-MLH3) exhibit multiple molecular activities including DNA binding, DNA cleavage, ATP binding and hydrolysis [43]. In our recent study, we have uncovered an important function

• Whole body loss of ACLY is early embryonic lethal

  2024-08-09

  

  Whole-body loss of ACLY is early embryonic lethal, indicating that it serves non-redundant roles during development (Beigneux et al., 2004). Silencing or inhibition of ACLY suppresses the proliferation of many cancer cell lines and impairs tumor growth (Bauer et al., 2005, Hanai et al., 2012, Hatziv

• Acknowledgments br Introduction Prostate cancer is

  2024-08-09

  

  Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi

• Placental cells also express P aromatase CYP A

  2024-08-09

  

  Placental cells also express P450 aromatase (CYP19A1, encoded by CYP19A1). In the placenta, this enzyme requires an external source of androgens, provided by the adrenal gland of the fetus, to form estrogen. The fetal adrenal gland produces dehydroepiandrosterone (DHEA) [9] and, in the placenta, it

• br Material and methods br Results br

  2024-08-09

  

  Material and methods Results Discussion Didox was originally created asa cytostatic drug to inhibit cancer cell proliferation by antagonizing RNR [11]. When used to target highly proliferative cells, Didox has extensive activity in vitro and in vivo. It has also been employed in clinical st

• The crucial role of AP in

  2024-08-09

  

  The crucial role of AP-1 in establishing and maintaining cell type-specific gene expression programs and cell identity is further apparent during reprogramming of mouse embryo fibroblasts (MEFs) into iPSCs with either Oct4/Sox2/Klf4/cMyc (OSKM ) factors , or chemicals . Using ATAC-seq to profile ch

• PD 151746 br Mechanism of action In

  2024-08-09

  

  Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra

• ESI-09 br Antibiotic drug discovery approaches Traditionally

  2024-08-09

  

  Antibiotic drug discovery approaches Traditionally, novel ESI-09 were largely discovered by phenotypic screening approaches of various sources of compounds, such as natural products isolated from extracts of soil microbes and semi-synthetic or fully synthetic compound libraries derived from known

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