• br Results and discussion br Conclusion

  2021-06-11

  

  Results and discussion Conclusion We have constructed a series of potent and greatly selective DPP-4 inhibitors with pyrazolo[1,5-a]pyrimidin-7(4H)-one core surrogates. The modification of the core led us to b2 which has IC50 of 80 nM and > 1000 fold selectivity over DPP-8 and DPP-9. We utiliz

• br Introduction Biocatalysis can be

  2021-06-10

  

  Introduction Biocatalysis can be used to synthesize chiral building blocks, such as monomers for polymer materials, and precursors for pharmaceuticals [[1], [2], [3], [4]]. Enzymes are very suitable for catalyzing reactions with high enantioselectivity to obtain chiral products. For instance, alc

• Consistent with previous simulations on the

  2021-06-10

  

  Consistent with previous simulations on the DFG-Asp-out/-in interconversion of Abl kinase, we only observe the DFG flip with protonated Asp747 (Shan et al., 2009). We showed previously that the pKa for the DFG-Asp in Abl is elevated at 6.5. Further “constant pH” simulations whereby protonation event

• Given the importance of cysteine cathepsin inhibitors

  2021-06-10

  

  Given the importance of cysteine cathepsin inhibitors as putative therapeutic molecules and microbial virulence factors, we chose to investigate whether Yersinia enterocolitica may be a potent producer of such inhibitors. Y. enterocolitica is the most heterogeneous species within the genus Yersinia.

• br Acknowledgements br Introduction Anxiety and

  2021-06-10

  

  Acknowledgements Introduction Anxiety and depression are major components of maintaining the cycle of addiction, and are responsible for the negative reinforcement of drug seeking behaviors (Sarnyai et al., 1995, Koob and Le Moal, 2008). Both rats and humans exhibit increased anxiety states du

• br Materials and methods br Results br Discussion

  2021-06-10

  

  Materials and methods Results Discussion Chicken thrombocyte stimulation with LPS leads to a number of inflammatory responses through TLR4-linked pathways (Scott and Owens, 2008). In mammals, LPS binds to LPS-binding protein (LBP) in the blood serum and this complex is subsequently recogniz

• Introduction The COMT gene is located on chromosomal

  2021-06-10

  

  Introduction The COMT gene is located on chromosomal band 22q11.2, extends over 28 kb, contains six exons, and encodes for catechol-O-methyl-transferase (Weinshilboum and Raymond, 1977; Grossman et al., 1992; Lundström et al., 1995; Bearden et al., 2005). This enzyme plays a major role in regulatio

• Finally considering the encouraging inhibitory

  2021-06-10

  

  Finally, considering the encouraging inhibitory and selectivity properties of compound and against isolated CK1δ, we have also acquired a very preliminary cytotoxicity profile on human ovarian carcinoma cell line (2008) and on its cisplatin-resistant clone (C13). Results showed that after 48h of exp

• br Acknowledgements This work was supported

  2021-06-10

  

  Acknowledgements This work was supported by a grant from the Deutsche Forschungsgemeinschaft to Uwe Knippschild and Martin Wabitsch (SFB 1149/B4). P. Fischer-Posovszky is funded by a Margarete von Wrangell scholarship financed by the Ministerium für Wissenschaft, Forschung und Kunst Baden-Württem

• The anticholinesterase activities of all subfractions

  2021-06-10

  

  The anticholinesterase activities of all subfractions derived from EtOAc extract were detected and summarized in . Fraction 5 and its resulting subfractions (5B, 5C, 5D, 5C3, 5C4, 5D3, and 5D4) were found to show attractive activities. Subsequently, ten compounds (–) were obtained from these active

• br Conflicts of interest br Acknowledgements This study

  2021-06-10

  

  Conflicts of interest Acknowledgements This study was funded by Kuwait University Research Administration (Project MI03/10). Introduction Epidemiological, experimental and biologic plausibility support a cardioprotective effect of estrogens in women [1]. Indeed, women are protected until t

• Finally we demonstrated for the first time that the

  2021-06-10

  

  Finally, we demonstrated for the first time that the physiological combinations of estradiol and progesterone levels of premenopausal and postmenopausal women efficiently stimulated the growth of T47D spheroids while clinically relevant concentrations of TPA and UPA suppressed the growth of T47D sph

• The relatively low overall response rates suggest the

  2021-06-10

  

  The relatively low overall response rates suggest the need for better predictive markers for response. The patient demographics in the SARC trial did not reflect typical Ewing sarcoma demographics as the patients tended to be older and had primarily soft tissue tumors. In addition, although accrual

• br Activatable bioorthogonal reactions reagents br Cycloprop

  2021-06-10

  

  Activatable bioorthogonal reactions/reagents Cyclopropenes as bioorthogonal reagents for IEDDA substrates Cyclopropenes have become popular bioorthogonal reagents due to their small size, inertness to biological nucleophiles, ability to be genetically encoded (Yu et al., 2012), and participati

• br Introduction Rheumatoid arthritis RA is a

  2021-06-10

  

  Introduction Rheumatoid arthritis (RA) is a chronic, systemic inflammatory disease that can be divided in at least two subsets based on the presence of antibodies to citrullinated proteins (ACPAs) [1]. Importantly, such ACPA target proteins [[2], [3], [4], [5]] also represent candidate autoantige

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