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br Conclusions br Acknowledgements The authors thank Matt
2022-07-15

Conclusions Acknowledgements The authors thank Matt JM Wood and colleagues (AstraZeneca, UK) for permission to use logD and protein binding data presented in Sup. Table S2. Introduction The number of people suffering from type 2 diabetes mellitus (T2DM) has escalated worldwide as a consequ
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SM-164 In previous work we showed that benzophenanthridines
2022-07-15

In previous work we showed that benzophenanthridines do not affect the surface expression of GlyT1 (Jursky and Baliova, 2011). The results from the surface biotinylation studies reported in Fig. 3 show that the surface expression of the Y370F mutant is not significanly affected by the alkaloids in t
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Abnormal expression and higher activity of GLO I
2022-07-15

Abnormal expression and higher activity of GLO I have been detected more in various tumor APETx2 than in normal cell samples., , , , , , , Among cancer cell lines, lung carcinoma cells frequently showed higher GLO1 activity. Human NSCLC cell line NCI-H522 cells possess high activity and expression
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Pergolide mesylate The observed increase in macroscopic cond
2022-07-14

The observed increase in macroscopic conductance could be due to a left shift in the open state probability vs. voltage curve for the high-activity state causing an increase in the open state probability at all potentials. However, an increase of the apparent single channel conductance cannot be ent
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Next we studied the effects of the
2022-07-14

Next, we studied the effects of the compounds PA-Glu, PA-hSuc, and PA-hPim on the IGly of rat hippocampal neurons. As in the experiments with IGABA, IGly was affected by steroids with a pregnane skeleton, but not those with an androstane skeleton. At the same time, androstane steroids were shown to
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No G C pattern managed to capture
2022-07-14

No G4C pattern managed to capture all GQ forming sequences of the reference dataset. The sequences that were missed by even the most flexible models were AGATGGAGTGGAGAGG, AGGAGATGCAGGAG, AGAGGGTAGATGG and TTTTTAAAAGAAGGGGAGGAATAGGGGATATGA. In fact, the former three are not expected to form any unim
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With the identification of small nonpolar substituents at
2022-07-14

With the identification of small nonpolar substituents at R3 of the phenylpropanoic acid ring providing improved activity at FFA4, exploration of the benzyl SAR was undertaken (). Small substituents were well tolerated at both the and positions (–) with the 2-bromo- (), 2-isopropoxy- (), and 3-met
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br Materials and methods br Results and
2022-07-14

Materials and methods Results and discussion In order to identify genes required for photoautotrophic growth, we screened a random insertion mutant library of Synechocystis 6803 and obtained many mutants with impaired photoautotrophic growth. About 6000 random insertion colonies of the mutant
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In order to understand the determinants of
2022-07-14

In order to understand the determinants of high affinity of with amide side chain, an X-ray crystal structure of human liver FBPase in complex with was determined (). The position of phosphonate group and tricyclic scaffold of is similar to those of with no side chain, which suggests the formati
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br Rationale The present study was motivated to get
2022-07-14

Rationale The present study was motivated to get further insight into the molecular recognition processes of 2-alkyl(amino)ethyl-1,1-bisphosphonates taking compounds 12–14 as reference structures. We have recently demonstrated that TcFPPS inhibitors 12 and 13 bind to the allylic site of the enzym
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Murine models of AML were
2022-07-14

Murine models of AML were used to identify differentially expressed proteins following treatment with the EZH2 inhibitor, DZnep. Sandow and coworkers demonstrated that inhibition of EZH2 induces leukemia ryanodine arrest through regulation of cyclin-dependent kinases and increased expression of p53
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The most abundant form of Hat p in the nucleus
2022-07-14

The most abundant form of Hat1p in the nucleus is apt to be in the form of the NuB4 complex [96]. In the context of MK-2048 assembly, the function of the NuB4 complex may be similar to that ascribed for the cytoplasmic HAT1 complex. That is, the NuB4 complex may be involved in directing newly synth
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Several recent studies have linked clock function with the c
2022-07-14

Several recent studies have linked clock function with the cell cycle and reported that clock components, such as PER1, PER2, BMAL1, and CRY1/2 decrease cell proliferation or improve the action of anti-cancer drugs in different cancer cell lines. Moreover, certain types of human cancer show an alter
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To date several studies have suggested that serum
2022-07-14

To date, several studies have suggested that serum HER2 could be used as a biomarker for monitoring the disease course and the patient's response to therapy [110], [111]. However, the clinical usefulness of serum HER2 has not been fully validated because of conflicting data [31]. The enzyme-linked i
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We have previously reported on
2022-07-13

We have previously reported on the effects of replacing the isoquinoline P2∗ moiety with a naphthalene ring and modifying the connectivity for this element to the P2 proline ring, as demonstrated by compounds – (). Therein, it was hypothesized that the reduced potency observed with – when compared t
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