• The lactam emerged as lead candidate due to

  2023-12-15

  

  The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok

• br Materials and Methods br

  2023-12-15

  

  Materials and Methods Results A total of 28 NSCLC tumor samples from 26 patients (2 patients with paired tumor samples) were included. According to the initial FISH (Abbott Molecular probes) and IHC results, 13 samples were ALK IHC+FISH+, 5 samples were ALK IHC+FISH−, 2 samples (from the same

• br Author contributions br Funding This

  2023-12-15

  

  Author contributions Funding This work was supported by the Czech Science Foundation, project no. 14-16220S. Additional support was provided by NIH R01CA117907 grant awarded to J.M.E. Conflict of interest Introduction The dioxin-like family includes polyhalogenated aromatic hydrocarbons

• br Author contributions br Acknowledgements

  2023-12-15

  

  Author contributions Acknowledgements We thank Dr. Bob Hammer and the Transgenic Core Facility at UTSW for the generation of the transgenic lines, John Shelton and the Histology Core for assistance with histology and the UTSW Metabolic Core Unit for help in phenotyping. We acknowledge support

• The cellular mechanism underlying the CGS mediated inhibitio

  2023-12-15

  

  The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w

• Moreover our present work suggests that AXL could be a

  2023-12-15

  

  Moreover, our present work suggests that AXL could be a modulator of sunitinib response, at least for cell lines that present high endogenous levels of this RTK activation, since we observed an increased responsiveness to sunitinib in ALW-II-41-27 activated with AXL receptor ligand. A role for AXL

• The mechanism by which Gas prevents

  2023-12-15

  

  The mechanism by which Gas6 prevents inflammation has been reported to be via inhibition of Toll-Like receptors (TLRs) signaling (Cui et al., 2016). After injury, TLRs become stimulated, leading to downstream activation of TRAF3 and TRAF6 and translocation of several transcription factors, such as I

• The present study indicates elevated ATX activity as

  2023-12-15

  

  The present study indicates elevated ATX activity as a highly sensitive and specific biomarker to differentiate ICP from other pregnancy-related liver disorders or pruritic dermatoses. In torin to the current gold standard for diagnosis, total fasting serum bile salt levels, ATX appeared as a very

• br Acknowledgements We thank the National

  2023-12-14

  

  Acknowledgements We thank the National Natural Science Foundation of China (41576156), Shandong Province Science and Technology Development Plan (2015GSF121045), Yantai Science and Technology Development Plan (2015ZH078), and the Public Science and Technology Research Funds Projects of Ocean (No.

• br Method of literature search br

  2023-12-14

  

  Method of literature search Disclosures Acknowledgment The authors thank and acknowledge Mrs. Jaini Parekh, BFA, for illustrating the diagram in Figure 1. An overview of angiogenesis Angiogenesis is a biological process through which there is the formation of new blood vessels from pre-

• In order to postulate its binding mode in APN

  2023-12-14

  

  In order to postulate its binding mode in APN, Z-IETD-FMK 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by the

• br Materials and methods br Results br Discussion

  2023-12-14

  

  Materials and methods Results Discussion In the present study, we identified HBP1 as a novel substrate of AKT. This was demonstrated by in vitro phosphorylation assays and western blotting using phosphosite-specific antibodies. Three sites were identified by mass spectrometry and mutagenesi

• Involvement of Adiponectin in the

  2023-12-14

  

  Involvement of Adiponectin in the regulation of imatinib resistance in human CML cells has not been hitherto examined. Therefore, in this study, we first established imatinib-resistant K562 CML cells, and then evaluated the effect of Adiponectin in reversing imatinib resistance. The data presented h

• Pituitary adenylate cyclase activating polypeptide PACAP is

  2023-12-14

  

  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

• Introduction Microdialysis is an in vivo technique

  2023-12-14

  

  Introduction Microdialysis is an in vivo-technique which allows continuous sampling of small molecular weight substances (such as neurotransmitters, metabolites and neuropeptides) from the extracellular space of different tissues or organs, e.g. brain, muscle or skin. While the implantation of the

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