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During the course of our research on
2020-04-24

During the course of our research on mGlu PAMs,, the hydroxyacetophenone scaffold was found to possess dual mGlu PAM and CysLT1 antagonism activity, presumably as orthosteric antagonist (). There is currently an increasing interest in drug discovery to explore multitarget drugs or polypharmacology,
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The enzymatic activity of recombinant sponge P H
2020-04-22

The enzymatic activity of recombinant sponge P4H was assayed in vitro both at 37°C, the standard enzymatic kinetics temperature, and at 15°C, the typical sea temperature of C. reniformis marine environment (Fig. 2C). Surprisingly the data obtained indicate that the sponge enzyme has a lower activity
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In a recent study a
2020-04-22

In a recent study, a CMV DNA load cut-off of 500 IU/ml in BAL fluid was found to have a positive predictive value of ∼50% for the presence of probable CMV pneumonia (considering a prevalence of this event of 10% among patients at risk and undergoing BAL testing). Tan et al., in contrast, found CMV D
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br Acknowledgements br Introduction Water
2020-04-22

Acknowledgements Introduction Water and electrolytes constitute an integral part of all living things, and 6 ohda synthesis governing their movements play important roles in a wide variety of physiological and/or pathophysiological processes. Given the importance of channel proteins in cancer
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TgTCEA from petals TgTCEA and TgTCEB
2020-04-22

TgTCEA from petals (TgTCEA1) and TgTCEB from pollen grains (TgTCEB1) were used throughout the study. The recombinant enzymes were expressed in , and purified as the His-tag-free forms as described previously., Enzyme reactions were performed at 4 mM substrates under the same conditions as described
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Through an unknown mechanism RING Ubox type E
2020-04-22

Through an unknown mechanism, RING/Ubox-type E3 dimers and the N-terminal tail have been shown to function as a modulator of full E3 ubiquitin ligase activity [27]. LRSAM1 promotes a significant enhancement in the formation of the high-molecular-weight products or E3 activity when the RING domain is
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Given the fact that most criticism on genetic
2020-04-22

Given the fact that most criticism on genetic association studies is the lack of replicability (Hirschhorn, Lohmueller, Byrne, & Hirschhorn, 2002), the aim of the present study is to investigate the influence of the DBH polymorphism rs1611115 (C-970T) on RD in two independent samples of healthy part
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Biocytin The authentic PPase was purified
2020-04-22

The authentic PPase was purified from B. subtilis as described previously [21], whereas the recombinant enzyme was purified to homogeneity from E. coli by a simplified procedure including only phenyl-Sepharose CL-4B column chromatography and DEAE-HPLC [21]. About 26 mg of pure enzyme was obtained fr
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The possibility that a carboxyl group attached
2020-04-22

The possibility that a carboxyl group attached to the or position of an -arylaminomethylenemalonate ester would lead to increased selectivity for DHODH has been tested and found not to be the case. Indeed, reduced selectivity compared with the corresponding ester is observed and is attributed to a
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For the current studies we used the selective
2020-04-21

For the current studies, we used the selective Epac agonist 8CPT-AM to directly activate the proteins. We chose this pharmacological approach since it allows a direct activation of Epacs rather than using receptor agonists such as PGE2 which could introduce confounding variables. One potential conce
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Recoverin is a kDa retinal protein that binds to calcium
2020-04-21

Recoverin is a 23-kDa retinal protein that binds to calcium. It regulates the GSK1210151A of rhodopsin during visual transduction within photoreceptor cells. Since the pathogenicity of anti-recoverin antibody is potent, anti-recoverin CAR patients often have progressive visual impairments, characte
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The isomeric phenyloxazole not only exhibited increased
2020-04-21

The isomeric 5-phenyloxazole not only exhibited increased potency against NEP, but also a decreased ACE inhibition thus providing encouraging selectivity. Changing the P1 group from an -propyl to a more polar methoxyethyl at the left hand (±)-J 113397 mg (as seen in compound pairs – and –) decreased
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br Rationale and hypothesis To
2020-04-21

Rationale and hypothesis To discover an allosteric inhibitor of EGFR, Jia et al. (2016) screened a library of 2.5 million compounds at 1 μM ATP concentration in opposition the purified EGFR L858R/T790M mutant enzyme. 1322 best hits were found from this round of screening. The pinnacle hits had be
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br Conclusions and future perspectives It
2020-04-21

Conclusions and future perspectives It is now evident that selective ETA or nonselective endothelin receptor antagonism provides therapeutic potentials against a variety of cardiovascular diseases such as hypertension, PAH, and diabetic microvascular dysfunction (Fig. 1). However, PAH is currentl
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ACE also known as Kininase II
2020-04-21

ACE also known as Kininase II is an important enzyme of the Renin angiotensin AS 101 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 works to induce
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