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In order to postulate its binding mode
2024-05-17
In order to postulate its binding mode in APN, Beclomethasone dipropionate 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 wer
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br Materials and methods br Results br Discussion
2024-05-17
Materials and methods Results Discussion Prostate cancer is the most common cancer in men in the United States and the second leading cause of cancer death. Therapeutic interventions include mainly: radical prostatectomy or radiation therapy (RT), with or without androgen deprivation therap
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Since the publication of the guidelines data
2024-05-17
Since the publication of the 2011 guidelines, data have continued to accumulate indicating that the cognitive decline in AD occurs continuously over a long period [6–8], and that progression of biomarker measures is also a continuous process that begins before symptoms [9–14]. Thus, the disease is n
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In brief serotonin can interact with classes
2024-05-17
In brief, serotonin can interact with 7 classes of receptors are differentiated into 14 subtypes (Barnes and Sharp, 1999). Specifically, 5-HT1A and 5-HT2C receptors have been the most widely studied in the modulation of anxiety responses (Deakin et al., 1992; Millan, 2003). However, the studies that
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Control of retinal vascularization during
2024-05-17
Control of retinal vascularization during development and OIR likely involves close interactions among endothelial cells, neurons and glial antibiotics (microglial and astrocytes) (see Fig. 2). In particular, the interaction between endothelial tip cells and astrocytes plays a critical role in deve
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plx4720 synthesis br Results and discussion The classical ra
2024-05-17
Results and discussion The classical radiochemical adenosine kinase assays developed to monitor AdK activity utilize [3H]adenosine or [14C]adenosine, respectively. The assays are terminated by spotting the incubation mixture onto diethylaminoethyl (DEAE) anion exchange filter disks or onto a poly
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A high throughput small molecule ACK biochemical inhibition
2024-05-17
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 AMG-458 to be both ATP-competitive and reversible. Early structure-activity relationship (SAR) work was perf
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An alternative to the agonist
2024-05-17
An alternative to the agonist or antagonist potential in drug discovery is the positive allosteric modulator (PAM) approach, which can augment the normal processes of neurotransmission as opposed to directly replacing or antagonizing them. PAMs are thought to bind to sites that are distinct from the
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Additional evidence for a putative role of COXs and
2024-05-17
Additional evidence for a putative role of COXs and 5-LOX in AD derives from pharmacological studies using inhibitors of these enzymes (for review, see Firuzi and Praticò, 2006). In addition to helping delineate the pathobiological mechanisms of AD, these results raise hope for discovering novel the
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Regarding brain tumors AXL has been implicated in gliomagene
2024-05-17
Regarding Tubastatin A HCl tumors, AXL has been implicated in gliomagenesis and chemoresistance [39]. Previous investigations found that AXL is constitutively phosphorylated in many glioma cell lines, murine xenograft tumors and primary patient tumor samples [40]. Immunohistochemical analysis of AX
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br The complementary role of chaperone mediated autophagy
2024-05-16
The complementary role of chaperone mediated autophagy Chaperone-mediated autophagy (CMA) mediates the degradation of specific cellular proteins and participates in the regulation of lipid metabolism, DNA repair, or the response to stress (Kaushik and Cuervo, 2018). CMA provides an alternative pa
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While it is known that circulating LDL
2024-05-16
While it is known that circulating LDL-C levels are largely regulated by either controlling the rate of hepatic production of its triglyceride-rich precursor VLDL particle or the rate of LDLR-mediated LDL particle clearance [58], it should be noted that important differences exist between rodents an
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AP activation is known to
2024-05-16
AP-1 activation is known to upregulate downstream target genes including stat 3 inhibitor D1, c-myc, Bcl-xl, MMP-9, EGFR, and specific miRNAs that are involved in progression and metastasis of tumors. Moreover, matrix metalloproteinase-2 has been shown as a downstream gene of AP-1, triggered by 15-H
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Another contributor for the G M arrest in
2024-05-16
Another contributor for the G2/M arrest in A549 and H1299 cells might be p21WAF1/CIP1 which was up-regulated upon ovatodiolide treatment. p21WAF1/CIP1 is a common CDKs inhibitor which blocks COG 133 G2/M phase progression in various types of cancer cells (Kim et al., 2015, Liberio et al., 2015). It
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The growth of cancer can control by
2024-05-16
The growth of cancer can control by inhibiting the rate of cell proliferation or increasing the rate of selective apoptosis and effectiveness of anticancer agents varies according to genetic constitution of cancer. Hence, we investigated the anticancer activity of arginase against different kinds of
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