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Our previous studies found that some
2023-10-20
Our previous studies found that some steroid mimetic structures such as stilbene, biphenyl, naphthalene and benzothiophene rings were suitable for lipophilic moieties of 17,20-lyase inhibitors, and several inhibitors obtained using a steroid A, C-ring mimetic approach have already been published. Du
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Thus one possible target for CRPC treatment
2023-10-20
Thus one possible target for CRPC treatment is the enzyme 17,20-lyase, which plays a crucial role in androgen biosynthesis. This is because inhibition of 17,20-lyase would be expected to decrease serum androgen levels secreted not only by the testes but also by the adrenal glands.7, 8, 9 In recent
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Because the V ATPase inhibitors
2023-10-20
Because the V-ATPase inhibitors that have been employed in these studies (including bafilomycin and concanamycin), are membrane permeant, they inhibit all the V-ATPases in the cell. This is important since it is possible that intracellular V-ATPases, in addition to those present at the plasma membra
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An alternative more rarely used electron microscopy based ap
2023-10-20
An alternative, more rarely used, electron microscopy-based approach exploits labeling of phagosomes with DAMP (3-(2,4-dinitroanilino)-30-amino-N-methyldipropylamine). DAMP is a weakly basic compound which is membrane-impermeable once it has been protonated. This way, DAMPH+ accumulates in acidic in
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br Introduction Lung cancer is
2023-10-20
Introduction Lung cancer is the leading cause of cancer death worldwide and is one of the most refractory of solid tumors along with pancreatic cancer. Since 1975 there have been notable improvements in the 5-year survival rate of patients with lung cancer [1]. This improvement in survival is tho
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Although the exact mechanisms are not
2023-10-20
Although the exact mechanisms are not fully understood, IGF-1 is tightly linked with ER and estrogen actions and a crosstalk occurs between these two systems in breast cancer. To illustrate this close relationship, studies have identified a synergy between IGF-1 and estrogen in Bikinin expressing b
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Pancuronium dibromide br Materials and methods br Results br
2023-10-20
Materials and methods Results Discussion Pulmonary fibrosis is a progressive and chronic lung disease and its typical features include Pancuronium dibromide proliferation, epithelial injury, chronic interstitial inflammation, increased extracellular matrix (ECM) production, and collapse of
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In order to postulate its binding mode
2023-10-19
In order to postulate its binding mode in APN, trovafloxacin 13v was docked into the active site of APN (PDB code: 2DQM) using Sybyl_X 1.3. As illustrated in Fig. 5A, the catalytic zinc ion of APN was chelated by the hydroxamate moiety of 13v, and the S1, S1′ and S2′ pockets of APN were occupied by
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OCT also is known as POU F plays
2023-10-19
OCT4 (also is known as POU5F1) plays an important role in embryonic stem cell self-renewal, development and reprogram somatic cell into pluripotent stem cell [[5], [6], [7]]. Recently, many studies also find OCT4 promotes the progression of many tumors. For example, Wnt/β-catenin promotes the expans
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There are two ways to transport FFAs
2023-10-19
There are two ways to transport FFAs into cells. First by passive diffusion. Second as the putative long-chain fatty Ac-YVAD-CHO transporters are proposed, CD36 the plasma membrane-associated fatty acid-binding protein (FABPpm) and fatty acid transport proteins (FATP) [11], where CD36 is responsibl
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NLX a k a F
2023-10-19
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity at 5-HT1A receptors, and, in dextromethorphan hydrobromide to the 5-HT1A receptor agonists listed above, it presents exceptional selectivity and high efficacy at these receptors (Colpaert et al., 2002, Newman-Tancredi et al., 2017).
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In the previous study we
2023-10-19
In the previous study, we demonstrated the importance of the mPFC postsynaptic 5-HT1A receptor in the sustained antidepressant effects, because a sustained antidepressant effect was obtained with intra-mPFC injection, but not systemic injection of 8-OH-DPAT, a 5-HT1A receptor agonist (Fukumoto et al
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The second evidence comes from the results obtained by patch
2023-10-19
The second evidence comes from the results obtained by patch-clamp recordings carried out at the endplate region of isolated mouse FDB fibers, where adenosine and the P1R agonist NECA significantly affected the NPo, the open frequency and the time constant τ of the adult nAChR channels. It is genera
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JNJ-38877605 br Patients and methods The severity
2023-10-19
Patients and methods The severity of disease documented at each outpatient visit was graded according to the modified Osserman classification: grade I, focal disease (e.g. restricted to ocular muscles); grade II, generalised disease that is mild (IIa) or moderate (IIb); grade III, severe generali
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CYP A is one of the key metabolizing enzymes
2023-10-19
CYP3A4 is one of the key metabolizing Helioxanthin derivative 5-4-2 of the cytochrome P450 (CYP) superfamily of heme-containing monooxygenases. As the CYP family of enzymes plays important roles not only in the xenobiotic metabolism and detoxification of a large number of drugs, but also in the bio
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