• Modulating protein stability specifically inhibiting ubiquit

  2020-06-08

  

  Modulating protein stability, specifically inhibiting ubiquitin E3 ligases, provides potential advantages over other druggable targets given the presence of biochemically multiple, unique pharmacophores within complexes that can bind a variety of small molecules [12]. The FBXO3 inhibitors used here

• Ubiquitination is a reversible posttranslational modificatio

  2020-06-08

  

  Ubiquitination is a reversible posttranslational modification. The removal of Ub is carried out by enzymes known as deubiquitinases (DUBs). The antagonistic role played by these enzymes in the Ub pathway regulates the function of the ubiquitinated proteins, while maintaining the free Ub pool in euka

• The first hint that GLP might

  2020-06-08

  

  The first hint that GLP-1 might not be completely stable came from a meeting abstract in 1992, reporting that GLP-1 could be degraded in plasma incubations [16], although the enzyme(s) involved was not identified. A year later, Mentlein and colleagues [17], in a search for peptide substrates of the

• Dipeptidyl peptidase inhibitors DPP is or gliptins stimulate

  2020-06-08

  

  Dipeptidyl peptidase-4 inhibitors (DPP-4is or gliptins) stimulate both post-meal insulin secretion and inhibit 57 9 sale secretion in a glucose-dependent manner, rendering the risk of hypoglycaemia minimal [10]. They are weight-neutral or may even induce slight weight loss. Their good efficacy has

• CAA is a carcinogenic metabolite of vinyl chloride

  2020-06-08

  

  CAA is a carcinogenic metabolite of vinyl chloride, forming several different DNA adducts including the cyclic Dorsomorphin adducts 3,N4-ethenocytosine (εC), 1,N6-ethenoadenine (εA), N2,3-ethenoguanine (εG), and 1,N2-ethenoguanine (1,N2-εG), with the A and C cyclic adducts the most predominant, and

• Present malarial chemotherapies mainly rely on a

  2020-06-08

  

  Present malarial chemotherapies mainly rely on a very few chemotypes or their allied structures such as quinolines, anti-folates and some cyclic endo-peroxides (Nayyar et al., 2012). Over the last few decades, the extensive and repetitive deployment of these drugs has stimulated resistance in the pa

• Adriamycin As for antiviral activity eight out of synthesize

  2020-06-08

  

  As for antiviral activity, eight out of 23 synthesized compounds were active against influenza B virus with EC50 values in the range of 0.19–39 μM. Four of the eight influenza B hits were active against influenza A and two were also active against RSV (4 and 6, EC50 = 0.40 and 1.8 μM, respectively).

• Cysteine protease inhibitors representing several

  2020-06-08

  

  Cysteine protease inhibitors representing several chemical scaffold types are effective in halting parasite replication without toxicity to the host (Renslo and McKerrow, 2006). A vinyl sulfone cysteine protease inhibitor, K11777, is completing final Good Laboratory Practice (GLP) preclinical tests

• Proteins that associate to PCNA are characterized

  2020-06-08

  

  Proteins that associate to PCNA are characterized by having conserved motifs as the PCNA-interacting protein (PIP) motif [29,30], its variant PIP-like motif [31,32] or the APIM motif (Alk B homologue 2 PCNA interacting motif [33,34]); for instance, p21 contains a PIP motif [30], and DNA polymerases

• The Ewing sarcoma breakpoint region gene EWSR is a

  2020-06-05

  

  The Ewing sarcoma breakpoint region 1 gene (EWSR1) is a partner in a large, diverse range of mesenchymal (and some nonmesenchymal) tumors (Tables 1 and 2). As the 5′ partner, EWSR1 is able to fuse with an array of genes. These fusions can generate genetically different but phenotypically identical n

• cAMP mediated signaling pathways are important for maintaini

  2020-06-05

  

  cAMP-mediated signaling pathways are important for maintaining metabolic homeostasis, and the effects of the glucagon/catecholamine–cAMP–PKA axis on energy balance have been well documented [20]. For example, Ciclopirox ethanolamine australia of the PKA 2β regulatory subunit (RIIβ) in mice leads to

• SU 4312 br Materials and methods br Results br Discussion In

  2020-06-05

  

  Materials and methods Results Discussion In particular, we showed that pancreatic neuroendocrine tumor SU 4312 recognize cAMP as a stimulatory signal for cell proliferation. Conversely, cAMP was found to have an inhibitory effect on cell proliferation in bronchial carcinoids cells. The div

• ACE also known as Kininase

  2020-06-05

  

  ACE also known as Kininase II is an important enzyme of the Renin angiotensin Plerixafor 8HCl system (RAAS) (Novo et al., 1987), it is believed to be a potent blood pressure regulator and also plays a crucial role in activation of the bradykinin receptor via inactivation of bradykinin which works t

• In this study we implicate SCFFBXO

  2020-06-05

  

  In this study, we implicate SCFFBXO3 E3 ligase as a critical modulator of inflammation in atherosclerosis and demonstrate the efficacy of a small molecule FBXO3 inhibitor in suppressing inflammatory responses important in atherosclerosis. Specifically, individuals carrying a hypofunctioning genetic

• br Introduction DNA ligation is required during DNA

  2020-06-05

  

  Introduction DNA ligation is required during DNA replication and to complete almost all DNA repair events. In human cells, the DNA ligases encoded by three LIG genes are responsible for joining interruptions in the phosphodiester backbone [1]. These enzymes have distinct but overlapping functions

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