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We recently described the benzoxazin one analogue of
2021-08-02
We recently described the 1,3-benzoxazin-4-one analogue of LY294002 and showed it to have pan-PI3K and DNA-PK activity [2]. We have also reported on the activity of other family members, such as 3 which causes sensitization of lung cancer and colon cancer cells to radiation [11] and 4 (LTUSI122) as
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Our observation that FAK is
2021-08-02
Our observation that FAK is downregulated in vascular smooth muscle 5-Methyl-CTP on fibrillar collagen confirms observations reported for other cell types [14]. However, unlike the results reported previously [14], our work suggests that matrix rigidity per se does not determine FAK downregulation.
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glp-1 receptor DDR expression is upregulated in the glomerul
2021-08-02
DDR1 expression is upregulated in the glomeruli and tubules of injured kidneys [7], [8], [19]; however, what role this receptor plays in kidney resident glp-1 receptor is unclear. A plausible hypothesis is that DDR1 might contribute to kidney injury by directly exerting a pro-fibrotic action. In fa
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Aminoallyl-dCTP - Cy3 In a recent study Tomkins et al analyz
2021-08-02
In a recent study, Tomkins et al. [7] analyzed the protein-protein interaction network of ROCO proteins. Based on a database analysis, and only taking into account interactions reported in at least two peer-reviewed papers and/or confirmed by two different methods, 113 interactors were revealed for
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Cells expressing the CDK S D mutant exhibit
2021-08-02
Cells expressing the CDK5 S47D mutant exhibit impaired migration and enhanced proliferation: Finally, we wished to determine the functional significance of this phosphoevent. Multiple studies have implicated active CDK5 in promotion of cell migration [9,16,[21], [22], [23], [24]] and in one study th
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The HPV E proteins are acidic oncoproteins of approximately
2021-08-02
The HPV E7 proteins are acidic oncoproteins of approximately 98–103 protease inhibitor that contain 3 domains: the conserved region (CR) 1, CR2, and the carboxyl terminal (C-terminal) domain. The CR1 domain is necessary for cellular transformation and RB degradation in mucosal high risk HPVs. The C
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The anxiolytic like responses produced by anti
2021-08-02
The anxiolytic-like responses produced by anti-SVG-30 suggests that CRF2 receptors mediate not only the elicitation of anxiety behavior induced by prior stress, i.e. conditioned freezing, but also unconditioned anxiety behavior induced by exposure to the unfamiliar environment of the elevated plus m
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br Acknowledgements We are grateful to the
2021-08-02
Acknowledgements We are grateful to the National Natural Science Foundation of China (Grant Nos. 21571033 and 81503099) and the New Drug Creation Project of the National Science and Technology Major Foundation of China (Grant No. 2015ZX09101032) for financial aids to this work. The research was a
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Given that dimethylamine substitution was
2021-08-02
Given that dimethylamine substitution was tolerated as in SR106447 (), we investigated Thioguanine amine substitutions as replacements for the -butyl group (). Cyclic amines (SR19880, 19882) or simple mono-substituted anilines (SR20037) were not active, nor was an acetylated version (SR20039). The
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AVE 0991 There has recently been some interest in Uba
2021-08-02
There has recently been some interest in Uba6, which is most similar to slime mold, with BLAST identities of 59% and positives 73% in the 400–600 ADD range. The 400–600 ADD correlation of the two profiles is a striking 87%, so functional differences probably arise outside the ADD binding domain. Hu
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br GPCRs form heterotetramers In addition to homodimers and
2021-07-31
GPCRs form heterotetramers In addition to homodimers and heterodimers, for several family A receptor heteromers, experimental evidence supports the presence of higher order rearrangements as tetrameric structures, comprised of two different homodimers, each able to signal with its preferred G pro
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LPA is known to regulate the peroxisome proliferator
2021-07-31
LPA is known to regulate the peroxisome proliferator-activated receptor γ and the reorganization of actin cytoskeleton [58]. However, the physiological functions of LPA in cells are still poorly understood. The simultaneous production of PA with/without 1-LPA or 2-LPA may be important to maximize a
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The data from drug screening in P berghei Fig D
2021-07-31
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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Since these first results KSTD activity has been
2021-07-31
— Since these first results, Δ1-KSTD activity has been identified in many other microorganisms, albeit sometimes with different substrate preferences. For instance, Comamonas testosteroni ATCC 11996 (formerly Pseudomonas testosteroni) is active on several steroid substrates, but it cannot use 11β-hy
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Primary human GBM neurospheres expressed
2021-07-31
Primary human GBM neurospheres expressed high levels of the metabolic enzyme fatty acyl-CoA synthetase VL3 (ACSVL3) that were associated with CSCs self-renewal and tumorigenic capacity. ACSVL3 knockdown significantly decreased ALDH levels, indicating its contribution to cell metabolism and maintenan
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