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Our data indicate that the D domain only
2024-12-16
Our data indicate that the D1 domain only needs to hydrolyze ATP a few times, or perhaps even just once, during the processing of a given substrate molecule, whereas the D2 domain hydrolyzes ATP many times. Consistent with this model, only D2 contains the canonical aromatic pore loop residues implic
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In HepG cells compound showed
2024-12-16
In HepG2 cells, glucokinase 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 s
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Bioavailability has been defined as the amount of a
2024-12-16
Bioavailability has been defined as the amount of a drug given by any route, other than intravenously, that reaches general circulation and is available at the site of action [86]. The low bioavailability observed with the initial intravaginal devices (16%) was attributed to the melting point of the
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Introduction It has long been
2024-12-16
Introduction It has long been recognized that angiogenesis is critical to the growth, progression, and metastasis of many solid tumor types [1], and thus, drugs targeting the angiogenic pathway have been a topic of clinical investigation in the oncology community for many years. Angiogenesis is reg
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Since natural and recombinant glycoprotein hormones exhibit
2024-12-16
Since natural and recombinant glycoprotein hormones exhibit some differences in their carbohydrate structures, we checked whether this could affect the permissive effect on FSK-induced cyclic AMP response in MLTC-1 cells. Fig. 6 shows that the same sensitizing effect to FSK is observed with pituitar
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5-Ethynyl-2'-deoxyuridine The most widely recognized eff
2024-12-16
The most widely recognized effects of adenosine are operated through inhibiting A1R, one of the most abundant G protein-coupled receptors in 5-Ethynyl-2'-deoxyuridine tissue [53]. A1R are located presynaptically, postsynaptically and nonsynaptically [54]. Effect of adenosine in neuronal circuits of
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At the last follow up nine patients had discontinued
2024-12-13
At the last follow-up, nine patients had discontinued pyridostigmine within the first year postoperatively. Only one patient required pyridostigmine at a higher dose, but this was accompanied by successful weaning of prednisolone. None of the 5 patients who were on pyridostigmine treatment alone pri
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br ARIs in the prevention of
2024-12-13
5ARIs in the prevention of prostate cancer Prostate cancer continues to be a leading cause of male deaths worldwide. In 2009, it was estimated there would be 192,280 new cases of prostate cancer with a predicted 27,360 deaths [25]. Because androgens, and specifically DHT, play a large role in bot
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Finasteride was the first steroidal
2024-12-13
Finasteride (13) was the first steroidal 5α-reductase inhibitor approved by the US Food and Drug Administration (FDA) in 1992 for treatment of BPH. In fact, long term clinical studies with this drug demonstrated a sustained reduction of the prostatic specific antigen and an overall improvement in B
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Aurora A and B are required
2024-12-13
Aurora A and B are required for the control of mitosis whereas Aurora C is mainly invoved in meiosis (Goldenson and Crispino, 2015). Interestingly, Aurora B is partnered with inner centromere protein (INCENP), survivin and Borealin to form a chromosomal passenger complex (CPC) that is critical for
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Functional implications notwithstanding the intermolecular
2024-12-13
Functional implications notwithstanding, the intermolecular contact appears to shield the Y361 side chain (Fig. 3) from being accessible for regulation by phosphorylation/dephosphorylation as has been proposed [18,19]. It is, therefore, likely that Src kinase and PTP1B phosphatase bind to an AROM mo
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The renin angiotensin system RAS is a
2024-12-13
The renin-angiotensin system (RAS) is a hormonal system which plays a role in the regulation of blood pressure and body fluid Plumbagin [14]. The main bioactive peptide of RAS is angiotensin II (Ang II) whose biological functions are interposed through angiotensin type 1 receptor (AT1R) and angiote
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The functional significance of the
2024-12-12
The functional significance of the cap residues with regard to the established role of PfA-M1 in hemoglobin catabolism in the food vacuole is a key question that is difficult to address with in vitro studies. We note that three of the dipeptide substrates used in our study are found in the sequences
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neurokinin receptor N terminally extended antigenic peptide
2024-12-12
N-terminally extended antigenic peptide precursors that survive cytosolic degradation and enter the ER, need to be further processed by ERAP1 and/or ERAP2, in order to acquire the right length required for MHCI binding. ERAP1 (ERAAP in mouse) is an IFN-γ-inducible, metalloaminopeptidase that trims N
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To date LOX is the only LOX isoform
2024-12-12
To date, 12-LOX is the only LOX isoform that has been identified in the platelet [17]. Interestingly, while 12-LOX is highly expressed (∼14000 molecules/platelet) in the platelet, 12(R)-LOX expression is absent in the hematopoietic lineage and has therefore not been reported to be expressed in plate
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