• In conclusion AXL overexpression preexisted in

  2024-05-21

  

  In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi

• br Conclusion br Acknowledgments This research

  2024-05-21

  

  Conclusion Acknowledgments This research has been supported by the Ratchadaphiseksomphot Endowment Fund 2013 of Chulalongkorn University (CU-56-341-AS) and the Ratchadapiseksompotch Fund (RA55/22), Faculty of Medicine, Chulalongkorn University. The authors commemorate the 100th Anniversary of

• The surprising finding of our study

  2024-05-21

  

  The surprising finding of our study is that human M1 macrophages stimulated by LPS express ALOX15B to high levels. So far 12/15-lipoxygenase activity was only reported for IL-4 stimulated anti-phlogistic M2 macrophages [9] but not for the classically activated M1 macrophages. Our data suggest that

• A high throughput screening campaign led

  2024-05-21

  

  A high-throughput screening campaign led to the discovery of the first series of both potent and selective ATR kinase inhibitors by Vertex Pharmaceuticals (Charrier et al., 2011). One of these compounds, VE-821, was shown to be a potent ATP-competitive inhibitor of ATR with minimal cross-reactivity

• Somatostatin analogs also bind to

  2024-05-21

  

  Somatostatin analogs also bind to somatostatin receptors. It has been reported that octreotide has a high affinity for hSSTR2, moderate affinity for hSSTR3 and hSSTR5, and does not bind to hSSTR1 or hSSTR4 (Ben-Shlomo and Melmed 2008). Compared to octreotide, pasireotide displays 40-, 30-, and 5-fol

• Based on the extracellular domain structures we can

  2024-05-21

  

  Based on the extracellular domain structures, we can infer that the dimer arrangement of GABAB receptor will undergo substantial changes upon receptor activation (Geng et al., 2013). First, agonist-stimulated closure of GABAB1 VFT would cause an upward rotation of its LB2 domain, coupled with an inw

• It is well known that neurosteroids

  2024-05-21

  

  It is well-known that neurosteroids such as testosterone and their metabolites endogenously modulate neural excitability in animals and humans. Testosterone has protective effects against seizures induced by KA and PTZ (Frye et al., 2001b; Reddy, 2004b). Estrogens, on the other hand, have proconvuls

• Asparagine synthetase ASNS is a glutamine amidotransferase t

  2024-05-21

  

  Asparagine synthetase (ASNS) is a glutamine amidotransferase that catalyzes ATP-dependent synthesis of asparagine and glutamate from aspartate and glutamine. Upregulation of ASNS expression renders leukemia cells resistant to l-asparaginase treatment, and ASNS is essential for cell survival in the a

• AHR mediated MMP upregulation has been shown in

  2024-05-21

  

  AHR-mediated MMP1 upregulation has been shown in response to tobacco smoke [32]. Tobacco smoke contains various AHR ligands such as benzo[a]pyrene. Both benzo[a]pyrene [15] and FICZ [13] are high-affinity ligands for AHR and upregulate CYP1A1 and CYP1B1. FICZ is rapidly degraded by CYP1A1 [20], [33]

• The CK catalyzes the reversible conversion of creatine into

  2024-05-20

  

  The CK catalyzes the reversible conversion of creatine into creatine phosphate using ATP and thereby releasing ADP. The CK isoenzymes, specifically localized in places where there is a demand and production of energy, are linked to a creatine/creatine phosphate shuttle (Wallimann et al., 1998). Thi

• The potential use of derivatives belonging to this series

  2024-05-20

  

  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 adult muscle type acetylcholine receptor AChR

  2024-05-20

  

  The adult muscle-type Azaserine receptor (AChR), the exemplar pLGIC, is a heteropentamer comprising two α subunits, and one each of the β, δ, and ɛ subunits (Sine, 2012). These five subunits come together in a counterclockwise α-ɛ-α-δ-β arrangement (Figure 1A). Binding of acetylcholine to the AChR'

• KT 5823 synthesis The lanthanide series of chemical elements

  2024-05-20

  

  The lanthanide series of chemical elements comprises the fifteen metallic chemical elements with atomic numbers 57 through 71, from lanthanum to lutetium. Though originally described as ‘‘rare earths’’ because of their natural occurrence as metal oxides, they are not particularly rare. The lanthanid

• br LOX in pancreatic cancer

  2024-05-20

  

  5-LOX in pancreatic cancer 5-LOX is a key player in pancreatic cancer (PC) progression. The upregulation of 5-LOX mRNA has been observed in pancreatic adenocarcinoma (PDAC) and also in neoplastic pancreatic tissues (Kennedy et al., 2003). Higher levels of 5-LOX transcripts (messengers) are presen

• Doramapimod mg br Discussion Here we focused on seven plant

  2024-05-20

  

  Discussion Here, we focused on seven plant alkaloids extracted from yokukansan. These alkaloids individually inhibited 5-HT-mediated 5-HT3A and 5-HT3AB receptor currents weakly. Simultaneous administration of these alkaloids, however, inhibited the 5-HT3A and 5-HT3AB receptor currents strongly. T

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