• Brain damage diseases such as cerebral

  2023-10-01

  

  Brain damage diseases, such as cerebral ischemia, brain trauma and infection are characterized by the increase in oxygen free radicals. Therefore, deeper understanding of the character and mechanism of free radical damage in the brain is important to ultimately relieve diseases and promote recovery

• The inhibition of ACLY induces an anticancer effect that has

  2023-09-28

  

  The inhibition of ACLY induces an anticancer effect that has been reported to be involved in mitochondrial reactive oxygen species (ROS) generation [14], [16], dual blockade of mitogen-activated protein kinase and phosphatidylinositol-3-kinase/AKT pathways [11], and the glycolytic phenotype of tumor

• Illustrated in is the protocol we

  2023-09-28

  

  Illustrated in is the protocol we applied for the screens of novel furoic acids as ACL inhibitors. We constructed our furan carboxylate library that contained 1446 2-furoic Benzoylmesaconitine derivatives and 501 3-furoic acid derivatives by performing substructural searches of the ZINC database.

• br Results br Discussion ER

  2023-09-28

  

  Results Discussion ER and GR play opposite phenotypic roles in the normal endometrium, with ER promoting growth and GR inhibiting growth. Here, we show that in endometrial cancer, GR expression is associated with worse outcomes and higher-grade tumors, and this association is observed only in

• Castanospermine TUNEL assay Apoptotic DNA fragmentation in c

  2023-09-28

  

  TUNEL assay. Apoptotic DNA fragmentation in Castanospermine was measured using a commercially available TUNEL assay kit (Thermo Fisher). Frozen cells were fixed with 10% paraformaldehyde/PBS. Apoptosis was determined by staining the 3′-OH ends of fragmented DNA with biotin-dNTP using DNA I klenow f

• br Other Strategies for HIF Inhibition NSC is another

  2023-09-28

  

  Other Strategies for HIF-α Inhibition NSC-644221 is another HIF-α inhibitor acting at the translational level, independently of proteasomal degradation and VHL status, and is devoid of DNA damage-inducing properties [70]. NSC-644221 arrests dna ligase in G2–M through a cell type-specific Topo-2-

• In addition to differential expression of AR protein primari

  2023-09-28

  

  In addition to differential expression of AR protein primarily in surgical specimens, genetic alterations involving the AR gene have been documented in human U 18666A cancer. Loss of heterozygosity at the AR locus was identified in all 3 informative cases of muscle-invasive bladder tumors, whereas,

• While there is much in vivo work on

  2023-09-28

  

  While there is much in vivo work on prion-like Aβ, it has not been shown that one can induce inclusions of Aβ in cultured cells as has been shown for tau and α-synuclein. One reason is practical; Aβ is a low molecular weight metabolite cleaved from within the larger amyloid precursor protein (APP) a

• br Material and methods br Results Table shows that in

  2023-09-28

  

  Material and methods Results Table 1 shows that in addition to Leu/CysAP and DPPIV, genes for AspAP, ArgAP, MetAP, APM and PSA are expressed in adipocytes. The kinetic parameters of these AP are also shown in Table 1, revealing that APM has the highest Vmax and catalytic efficiency (Kcat/Km),

• Secondly as pointed out by Sulentic and

  2023-09-28

  

  Secondly, as pointed out by Sulentic and Kaminski in their recent paper [90], most of the AhR literature to date has focused on mouse AhR. Although both mouse and human AhR are interchangeable in many in vitro systems, the in vivo ligand binding affinity is drastically different between the two AhRs

• agonists simulate norepinephrine NE in binding to presynapti

  2023-09-28

  

  α2 agonists simulate norepinephrine (NE) in binding to presynaptic surface autoreceptors, which in turn mediates feedback inhibition of NE release. Another major control mechanism for noradrenergic neurotransmission is termination of signaling by presynaptic NE transporter (NET)-mediated NE reuptake

• The physiological effect of adenosine is now considered a ne

  2023-09-28

  

  The physiological effect of adenosine is now considered a new direction in halting the progression of organ damage in cardiovascular disease [24], [25], [26]. Adenosine has diverse functions, depending on its interaction with different receptor subtypes: A1, A2A, A2B, and A3[24], [25], [26]. Stimula

• Small RhoGTPases are single domain

  2023-09-28

  

  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

• In conclusion AXL overexpression preexisted in

  2023-09-27

  

  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

• Pyrimidine is the important pharmacology

  2023-09-27

  

  Pyrimidine is the important pharmacology core in many Aurora inhibitors, such as VX-680, ENMD-2076, CYC-116 and ENMD-2076 [12]. To identify additional effective Aurora inhibitors, we designed a series of 2,4-diaminopyrimidine compounds, our modeling studies suggested that the future core as well a

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