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When six chemical inhibitors were incubated with TRB
2020-11-13

When six chemical inhibitors were incubated with TRB or TRC and human liver microsomal preparation, HLM2, the results showed that ketoconazole (a CYP3A4 inhibitor) was very effective in inhibiting 4β-C hydroxylation of TRB and TR, whereas sulfaphenazole (a CYP2C9 inhibitor) and quinidine (a CYP2D6 i
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The totality of evidence from randomized clinical trials sup
2020-11-13

The totality of evidence from randomized clinical trials supports the premise that worsening 2-Amino-ATP failure is a class effect of DPP-4 inhibitors. A meta-analysis by Verma et al. (54) of 100 randomized controlled clinical trials reported that the use of DPP-4 inhibitors was accompanied a signi
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Lately using receptor TM peptides
2020-11-13

Lately, using receptor TM peptides, BiFC and PLA experiments, we have also obtained experimental evidence for the tetrameric structure of A1R–D1R, which explains the canonical interaction on Gi and Gs, respectively (Fig. 2). We have demonstrated for the first time the presence of this heterotetramer
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Given the widespread occurrence of oncogene
2020-11-13

Given the widespread occurrence of oncogene-induced RS and the increasing clinical interest in small molecule inhibitors that further exacerbate RS in human cancers (such as ATR inhibitors), our findings point to a protective role for RAD52 in the maintenance of cancer cell viability. As such, RAD52
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As DNA methylation plays a critical
2020-11-13

As DNA methylation plays a critical role in organismic development and human diseases, the interest in DNA methyltransferases is constantly increasing. Extensive studies on the repertoires of dnmts genes have indicated increasing dnmts members in eukaryotes (Goll and Bestor, 2005; Ponger and Li, 200
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Some family I DNA ligases can
2020-11-13

Some family I DNA ligases can use dATP as nucleotide cofactor. For instance, human Gap19 I uses dATP with a catalytic efficiency that is only 36-fold lower in comparison to ATP [9]. EhDNAlig is unable to use dATP as a nucleotide cofactor, indicating a more constrained active site in comparison to hu
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br Introduction Although not fully understood the molecular
2020-11-13

Introduction Although not fully understood, the molecular toxicology of sulfur mustard (bis(2-chloroethyl)sulfide, SM; CAS–Nr. 505-60-2), an alkylating warfare agent, has been attributed to DNA alkylation [1], [2], [3]. The same principle holds true for other alkylating compounds such as nitrogen
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br Experimental section br Author contributions br Acknowled
2020-11-13

Experimental section Author contributions Acknowledgements Introduction Many 740 Y-P in cells are sequential enzymatic reactions where the product of one enzyme serves as the substrate of a second enzyme (1, 2). Experimental evidence suggests that some of these consecutive enzyme-cataly
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Global inhibition of integrin signaling with EDTA here sugge
2020-11-13

Global inhibition of integrin signaling with EDTA here suggests that integrin signaling potentially cooperates with DDR2 in collagen induction of lysyl oxidase. This notion is supported by a recent study that shows DDR2 cooperation with specific integrins in cell adhesion to collagen [47]. It is of
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GSK126 receptor DDR distribution in healthy fibrotic and inf
2020-11-13

DDR1 distribution in healthy, fibrotic and inflamed tissues Whereas we can easily mine publicly available databases to infer DDR1 expression profile in different tissues (as reported in Fig. 1), fine comprehension of DDR1 biology has been hampered by the absence of a commercially available specific
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A number of immune relevant genes have
2020-11-13

A number of immune-relevant genes have been studied to explore the immunologic mechanisms in large yellow croakers; however, the chemokine receptor CXCR family has never been studied in this organism. Chemokines are a large superfamily of chemotactic cytokines that are utilized to direct the traffic
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br Material and methods br Results br Discussion br Conclusi
2020-11-12

Material and methods Results Discussion Conclusions To conclude, although CPT2 and CPT1 must have co-evolved to establish the carnitine shuttling, these enzymes are the most distantly related carnitine transferases, split early in evolution, during which a switch occurred in their locati
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P H is a nonheme iron
2020-11-12

P4H is a nonheme iron(II) dioxygenase that uses O2 and α-ketoglutarate as co-substrates (Fig. 1A). The three-dimensional structure of mammalian P4H is unknown. We reasoned that an electrophilic analog of α-ketoglutarate could serve as an irreversible inhibitor of the enzyme and, hence, a useful prob
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br Agonist binding ETA activation is promoted by binding of
2020-11-12

Agonist binding ETA activation is promoted by binding of the endogenous peptidergic agonists to their orthosteric binding site on the receptor. ET1 and ET2 (Trp6-Leu7-ET1) bind with equal high affinity to ETA, whereas the third endogenous isopeptide ET3 (Thr2-Phe4-Thr5-Tyr6-Lys7-Tyr14-ET1) binds
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br Introduction The cervix is a poorly
2020-11-12

Introduction The Irsogladine is a poorly studied component of the mare’s reproductive tract. It has anatomical and biological defense mechanisms involved in the delicate balance between immunological tolerance, sperm transport and biological defense. Anatomically, the cervix is composed of epith
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