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erk inhibitor The co crystal structure of GPR complexed with
2022-09-03
The co-crystal structure of GPR40 complexed with TAK-875 provided precise structural information for the rational design of novel GPR40 agonists. The key interactions between the carboxylate with the residues Arg183, Arg258, Tyr91 and Tyr240 of GPR40 were observed. And Trp174ECL2 was oriented nearly
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depicts the synthesis of series with
2022-09-03
depicts the synthesis of series with a four-step sequence. First, the commercially available 4-hydroxybenzaldehyde () was condensed with 2-bromoethanol through Mitsunobu reaction to give the key intermediate (). Next, conventional nucleophilic substitution reaction with the privileged structures (–
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Andexanet alfa works as a decoy
2022-09-03
Andexanet alfa works as a decoy for the FXa inhibitor to bind to irreversibly. The recently completed ANDEXA-4 trial, which was a prospective, open-label, single group study, found that patients achieved good or excellent hemostasis in 82% of subjects [, , ]. There was an overall 10% thromboembolic
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br Introduction Nasopharyngeal carcinoma NPC is a head and
2022-09-03
Introduction Nasopharyngeal carcinoma (NPC) is a head and neck epithelial malignancy with high prevalence in southern China, southeast Asia, and northern Africa [1,2]. NPC is caused by a combination of factors: infection with Epstein-Barr virus (EBV), environmental influences, and heredity [3]. A
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The first suggestion that the Hh pathway might
2022-09-02
The first suggestion that the Hh pathway might be involved in the pathogenesis of chronic liver disease was reported at the beginning of this millennium by Shackel et al. who noted that Patch and Gli were upregulated in their microarray analysis of liver tissues from patients with primary biliary c
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Cyclopamine a steroidal alkaloid type secondary
2022-09-02
Cyclopamine, a steroidal alkaloid type secondary metabolite from Veratrum californicum Durand (Melanthiaceae), serves as an anti-Hh constituent blocking the activation of Smo [96,100]. According to previous studies, cyclopamine was shown to inhibit the development of human hepatocellular carcinomas
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Camptothecin is a type of topo I
2022-09-02
Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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Roughly million people who are currently infected with
2022-09-02
Roughly 15 million people who are currently infected with HBV are co-infected with the hepatitis D virus (HDV) (WHO, 2017b). The superinfection not only leads to more severe liver damage and early onset of cirrhosis, but also to a higher mortality than HBV mono-infection (Rizzetto, 1983; WHO, 2017b)
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In recent large clinical studies AIM HIGH and HPS
2022-09-01
In recent large clinical studies, AIM-HIGH and HPS2-THRIVE, the additional treatment of nicotinic Baicalin australia to statin-based LDL-C lowering therapy did not decrease the major vascular events on the patients who had atherosclerotic vascular diseases [43,44]. In the AIM-HIGH study, the second
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One difficulty in studying gp is that it
2022-09-01
One difficulty in studying gp120 is that it binds to more than one receptor. Understanding how Norfloxacin respond to gp120 is complex because of this promiscuity. In an attempt to establish the contribution of CXCR4 in the antagonistic effect of gp120 on morphine-induced antinociception, AMD3100 w
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br Introduction The generic antifibrinolytic drug tranexamic
2022-09-01
Introduction The generic antifibrinolytic drug tranexamic Epidermal Growth Factor (EGF), human recombinant synthesis (TXA) inhibits the protein-protein interaction between plasminogen and fibrin [9]. TXA is frequently used to reduce bleeding in various hemorrhagic conditions, such as during surg
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br Conclusion Membrane transporters remain relatively
2022-09-01
Conclusion Membrane transporters remain relatively understudied in human disease, especially TBI (Cesar-Razquin et al., 2015), and considerably less is known in terms of expression, function and substrates of membrane transporters in pediatric patients. However, their importance in maintaining ar
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To maintain low Glu concentrations in the
2022-09-01
To maintain low Glu concentrations in the synaptic cleft below the affinity of its receptors, this amino description is rapidly removed from the extracellular space by a family of sodium-dependent high-affinity transport systems located mainly in the plasma membrane of perisynaptic astrocytes, and
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Ropivacaine HCl br Materials and methods br Results br Discu
2022-09-01
Materials and methods Results Discussion In nerve terminals, Na+-dependent glutamate transporters of the plasma membrane are responsible for the maintenance of low (non-toxic) extracellular glutamate concentrations and accomplish uptake of glutamate into the Ropivacaine HCl of neurons and
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br Regulation of Glu transporters The pivotal role of
2022-09-01
Regulation of Glu transporters The pivotal role of Glu transporters in the fine tuning and turnover of this excitatory amino terbinafine hydrochloride calls for a detailed characterization of its regulation. Several general mechanisms that modify Glu uptake activity have been described. These inc
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