• A high throughput small molecule ACK biochemical inhibition

  2024-03-15

  

  A high-throughput small molecule ACK1 biochemical inhibition screen was performed in-house and led to the identification of 1μM inhibitor furanopyrimidine (). Further binding studies found BAPTA-AM synthesis to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) wo

• Imatinib is a well known anticancer drug

  2024-03-15

  

  Imatinib is a well-known anticancer drug used in Chronic Myeloid Leukemia (CML) against the altered expression/activity of tyrosine kinase resulting from the fusion of BCR-ABL in leukemic blasts. It has been demonstrated that Imatinib can induce autophagy in BCR-ABL expressing Gliotoxin (K562 cell

• br Aurora A Aurora B and Aurora C

  2024-03-15

  

  Aurora-A, Aurora-B and Aurora-C small molecule inhibitors Nicholas et al. described phenotypic cellular screening of new highly potent and selective class of Aurora kinase inhibitors. Fragment based approach was utilized; core structure of 57 (Fig. 5) was optimized and selective inhibitor 58 (Fig

• br Acknowledgements We would like to thank Dr Thomas Blanpie

  2024-03-15

  

  Acknowledgements We would like to thank Dr. Thomas Blanpied, Sai Sachin Divakaruni, Dr. Helmut Kessels, Feline Lindhout, Dieudonnée van de Willige, and all members of the MacGillavry lab for discussions and critical reading of the manuscript. This work was supported by NWO (ALW-VENI 863.13.020, A

• br Conclusion We have identified

  2024-03-15

  

  Conclusion We have identified potential inhibitors of C. albicans fungus specific nuclear target outer kinetochore Dam1 complex subunit Ask1, virtually screened through the PubChem compounds database (NCBI, USA) by utilizing state-of-art in silico methods in a pipeline. The 3D protein structure o

• TLX may promote survival and prevent apoptosis in

  2024-03-15

  

  TLX may promote survival and prevent apoptosis in NB furin [12]. Here, we ask whether the survival-promoting effects of TLX are mediated by Apoptosis Signal-regulating Kinase-1 (ASK1, MAP3K5). ASK1 is a member of the Mitogen-Activated Protein (MAP) kinase family and it preferentially activates the

• Besides Arg overexpression our data revealed that AGEs could

  2024-03-15

  

  Besides Arg2 overexpression, our data revealed that AGEs could decrease eNOS mRNA levels, which is considered a significant cause for attenuated NO production and vasodilation. It was found recently that AGEs significantly reduce eNOS expression levels and NO bioavailability in human carotid artery

• The putative residue apelin proprotein proapelin or apelin i

  2024-03-15

  

  The putative 55-residue apelin proprotein (proapelin or apelin-55) is processed from a 77-residue preproprotein through removal of a 22-residue signal peptide (Table 1). Apelin-55 is further processed into bioactive isoforms of 36, 17, or 13 residues, likely through protease-mediated mechanisms. To

• Fig shows a possible scheme of

  2024-03-14

  

  Fig. 8 shows a possible scheme of the generation of AP(+)-exosomes based on this study. In response to inflammatory stimuli, ERAP1 is secreted from ER into the extracellular milieu through the conventional secretion pathway. On the other hand, exosomes are derived from the endosomal pathway, and are

• Targeted disruption of the Akt gene

  2024-03-14

  

  Targeted disruption of the Akt1 gene in mice induces a growth retardation phenotype [4,19]. Akt2 KO mice reveal mild growth retardation and insulin resistance [4,20,21]. Akt1/2 double KO (DKO) mice display severe growth deficiency and die shortly after birth. These mice exhibit impaired bone and ski

• However there are a lot of

  2024-03-14

  

  However, there are a lot of external magnetic field disturbances in urban environments, for example when the AHRS is close to a ferrous or magnetic object, which will disturb the output of magnetometer, then the observational errors cannot satisfy the assumption of Kalman filtering, and so, the atti

• Polycyclic aromatic hydrocarbons PAHs are abundant

  2024-03-14

  

  Polycyclic aromatic hydrocarbons (PAHs) are abundant environmental contaminants that are produced by the incomplete combustion of organic matter, combustion engines, residential heating, Adenosine burning, and industrial activities (Gelboin, 1980; Phillips, 1999, Phillips, 2002). Some PAHs have bee

• Pituitary adenylate cyclase activating polypeptide PACAP is

  2024-03-14

  

  Pituitary adenylate cyclase-activating polypeptide (PACAP) is a member of the secretin/growth hormone-releasing hormone (GHRH)/vasoactive intestinal peptide (VIP) family, with potent anti-inflammatory and potent cytoprotective properties [[6], [7], [8], [9], [10], [11], [12], [13]]. PACAP exists as

• br Conflicts of interest br Acknowledgments br Significance

  2024-03-14

  

  Conflicts of interest Acknowledgments Significance Introduction Androgen receptor (AR) plays a paramount role in the onset and progression of prostate cancer (PC) (Burnstein, 2005, Lonergan and Tindall, 2011, Watson et al., 2015). This very facet underlies androgen deprivation therapy (A

• Until now five muscarinic receptor M genes

  2024-03-14

  

  Until now, five muscarinic receptor (M1-5) genes have been cloned, but, M1-3 receptors are functionally recognized in the lungs. Smooth muscle contraction is mainly mediated by M3. M2 may also participate in the contraction via Gi protein which leads to a decrease in cAMP. On the other hand, M2 is l

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