• During the past decade it became

  2020-03-03

  

  During the past decade, it became increasingly clear that the affinity and efficacy of small agonists acting on the orthosteric binding site of a GPCR can be modulated by ligands that bind to a topographically distinct (allosteric) binding site on the same GPCR molecule 33, 39, 40, 41, 42. This allo

• br Introduction Breast cancer is the most common malignant t

  2020-03-03

  

  Introduction Breast cancer is the most common malignant tumor in women and the second leading cause of female death [1]. In recent years, with the improvement of early detection and the emergence of new treatment methods, the mortality rate of breast cancer has been greatly reduced. However, the

• Both progesterone and the calcium ionophore A rely

  2020-03-03

  

  Both progesterone and the calcium ionophore A23187 rely on the synthesis of cAMP by sAC to elicit exocytosis in human sperm (Fig. 2E-H and [8], [60]). We had reported earlier that digestion of endogenous cAMP with recombinant cAMP-specific phosphodiesterase 4D [9] or inhibition of its synthesis with

• Due to the high attractiveness of E and E ligases

  2020-03-03

  

  Due to the high attractiveness of E2 and E3 ligases as drug targets, a number of drug discovery assays have been published, based on detection by fluorescence (Dudgeon et al., 2010, Krist et al., 2016, Zhang et al., 2004), Bcl Family Set I (Davydov et al., 2004, Huang et al., 2005, Kenten et al., 2

• br Funding This work was

  2020-03-02

  

  Funding This work was supported by a research grant of the Deutsche Forschungsgemeinschaft (SCHN477-9-2 to R.S.S), the Manfred-Stolte-Stiftung (to R.S.S.) and by a research grant from the German Cancer Aid (Deutsche Krebshilfe, No. 106696/TP 5 to T.F.). Introduction Death-associated protein k

• In the present study we have

  2020-03-02

  

  In the present study, we have examined, an alternative approach for introduction of Hyp into bacterial, non-animal collagens. Previously, Gruskin and colleagues [27] had shown that Hyp could be introduced into recombinant mammalian collagen sequences in E. coli through a mechanism of co-translationa

• Quantum walks can be connected to extended CMV

  2020-03-02

  

  Quantum walks can be connected to extended CMV matrices as follows. If all Verblunsky coefficients with even index vanish, then the extended CMV matrix becomes which resembles the matrix representation U. One may notice, however, that in the extended CMV matrix , whereas in the quantum walk matri

• c-JUN peptide NPC L NPC Niemann Pick C

  2020-03-02

  

  NPC1L1 (NPC1 [Niemann-Pick C-like-1]-like intracellular cholesterol transporter) is the rate-limiting transmembrane transporter for cholesterol c-JUN peptide from the intestinal lumen, and it mediates the absorption of both dietary and biliary cholesterol., , NPC1L1 is the target of the cholester

• br Nuclear estrogen receptors Indirect genomic signaling

  2020-03-02

  

  Nuclear estrogen receptors: Indirect genomic signaling As mentioned earlier, the transcription of several genes that do not contain EREs in their promoter regions can also be regulated by estradiol, without direct binding of the estrogen receptors to the DNA. According to the most recent reports,

• br Halogenases Enzymatic C H activation

  2020-03-02

  

  Halogenases Enzymatic C–H activation leading to halogenation is another emerging area in biocatalysis [55,56]. Incorporation of halogen atoms during medicinal chemistry eff ;orts is a well-established practice, presenting an effective means to control the molecule’s bioactivity and physicochemical

• While a number of studies have helped elucidate the principl

  2020-03-02

  

  While a number of studies have helped elucidate the principles of target amino group specificity, UBL selectivity, and Ub hyPerFUsion™ high-fidelity DNA polymerase specificity [3], [4], [9], [10], [14], [19], [20], [23], [24], [33], [34], [37], [38], [39], [40], [41], the role of the canonical E2-R

• Gastrointestinal tone can be effectively modulated by

  2020-03-02

  

  Gastrointestinal tone can be effectively modulated by cholinesterase inhibitors. As parasympathetic fibers release XL-888 to contract the circular and longitudinal intestinal muscles, AChE inhibition can facilitate those actions. Postoperative ileus (delayed gastric emptying after surgery) can aris

• Our previous work has demonstrated

  2020-03-02

  

  Our previous work has demonstrated that two glutamate residues (Glu-305 and Glu-331 in murine and human TPP II) in the active site are important for exopeptidase activity in mTPP II [17]. At least one of these, Glu-331, seems to form a salt bridge to the N-terminal amino group of the substrate, posi

• br Materials and methods br Results br

  2020-03-02

  

  Materials and methods Results Conclusion Conflict of interest Acknowledgements This work was supported by the National Key Research and Development Program of China (2018YFD0400302) and General Program of National Natural Science Foundation of China (31471602). Introduction A sign

• Since the initial identification of DNA ligase inhibitors by

  2020-03-02

  

  Since the initial identification of DNA ligase inhibitors by a structure-based approach [[18], [26]], there have been several reports describing LigI inhibitors using computer modelling and derivatives of the original DNA ligase inhibitors [[49], [50], [51]]. While these studies have shown that the

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