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All these recent results show the interconnection between th
2021-11-08

All these recent results show the interconnection between the Hippo pathway as a tumor-suppressor on the one hand and its function as regulator of metabolic homeostasis on the other. Disruption of the Hippo pathway leads to cancer growth, which is often associated with pathological disturbances in t
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Tylophora atrofolliculata is a centuries used folk medicine
2021-11-08

Tylophora atrofolliculata is a centuries-used folk medicine for the treatment of rheumatism in China (Jiangsu New Medical College, 1977). One group of its bioactive components is phenanthroindolizidine alkaloids, which have been demonstrated as lead compounds of anti-tumor agents in our previous stu
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br Materials and Methods A human skin SCC and HT
2021-11-08

Materials and Methods A431 (human skin SCC) and HT-297.T (human AK) cell lines were purchased from ATCC (Manassas, VA) and were maintained in DMEM supplemented with 10% fetal calf serum, 4 mM L-Gln, 1 mM sodium pyruvate, 100 U/mL penicillin, and 1 μg/mL streptomycin. Human HK1 and HK2 plasmids we
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In order to study the role
2021-11-08

In order to study the role of haspin’s kinase activity in mitosis (and other cellular processes) and its potential role in cancer, we sought to identify and optimize inhibitors. Utilizing a recently developed time-resolved fluorescence resonance energy transfer (TR-FRET) high throughput screening (H
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Importantly lactate and H exert some
2021-11-06

Importantly, lactate and H+ exert some of their biological effects independently of each other, though sometimes through redundant pathways leading to a same biological effect, as for angiogenesis. In other cases, they can have antagonist effects: lactate was shown to stimulate extracellular matrix
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We have previously established the pharmacokinetic profile a
2021-11-06

We have previously established the pharmacokinetic profile and effective dose of MNF in the rat [43] and demonstrated the effectiveness of MNF as an anticancer drug in guanidine hydrochloride and xenograft models [44]. Moreover, MNF was found to effectively block GPR55 signaling in tumor cells [21]
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Compound was synthesized in a racemic fashion with
2021-11-06

Compound was synthesized in a racemic fashion with this study and plans for an enantioselective synthesis could be developed based on the activity of racemic . Synthesis of compound followed a slightly different synthetic route due to the ineffectuality of the S2 reaction on the secondary position (
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TGR is a class A GPCR transducing signal through Gs
2021-11-06

TGR5 is a class A GPCR, transducing signal through Gs-protein mediated cAMP accumulation, and was recently reclassified as the founder member of the bile–acid receptor subclass of GPCRs [22]. The cAMP-mediated signaling of TGR5 activation has been implicated in a range of cellular physiological acti
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The kinetic data obtained from incubation of
2021-11-06

The kinetic data obtained from incubation of 4BAB with GLO1 show that 4BAB does not completely inactivate the enzyme (Figs. 2A and S6a). At low concentrations (4.7 and 14.4μM), 4BAB seemed to follow biphasic kinetics (Fig. 2A); even though regardless of the concentration 4BAB, there was a plateau at
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So far only few studies report
2021-11-06

So far only few studies report about GAL in the visual system: GAL has been detected in the cornea of rat (Jones and Marfurt, 1998), mouse (Henken and Martin, 1992) and pig (Stone et al., 1988), and in the uvea of rat (Strömberg et al., 1987), pig (Stone et al., 1988) and cat (Grimes et al., 1994),
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br Experimental br Results and
2021-11-06

Experimental Results and discussion Conclusion In conclusion, four bisnaphthalimides have been investigated for their potential G-quadruplex binding. The compounds 3a, 3b and 5b display high affinity for telomeric and oncogenic G-quadruplexes. On the other hand, 5a only show high affinity f
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To meet the requirement of ferroptosis
2021-11-06

To meet the requirement of ferroptosis-based therapy, a couple of small molecule drugs and nanomaterials were introduced to the design of ferroptosis inducers, separately. As we know, iron is a key regulator of ferroptosis. When small molecule drugs are employed to induce ferroptosis, the endogenous
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The membrane metalloendopeptidase MME gene is
2021-11-06

The membrane metalloendopeptidase (MME) gene is located at human chromosome 3q21-27. It encodes a 100-kD type II transmembrane glycoprotein, a widely expressed membrane metalloendopeptidase that degrades a number of substrates. The active site of the enzyme faces the extracellular space. MME is wide
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A few previous studies have examined Factor
2021-11-06

A few previous studies have examined Factor Xa inhibitors for VTE prophylaxis in hip fracture patients. In a 2001 paper, Eriksson et al. studied 1250 patients with hip fractures that had been randomized to either postoperative Factor Xa inhibitor or enoxaparin [13]. Each patient received bilateral v
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SEA0400 br Conclusions and perspectives In conclusion offeri
2021-11-06

Conclusions and perspectives In conclusion, offering duly validated and highly performing assays for measuring DiXaIs in plasma is a step, but not the final issue. More dedicated and individual assays will continue this innovative development, which witnesses the need for collaboration between co
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