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Overexpression of AR can lead to sorbitol accumulation leadi
2024-03-06
Overexpression of AR can lead to sorbitol accumulation, leading to diabetic complications (Ransohoff and Cardona, 2010). Therefore, AR is an important enzyme in the growth and development of organisms. With the aim of inhibiting the activity of AR in diabetic patients, screening for inhibitors and i
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br Concluding Remarks and Future
2024-03-06
Concluding Remarks and Future Perspectives Disclaimer Statement Introduction Aldehyde dehydrogenase ALDHs (E.C. 1.2.1.3) are multigene family of NAD(P)+-dependents group of structurally and functionally related ubiquitously distributed enzymes involved in the specific and irreversible oxida
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br Theoretical mechanism of ABCA activity in
2024-03-06
Theoretical mechanism of ABCA2 activity in LE/LY in modulation of cholesterol trafficking It is important to confirm that ABCA2 is a lipid transporter and identify the substrates that are mechanistic in its cholesterol sequestering activity. We hypothesize that ABCA2 modulates cholesterol sequest
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Molecular docking is widely used
2024-03-05
Molecular docking is widely used to predict the interaction between an enzyme and its inhibitors. This is a computational simulation approach that can be used as a tool to investigate the structure-activity relationship of ACE inhibitory peptides (Goodsell, 2009). It has been recently shown that ACE
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Ginkgolic Acid C15:1 receptor HT modulates cortical and hipp
2024-03-05
5-HT modulates cortical and hippocampal pyramidal cell function in a very complex manner, since most 5-HT receptor subtypes (excitatory as well as inhibitory) are expressed on pyramidal Ginkgolic Acid C15:1 receptor as well as GABAergic interneurons that exert inhibitory control over pyramidal cell
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A review has recently been published
2024-03-05
A review has recently been published to evaluate the potential effects of food, alcohol and 17-ODYA juices on the pharmacokinetics and pharmacodynamics of the drugs for BPH. The authors reviewed the PubMed database during the years 1991–2015. In addition, a digital version of Stockley on drug inter
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Thus one possible target for CRPC treatment
2024-03-05
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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A previous review article suggested different
2024-02-23
A previous review article suggested different washout intervals based on specific clinical contexts [4]. While no consensus was reached for the optimal interval between last dose of BV and surgery for CRLM, the authors of the review suggested waiting 6 to 8 weeks after BV before surgery, particularl
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To the best of our knowledge this is the
2024-02-23
To the best of our knowledge, this is the first study documenting the SCC modulatory effect at central and kidney level on the shift in the vasoconstrictor-vasodilator ratio of mRNA expression of angiotensin receptors toward vasoconstriction in XY-SCC and/or vasodilation in XX-SCC mice. From these r
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In order to postulate its binding
2024-02-23
In order to postulate its binding mode in APN, rock pathway 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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br Introduction Several studies have found that hypothalamic
2024-02-23
Introduction Several studies have found that hypothalamic Akt-mediated signaling pathways play critical roles in the regulation of food intake and BQ-123 metabolism in mammals [[1], [2], [3], [4], [5], [6]]. Central injections of the inhibitor of phosphoinositide 3- kinases (PI3 K, an upstream re
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This chemistry paved way for
2024-02-23
This chemistry paved way for multi-gram synthesis of which was utilized for extensive piperazine benzamide SAR exploration. Depicted in , the two-step operation towards final targets involved standard amide coupling conditions with EDC or HATU followed by Boc deprotection under acidic conditions. S
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LiCl The enzyme mediated ATP sensing mechanism in
2024-02-23
The enzyme-mediated ATP-sensing mechanism in zebrafish can be compared with previous studies in other animal species reporting that enzymatic conversion of chemicals in the peripheral olfactory organ results in either “activation” or “inactivation” of odorants and pheromones. In male silkmoth, the a
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dofetilide Later the same group designed and prepared severa
2024-02-23
Later, the same group designed and prepared several Δ16-steroidal C17 benzoazoles and pyrazines and evaluated their CYP17 and 5α-reductase inhibitory activities, binding to and transactivation of the AR, as well as their antiproliferative effects against two human PC cell lines (LNCaP and LAPC4) [18
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In this paper we described
2024-02-23
In this paper, we described synthesis, biological evaluation and docking study of 3-aroyl-1-(4-sulfamoylphenyl)thiourea derivatives 4a–o as 15-lipoxygenase inhibitors. Results and discussion Conclusion We designed and synthesized a novel of thiourea derivatives containing phenylsulfonamide mo
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