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The extent to which GPCR oligomerization
2023-07-19

The extent to which GPCR oligomerization is a regulated process still remains unclear. Reported effects of ligands on both GPCR homo- and heteromers are highly variable and depend on GPCR subtypes and the specific ligand used. According to our data, chronic treatment of mice with both paroxetine or
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br There are three types of
2023-07-19

There are three types of 5-HT2 receptors. 5-HT2A, 5-HT2B and 5-HT2C receptors Exhibit 46–50% overall sequence identity and couple preferentially to Gq/11 to increase inositol phosphates and cytosolic [Ca2+] and in agreement with their long known role in muscle contraction and stimulation in the br
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Nalidixic acid synthesis Cofilin is an additional actin seve
2023-07-19

Cofilin is an additional Nalidixic acid synthesis severing protein present in sperm cells that undergo phosphorylation/inactivation on serine 3 by Lim kinases (LIMK) and by Tes kinases (TESK) [48]. LIMK can be activated by several pathways, including one through the Rho/ROCK/LIMK cascade [49], [50]
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ACK can be localized to clathrin
2023-07-19

ACK1 can be localized to clathrin-coated vesicles [1]. The association of SNX9 with synaptojanin-1 would suggest the two cooperate during endocytosis at the synapse by coupling the sorting nexin to changes in phospholipid composition. ACK1 in turn negatively regulates the association of SNX9 with ta
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br Methods br Transparency document br Introduction Epinephr
2023-07-19

Methods Transparency document Introduction Epinephrine (EP) is a critical hormone and catecholamine neurotransmitter in nervous system of mammals.1, 2, 3 It has been known to accelerate and regulate heartbeat, blood pressure, bronchodilation, mydriasis, blood sugar and lipolysis, and can he
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Given that there are substitutions between Anc and
2023-07-19

Given that there are 132 substitutions between βAnc and the human β subunit, we wondered whether βAnc could replace the human β subunit in hybrid AChRs formed from ancestral and human subunits. We first confirmed that the β subunit is required for expression of human AChRs in HEK293 PF2341066 by co-
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LO is a soluble kDa enzyme
2023-07-19

5-LO is a soluble 78 kDa enzyme, composed of an α-helix-rich catalytic domain and a regulatory β-sheet-rich C2-like domain. Depending on the cell type, 5-LO may be located in the cytosol, in the nucleoplasm, or in both compartments (Werz, 2002). Upon cell stimulation by agents that elevate intracell
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Docetaxel The knowledge on the structure of CYP
2023-07-19

The knowledge on the structure of CYP17, including its active site, provides a rationale for understanding many mutations that are found in enzyme dysfunction in clinical disease as well as the enzyme's dual hydroxylase and lyase catalytic capabilities. This knowledge will assist rational drug desig
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Axl has been reported to mediate cell cell adhesion
2023-07-19

Axl has been reported to mediate cell-cell adhesion and sphere-growth [11], [18] and to be important for metastasis to secondary organs [12], [14], [20]. We found an Axl-dependent CCRCC-ability of sphere-formation and repopulation after non-adhesive growth. Axl-inhibited cells could not attach to ea
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Small kinase inhibitors have been developed to block AXL by
2023-07-19

Small kinase inhibitors have been developed to block AXL by interacting with the kinase cytoplasmic ATP binding site. Up to date, no AXL selective kinase inhibitors are marketed. As depicted in , some marketed kinase inhibitors such as Bosutinib and Cabozantinib or kinase inhibitors in clinical pha
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Axl which belongs to the Tyro Axl
2023-07-19

Axl, which belongs to the Tyro-Axl-Mer (TAM) family of RTKs, has been reported to regulate a variety of physiological processes including cell survival, proliferation, migration and adhesion, through the activation of the phosphoinositide 3-kinase (PI3K)/V-akt murine thymoma viral oncogene homolog (
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Cancer cells manifest characteristic abnormal growth propert
2023-07-19

Cancer Anacardic acid manifest characteristic abnormal growth properties accompanying clonal evolution of cells displaying progressively increasing genomic instability capable of invasion and metastasis to distant organ sites. With the emerging knowledge about the role of known oncogene and tumor s
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flap inhibitor In our H K ATPase assay Fig and Supplementary
2023-07-19

In our H+, K+-ATPase assay (Fig. 1 and Supplementary Fig. 1), myricetin (IC50 = 0.58μM) was more potent than acid-activated omeprazole (IC50 = 1.50μM). In contrast, in oral administration in mice (Fig. 3), omeprazole (20mg/kg) more effectively inhibited gastric flap inhibitor secretion compared to
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In HepG cells compound showed inhibition of
2023-07-19

In HepG2 cells, Calyculin A showed inhibition of total lipid syntheses with an IC of 8μM. A cell based Alamar Blue cytotoxicity assay was used in parallel to differentiate the effect on the inhibition of lipid synthesis versus potential cytotoxicity. Under identical incubation conditions, compound
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Additionally we used the predicted Cyp a b
2023-07-19

Additionally, we used the predicted Cyp19a1b amino actin polymerization inhibitor sequence from a number of bony fish species to infer their genetic relatedness and found that R. quelen occupies an ancient position within the Siluriformes group. A phylogenetic tree was constructed and it included b
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