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The aldehyde reductase AKR A and aldose reductase AKR
2023-01-30

The aldehyde reductase (AKR1A1) and aldose reductase (AKR1B1) belong to aldo-ketoreductase (AKR) superfamily catalyzing the reduction of corresponding aldehydes and ketones involved. Both the closely related enzymes AKR1A1 and AKR1B1 have 65% structural similarity and differ only at the active site.
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In particular we focused our attention on beta
2023-01-30

In particular, we focused our attention on beta2 adrenergic receptors, since their commercial inhibitors are effective in lowering IOP, the primary indication of glaucoma. The hypotensive action of a commercial sequence of beta2 adrenergic receptor siRNA was tested in rabbits. The results confirmed
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In another study authors found that ADORA were present
2023-01-30

In another study, authors found that ADORA1 were present on the intrinsically photosensitive retinal ganglion dna ligase (ipRGCs), and application of adenosine to rat retinas reduced light-evoked spiking of ipRGCs through suppression of a cAMP-mediated pathway (Sodhi and Hartwick, 2014). The ipRGCs
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br Functional consequences of ADK regulation
2023-01-30

Functional consequences of ADK regulation on astrocyte function As outlined above (see introduction), ADK critically regulates the extracellular adenosine levels in Zalcitabine sale (Boison, 2006, Etherington et al., 2009). Changes in the levels of adenosine, as a result of the regulation of ADK
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Materials and methods br Results br Discussion The BV tag
2023-01-30

Materials and methods Results Discussion The BV-tag-based electrochemiluminescence immunoassay is an extremely sensitive assay. It has been employed for detecting analytes present in only picogram quantities (e.g., bacterial toxins [26], thymidylate synthase inhibitors [19]), measuring the a
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Our initial approach to identify
2023-01-30

Our initial approach to identify hits was two-pronged and included a high-throughput screening (HTS) campaign of the OSI AMD-070 sale library as well as a virtual screening (VS) campaign, utilizing a publically available crystal structure of ACK1 (PDB code: ). A tolerance for protein flexibility was
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A combination of factors might however
2023-01-30

A combination of factors might, however, account for the low rate of success of drug development for neuropsychiatric disorders. First, in most neuropsychiatric disorders, the symptomatology is heterogeneous and the neurobiology remains poorly understood, making therapeutic targets difficult to iden
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Molecular docking is widely used to predict the
2023-01-30

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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For both the hydroxylation and lyase reactions the heme iron
2023-01-30

For both, the 17α-hydroxylation and 17, 20-lyase reactions, the heme iron center of P450 17A1 receives electron reducing equivalents from CPR. Both reactions require one pair of electrons and molecular oxygen for the conversion of the substrate into product in each catalytic cycle. However, the 17,2
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Acknowledgments br Introduction Prostate cancer is
2023-01-30

Acknowledgments Introduction Prostate cancer is the first leading cause of cancer-related deaths among males in the UK and the second in the US. Despite recent advances in surgery, radiation, medical management and screening, prostate cancer patients suffer high morbidity and mortality and signi
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We used the lead compound C to demonstrate that small
2023-01-30

We used the lead compound C4 to demonstrate that small molecule ACL inhibitors can recapitulate ACL knockdown (KD) in modulation of cancer stemness. We have shown previously that ACL KD reduced the CSC population in multiple cancer cell lines. The E-snail cells are an established CSC model system.
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Introduction Initially postulated to represent
2023-01-30

Introduction Initially postulated to represent the main source of ATP production in eukaryotic cells, mitochondria are recently recognized to perform manifold essential functions beyond energy production, impacting most areas of cell biology and medicine [1]. Mitochondrial metabolism is both the ba
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Estrogen exerts its genomic action via
2023-01-30

Estrogen exerts its genomic action via bapta nuclear receptor: ERα and ERβ. The distribution of ERα and/or ERβ positive neurons in CNS of different species has been mapped extensively by various methods [41], [42], [43], [44], [45], [46], [47], [48], [49], [50], although there are some differences
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There is a growing literature
2023-01-29

There is a growing literature on ABCA2 expression in human biopsies, where it has been described as a potential biomarker of leukemias. In childhood T-cell acute lymphoblastic leukemia, ABCA2 and ABCA3 were expressed at high levels, which upon treatment with methotrexate, vinblastine and doxorubicin
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Constitutive tyrosine kinase activity of BCR ABL fusion
2023-01-29

Constitutive tyrosine kinase activity of BCR/ABL fusion genes causes uncontrolled cell growth and is also thought to be responsible for a variety of changes in normal cellular functions like differentiation, adhesion, migration and apoptotic response in CML. Therefore it is important to know the exp
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