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Raltitrexed Aromatization of the pyrrole ring after anion
2024-10-17

Aromatization of the pyrrole ring after anion capturing, using acceptor atoms with electron deficiency (B & Be), and substitution of strong electron withdrawing groups such as CN were three strategies used to design a new class of anion receptors. Comparison of the anion affinities of these anion re
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As aforementioned this study aimed to design
2024-10-17

As aforementioned, this study aimed to design, synthesize and investigate aromatase inhibitory and anti-breast cancer activities of N,N′-disubstituted thiourea derivatives. Based on the attractive phenotypic molecule 1, the synthetic N,N′-disubstituted thioureas have been designed including monothio
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On the other hand our
2024-10-17

On the other hand, our study permits to draw general conclusions about the complex functional pattern of C4HT, C8HT and C12HT, in comparison with the parent molecule HT and two reference compounds like Trolox and vitamin E. Table 1 summarizes the results obtained in the present investigation (for th
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br Epidemiology br Genetics The dominantly inherited
2024-10-17

Epidemiology Genetics The dominantly inherited PrP cerebral amyloidoses are genetically transmitted with a penetrance of almost 100%. Early linkage analysis studies helped to established the relationship between GSS and mutations in the PRNP gene. PRNP is located on the short arm of chromosome
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br Selective Androgen Receptor Modulators SARMs
2024-10-17

Selective Androgen Receptor Modulators (SARMs) The AR and its endogenous ligands, androgens, are important for development and maintenance of muscle and bone, secondary sexual organs, and development of other tissues (Mooradian et al., 1987). Although androgens are important for normal developmen
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br Obstructing SNARE zippering Sharma et al demonstrated for
2024-10-17

Obstructing SNARE “zippering” Sharma et al. demonstrated for the first time that in the postmortem AD brains, the level of SNARE complex formation, which is necessary for driving synaptic vesicle fusion at the presynaptic active zone, is significantly reduced [123]. In the absence of changes in e
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br Introduction There are greater
2024-10-17

Introduction There are greater than five million Americans living with Alzheimer's dementia and more than 35 million people worldwide [1], and without a way to stop or slow the progression, there will be nearly a tripling of individuals affected by 2050 (13.8 million) [1]. The urgency to develop
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These results validate the docked
2024-10-17

These results validate the docked pose of the ALR2-3e complex in comparison to the docked complex of the ALR2-4c complex of which the compound docked completely out of the binding pocket of ALR2 (). This concludes to that the removal of the acetic p-Cresyl sulfate moiety leads to inactive or weakl
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Additionally regulation of GPCR heteromerization
2024-10-16

Additionally, regulation of GPCR heteromerization by specific ligands may depend not only on the affinity of ligands for receptors, but also on presence of different interacting proteins co-localizing with the receptors in the specific cell, which may induce some conformational changes and contribut
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Fig A shows a schematic
2024-10-16

Fig. 2A shows a schematic representation of histological results according to the Franklin and Paxinos Mouse Brain Atlas (2001). The black circles represent the sites of drug infusion that were on-target within the amygdala. Gray circles represent the animals that had infusion locations outside the
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To assess relative metabolic activity and proliferation of c
2024-10-16

To assess relative metabolic activity and proliferation of fgfr inhibitor attached to various substrates we used the MTT assay [29], [30]. In order to compare the metabolic activity of cells under the various conditions irrespective of the number or viability of the cells, we performed a PicoGreen D
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Thus one possible target for CRPC treatment is
2024-10-16

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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Consistent with the observation that mutations in the redox
2024-10-16

Consistent with the observation that mutations in the redox-partner binding site of P450c17 that reverse charge from basic to acidic (R347H, R358Q) cause 17,20-lyase deficiency (Geller et al, 1997, Geller et al, 1999), at least one POR mutation that changes a residue in the FMN domain from neutral t
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br Dual role of autophagy in human diseases Emerging
2024-10-16

Dual role of autophagy in human diseases Emerging evidence suggests that autophagy serves as a double-edged sword in several human diseases, such as CNS diseases (Rubinsztein et al., 2015), arteriosclerosis (Schrijvers et al., 2011) and cancer (Ozpolat and Benbrook, 2015). Likewise, currently the
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With regard to the first
2024-10-16

With regard to the first question, subcellular fractionation studies revealed that BDK and PPM1K are clearly detectable in both the mitochondrial and cytosolic subcellular fractions, thus making it possible for these enzymes to interact with both the BCKDH and ACL substrates. The preferential presen
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