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The results of our study indicate
2022-07-04

The results of our study indicate the general importance of the gp120 V3 loop Epoxomicin patch in the subunit association of primate immunodeficiency virus Env trimers. Our observation that the stem insertion mutants and hydrophobic patch mutants exhibit similar phenotypes with respect to gp120 she
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Molecular properties as well as metabolic
2022-07-04

Molecular properties as well as metabolic stability in rat and human liver microsomes for the most active nitro (), nitrile (), methylsulfone (), and sulfonamides () analogues were measured (). All these derivatives possessed excellent membrane permeability as measured in the Pampa assay and further
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Among the compounds prepared at
2022-07-04

Among the compounds prepared at this stage, the cyclopropylmethylenoxy analogue attracted our most attention since it demonstrated particularly good in vitro potency at GlyT1 (16nM), no activity at the GlyT2 isoform up to the highest concentration tested (30μM), good physical properties with modera
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HSOR belonging to the aldoketo
2022-07-04

3α-HSOR, belonging to the aldoketo reductase superfamily, is a rate-limiting enzyme for the synthesis of 3α-reduced steroids, such as allopregnanolone and tetrahydrodeoxycorticosterone. 3α-HSOR was extensively expressed in the spinal dorsal horn and was upregulated following peripheral nerve injury,
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The ghrelin receptor is expressed in a number
2022-07-04

The ghrelin receptor is expressed in a number of human malignancies including prostatic carcinoma cell lines [18,19] and tissues [20], breast carcinoma tumours and cell lines [21], testicular tumours [22], and malignant ovarian cysts and tumours [23]. In addition, it has an elevated level of express
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By using pharmacological treatment with CBX
2022-07-04

By using pharmacological treatment with CBX or transgenic animals lacking the two major astroglial Cxs, the Double KO mouse, we demonstrated that the gap-FRAP technique was able to detect the total inhibition of GJC with a reduction of about 39% and 38% compared to control, respectively. The residua
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C prevents the glutamate and erastin
2022-07-02

C16 prevents the glutamate- and erastin-induced ROS accumulation but does not affect the decrease in GSH, indicating that prevention of ROS accumulation by C16 is not due to the restoration of GSH levels. Instead, C16 itself possessed superoxide anion scavenging activity in vitro at similar concentr
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br Introduction Fructose bisphosphatase FBPase
2022-07-02

Introduction Fructose 1,6-bisphosphatase (FBPase; EC 3.1.3.11) catalyses the irreversible reaction of hydrolysis of fructose 1,6-bisphosphate to fructose 6-phosphate and inorganic phosphate [1]. Genetic and kinetic studies so far have demonstrated that at least two distinct isoenzymes of FBPase e
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The binding of DHAP to aldolase resulted in a
2022-07-02

The binding of DHAP to aldolase resulted in a dramatic decrease of aldolase affinity to FBPase – KAapp was reduced more than 100 times. The dependence of the complex activity versus increasing DHAP concentration was biphasic (Fig. 3a). Supposedly, the first phase of the curve represents the state i
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Sumoylation is involved in regulating protein protein intera
2022-07-02

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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br Interference in coagulation assays Conversely to heparin
2022-07-02

Interference in coagulation assays Conversely to heparin, or heparin like octanoic acid (LMWH, Fondaparinux, Sodium Danaparoid), which are catalytic inhibitors requiring the presence of AT for their activity, as depicted on Fig. 2, DiXaIs are directly targeted to Factor Xa, and are reversible [39
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Introduction Post translational modifications to the N termi
2022-07-02

Introduction Post-translational modifications to the N-terminal tails of the histone proteins play crucial roles in genome regulation [1]. These modifications (e.g. acetylation, methylation, phosphorylation) are deposited by so-called ‘writer’ enzymes and dynamically removed by the action of ‘erase
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Recently IL was also identified
2022-07-01

Recently, IL-10 was also identified as an important mediator of collagen deposition in the development of HF [64,65]. It was shown, that this cytokine activates macrophages found in the hearts of mice suffering from diastolic dysfunction in the autocrine manner [64]. In response, specific subset of
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Finally we find that in the absence of
2022-07-01

Finally, we find that in the absence of Aurora B, Sgo1 is delocalized from centromeres and found along chromosome arms, as reported after depletion of Bub1 (Kitajima et al., 2005, Riedel et al., 2006). The increased arm cohesion observed in the absence of Aurora B activity is dependent on the presen
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To solve the atomic structures of several individual domains
2022-07-01

To solve the atomic structures of several individual domains and a complete molecular architecture of sGC, tangible experimental research work has been done which resulted in a cryo-electron density map of R. norvegicus. However, the full structure of the human sGC remains to be determined. In the p
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