• Camptothecin is a type of topo I inhibitor and its

  2021-12-30

  

  Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s

• These inhibitors possess a cap group build

  2021-12-30

  

  These inhibitors possess a cap group build from cyclization of several amino-acid or non-amino-acid residues, four or more, with one residue bearing an alkyl arm terminated by ZBGs of various types: thiols, ketones or epoxides. In the case of romidepsin 30 (Fig. 7), the thiol group is initially in a

• stock solution calculator Aurora kinase B AURKB and

  2021-12-30

  

  Aurora kinase B (AURKB) and haploid cell-specific protein kinase (Haspin) are two well-known participants in N-terminal histone H3 phosphorylations during mitosis. A related role played by these kinases relates to the fact that AURKB is activated by Haspin promoted phosphorylation at T3. Irrespectiv

• The balance and composition of the gut microflora

  2021-12-30

  

  The balance and composition of the gut microflora can be altered by the use of antibiotics or by colonization of the intestine by pathogens. This change may also induce, or be induced by, modifications in the body’s immune response, ultimately leading to disease. Thus, when intestinal homeostasis is

• The number of small molecule GSK inhibitors is continuously

  2021-12-30

  

  The number of small molecule GSK-3 inhibitors is continuously rising and many have been tested in animals. These studies have provided additional support for specific roles of GSK-3 in neuronal functions under both normal and pathological conditions. Inhibition of GSK-3 has profound effect on neurop

• Recently we suggested that KYNA an endogenous GPR agonist co

  2021-12-30

  

  Recently, we suggested that KYNA – an endogenous GPR35 agonist could be produced in a human cornea since we showed the presence of the enzymes that catalyze the synthesis of KYNA – kynurenine aminotransferases I-III in corneal epithelium, stroma and endothelium (). Therefore, these findings provided

• PSI-7977 mg The rat model was validated

  2021-12-30

  

  The rat model was validated with another agonist of GPR109A, acipimox. Acipimox has been shown to induce vasodilatation in man, by a mechanism dependent on the release of vasodilator prostaglandins (Edlund et al., 1990, Pontiroli et al., 1992). Acipimox is a weaker agonist of the GPR109A receptor (L

• As well as the above studies Meier and coworkers

  2021-12-30

  

  As well as the above studies, Meier and coworkers used TUG-891, alongside omega-3 fatty acids, to show a potential role for FFA4 in inhibiting proliferation of DU145 prostate cancer cells [68]. Given that these cells express both FFA4 and FFA1 and the current view that TUG-891 may not be sufficientl

• vasopressin receptor antagonist Based on these findings we

  2021-12-30

  

  Based on these findings, we set out to identify GPR109A agonists capable of biasing the receptor's signaling towards the functional anti-lipolytic and presumed therapeutic response, and away from the flushing side-effect pathways. Indeed, using recombinantly expressed GPR109A, two classes of compoun

• br Methods and materials br Results and

  2021-12-30

  

  Methods and materials Results and discussion Conclusions This is the first study that attempted to isolate, purify and identify the characteristics of gap junctions from ginseng. In vitro studies have demonstrated that PGL-1 efficiently suppressed SH-SY5Y cell apoptosis induced by Aβ25–35,

• The occurrence of MDR in cancer patients undergoing chemothe

  2021-12-30

  

  The occurrence of MDR in cancer patients undergoing chemotherapy can be mimicked in the laboratory by culturing cancer IU1 receptor in the presence of chemotherapeutic drugs, thereby enforcing the evolution of acquired drug resistance. This has been described in multiple model systems including the

• Excessive extracellular glutamate can be removed from brain

  2021-12-30

  

  Excessive extracellular glutamate can be removed from Caspase-3, human recombinant proteinase receptor interstitial fluids to the blood plasma for the maintenance of proper extracellular glutamate homeostasis in the mammalian central nervous system [[5], [6], [7]]. The glutamate concentration in th

• In the GLUT family glucose

  2021-12-30

  

  In the GLUT family, glucose transporter 1(GLUT1) is primarily responsible for basal glucose uptake and maintenance of glucose basal metabolism in cells (Olson and Pessin, 1996). High GLUT1 expression occurred in various types of human cancers, like brain tumor, lung cancer and esophageal cancer (Nis

• Herein in consider of the high similarity between GR HBP

  2021-12-30

  

  Herein, in consider of the high similarity between GR HBP site and AR HBP site, we applied rational drug design strategy to develop AR/GR antagonists based on the chemical structures of antiandrogens and crystal structure of GR. The following bioassay identified Z19 as a dual AR/GR antagonist. Z19 i

• MAPK are involved in a large variety of

  2021-12-30

  

  MAPK are involved in a large variety of solid and hematolgical neoplasms and, indeed, several components of the MAPK network have already been proposed as targets in cancer therapy, such as p38, JNK, ERK1/2, MEK1/2, RAF, RAS, DUSP1 and ERK5 [11], [12]. Among them, alteration of the RAS-RAF-MEK1/2-ER

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