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TXNIP interacts with various proteins including NLRP Yoshiha
2021-10-07
TXNIP interacts with various proteins, including NLRP3 (Yoshihara et al., 2014, Zhou et al., 2010). Emerging evidence suggests that TXNIP plays a role in ER stress-mediated cell death and in the NLRP3 inflammasome activation step (Abderrazak et al., 2015, Lerner et al., 2012, Oslowski et al., 2012,
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According to the World Health Organization the average
2021-10-07
According to the World Health Organization, the average global intake of fat has increased by 20 g per person over the last half-century [21]. However, not all fats are the same and it is now well established that saturated and unsaturated fats, as well as trans fats, can act in opposing ways to inf
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The typical pharmacophore for GPR agonists contains four par
2021-10-07
The typical pharmacophore for GPR40 agonists contains four parts: head (acid moiety), central (phenyl ring), linker and tail (aromatic carbocyclic or heterocyclic ring) [20]. On the other hand, the chemical features that are required for the PPARγ agonists include hydrogen bond donors and acceptors
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Sumoylation is involved in regulating protein protein intera
2021-10-07
Sumoylation is involved in regulating protein-protein interactions, subcellular protein localization, protein stability, and transcriptional factor activity (reviewed in [29]). The small ubiquitin-like modifier (SUMO) protein is covalently attached to a lysine residue in a Ψ-K-X-D/E consensus sequen
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Current guidelines for thromboprophylaxis recommend the use
2021-10-07
Current guidelines for thromboprophylaxis recommend the use of vitamin K antagonists (eg, warfarin), low-molecular-weight heparin (LMWH), or indirect inhibitor of factor Xa . Aspirin is also used for thromboprophylaxis in patients undergoing orthopedic procedures , . The efficacy and safety of LMWH
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A compound structurally similar to PF has been developed
2021-10-07
A Erismodegib structurally similar to PF-03654746 has been developed by Pfizer (PF-03654764), with a minor change in the substituent attached to the cyclobutanecarboxamide moiety (Wager et al., 2011). This compound, with the chemical name trans-3-fluoro-3-[3-fluoro-4-(pyrrolidin-1-ylmethyl)phenyl]-
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It should be noted that
2021-10-07
It should be noted that one of the two phenyl groups of 15 is found in the main western pocket and the second phenyl group occupies the western secondary pocket (Ser53, Leu54, and Leu213). The nitrogen of the amide bond is involved in a hydrogen bonding interaction with Asp140. The alcoholic functio
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The rationale for developing HDACi as anticancer
2021-10-07
The rationale for developing HDACi as anticancer agents was based on their ability to induce the hyperacetylation of histones and nonhistone proteins, resulting in increased differentiation, apoptosis, and NNC 55-0396 arrest of cancer cells 1, 2, 3. HDACi have been used in the treatment of hematolo
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HPgV coinfection has been associated with
2021-10-07
HPgV coinfection has been associated with reduced liver disease in HPgV/HCV/HIV triply infected patients (Barbosa Ade et al., 2009, Berzsenyi et al., 2007, Berzsenyi et al., 2009, Berzsenyi et al., 2011). It is possible that HCV NS3 protease inhibitors could inhibit HPgV replication diminishing its
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br Activation of soluble guanylate cyclase The molecular ste
2021-10-07
Activation of soluble guanylate cyclase The molecular steps involved in sGC activation have evolved significantly over the last several years. The key studies are outlined below, but here we provide an overall summary. The activation mechanism of sGC was initially proposed to be relatively simple
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SJB2-043 br Structural studies of GCAP
2021-10-07
Structural studies of GCAP Recoverin was the first member of this subfamily of Ca2+-binding SJB2-043 to be investigated by structural methods [27], [54], [55], [56], [57], [58]. These proteins have four EF-hands arranged in pairs that give rise to amino- and carboxyl-terminal domains. The crysta
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Importantly both genetic deletion and pharmacological inhibi
2021-10-03
Importantly, both genetic deletion and pharmacological inhibition of FAAH also reduced NTG-induced neuronal hyperactivity in the trigeminal nucleus, which receives sensory input from craniofacial deep tissues. NTG is known to evoke the robust neuronal activation, as evidenced by the induction of the
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This crosstalk may be responsible for the beneficial effects
2021-10-03
This crosstalk may be responsible for the beneficial effects of histamine H2 receptor inverse agonists on Zacopride hydrochloride pathologies and may also explain unwanted effects of these drugs on other tissues. In this way, Allen et al. reported an anaphylactoid reaction following cessation of hig
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br Introduction Hepatitis B virus HBV infects about
2021-10-03
Introduction Hepatitis B virus (HBV) infects about 2 billion people worldwide and is a leading cause of liver disease including liver fibrosis, cirrhosis and hepatocellular carcinoma (Trepo et al., 2014). Most current HBV therapies are based on nucleos(t)ide analogs and pegylated interferon alpha
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Next to their indirect effect on
2021-10-02
Next to their indirect effect on ASBT expression, microbiota are also directly involved in BA homeostasis and FXR-FGF15/19 signaling. Different species of intestinal microbiota have the ability to biotransform BAs mainly by deconjugation and subsequent de-hydroxylation, the latter resulting in more
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