• Natural progestogens play an important role in

  2019-12-24

  

  Natural progestogens play an important role in the stimulation of oocyte growth and maturation as well as in spermatogenesis and sperm maturation, and they act as sex pheromones in teleost fish (Kime, 1990, Kobayashi et al., 2002, Nagahama and Yamashita, 2008, Scott et al., 2010). A complex series o

• Binding affinity was measured by

  2019-12-24

  

  Binding affinity was measured by a scintillation proximity binding assay using [H]4-OHT (ERRγ) or [H]estradiol (ERα/β) as radioligand. In all cases, the ERβ affinity was not significantly different from ERα. Compounds were compared to , which showed high affinity for both receptors and moderate (six

• It is without doubt that the vagina

  2019-12-24

  

  It is without doubt that the vagina plays a significant role in the perception of coital stimulation leading to sexual arousal and, finally, orgasm. In response to sensory stimulation, relaxation of vaginal vascular and nonvascular smooth muscle occurs, resulting in an increase in local blood flow a

• In principle in vitro techniques for assessing

  2019-12-24

  

  In principle, in vitro techniques for assessing enzyme induction might include the use of cultured hepatocytes, precision-cut liver slices, immortalized 2179 sale lines (such as those derived from hepatomas) and reporter gene constructs (where appropriate cells are transfected with recombinant DNA

• Recent studies support the concept that dietary metabolites

  2019-12-24

  

  Recent studies support the concept that dietary metabolites, such as retinoids and AHR ligands, regulate ILC3 function. These metabolites act through intracellular nuclear receptors that function as transcription factors, thereby controlling ILC activity through the stimulation of specific transcrip

• In all available E E structures the RING

  2019-12-24

  

  In all available E2:E3 structures, the RING-type domain binds the E2 on a surface that is remote from the active site Cys (and therefore from the ubiquitin thioester) (Fig. 2). The non-contiguous E3-binding and active sites on the E2 imply that the role played by a RING to facilitate ubiquitin trans

• An important role for the precursor molecule of

  2019-12-23

  

  An important role for the precursor molecule of the main EBI2 ligand, 25-OHC, in the inhibition of inflammation was recently shown. 25-OHC was demonstrated to inhibit inflammasome induction in mouse macrophages [28]. Inflammasome assemblies are the sites of caspase 1 activation and lead to the gener

• Introduction Ubiquitylation is a post

  2019-12-23

  

  Introduction Ubiquitylation is a post-translational modification which impacts almost every biological process in the cell. Dysregulation of the ubiquitylation pathway is associated with several diseases, including cancer, neurodegenerative disorders, and immunological dysfunctions. Single ubiquiti

• Interest in DGKs increased as it became clear that

  2019-12-23

  

  Interest in DGKs increased as it became clear that not only are they important for lipid homeostasis, they serve to modulate the relative levels of diacylglycerol (DAG) and phosphatidic Rapalink-1 mg (PtdOH) that play critical roles in a variety of signaling pathways (Eichmann and Lass, 2015; Liu e

• Manidipine 2HCl Previous studies showed that many steroidoge

  2019-12-23

  

  Previous studies showed that many steroidogenic enzymes act when the enzyme binds to the cofactor first [30]. In the present study, we showed that HPTE inhibited both AKR1C14 and RDH2 in a mixed mode when cofactor was used. This indicates that HPTE interferes with cofactor-binding residues although

• br Fragment based drug discovery FBDD is a powerful

  2019-12-23

  

  Fragment-based drug discovery (FBDD) is a powerful method to discover drug leads and has been widely adopted in both academia and industry. FBDD can be used to explore chemical Erastin space with libraries which are smaller in size, producing drug leads with high ligand-binding efficiency. It als

• blz Accurate equilibrium predictions of CO containing mixtur

  2019-12-23

  

  Accurate equilibrium predictions of CO2 containing mixtures, however, are challenging with traditional equations of state. The reason for this may be that CO2 has a large quadrupole moment. The large quadrupole moment of CO2, as well as size asymmetry, are for instance believed to be the reasons for

• Cx platin could improve the level of cellular

  2019-12-23

  

  Cx-platin could improve the level of cellular uptake and DNA platination, hence triggering distinct DNA damage repair pathways. The data (Fig. 3B, C and D) demonstrated that Cx-platin could increase the foci number of γH2AX in cancer cells, preventing the efficient DSBs repair. This gives a good exp

• In our former work our

  2019-12-23

  

  In our former work, our interest was in discovery of novel VEGFR-2 inhibitors as anti-angiogenesis agents. Along this line, with natural alkaloid taspine as the lead compound, rounds of structure optimization were performed to develop novel VEGFR-2 inhibitors [[13], [14], [15]]. Among them, BPS-7, b

• br Introduction O Methylguanine DNA methyltransferase MGMT

  2019-12-20

  

  Introduction O6-Methylguanine-DNA methyltransferase (MGMT) is a DNA-repair enzyme that specifically transfers alkyl adducts from the O6 position of guanine to the cysteine residue (Cys145) in its active site. In cancer cells, this ability of MGMT disrupts the cytotoxic actions of alkylating antic

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