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The results show that pimarane and strobane diterpenoids exe
2022-06-14

The results show that -pimarane and -strobane diterpenoids exert inhibitory effects on FXa suggesting that they may have potential as FXa inhibitor. However, it should be noted that some compounds such as compounds , , , and are poorly bioavailable. Thus, the current study indicates that the number
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Our understanding of the genetic basis of myeloid
2022-06-14

Our understanding of the genetic basis of myeloid malignancies has been profoundly improved in recent years. Studies have revealed new recurrent somatic mutations in myeloid malignancies, including myeloproliferative neoplasms (MPNs), myelodysplastic syndrome (MDS) and acute myeloid leukaemia (AML).
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Our biological data also showed that
2022-06-14

Our biological data also showed that, in presence of LEDGF/p75, R or S of glycerol T instead of T4, T8 or T12 loop in the T30695-GQ differently affected the integration activity of the enzyme (Table 2), whereas the position but not the chirality of glycerol T affected the inhibitory efficiency of T3
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Protein structures determined in high
2022-06-13

Protein structures determined in high resolution by X-ray crystallography and NMR techniques provide wealth of structural information on intra-domain and inter-domain protein interactions of small sized proteins. In addition, cryo-EM often provides low resolution structures of multi-component protei
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topotecan synthesis br Conclusion The wild study reports
2022-06-13

Conclusion The wild study reports seasonal variations in reproductive physiology, behavior and topotecan synthesis plasticity at different age stages in wild-caught Mongolian gerbils. The gerbils in breeding seasons have more mature sexual development, higher exploratory behavior, higher novelty
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Based on work from our labs with mGlu NAMs
2022-06-13

Based on work from our labs with mGlu NAMs, and the ability of [3.3.0] systems, such as the octahydropyrrolo[3,4-]pyrrole, to effectively mimic piperazines, we focused our attention on the potential bioisoteric replacement of the [3.1.0] system of and , as well as the piperidine of , with a [3.3.0]
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br Acknowledgments This work was supported by
2022-06-13

Acknowledgments This work was supported by the Russian Foundation for Basic Research [grant number 16-04-00205], The Russian Science Foundation [grant number 16-15-00235], Czech Academy of Sciences [grant number RVO 61388963], and the Technology Agency of the Czech Republic [grant number TE01020
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br Materials and methods br Results and discussion br
2022-06-10

Materials and methods Results and discussion Conclusions Acknowledgements This study was supported by the Portuguese Foundation for Science and Technology (FCT) under the scope of the strategic funding of UID/BIO/04469/2013 unit and COMPETE 2020 (POCI-01-0145-FEDER-006684), and also by t
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Based on the above considerations the galactosidase gene
2022-06-10

Based on the above considerations, the β-galactosidase gene from Exiguobacterium acetylicum MF03 (not previously reported) was cloned, expressed and purified with the aim of assessing the potential of this novel enzyme for catalyzing reactions of synthesis and hydrolysis of glycosides. Because of E.
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VS strategies have been building momentum in G drug discover
2022-06-10

VS strategies have been building momentum in G4 drug discovery both as a low-cost enrichment step and as a lead development step in the discovery pipeline, which our laboratory has previously discussed [31]. Whereas traditional HTS methods rely on obtaining and screening hundreds or thousands of com
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Some malignant human tumors cells also express FPRs and
2022-06-10

Some malignant human tumors 5,7-dihydroxychromone synthesis also express FPRs and respond to bacterial or endogenous agonists by increased motility and growth. For instance, FPRs expressed by human gastric cancer cells, mediate epithelial–mesenchymal transition, cell proliferation, migration, and r
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LPCs have been previously described
2022-06-10

LPCs have been previously described as potential anti-diabetic factors due to stimulation of secretory activity from the isolated rodent pancreas, L-type cells, ands insulin-producing cell lines, with LPC 18:1 as the main structure of interest (Soga et al., 2005, Sakamoto et al., 2006, Overton et al
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br Declaration of interest br Acknowledgments br This work w
2022-06-10

Declaration of interest Acknowledgments This work was supported by grants from the Polish National Science Centre (PRELUDIUM grant no. 2013/11/N/NZ5/00270) and the European Commission FP7 Project Beta-JUDO (grant number 279 153), European Union EIT Health project DeTecT2D, Swedish Diabetes A
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br Experimental procedures br Results
2022-06-10

Experimental procedures Results Discussion This study demonstrates that the genetic disruption or pharmacological inhibition of FAAH completely prevented all manifestations of pain symptoms in an NTG-induced migraine animal model. Thus, FAAH disruption or blockade abolished the activation o
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One PKC target that controls cortical actin
2022-06-10

One PKC target that controls cortical Tirofiban structure is a well-known actin crosslinking protein, myristoylated alanine-rich C-kinase substrate (MARCKS). MARCKS cross-links actin and binds PIP2 and this binding activity is regulated by PKC phosphorylation [82]. Activation of PKC releases MARCKS
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