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To date methods for the simultaneous analysis
2019-12-06
To date, methods for the simultaneous analysis of multiple probe drugs in the plasma have been described by using HPLC-DAD or LC–MS/MS. Although previous cocktail methods have used combinations of those four or other probe drugs with LC–MS/MS methods, most of those studies focused on only the analys
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Pyrazolopyrimidines are bioisostere of purine exhibit promis
2019-12-06
Pyrazolopyrimidines are bioisostere of purine exhibit promising antitumor activity by competitively binding to the ATP active site of different kinase C527 [16,17]. Several compounds of this family were found to induce apoptosis and/or reduce cell proliferation in various solid tumour and leukaemia
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Signal transduction through IL c FMS ligand receptor also le
2019-12-06
Signal transduction through IL-34/ c-FMS ligand receptor also leads to the differentiation, survival and, angiogenesis, proliferation, adhesion and migration of cells of the monocyte/macrophage lineage similar to that of CSF-1 through the various pathways-First is through FAK (Focal Adhesion Kinase)
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Although the implication of DA
2019-12-05
Although the implication of DA and glutamate signaling crosstalk in drug-evoked neuronal adaptations is well acknowledged, targeting the cognate receptors to alleviate symptoms is associated with a loss of efficacy over time and the appearance of severe sides effects, likely due to the involvement o
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Both meiotic COs and NCOs require DNA synthesis
2019-12-05
Both meiotic COs and NCOs require DNA synthesis, current data from sequencing also suggest that COs require more DNA synthesis than NCO 63., 64., 65.. However, analysis of the role of DNA synthesis in NCOs remains relatively uncharacterized. Emerging evidence points to a role for either Polδ or Polε
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Prostaglandin E receptor subtype EP
2019-12-05
Prostaglandin E receptor subtype 4 (EP4) is a transmembrane G-coupled protein receptor activated by prostaglandin E2 (PGE2). EP4 activation exerts anti-inflammatory effects in adipose tissue by dampening the levels of inflammatory chemokines [12]. In the mouse, EP4 deficiency aggravates fragmentatio
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In terms of its protease activity
2019-12-05
In terms of its protease activity, MME has a broad range of substrates being able to target glucagon, bradykinin, GLP1, and several other AZD 7762 of circulating small molecules [25]. MME has been shown to target free insulin B-chain [32], although whether MME could target and degrade the insulin r
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CYP A and CYP D are among the
2019-12-05
CYP3A4/5 and CYP2D6 are among the main drug-metabolizing enzymes in humans that are responsible for the metabolism of more than 50% of marketed drugs [19], [21]. Drugs metabolized by CYPs are prone to drug–drug interactions, thereby modifying their response [18], [32]. Metabolic inhibition is also i
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Nimodipine is an L type calcium
2019-12-05
Nimodipine is an L-type calcium channel antagonist that reduces excessive calcium influx during pathological conditions, contributing to its neuroprotective properties (Zornow and Prough, 1996; Kobayashi and Mori, 1998). Autophagy can be induced by increased [Ca2+] (Rami et al., 2008). Nimodipine si
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Studies have focused on a hydrophobic cage at
2019-12-05
Studies have focused on a hydrophobic cage at the CULT domain, conserved from bacteria to mammals, as it binds to substrates and IMiDs (Chamberlain et al., 2014, Lupas et al., 2015). In addition, CRBN ligand-mediated protein degradation was highly conserved, which was confirmed in vertebrates by foc
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These studies suggested that PV PVH might
2019-12-05
These studies suggested that PV/PVH might promote bone formation activities and/or inhibit bone resorption activities probably due to its anti-inflammation activity; however, the underlying mechanism remained unknown. Furthermore, it is unclear if PVH shows better activity than that of PV; this is i
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Over the past decade targeting DNA repair proteins has
2019-12-05
Over the past decade, targeting DNA repair proteins has emerged as an effective tool to enhance chemosensitivity of malignant cells [9]. However, identification and selection of the proper target of DNA repair pathways is critical to increase cytotoxic activity of chemotherapeutic agents in cancer c
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We propose two different pathways for the production of
2019-12-04
We propose two different pathways for the production of this species: either that described by Dooley [24], where the phenol ring is first activated by binding of its oxygen to copper, or one where a copper-peroxo species would directly react with an active site tyrosine residue (Scheme 1B). This se
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br Prospect of DDR antagonist DDR
2019-12-04
Prospect of DDR2 antagonist DDR2, a receptor of tyrosine kinase has been found now to be reported to play a significant role in onset of osteoarthritis at the early stage of diseases progression. The DDR2 are the receptor for extracellular collagen and activated upon the binding of collagen resul
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br Hypothesis on DDR protective mode of action
2019-12-04
Hypothesis on DDR1 protective mode of action The documented protective role of DDR1 is quite impressive, demonstrated using different preclinical models (immunologic [46,54,58], obstructive [45], and hypertensive [50]) with different intervention paradigms: genetic ablation [45,50,58,72], silenci
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