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Many metalloenzyme inhibitors consist of two chemical compon
2024-01-04
Many metalloenzyme inhibitors consist of two chemical components: the MBG, the portion of the inhibitor designed to bind to the metal, and the scaffold, the portion of the inhibitor recognized by the amino Dihydroartemisinin mg residues that form the substrate-binding site of the metalloenzyme. The
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Materials and methods br Results br Discussion ATX
2024-01-04
Materials and methods Results Discussion ATX plays a significant role in initiating and sustaining tumor metastasis [43]. LPA stimulates cell proliferation, migration and survival by acting on its cognate G-protein-coupled receptors. Aberrant LPA production, receptor RPC1063 and signaling pr
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br Acknowledgements This work is
2024-01-03
Acknowledgements This work is sponsored by the National Natural Science Foundation of China (grant no. 31201963) and Youth Backbone Teachers Project in Henan Province Department of Education, China (grant no. 2016GGJS-061). Introduction Acute lymphoblastic leukemia (ALL) is a malignant disord
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In the present study a splice acceptor site mutation c
2024-01-03
In the present study, a splice acceptor site mutation (c.1769-1G > C) was identified in AR gene from patients with CAIS. The c.1769-1G > C mutation results in replacement of the normal sequence (CAG/G) with a new sequence (CAC/G) at the splice acceptor site of intron 2. In the splice acceptor site r
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An unbiased evaluation of hepatic mRNA was
2024-01-03
An unbiased evaluation of hepatic mRNA was performed to assess the impact of hepatocyte AMPK activation on the transcriptome. The expression of 913 genes were altered in control mice after chronic PF-06409577 treatment, 188 genes were affected by knocking out AMPK in hepatocytes, and expression of 2
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Our results lead to the discovery and
2024-01-03
Our results lead to the discovery and characterization of VvAAT2, a gene potentially involved in acetate accumulation in grape berries discovered through amino-acid feeding experiments. Incubation with exogenous amino acids has also been a key in the discovery of new genes affecting fruit aromas [13
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Introduction Aldose reductase ALR is
2024-01-03
Introduction Aldose reductase (ALR2) is the first enzyme of the polyol pathway that catalyzes the reduction of glucose to sorbitol utilizing NADPH as a cofactor. The intracellular accumulation of sorbitol, due to increased aldose reductase activity at high blood glucose levels, such as those occurr
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Studies on both TCDD treated mice and AhR null
2024-01-03
Studies on both TCDD treated mice and AhR null mice have also pointed to a role of AhR in hematopoiesis [65], [66]. Singh et al. showed that AhR is a negative regulator of HSC (hematopoietic stem cell) proliferation, while deletion of AhR leads to spleen enlargement in juvenile and adult mice [67].
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The excellent potencies selectivities and improved
2024-01-03
The excellent potencies, selectivities and improved PK associated with the piperazine class triggered more extensive off-target screenings of the highlighted compounds. A screen of more than 100 enzymes, receptors, and ion channels resulted in activity at the norepinephrine transporter (NET). This
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br Acknowledgments and Disclosures br Introduction In mammal
2024-01-03
Acknowledgments and Disclosures Introduction In mammals, ejaculated sperm requires a finite period of residence in the female reproductive tract to become competent for fertilization (Visconti et al., 1995a, Visconti et al., 1995b). Once oocytes are matured, it is important for these cells to
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Since the cloning of ARs in the beginning of
2024-01-03
Since the cloning of ARs in the beginning of the 1990s, the efforts to characterize them have led to the accumulation of a substantial amount of experimental data. Decades of site-directed mutagenesis (SDM; Box 1) studies, in combination with pharmacological data and computational modeling, have pav
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In summary this study reveals that
2024-01-03
In summary, this study reveals that the stability of rapsyn is critically dependent on HSP90β, highlighting a novel function of HSP90β in NMJ formation and maintenance. It also identifies a mechanism in agrin signaling for AChR clustering, i.e., by upregulating the interaction between HSP90β and rap
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The theoretical calculations of ADME parameters
2024-01-03
The theoretical calculations of ADME parameters (molecular weight (MW), log P, topological polar surface are (tPSA), number of hydrogen donors (nON) and acceptors (nOHNH), and volume) and DLS are presented in along with the violations of Lipinski’s rule. According to these data, all compounds (–) c
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For the TSH receptor signaling
2024-01-02
For the TSH receptor, signaling at the Golgi/trans-Golgi network appears required for both rapid effects of TSH − such as Doxorubicin HCl synthesis depolymerization, which is implicated in thyroglobulin reuptake and, thus, thyroid hormone release − and late ones, such as those on gene transcription
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br Experimental procedures br Results br
2024-01-02
Experimental procedures Results Discussion Although previous studies have indicated that astrocyte aromatase plays a role in nociceptive processes (O'Brien et al., 2015, Smeester et al., 2016), the mechanisms responsible for the regulation of aromatase and its involvement in nociception rem
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