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Several approved and or experimental drugs together with nat
2024-02-06
Several approved and/or experimental drugs, together with natural compounds, have been reported to induce autophagy in different cancer types [70], [71], [72] (Table 1). In the next paragraphs, we will review more in detail a group of these agents selected in relation to their promising future outco
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br ACL Inhibition Lowering Blood LDL C to
2024-02-05
ACL Inhibition: Lowering Blood LDL-C to Reduce ASCVD Risk Given its strategic position in the lipid biosynthesis pathway, ACL has been considered an attractive target for lipid-lowering even before statins and their effects on cholesterol homeostasis were elucidated (Box 2). Cells carefully maint
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gallic acid br ACL Regulation and Role
2024-02-05
ACL Regulation and Role in Lipid Metabolism ACL is a ubiquitous enzyme at the nexus of nutrient catabolism and synthesis of cholesterol and fatty acids. In mammals, it is highly expressed in lipogenic tissues including adipose, liver, and lactating mammary glands [9]. In the presence of ATP and C
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A third motif involves the toggle switch and consists
2024-02-05
A third motif involves the toggle switch and consists of the conserved FxxCWxP sequence in TM6 of class A GPCRs (Hofmann et al., 2009, Rosenbaum et al., 2009). Rotamerization of Trp in combination with a kink caused by Pro facilitates the outward movement of TM6 upon activation (Hofmann et al., 2009
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br Extracellular domain architecture The extracellular regio
2024-02-05
Extracellular domain architecture The extracellular region of GABAB receptor exists in a heterodimeric configuration regardless of interactions within the rest of the protein (Geng et al., 2012, Liu et al., 2004, Nomura et al., 2008). The extracellular domains of the GABAB1 and GABAB2 subunits ar
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Recently competitive inhibitors of arginase have
2024-02-05
Recently, competitive inhibitors of arginase have been developed which have greater specificity for the enzyme. Initial development of these compounds involved determination of the crystal structure of arginase. Christianson and colleagues found that a binuclear manganese cluster was required for ca
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17-Hydroxyprogesterone synthesis We have shown that an exten
2024-02-05
We have shown that an extensive region in SERBP1 (amino acids 354 to 474, using co-ordinates based on the full-length isoform, Figs. 1a and 2) is necessary for it to interact with RACK1; since this region has substantial homology to the corresponding region of HABP1 (Fig. 3) it is a reasonable hypot
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ha141 It has been reported that NLRP
2024-02-05
It has been reported that NLRP3 product, caspase-1, is increased in the brains of AD patients and experimental AD animals. NLRP3- and caspase-1-deficient animals are resistant to experimental development of AD, and have decreased IL-1β production and significantly increased Aβ clearance (Heneka et a
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The lactam emerged as lead candidate due to
2024-02-05
The lactam (6) emerged as lead candidate due to its high selectivity, outstanding potency (against ALK or in clinically known ALK mutants), low in vitro clearance, and low efflux potential. The lactam (6) was selected for further profiling against the resistant ALK mutants. Preclinical rat pharmacok
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Liver plays a pivotal role in metabolism of
2024-02-05
Liver plays a pivotal role in metabolism of xenobiotic compounds, such as environmental contaminants and drugs. Some of these compounds generate hepatic damage and impair its function. It was well-known that 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD) could induce pathological changes in mouse and ra
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A decrease in lactate concentration in the incubation medium
2024-02-05
A decrease in lactate concentration in the incubation medium was observed in samples treated with heparin and 2′,5′-dideoxyadenosine compared with the control (0.05; Fig. 2B). Discussion In the present study we compared the oxidative metabolism and intracellular signals of heparin, the glycosami
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Renal fibrosis is regarded as the final
2024-02-05
Renal fibrosis is regarded as the final common pathway for most forms of progressive renal disease, and mouse UUO is a widely accepted experimental model of renal injury leading to extreme fibrosis localized to the interstitial compartment. A-306989 attenuated the mRNA expression levels of several k
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Axl has been reported to mediate
2024-02-04
Axl has been reported to mediate cell-cell adhesion and sphere-growth [11], [18] and to be important for metastasis to secondary organs [12], [14], [20]. We found an Axl-dependent CCRCC-ability of sphere-formation and repopulation after non-adhesive growth. Axl-inhibited cells could not attach to ea
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Maintaining the normal vaginal fluid acidity is important fo
2024-02-04
Maintaining the normal vaginal fluid acidity is important for vaginal functions (Wagner and Levin 1984). Estrogen has been shown essential in maintaining the acidity of vaginal fluid, in which its deficiency could cause vaginal fluid pH to increase (Gorodeski et al. 2005). After menopause, low estro
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Investigating these possibilities will illuminate
2024-02-04
Investigating these possibilities will illuminate whether MMP-2 Inhibitor I possess mechanisms to differentially detect ACLY-generated versus ACSS2-generated acetyl-CoA as well as define the functional relationship between histone acetylation levels and cellular functions and phenotypes. Given that
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