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Our finding that one enzyme acts
2021-06-15
Our finding that one enzyme acts both as a primase and a DNAP poses evolutionary and mechanistic questions. In particular, why do cellular organisms require two enzymes to fulfill de novo DNA synthesis? The inability of cellular replicases to perform as primases might be dictated by the challenges a
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Recent studies from the literature have identified new class
2021-06-15
Recent studies from the literature have identified new sonidegib of antiviral agents able to target diverse host factors indispensable for efficient virus replication: as an example, the human DEAD-box polypeptide 3 (DDX3) inhibitor, 1-[4-(4-methyl-1H-1,2,3-triazol-1-yl)phenyl]-3-o-tolylurea (16d),
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In addition we investigated if
2021-06-15
In addition, we investigated if the previously reported papain inhibitor can inhibit rhodesain, and found that it was not active at inhibiting rhodesain. The vinyl sulfone analogue of () was then synthesized and tested, and it was also inactive towards rhodesain. We then determined the time depend
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CYP enzymes have an important role in microsomal oxidase fun
2021-06-15
CYP450 LDN-212854 have an important role in microsomal oxidase function across a broad range of taxa (Pakharukova et al., 2012). They are involved in metabolism and detoxification of both internally generated compounds and xenobiotics as the phase I metabolizing enzymes and play an important role i
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We have previously disclosed the discovery of a azaindole ac
2021-06-15
We have previously disclosed the discovery of a 7-azaindole-3-acetic THZ1 Hydrochloride CRTh2 antagonist chemotype 1 from HTS and its subsequent optimization to give 2 as a potent and orally bioavailable inhibitor of eosinophil shape change (SC) in human whole blood. Subsequent to disclosure of that
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Immune modulation by steroid hormones is a
2021-06-11
Immune modulation by steroid hormones is a rather new aspect of the research on endocrine interactions in lower vertebrates (Harris and Bird, 2000). In the classical view, steroids exert their effects by binding to specific intracellular receptors that function as ligand-activated transcriptional re
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br Experimental Procedures br Author Contributions br Acknow
2021-06-11
Experimental Procedures Author Contributions Acknowledgments Introduction Estrogen-related receptors (ERRα, ERRβ, and ERRγ) are orphan nuclear receptors whose physiological ligands have not yet been identified. Although ERRs are closely related to estrogen receptors (ERs) they do not res
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CP 154526 There is an opposite opinion indicating that EphB
2021-06-11
There is an opposite opinion indicating that EphB plays a role as cancer suppressor. Batlle et al. showed that loss of EphB expression represented a critical step in CRC progression, and CRCs that lacked EphB2 expression have been correlated with more advanced tumour stage, poor differentiation, and
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hydroxychloroquine sulfate EphB promotes tumor growth by sti
2021-06-11
EphB4 promotes tumor growth by stimulating angiogenesis through EphrinB2 [18]. However, the distinct and specifically involvement of hydroxychloroquine sulfate and veins in the tumor angiogenesis of all tumor grades is unclear. Our results indicate that the relation between EphrinB2 and EphB4 stain
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Since OH PGE is a moderately selective EP agonist
2021-06-11
Since 1-OH-PGE2 is a moderately selective EP4 agonist which could bind to mouse EP3 and EP4 with a relatively similar affinity (Kiriyama et al., 1997), we have used a highly selective EP4 agonist CAY10580 to evaluate the involvement of EP4 activation in PGE2-facilitated EP4 internalization and recyc
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The aim of this paper
2021-06-11
The aim of this paper is to study the long-term socioeconomic impacts of local heat entrepreneurship from 2000 to 2016. The analysis focuses on impacts of the biomass-based district heat production on employment and income in a small peripheral community, called Eno, located in North Karelia, Finlan
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Several main strategies for targeting E s described in
2021-06-11
Several main strategies for targeting E3s described in the literature include: in vitro screening using functional assays [86]; computer programs for predicting potential druggable pockets, including those at protein-protein interfaces, and subsequent docking-based in silico ligand screening [87]; f
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The synthesis of compounds a and
2021-06-11
The synthesis of compounds 7a and 7b are outlined in Scheme 2. Compound 5 was obtained by di-tert-butyl pyrocarbonate protection of DZNep 4a. Then, compounds 6a and 6b were obtained by amination of the fluoride with a morpholino and dimethylamine, respectively. Target compounds 7a and 7b were obtai
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Until recently the first line
2021-06-11
Until recently, the first line treatment of RLS was the administration of low dose of three dopaminergic drugs, which has been approved by the US Food and Drug Administration and the European Medicines Agency for the treatment of moderate to severe RLS. These compounds are pramipexole (Mirapex), rop
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The data from drug screening in P berghei
2021-06-10
The data from drug screening in P. berghei (Fig. 3D) provide proof of concept that chemogenomic profiling can be accomplished in P. berghei in the same manner as P. falciparum, in that significant increases in the EC50 ratio were found only for antifolate drugs in the parasite with attenuated TgDHFR
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