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During the course of our ACK
2023-12-04
During the course of our ACK1 inhibitor program, a high-throughput screening (HTS) campaign of our internal sample collection was conducted. A series of -aryl pyrimidine-5-carboxamides of the general structure () was identified. Earlier studies of the structure–activity relationship (SAR) of ident
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Most studies on d penicillamine induced MG were
2023-12-04
Most studies on d-penicillamine-induced MG were performed before the discovery that some MG patients have anti-MuSK antibodies. After the identification of the present case, we retrospectively tested the stored frozen sera of ten earlier identified d-penicillamine MG patients with anti-AChR CHZ868 a
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Even within the context of evidence based interventions
2023-12-04
Even within the context of evidence-based interventions for tobacco screening, the science is imperfect. For example, patients who screen positive for current smoking should receive cessation counseling and prescribed known effective nicotine replacement therapy based on the Public Health Services G
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The small fishers with little
2023-12-04
The small fishers with little or no quota who remained relied on quota leasing arrangements to continue their fishing operations. Such arrangements had relatively high transaction costs and by early 2000 it appeared that the demise of the small fisher was imminent [2]. The introduction in 2001 of t
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The reaction of LOX with
2023-12-04
The reaction of 5-LOX with unlabeled AA generated products from hydrogen abstraction at C7 (95% 5-HETE) with minor products derived from abstraction at C10 (5% 8-HETE). With 7,7--AA the selectivity remained skewed towards C7 hydrogen abstraction (59%) compared to C10 hydrogen abstraction products (4
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br Regulation and pharmacology of mPGES mPGES kDa amino acid
2023-12-04
Regulation and pharmacology of mPGES-1 mPGES-1 (16 kDa, 152 amino acids) is a trimeric integral membrane protein of the endoplasmic reticulum with each monomer containing four transmembrane domains (Samuelsson et al., 2007; Sjogren et al., 2013). The three active site cavities are located at the
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Several tertiary prevention studies are
2023-12-04
Several tertiary prevention studies are currently underway examining the use of dutasteride for prostate cancer treatment: (1) during expectant management of prostate cancer, (2) after radical prostatectomy in men at high risk for relapse, and (3) in men with metastatic disease. The Reduction by Dut
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Regarding androgens it is known that they are
2023-12-04
Regarding androgens, it is known that they are also essential for reproductive success (Walters et al., 2010). At the molecular level, their effects are produced mainly by dihydrotestosterone (DHT), arising from the conversion of testosterone by the enzyme 3-oxo-5-alpha-steroid-4-dehydrogenase (enco
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The most potent compounds within the current
2023-12-02
The most potent compounds within the current series of compounds were therefore , , , , and , with 96 4 possessing the best selectivity towards the lyase reaction in comparison to the hydroxylase reaction, indeed, this compound was found to possess an IC value of 1210nM against the 17α-OHase compone
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br Autophagy at the Synapse The synapse is
2023-12-02
Autophagy at the Synapse The synapse is a highly specialized neuronal compartment that forms the basic unit of communication between neurons. Communication relies on electrical signals that are propagated down the axon of the presynaptic neuron, where they trigger the quantal release of neurotran
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These results show that quercetin
2023-12-02
These results show that quercetin can restore the enzyme activity of the cholinergic system nonneural induced by demyelination. The AChE activity has been used as an indicator of human cell aging with lowered levels commonly associated with older human red blood CRT 0066101 [51]. The enzymes AChE an
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br Steroidogenesis in the skin The synthesis of
2023-12-02
Steroidogenesis in the skin The synthesis of steroid hormones takes place in many tissues of which the adrenal glands, ovaries, testis, placenta and Forskolin are considered to be classical steroidogenic organs. Nevertheless, skin constitutes an important peripheral steroidogenic tissue. Steroid
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Atypically BcALDH has a minor reducing activity for all tran
2023-12-02
Atypically, BcALDH has a minor reducing activity for all-trans-retinal, which requires the binding of the reduced form of the NADP+ (NADPH) cofactor that is a side-product of the canonical oxidation activity of BcALDH. The reduction activity that converts all-trans-retinal to all-trans-retinol was r
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Thus we presumed that ALDH
2023-12-02
Thus, we presumed that ALDH1A3 might play an important role in TMZ-chemoresistance in glioblastoma patients. As we expected, the glioblastoma cell lines and primary glioma Remodelin were more sensitive to TMZ treatment when ALDH1A3 was inhibited or depleted. Consistently, it has been shown that dow
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Introduction A defining feature of cancer cells is
2023-12-02
Introduction A defining feature of cancer cells is disruption of the normal controls of the cell cycle; a tumor suppressor or inhibitor may act by restricting progression of the cell cycle. P27 (also known as cyclin-dependent kinase inhibitor 1B, P27, or Kip1) is a putative cell-cycle inhibitor pro
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