• The inhibition of the exacerbated inflammatory response that

  2023-01-16

  

  The inhibition of the exacerbated inflammatory response that follows injury may be an alternative approach to induce a more efficient repair [17,83]. In line with that, 5-LO is one of the most consolidated targets for dampening inflammation, mainly through the therapeutic effects of 5-LO inhibitors

• br LOX in pancreatic cancer LOX is a

  2023-01-16

  

  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

• An AXL decoy receptor with enhanced GAS

  2023-01-16

  

  An AXL decoy receptor with enhanced GAS6-binding properties, MYD1, was engineered as a therapeutic tool to disrupt GAS6/AXL signaling in vivo (Kariolis et al., 2014). MYD1 was shown to block metastasis of human ovarian cancer bibn and a murine breast cancer cell line in grafting assays in mice. Thes

• br Materials and methods br Results br Discussion We have

  2023-01-16

  

  Materials and methods Results Discussion We have developed a high-throughput functional genomic screen that allows the identification of genes that confer drug resistance. Several factors have been identified which must be taken into account to develop a reliable screen. In particular, cons

• Having demonstrated that Gq coupled mGluR a was

  2023-01-16

  

  Having demonstrated that Gq-coupled mGluR1a was necessary for estradiol-induced enhancement of CREB phosphorylation, we hypothesized that activation of a separate G-protein signaling pathway could explain the effect of estradiol on L-type calcium channel signaling (Boulware et al., 2005). Indeed, in

• HMGN proteins are subject to extensive post translational mo

  2023-01-16

  

  HMGN proteins are subject to extensive post-translational modifications which influence both their mode of binding to 3463 mg and their functional activity. Like the other HMG protein families, HMGNs are substrates for many of the same enzymes that modify histone proteins (review in [175]). The his

• br Introduction Increasing number of mycosis infections has

  2023-01-16

  

  Introduction Increasing number of mycosis infections has been reported during the past several years because of the rise in the number of immuno-compromised individuals in subtropical and tropical countries with high mortality and morbidity [1], [2]. Trichophyton mentagrophytes, Trichophyton rubr

• The zinc transporter proteins are members

  2023-01-16

  

  The zinc transporter proteins are members of the SLC superfamily of metal transporters, and comprise two structurally and functionally different groups, the zinc-importer (ZIP; Zrt-, Irt-like proteins) family (SLC39A), which regulate zinc transport into the cytoplasm from outside the cell and from i

• It remains to elucidate whether proteolytic activity is

  2023-01-14

  

  It remains to elucidate whether proteolytic activity is the cause or the consequence of changing levels of peptidergic substrates. In fact, in some cases, the expression of the enzyme does not necessarily parallel with its activity [26], [55], [57] and other factors such as a definite biochemical en

• Recently two distinct small molecule inhibitors of PHGDH wer

  2023-01-14

  

  Recently, two distinct small-molecule inhibitors of PHGDH were identified using high-throughput screens, both of which inhibit de novo serine biosynthesis and show selective toxicity to cancer SB 265610 australia with high SSP flux [50,51]. The inhibitor NCT-503, which has an IC50 of 2.5μM, reduces

• Gratifyingly compound also demonstrated improved physicochem

  2023-01-14

  

  Gratifyingly, compound also demonstrated improved physicochemical properties with significant improvement in aqueous solubility. Compound was sufficiently potent to determine its pharmacokinetic (PK) and pharmacodynamics (PD); data is summarized in . shows ADME characteristics for compound and as

• Mass spectrometry MS analysis and

  2023-01-14

  

  Mass spectrometry (MS) analysis and selective enrichment methods of phosphorylated proteins are powerful tools that can help address these challenges. Recent advances in MS have made it possible to analyze signaling pathways by facilitating high-throughput identification of phosphorylation sites wit

• Small RhoGTPases are single domain nucleotide

  2023-01-14

  

  Small RhoGTPases are single-domain nucleotide-dependent binary switches that act as highly-tuned regulators in signal transduction [1]. The cycling between active GTP-bound and inactive GDP-bound forms allows RhoGTPases to bind to or to dissociate from downstream effectors, respectively [2]. Guanine

• br LO and the secretase complex Supporting this

  2023-01-13

  

  5LO and the γ-secretase complex Supporting this concept, during a recent trial testing the γ-secretase inhibitor semagacestat (LY 450139), AD patients actually experienced a functional decline compared to patients who took a placebo in addition to several other significant adverse effects (Doody

• 3-Methyladenine Application of the broad acting HTR antagoni

  2023-01-13

  

  Application of the broad-acting 5-HTR antagonist methiothepin (Bard et al., 1996, Hoyer et al., 1994, Peroutka, 1990) converted the TBS-induced response of both thalamocortical and intracortical A1 synapses from LTP to LTD, an effect that was mimicked by the selective 5-HT2R antagonist ketanserin (L

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