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The zinc transporter proteins are members of the SLC superfa
2024-05-27
The zinc transporter proteins are members of the SLC superfamily of metal transporters, and comprise two structurally and functionally different groups, the zinc-importer (ZIP; Zrt-, Irt-like proteins) family (SLC39A), which regulate zinc transport into the cytoplasm from outside the cell and from i
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Whereas allostery in the cell
2024-05-27
Whereas allostery in the β cell is relatively understudied, significant progress has been made in understanding the physiology and mechanistic biology of how AMPK and its upstream kinases govern β cell function. LKB1 phosphorylates AMPKα at Thr172 [21], and loss of LKB1 in β cells abolishes phospho
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Overexpression of AR can lead
2024-05-27
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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The numbers and types of molecules needing to
2024-05-27
The numbers and types of molecules needing to be transported across membranes are very large, and there is a corresponding very large and diverse number of transporters expressed throughout the body. Hundreds of proteins that have been assigned as having transporter function are broadly divided into
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The putative physiological meaning of epinephrine related he
2024-05-27
The putative physiological meaning of epinephrine-related hepatic drug transporter regulation remains to be established. It is nevertheless noteworthy that the catecholamine rather decreases expression of sinusoidal SLC transporters like NTCP, OAT2, OAT7, OCT1, OATP1B1 and OATP2B1 whereas those of c
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Indanone and its analogues are
2024-05-27
1-Indanone and its analogues are useful intermediates for the synthesis of compounds some of which have applications as pharmaceuticals, especially as analgesic and antihypertensive as well as tobacco flavoring agents. Indanones are commonly used as starting agent for the synthesis of ninhydrin whic
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Several dehidropregnenolone derivatives functionalized at C
2024-05-27
Several 16-dehidropregnenolone derivatives functionalized at C3, C4, C5 and C6 (Fig. 7) were prepared and evaluated as 5α-reductase inhibitors bearing in mind that after the formation of an enzyme-steroid complex a nucleophilic portion of the enzyme attacks the double bond of the steroid through Mic
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The uterine muscle also changes
2024-05-25
The uterine muscle also changes to meet the demands of pregnancy. Over the course of pregnancy, the myometrium undergoes structural remodeling to accommodate a growing fetus, followed by a functional switch from quiescent to contractile characteristics for parturition. Studies on the mouse model ind
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br Conclusions br Introduction In the modern
2024-05-25
Conclusions Introduction In the modern life of humans, CP 154526 are widely prescribed for therapy against bacterial diseases to prevent the onset of bacterial infections during a viral disease (Goossens et al., 2005; Van Boeckel et al., 2014). They have been massively administered and persis
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Maynard et al demonstrated that
2024-05-25
Maynard et al. [54] demonstrated that serum levels of sFlt-1 were five times higher in pregnant women with PE than in normotensive women; as a consequence, VEGF and PlGF levels were found to be proportionally reduced in these women [54]. The literature confirms that there is a sharp increase in sFlt
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br Transparency document br Introduction G
2024-05-25
Transparency document Introduction G protein-coupled receptors (GPCRs) comprise a diverse family of seven transmembrane domain-containing receptors represented by over 800 genes in humans. GPCRs respond to a range of stimuli, including peptides, hormones, growth factors, lipids, odorants, and
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The biology of the A BR is complex and needs
2024-05-24
The biology of the A2BR is complex and needs to be considered contextually as the expression and effect of receptor engagement varies according to time post hypoxic injury, cell type and downstream signaling pathway. For example, A2BR expression is dynamic - low under basal and increasing under isch
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vitamin d receptor br Experimental procedures Adk tg Adktm t
2024-05-24
Experimental procedures Adk-tg (Adktm1−/−:tg(UbiAdk) mice were created by breeding a loxP-flanked Adk transgene under the control of a human ubiquitin promoter into ADK knockout mice (Fedele et al., 2005,). Fb-Adk-def (Adktm1−/−:tg(UbiAdk):Emx1-Cre-tg3) mice were generated by pairing Emx1-Cre-tg3
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br Conclusions and clinical relevance Astrogliosis and
2024-05-24
Conclusions and clinical relevance Astrogliosis and an increase in ADK is a pathologcial hallmark of epilepsy. The consequence of increased ADK in the epileptic Imipramine hydrochloride receptor is a decrease in the ambient adenosine tone and A1R activity. As a result, systemic administration of
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Our initial approach to identify hits was
2024-05-24
Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI CNQX disodium salt library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibil
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