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The optimization of the lead compound was initiated and
2021-03-27
The optimization of the lead compound () was initiated and the initial key SAR and the results of the structural modifications of lead compound are summarized in . Replacement of the carboxylic Rucaparib free base moiety with other functional groups led to loss of functional activity against EP4 r
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To our knowledge this is the first report of
2021-03-26
To our knowledge, this is the first report of an oncocytoma expressing alpha-enolase or causing autoimmune retinopathy and optic neuropathy. Although generally considered benign, oncocytomas have rarely been associated with paraneoplastic syndromes, including tumor-induced hypertension, erythrocytos
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br Materials and Methods br
2021-03-26
Materials and Methods Results Discussion Viral infection of eukaryotic thorough activate signaling pathways both via specific interaction with pattern recognition receptors (TLRs, RIG-I, MDA5) and more nonspecific mechanisms such as accumulation of newly synthesized viral glycoproteins in t
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br Experimental Procedures br Author
2021-03-26
Experimental Procedures Author Contributions Acknowledgments Introduction Breast cancer is one of the most common malignancies for women worldwide, representing approximately 22% of women’s malignancies that pose a threat to women’s health [[1], [2], [3], [4]]. The morbidity rate of brea
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It is interesting to note that Eibinger and colleagues
2021-03-26
It is interesting to note that Eibinger and colleagues [23] recently reported chemotactic movement to 25-OHC in THP1 cells as well as in primary human monocytes. RNA interference suggested that in part this migration was mediated by EBI2. Competing financial interest statement Acknowledgments
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Like all other cellular processes
2021-03-26
Like all other cellular processes, ubiquitination is also tightly regulated; more so, as myriads of pathways are controlled via this conjugation and dysregulation of ubiquitination has been implicated in various diseases including cancer [16], [17]. Quite a few of such regulatory mechanisms that con
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The possibility of harm with DPP inhibitors in patients with
2021-03-26
The possibility of harm with DPP-4 inhibitors in patients with clinically overt heart failure has been recently highlighted by the results of the VIVIDD (Vildagliptin in Ventricular Dysfunction Diabetes) trial (68), the only trial to date that has been designed to evaluate the effects of a DPP-4 inh
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br Experimental section br Results and discussion
2021-03-26
Experimental section Results and discussion Conclusions In conclusion, we have presented an autocatalytic recycling amplification electrochemical biosensing platform for simple, rapid and ultrasensitive detection of MTase activity by combining methylation-sensitive restriction endonuclease
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As for antiviral activity eight out of synthesized
2021-03-26
As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).
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serine threonine protein kinase Substituents at the C positi
2021-03-26
Substituents at the C11 position — An oxygen-containing substituent at the C11 position also affects the catalytic activity of Δ1-KSTDs. The Δ1-KSTDs from the Gram-positive bacteria R. equi [29], N. simplex ATCC 6946 and IFO 12069 [48,49,52], and R. rhodochrous IFO 3338 [27] were able to 1(2)-dehydr
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Each nsP plays a distinct defined and indispensable
2021-03-26
Each nsP plays a distinct, defined and indispensable role in the replication of viral genome. nsP1 is a membrane associated protein which possesses S-adenosyl-L-methionine (SAM)-dependent methyltransferase (MTase) and guanylyltransferase (GTase) activities to catalyze the viral RNA capping reaction
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br Chagas disease Chagas disease
2021-03-26
Chagas disease Chagas disease, an NTD caused by the protozoan Trypanosoma cruzi, affects 8–10 million people globally. More than 10,000 deaths are caused by the disease each year, and nearly 70 million people are susceptible to infection (Manne-Goehler, Umeh, Montgomery, & Wirtz, 2016). Chagas di
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In the course of our program which was aimed
2021-03-26
In the course of our program, which was aimed at developing CRTH2 antagonists for the treatment of allergic diseases, we have been pursuing a new class of potent and selective CRTH2 antagonist lead based on the structures of CRTH2 antagonists known to date (, , ). Using a fused 6–6-membered ring sys
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So far several important flovonoids and polyphenoilc compoun
2021-03-25
So far, several important flovonoids and polyphenoilc compounds were subjected to various human studies regarding their potential therapeutic and adverse effects (Ide et al., 2014; Turner et al., 2015; Witte et al., 2014) (Table 1). Resveratrol (trans-3,4, 5-trihydroxystilbene) is widespread stilb
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br Materials and methods br Results br Discussion
2021-03-25
Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor pim kinase inhibitor recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoids ce
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