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Drug resistance to both pathogens and cancer
2020-11-17
Drug resistance to both pathogens and cancer has been a big hindrance in healthcare. Integrated research undertakings are being pursued to find the exact causes of the lack of response towards drugs. Surprisingly, host pumps are the key factors in failure of most drugs. The pumps either do not allow
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Generally glycines and other small residues such as alanine
2020-11-16
Generally, glycines (and other small residues such as alanine) present in a helical GxxxG-motif that are facing the same side of the helix form a uniform surface that enables direct contact with a second helix. Crystal structures of multipass membrane proteins have demonstrated that GxxxG-motifs are
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Intriguingly one E residue may serve as a molecular gate
2020-11-16
Intriguingly, one E2 residue may serve as a molecular ‘gate’ to allow the C-terminus of ubiquitin to access the closed E2~Ub conformations favorable for ubiquitin transfer. This residue, Asp87 in UbcH5 family members, resides on one side of the opening that leads to the active site Cys (Fig. 4D). In
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In the context of E ligase drug discovery it
2020-11-16
In the context of E3 ligase drug discovery, it is critical to identify the appropriate E2/E3 substrate pairing to ensure the development and use of the most physiologically relevant screening assay. There have been many reports of limited E2/E3 activity profiling with a small number of E2 and E3 ret
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br DUBs in regulation of critical steps in tumor metastasis
2020-11-16
DUBs in regulation of critical steps in tumor metastasis Tumor metastasis comprises a complicated series of biological processes in terms of the invasion-metastasis cascade that requires cancer fak inhibitor to (1) migrate and invade from the origin sites through the extracellular matrix (ECM) t
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In this report we present spectroscopic evidence on the effe
2020-11-16
In this report, we present spectroscopic evidence on the effect of different solvents having proton acceptor and proton donor ability and pH of the medium on the abstraction of amino proton of PI (Scheme 1) for controlling the nonradiative rates. Despite the general utility of PI as a DNA intercalat
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br Inhibition of DHODH The
2020-11-16
Inhibition of DHODH The final products 7a–n were assessed for their DHODH inhibitory activity on rat liver mitochondrial/microsomal membranes. A procedure adapted from the literature was employed (see Experimental), in which oxidation of DHO to ORO is monitored by following the concomitant reduct
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Mitochondrial depolarization induced by DHODH
2020-11-16
Mitochondrial depolarization induced by DHODH inhibition (Figure 5A) may also contribute to the selective effects of DHODH inhibitors on KRAS mutant cells. If so, the effect may arise more from pro-apoptotic effects of mitochondrial depolarization (Lemasters et al., 1998) than from impaired oxidativ
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Orange spotted grouper Epinephelus coioides
2020-11-16
Orange-spotted grouper (Epinephelus coioides) is a coral reef fish with a high commercial value in China and Southeast Asian countries. However, in recent years, various outbreaks of viral diseases have affected the grouper aquaculture industry (Wei et al., 2010). Specifically, Singapore grouper iri
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The serotonin transporter gene encodes an integral membrane
2020-11-16
The serotonin transporter gene () encodes an integral membrane protein that transports serotonin from the synaptic spaces into the presynaptic neurons. The encoded protein terminates the action of serotonin and recycles it in a sodium-dependent way. This protein is a target of psychomotor stimulants
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The Fontan circulation When first described in the Fontan
2020-11-16
The Fontan circulation When first described in 1971, the Fontan operation ushered in a new paradigm in the care of children born with the varied forms of complex congenital Isochlorogenic acid A disease (CHD) characterized by a single effective pumping chamber.1., 2. This procedure, which creates
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Functional studies revealed that these ESR mutations
2020-11-14
Functional studies revealed that these ESR1 mutations lead to constitutive activity of the ER, meaning that the receptor is active in absence of estrogen, conferring resistance against several endocrine agents. Recent studies reported that the occurrence of ESR1 mutations is rare in ER+ primary brea
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Estradiol the predominant circulating estrogen in humans
2020-11-14
Estradiol, the predominant circulating estrogen in humans, it is mainly secreted by the granulosa cells of the ovarian follicles, and the corpora lutea, by the mechanisms indicated above. On the other hand, estretrol is synthesized exclusively during pregnancy by the fetal liver and reaches maternal
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br Conflict of interest br Acknowledgements This work was
2020-11-14
Conflict of interest Acknowledgements This work was supported by the Basic Science Research Program through the National Research Foundation (NRF) funded by the Ministry of Science, ICT & Future Planning (2013R1A1A1076117) and also by the Priority Research Centers Program through the NRF funde
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Ultrasound is an acoustic wave with a frequency kHz that
2020-11-14
Ultrasound is an acoustic wave with a frequency >20 kHz that needs a medium to propagate [20]. Accompanied by the spread of an ultrasonic wave, a series of alternating cycles of compression and rarefaction emerge in the liquid medium. During the rarefaction cycle, microbubbles are formed because of
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