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Naltrindole hydrochloride Wu et al explored the anti
2021-07-23

Wu et al. explored the anti-inflammatory mechanisms by which osthole 35 acted on HepG2 cells cultured in a differentiated medium from cultured 3T3-L1 preadipocyte cells. HepG2 cells, a human liver cell line, were treated with various concentrations of osthole 35 in differentiated media from cultured
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LY 255283 Although further experiments are needed to determi
2021-07-23

Although further experiments are needed to determine definitively whether D–ETB receptor heterodimers exist, for example, by using fluorescence resonance LY 255283 transfer analysis or co-immunoprecipitation of receptors, the results of the study by Zeng and colleagues appear to indicate that D–ETB
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More importantly Santagata et al have suggested a new breast
2021-07-23

More importantly, Santagata et al. have suggested a new breast cancer subtyping method according to ER, androgen receptor (AR), and VDR with a higher prognostic value than the ordinarily used method based on ER, progesterone receptor (PR) and Her2 (Santagata et al., 2014). This implies that such com
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EPAC activation in VSMCs and ECs reverses
2021-07-23

EPAC activation in VSMCs and ECs reverses several processes involved in the development of in-stent restenosis. Of particular relevance is the ability of EPAC1 to induce SOCS3 gene expression, as SOCS3 exerts multiple protective effects in both cell types, while immunohistochemical studies have show
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Covalent inhibitors are well suited for targeting the E
2021-07-23

Covalent inhibitors are well suited for targeting the E1 BLZ945 of Ubl modifications. Because the E1 enzymes in Ubl modifications, such as the SUMO E1 and Atg7, have a slow turnover rate (Boggio et al., 2004), prolonged inhibition can be achieved without requiring compounds to be stable in circulat
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br Enzyme catalysis A biochemically spontaneous process proc
2021-07-23

Enzyme catalysis A biochemically spontaneous process proceeds in a direction where free Cy3-dUTP of the system decreases. However, every spontaneous or energetically favorable reaction needs to overcome an energy barrier known as the activation energy barrier because of the formation of an unsta
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br Materials and methods br Results Overexpression
2021-07-23

Materials and methods Results Overexpression of KLF2 increased the cell viability and reduced the LDH leakage rate and O2•− and ONOO− generation in H/R HUVEC model. To evaluate the effect of KLF2 on H/R HUVEC injury, KLF2 was overexpressed in HUVECs. Cell viability and extracellular LDH level
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Enolases are among the most abundantly expressed cytosolic p
2021-07-23

Enolases are among the most abundantly expressed cytosolic proteins. They are metalloenzymes that catalyze the conversion of 2-phosphoglycerate to phosphoenolpyruvate [18]. Eubacteria and archaebacteria have a single enolase gene (reviewed in [19]). Despite the lack of signal peptides or cognate pro
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Importantly MPO is not only a
2021-07-23

Importantly, MPO is not only a marker of cardiovascular disease but also emerges as a critical mediator of vascular inflammatory disease: Liberated MPO binds to the endothelium in a leukocyte-independent manner, is subsequently taken up by the endothelium and transcytoses and accumulates in the sube
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The discoidin domain receptors DDR and DDR are receptor tyro
2021-07-23

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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Nimodipine administration also inhibited the eIF
2021-07-23

Nimodipine administration also inhibited the eIF2α/ATF4 singnaling which is a crucial evolutionarily conserved adaptive pathway during cellular stresses including hypoxia and ischemia (Evans et al., 2016; Manwani and McCullough, 2013). While, the eIF2a/ATF4 pathway, activated by different forms of s
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br Rationale and hypothesis To discover an allosteric inhibi
2021-07-23

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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MuRF interacts with four and a half
2021-07-23

MuRF3 interacts with four-and-a-half LIM domain (FHL2) and γ-filamin leading to their degradation via UPS [64]. Conversely, abnormal aggregation of these proteins was observed in mice lacking MuRF3. Moreover, MuRF3-/- mice were found more prone to cardiac rupture after acute myocardial infarction (A
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br RING type E s
2021-07-23

RING-type E3s and their substrates There is enormous diversity in substrate ubiquitination and its regulation, as the targets of RING-type E3s are incredibly varied. RING-type E3s are implicated as tumor suppressors, oncogenes, and mediators of endocytosis, and play critical roles in complex mult
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While a number of studies have helped elucidate the
2021-07-23

While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub pcpt specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-RING interface in governing substrate
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