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A promising target that is involved in the biosynthesis
2024-10-26
A promising target that is involved in the biosynthesis of the precursor LTA4 is the 5-LO-activating protein (FLAP), which in vivo is seemingly indispensable for LT formation [8], [9]. FLAP, a member of the MAPEG family (membrane-associated proteins in eicosanoid and glutathione metabolism), is an i
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br Results and discussion br
2024-10-25
Results and discussion Conclusion In summary, a series of indazole-based derivatives were synthesized and SAR studies conducted, with view to the development of a novel Aurora kinases inhibitor. The carboxylic KU-0060648 synthesis group extending from the C-3 position of the aniline and subst
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br Introduction The term antioxidant derives from the
2024-10-25
Introduction The term antioxidant derives from the prevention of the oxygen consumption. In the late of 19th centuries, antioxidants were generally used in industrial processes such as against to metal corrosion, vulcanization of rubber. Later on, the use of antioxidants to prevent the rancidity
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br Mechanism of action In general
2024-10-25
Mechanism of action In general, the main targets for antifungal drug development are cell wall polymer (glucans, chitin, mannoproteins), cell membrane (especially ergosterol) biosynthesis, DNA and protein synthesis (topoisomerases, nucleases, elongation factors and myristoylation), and signal tra
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For the derivatives a c another likely explanation for
2024-10-25
For the derivatives 3a–3c, another likely explanation for antifungal properties is that polymers bearing primary amine groups and secondary phosphoryl groups formed, enhancing complexation with the phosphate groups, and the complexes are amphiphilic (Palermo, Lee, Ramamoorthy, & Kuroda, 2011). The a
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On the contrary Birrel and
2024-10-25
On the contrary, Birrel and colleagues observed divergent proliferative responses to androgens in different BC cell lines: DHT and mibolerone were found to inhibit the T47-D and ZR-75-1 bioactive growth, while the proliferation of MCF-7 cells was increased by both the androgens [53]. It is worth no
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Some members from the AAAP family
2024-10-25
Some members from the AAAP family, namely the AUX1 and the LAX proteins, transport auxin instead of amino acids [48]. While there is some structural relationship between IAA and Trp, the substrate recognition characteristics seem different for these proteins: the auxins do not have any amino group o
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br Conclusions br Introduction During numerous physiological
2024-10-25
Conclusions Introduction During numerous physiological processes, aldehydes are generated from a variety of endogenous and exogenous precursors including amino acids, carbohydrates, and lipids [1]. Most aldehydes are highly reactive and cytotoxic due to the strong electrophilic nature of the t
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Differentiation of skeletal myoblasts is
2024-10-25
Differentiation of skeletal myoblasts is a tightly orchestrated process that involves myoblast proliferation, Fmoc-Ile-Wang resin withdrawal, expression of muscle-specific genes, and fusion into multinucleated myofibers (Horsley and Pavlath, 2004; Krauss, 2010). The maintenance of muscle mass is im
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This chemistry paved way for multi gram synthesis of which
2024-10-25
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.
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br A novel therapeutic strategy based
2024-10-24
A novel therapeutic strategy based on the APN and obesity paradoxes As shown above, the relationship of the serum APN concentration with health and disease states shows an inverted-U correlation, suggesting that moderate concentrations of serum APN are beneficial (Fig. 3). Given that both hypo- a
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Both subcutaneous s c and mucosal administration of s
2024-10-24
Both subcutaneous (s.c.) and mucosal administration of short synthetic peptide derivatives of AChR prevent the onset of EAMG, but do not treat ongoing EAMG [80], [81], [82], [83], [84], [85]. The selection of peptides for treatment is mainly based on the identification of immunodominant T- and B-cel
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Odanacatib The cellular mechanism underlying the CGS mediate
2024-10-24
The cellular mechanism underlying the CGS12066-mediated inhibition of glutamate release from hippocampal nerve terminals through presynaptic 5-HT1B receptors remains to be elucidated. 5-HT1B receptors are coupled to PTX-sensitive G proteins (Gi or Go) that have been shown to inhibit AC activity as w
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The gene SRD A encodes the
2024-10-24
The gene SRD5A2 encodes the 5-α-reductase enzyme, which converts testosterone into dihydrotestosterone. Although dihydrotestosterone levels are considerably lower than testosterone, dihydrotestosterone has a five-fold stronger binding capacity to the androgen receptor and, thereby, a considerably mo
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In conclusion AXL overexpression preexisted in a subgroup
2024-10-24
In conclusion, AXL overexpression preexisted in a subgroup of treatment-naive lung adenocarcinoma specimens harboring an activating EGFR mutation or in those with wild-type EGFR. Anti-AXL therapeutics delivered up front in combination with the EGFR inhibitor might overcome intrinsic or acquired resi
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