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HT receptors are distributed throughout
2024-09-30

5-HT3 receptors are distributed throughout the brain, within the brainstem (e.g., nucleus tractus solitarius, area postrema and spinal trigeminal nucleus) and 1,3-PBIT dihydrobromide (e.g., hippocampus, amygdala, nucleus accumbens, putamen and caudate) (Abi-Dargham et al., 1993, Barnes et al., 1989,
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Ac-IETD-pNA receptor ATM is generally regarded to be the pri
2024-09-30

ATM is generally regarded to be the principal mediator of the G1 Ac-IETD-pNA receptor checkpoint, whereas the induction of the intra-S-phase and G2/M checkpoints are usually primarily related to ATR function. However, several studies have demonstrated that, depending on the cellular context and typ
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Madecassic acid Enhanced arginase activity and the resultant
2024-09-30

Enhanced arginase activity and the resultant decreases in L-arginine levels can also impair T cell mediated immune function and allow tumor growth by limiting the supply of L-arginine needed for the formation of cytotoxic levels of NO by iNOS [10]. Increased arginase expression/activity may also lim
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Protein microarrays represent just one of a variety
2024-09-29

Protein microarrays represent just one of a variety of experimental approaches that can be used to generate datasets of relevance to pathway mapping. Other approaches include protein Bezafibrate receptor profiling techniques, such as antibody arrays [29], tissue arrays [30] and 2-dimensional gel el
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The functional significance of the cap residues with
2024-09-29

The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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Further validation for a role in LOX
2024-09-29

Further validation for a role in 12/15-LOX pathway in mediating adipocyte function comes from studies revealing a regulatory role of lipocalin-2 on 12/15-LOX activity. Lipocalin-2, a glycoprotein member of the lipocalin superfamily, is a novel abundant adipokine implicated in obesity-mediated inflam
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br The role of LOX plays in autophagy Autophagy is
2024-09-29

The role of 12/15-LOX plays in autophagy Autophagy is a process by which cellular material is delivered to lysosomal to degrade the damaged organelles and proteins to facilitate nutrient recycling (Towers and Thorburn, 2016). There has been characterized three types of autophagy-macroautophagy, m
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Imatinib was first approved for
2024-09-29

Imatinib was first approved for the treatment of Philadelphia chromosome positive chronic myelogenous leukemia in 2001 [25]. This first approved small molecule antagonist is quite unusual in that it provides a durable response that lasts for more than a decade in the majority of patients. Imatinib h
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In our previous study we found that
2024-09-29

In our previous study we found that the total activity of aldehyde dehydrogenase in cancer HQNO of RCC is at the same level as in normal renal tissue [10]. These findings are similar to our results in serum patients with renal cancer. There is no significant difference between ALDH activity in seru
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WM-2474 Introduction Mammalian cells express the
2024-09-29

Introduction Mammalian WM-2474 express the seven STAT family members STAT1, −2, −3, −4, −5A, −5B, and −6 [1], [2]. All STATs exert physiologically important roles as homo- and heterodimers [2], [3], [4]. Cytokines and growth factors activate STATs through the activation of kinases that phosphorylat
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The first rationally designed dual mPGES
2024-09-29

The first rationally designed dual mPGES-1/5-LO inhibitor was reported in 2008 and represents a structural derivative of pirinixic bioactive mg - a synthetic agonist of PPARα with lipid-lowering properties (Koeberle et al., 2008b). Further α-alkyl- and α-aryl-substituted derivatives have been synth
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In an effort to determine if one ARI was
2024-09-29

In an effort to determine if one 5ARI was more effective than the other, the Enlarged Prostate International Comparator Study (EPICS) [17] compared treatment with finasteride and dutasteride in 1630 men over the age of 50 and concluded that after one year of treatment, both groups had statistically
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The benzimidazole group seems to be a key
2024-09-29

The benzimidazole group seems to be a key feature for the excellent anti-tumor activity of galeterone (159), which motivated the synthesis of new steroidal inhibitors containing N-heterocyclic groups structurally related to benzimidazole. Thus, several 1H- and 2H-indazole derivatives of dehydroepian
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Moreover showed reduction in fibroblast growth
2024-09-29

Moreover, showed 73% reduction in fibroblast growth factor–induced neovascularization in a mouse corneal micropocket assay at a dose of 100mg/kg and 50% reduction at 50mg/kg. Both results were highly statistically significant (PMilrinone synthesis have recently shown only moderate efficacy (40% inhi
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Matthew et al synthesized and carried
2024-09-28

Matthew et al. synthesized and carried out SAR studies of imidazo-[1,2-a]-pyrazine as Aurora kinase inhibitors with enhanced kinase selectivity and found that AG-126 39 showed optimal potency on Aurora-A and Aurora-B with IC50 value of 4 nM and 13 nM while on phosphorylation histone H3 (pHH3), EC50
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