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Chemotherapeutic approaches to glioblastoma which
2021-11-03
Chemotherapeutic approaches to glioblastoma, which are highly invasive, are still largely unsuccessful and have only a minimal impact on patients’ survival rate . New agents that target the specific molecular aberrations in the tumors are presently being investigated for their efficacy against this
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Introduction Protein tyrosine phosphorylation plays key role
2021-11-02
Introduction Protein-tyrosine phosphorylation plays key roles in a variety of intracellular signaling pathways involved in cell proliferation, differentiation, gene expression, cell adhesion, and metabolic changes [1]. While receptor-type tyrosine kinases localize to the plasma membrane, most of no
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br Hedgehog pathway in embryonic development It is
2021-11-02
Hedgehog pathway in embryonic development It is now well established that the Hedgehog pathway solves a role as one of the essential signaling mechanisms for the modulation of cellular growth and differentiation during embryogenesis. Operating through time- and position-dependent mechanisms, this
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Camptothecin is a type of topo I inhibitor and its
2021-11-02
Camptothecin is a type of topo I inhibitor, and its prodrugs irinotecan and topotecan have been approved by the FDA for clinical cancer treatment. It has been reported that SAHA can enhance the cytotoxicity of camptothecin derivatives in several cancer cell lines20., 21., 22., 23., 24.. Taking the s
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Interestingly the virulence of HBV may adaptively evolve thu
2021-11-02
Interestingly, the virulence of HBV may adaptively evolve, thus affecting the macroscopic propagation of hepatitis B. Higher virulence in vivo may result in a higher transmission rate and mortality. By assuming that the transmission rate is a monotonically increasing function of virulence, , we prop
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Our synthetic approach to GPR
2021-11-02
Our synthetic approach to GPR55 antagonists was designed so that many different structures could be accessed to rapidly explore initial SAR, along with validating or modifying our current model (). The synthesis begins with the coupling of a carboxylic meclofenamate to 4-piperidone by first forming
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Firstly the impact on activity and selectivity
2021-11-02
Firstly, the impact on activity and selectivity was made by replacing the 2, 3-di-F substitution of ring A with 2,3-OCHO- () and 2-NO () substitutions, and replacing the 3, 5-di-F substitution of ring B with 3,5-di-OMe () and 3,5-di-Me () substitutions. Compound kept moderate activity (EC = 220 nM)
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br Ligand binding free energies In order to compute the
2021-11-02
Ligand-binding free energies In order to compute the absolute free ml calculator associated with binding a ligand to a flexible iGluR LBD, a theory that accounts for all the principal thermodynamic contributions from ligand docking and LBD closure had to be developed. This was accomplished using
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Rare mutations can impair the molecular function of
2021-11-02
Rare mutations can impair the molecular function of GR and alter tissue sensitivity to GCs in humans, resulting in primary generalized GC resistance (PGGR) and hypersensitivity (PGGH) [14]. Familial and sporadic PGGR, or Chrousos Syndrome, is characterized by general and partial insensitivity of tis
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The rapid actions of glucocorticoids range
2021-11-02
The rapid actions of glucocorticoids range from the production of endocannabinoid as a retrograde messenger [9], to regulation of ion channels [10], [11], to inhibitory effects on immune PIK-75 [12], [13], [14]. Many different kinase signaling pathways have been implicated in the rapid actions of g
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Next the effects of a
2021-11-02
Next, the effects of a phenyl group at the 3- and 4-positions of the furan on GCGR affinity were investigated (). Surprisingly, despite the lack of a 4-phenyl group at the furan, compound exhibited almost the same GCGR affinity as compound . On the other hand, when the phenyl group at the 3-positio
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While the apparent complexity of gap junction regulation pre
2021-11-02
While the apparent complexity of gap junction regulation presents challenges, new technologies continue to propel the field forward. Advances in microscopy are increasingly able to capture rapid dynamics at the plasma membrane (e.g., biosensors [67] and lattice light sheet microscopy [100]) and to d
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br Results br Discussion secretase mediated proteolysis of i
2021-11-02
Results Discussion γ-secretase-mediated proteolysis of integral membrane proteins is required for diverse biological processes (Lal and Caplan, 2011). One γ-secretase target of particular interest is Notch, as recent work has shown Notch activity to be increased in obesity and associated metab
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Oxybutynin The presence of FBP in nuclei seems to accompany
2021-11-02
The presence of FBP2 in nuclei seems to accompany the cells' potential to divide as it has been shown that during differentiation of the satellite cells (myogenic progenitor cells) the amount of nuclear FBP2 decreases and in differentiated myotubes, the localisation of FBP2 is restricted to cytoplas
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EZH interaction with HADC and HDAC
2021-11-02
EZH2 interaction with HADC1 and HDAC2 through the EED subunit is known to recruit histone deacetylases [113,114]. Given that PRC2-mediated repression of transcription may be partly dependent on the function of HDACs in specific cell contexts [115], the leukemia cell treatment with hydroxamic Cyclo
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