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Cysteine protease inhibitors representing several chemical s
2021-02-08
Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests
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Myriocin br Materials and methods br Results br Discussion
2021-02-08
Materials and methods Results Discussion NB has been shown to induce cancers in many tissues including the kidney, liver, and thyroid, following chronic inhalation in animals (Hsu et al., 2007). The available data indicate that a lager majority of studies on NB evaluate the effects of toxic
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br Discussion Variable estradiol effects on cell proliferati
2021-02-08
Discussion Variable estradiol effects on cell proliferation have been reported according to animal species, tissues, and type of estrogen receptor [16,21,22,[29], [30], [31]]. In the kidney, 17βE was found to increase [3H]-thymidine incorporation in primary rabbit kidney proximal tubule hedgehog
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br Regulation of cadherin switching The downregulation of E
2021-02-08
Regulation of cadherin switching The downregulation of E-cadherin during cadherin switching is induced by multiple mechanisms, including methylation of the E-cadherin promoter and signaling pathways that activate E-cadherin-suppressing transcription factors [[61], [62], [63]]. During the progress
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Because sex steroids and growth hormone play an important ro
2021-02-08
Because sex steroids and growth hormone play an important role in the development and maintenance of hepatic CYP450 enzyme expression and ER expression, it is possible that exposure to endocrine active agents during gestation and perinatally could alter expression of these proteins. Therefore, these
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br TRIM TIF A RNF TRIM
2021-02-08
TRIM24 (TIF1A, RNF82) TRIM24 contains a RING-both B-boxes-coiled coil conserved structure at the N-terminus with bromo and PHD domains prior to C-terminal end (Fig. 3). This transcriptional intermediary factor is well studied in the context of transcriptional activation of nuclear receptor via ac
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Verapamil a calcium channel blocker used clinically as
2021-02-08
Verapamil, a calcium channel blocker used clinically as a coronary vasodilator, was amongst the first compounds identified that could reverse MDR and potentiate the effects of MDR1 substrates such as vincristine [15], [16]. Verapamil, along with a number of other MDR1 blockers, have proved largely u
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Crystal structures of various CRM
2021-02-07
Crystal structures of various CRM1 complexes have provided insight into molecular details of the interactions between CRM1 and its interaction partners during the transport cycle. CRM1 cooperatively binds RanGTP and cargo in the nucleus (Paraskeva et al., 1999). In this ternary complex, RanGTP is lo
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Tinnitus Met carriers with severe hearing
2021-02-07
Tinnitus Met carriers with severe hearing loss perceive their tinnitus as being louder, which is associated with increased activity in the PHC, increased PHC→pgACC connectivity, as well as decreased pgACC→PHC connectivity. This indicates that Met carriers with severe hearing loss have increased tinn
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br Results and discussion br
2021-02-07
Results and discussion Conclusion This study describes the development of a highly sensitive on-sorbent derivatisation technique, using the novel high-surface area CMV devices, to sample methamphetamine vapour. Previous methods for air sampling for methamphetamine such as sampling cassettes ha
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34450 Located on the fore tarsals of the
2021-02-07
Located on the fore-tarsals of the front pair of legs, the Haller’s organ is presumed central to tick chemosensation. Recent genomic, transcriptomic and proteomic investigations have identified several families of transmembrane proteins in the forelegs of ticks that are likely involved in olfactory
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We recently employed a functional drug screening approach to
2021-02-07
We recently employed a functional drug screening approach to identify mithramycin as an inhibitor of EWS–FLI1. In our study, we employed a stepwise approach involving a luciferase primary screen and a novel multiplex PCR screen to evaluate over 50,000 compounds to identify mithramycin as an inhibito
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br Substrate characterization of candidate peptide reporters
2021-02-07
Substrate characterization of candidate peptide reporters in a library Measurement of resistance to intracellular proteases Use of capillary zone electrophoresis for assay readout Selection of lead peptide from small library screen Characterization of final reporter Additional modif
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Previous studies demonstrated that cPLA translocates to the
2021-02-07
Previous studies demonstrated that cPLA2α translocates to the phagosomal membrane during macrophage phagocytosis through mechanisms that, in humans, involve phosphorylation of the enzyme by c-Jun N-terminal kinases and membrane association via the cationic cluster of four lysine residues present at
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ACE also known as Kininase
2021-02-07
ACE also known as Kininase II is an important enzyme of the Renin angiotensin sodium ion channel system (RAAS) (Novo et al., 1987), it is believed to be a potent blood pressure regulator and also plays a crucial role in activation of the bradykinin receptor via inactivation of bradykinin which work
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